Curcumin, demetoxycurcumin and xanthorrhizol are an active compounds contained in temulawak (Curcuma xanthorrhiza) which have activity in inhibiting the tyrosinase enzyme and α-melanocyte stimulating hormone (α-MSH ) in vitro. Docking simulation was done to determine and visualize the interaction of the three compounds with the tyrosinase enzyme and α-MSH. The results of docking simulations showed that the three compounds can interact spontaneously with the tyrosinase enzyme and α-MSH. On the tyrosinase enzyme, xanthorrhizol interact most easily through the formation of hydrogen bonds with Asn205. On the α-MSH, demethoxycurcumin interact most easily through the formation of two hydrogen bonds with His3 and Arg5. With the inhibitory effect on the enzyme tyrosinase and α-melanocyte stimulating hormone (α-MSH) means preventing the formation of skin coloring pigment melanin, indicating that the three compounds studied can be applied as skin whitening agents.
Piroxicam Nanostructured Lipid Carrier Drug Delivery SystemYogeshIJTSRD
Objective Nanostructured lipid carrier NLC based topical gel of Piroxicam PXM was formulated with the aim of controlled release action and to reduce systemic side effect for the treatment of an arthritic condition. Methods NLCs developed using high pressure homogenization method and optimized using a 32 factorial design with response surface methodology using design expert software. NLCs were characterized for particle size, zeta potential analysis, drug entrapment efficiency, and in vitro drug release studies to select the optimized formulation. The NLCs were suitably gelled and evaluated with respect to homogeneity, pH, viscosity, gel strength, spread ability, rheological characteristics, drug content, in vitro diffusion, and stability study. Safety of the NLC based gel was assessed using primary skin irritation studies, and efficacy was confirmed using carrageen an induced rat paw edema model. Results NLCs formulation comprising 2 of lipid 60 40 and surfactant 1.50 was confirmed as an optimized batch having a particle size 138.2±3.60 nm with polydispersibility index value 0.344±0.034. The zeta potential value indicates good physical stability. Based on the results from the in vitro release study it was shown that the formed gels had the ability to extend release of PXM for 24 h and showing percentage drug release of 90.92 ±1.96 at the end of 24 h. Skin irritation studies revealed that the optimized gel formulation shows no erythema, edema, or ulceration. Conclusion The overall results of the present study clearly indicated promising potentials of NLC based gel for delivering PXM topically over the conventional gel. Dr. G. Jagadish | Dr. Rita Mourya | Dr. Amith Nayak "Piroxicam Nanostructured Lipid Carrier Drug Delivery System" Published in International Journal of Trend in Scientific Research and Development (ijtsrd), ISSN: 2456-6470, Volume-5 | Issue-3 , April 2021, URL: https://www.ijtsrd.com/papers/ijtsrd39912.pdf Paper URL: https://www.ijtsrd.com/pharmacy/pharmaceutics/39912/piroxicam-nanostructured-lipid-carrier-drug-delivery-system/dr-g-jagadish
Microsponge containing acyclovir sodium as active
constituent with four different formulation by changing the properties of drug(acyclovir sodium), polymer(ethyl cellulose), emulsifier(PVA) were obtained using emulsion solvent
diffusion method.
The IOSR Journal of Pharmacy (IOSRPHR) is an open access online & offline peer reviewed international journal, which publishes innovative research papers, reviews, mini-reviews, short communications and notes dealing with Pharmaceutical Sciences( Pharmaceutical Technology, Pharmaceutics, Biopharmaceutics, Pharmacokinetics, Pharmaceutical/Medicinal Chemistry, Computational Chemistry and Molecular Drug Design, Pharmacognosy & Phytochemistry, Pharmacology, Pharmaceutical Analysis, Pharmacy Practice, Clinical and Hospital Pharmacy, Cell Biology, Genomics and Proteomics, Pharmacogenomics, Bioinformatics and Biotechnology of Pharmaceutical Interest........more details on Aim & Scope).
All manuscripts are subject to rapid peer review. Those of high quality (not previously published and not under consideration for publication in another journal) will be published without delay.
Piroxicam Nanostructured Lipid Carrier Drug Delivery SystemYogeshIJTSRD
Objective Nanostructured lipid carrier NLC based topical gel of Piroxicam PXM was formulated with the aim of controlled release action and to reduce systemic side effect for the treatment of an arthritic condition. Methods NLCs developed using high pressure homogenization method and optimized using a 32 factorial design with response surface methodology using design expert software. NLCs were characterized for particle size, zeta potential analysis, drug entrapment efficiency, and in vitro drug release studies to select the optimized formulation. The NLCs were suitably gelled and evaluated with respect to homogeneity, pH, viscosity, gel strength, spread ability, rheological characteristics, drug content, in vitro diffusion, and stability study. Safety of the NLC based gel was assessed using primary skin irritation studies, and efficacy was confirmed using carrageen an induced rat paw edema model. Results NLCs formulation comprising 2 of lipid 60 40 and surfactant 1.50 was confirmed as an optimized batch having a particle size 138.2±3.60 nm with polydispersibility index value 0.344±0.034. The zeta potential value indicates good physical stability. Based on the results from the in vitro release study it was shown that the formed gels had the ability to extend release of PXM for 24 h and showing percentage drug release of 90.92 ±1.96 at the end of 24 h. Skin irritation studies revealed that the optimized gel formulation shows no erythema, edema, or ulceration. Conclusion The overall results of the present study clearly indicated promising potentials of NLC based gel for delivering PXM topically over the conventional gel. Dr. G. Jagadish | Dr. Rita Mourya | Dr. Amith Nayak "Piroxicam Nanostructured Lipid Carrier Drug Delivery System" Published in International Journal of Trend in Scientific Research and Development (ijtsrd), ISSN: 2456-6470, Volume-5 | Issue-3 , April 2021, URL: https://www.ijtsrd.com/papers/ijtsrd39912.pdf Paper URL: https://www.ijtsrd.com/pharmacy/pharmaceutics/39912/piroxicam-nanostructured-lipid-carrier-drug-delivery-system/dr-g-jagadish
Microsponge containing acyclovir sodium as active
constituent with four different formulation by changing the properties of drug(acyclovir sodium), polymer(ethyl cellulose), emulsifier(PVA) were obtained using emulsion solvent
diffusion method.
The IOSR Journal of Pharmacy (IOSRPHR) is an open access online & offline peer reviewed international journal, which publishes innovative research papers, reviews, mini-reviews, short communications and notes dealing with Pharmaceutical Sciences( Pharmaceutical Technology, Pharmaceutics, Biopharmaceutics, Pharmacokinetics, Pharmaceutical/Medicinal Chemistry, Computational Chemistry and Molecular Drug Design, Pharmacognosy & Phytochemistry, Pharmacology, Pharmaceutical Analysis, Pharmacy Practice, Clinical and Hospital Pharmacy, Cell Biology, Genomics and Proteomics, Pharmacogenomics, Bioinformatics and Biotechnology of Pharmaceutical Interest........more details on Aim & Scope).
All manuscripts are subject to rapid peer review. Those of high quality (not previously published and not under consideration for publication in another journal) will be published without delay.
This presentation deals with they proposal of my M Pharm research project topic briefly. It consist of various areas which needs to answer during the course of project.
Preparation, In Vitro and In Vivo Characterization of Solid Dispersions of La...iosrphr_editor
The IOSR Journal of Pharmacy (IOSRPHR) is an open access online & offline peer reviewed international journal, which publishes innovative research papers, reviews, mini-reviews, short communications and notes dealing with Pharmaceutical Sciences( Pharmaceutical Technology, Pharmaceutics, Biopharmaceutics, Pharmacokinetics, Pharmaceutical/Medicinal Chemistry, Computational Chemistry and Molecular Drug Design, Pharmacognosy & Phytochemistry, Pharmacology, Pharmaceutical Analysis, Pharmacy Practice, Clinical and Hospital Pharmacy, Cell Biology, Genomics and Proteomics, Pharmacogenomics, Bioinformatics and Biotechnology of Pharmaceutical Interest........more details on Aim & Scope).
IJERA (International journal of Engineering Research and Applications) is International online, ... peer reviewed journal. For more detail or submit your article, please visit www.ijera.com
This presentation deals with the brief study of functionalized graphene oxide nanoparticles for the delivery of model anticancer drug. It represents benefits of targeted drug delivery over the conventional drug delivery,
It is one of the remingtons journal club seminar which is part of masters degree progam in pharmacy.
Intranasal delivery of drug loaded thiolated co-polymeric microparticles for...Gaurav Patil
E-Presentation at Two days 15th Indo-US virtual International Conference
on “Global advances in Pharmaceutical and Allied Science”
In collaboration with
APP Gujarat State branch, AAP American International branch,
AAP Pharmedu Healthcare Manag Division
Present study deals with the preliminary study of Glycine Max Ethanol Extract (GMEE). GMEE stacks more macro and micro nutrients with many pharmacological and nutraceutical standards. GMEE was preliminary screened by simple test methods and instrumentation methods such as RP-HPLC, IR and GC-MS. The obtained results from IR predicted the presence of different functional groups such as OH, CH2, C=O, C-O and cyclic ring. While, the RP-HPLC and GC-MS profiles of GMEE predicted the presence of lipids, polyphenols, alkaloids and flavonoids in the extract.
Combined effects of PEGylation and particle size on uptake of PLGA particles ...Nanomedicine Journal (NMJ)
Abstract
Objective:
At the present study, relationship between phagocytosis of PLGA particles and combined effects of particle size and surface PEGylation was investigated.
Materials and Methods:
Microspheres and nanospheres (3500 nm and 700 nm) were prepared from three types of PLGA polymers (non-PEGylated and PEGylation percents of 9% and 15%). These particles were prepared by solvent evaporation method. All particles were labeled with FITC-Albumin. Interaction of particles with J744.A.1 mouse macrophage cells, was evaluated in the absence or presence of 7% of the serum by flowcytometry method.
Results:
The study revealed more phagocytosis of nanospheres. In the presence of the serum, PEGylated particles were phagocytosed less than non-PEGylated particles. For nanospheres, this difference was significant (P<0/05) and their uptake was affected by PEGylation degree. In the case of microsphere formulation, PEGylation did not affect the cell uptake. In the serum-free medium, the bigger particles had more cell uptake rate than smaller ones but the cell uptake rate was not influenced by PEGylation.
Conclusion:
The results indicated that in nanosized particles both size and PEgylation degree could affect the phagocytosis, but in micron sized particles just size, and not the PEGylation degree, could affect this.
Physicochemical Properties of Gelatin Extracted from Buffalo Hide Pretreated ...UniversitasGadjahMada
The acid pretreatment of collagen molecules disrupts their crosslinks and assists in the release of acid-soluble proteins, fats, and other components. Generally, to achieve optimum extraction efficiency, strong acids may be used at a lower acid concentration compared to weak acids. This study aimed to determine the yield and physicochemical properties of gelatins extracted from buffalo hides pretreated with different acids. Hides were extracted with hydrochloric, citric, and acetic acids at concentrations of 0.3, 0.6, 0.9, 1.2, and 1.5 M. A completely randomized design and the least significant difference test were used in the experimental design, and all measurements were performed in triplicate. The highest yield (29.17%) was obtained from pretreatment with 0.9 M HCl. The gel strength did not differ significantly (p>0.05) according to acid type (280.26-259.62 g Bloom), and the highest viscosity was obtained from the 0.6 M citric acid pretreatment. All the gelatins contained α- and β-chain components and several degraded peptides (24-66 kDa). The color and Fourier-transform infrared spectrum of the gelatin extracted using 0.9 M HCl were similar to those of commercial bovine skin gelatin. In general, the physicochemical properties of the gelatin complied with the industry standard set by the Gelatin Manufacturers Institute of America, revealing that buffalo hide could serve as a potential alternative source of gelatin.
Self-nanoemulsifying drug delivery system (SNEDDS) of Amomum compactum essent...UniversitasGadjahMada
The main purpose of this study was to formulate and to characterize a self-nanoemulsifying drug delivery systems of cardamom (Amomum compactum) essential oil. The optimum formula was analyzed using a D-Optimal mixture designed by varying concentrations of oil component (Amomum compactum essential oil and virgin coconut oil), Tween 80, and polyethylene glycol 400 (PEG 400) (v/v) using a Design Expert® Ver. 7.1.5. Emulsification time and transmittance were selected as responses for optimization. The optimum formula was characterized by droplet size, zeta potential, viscosity, thermodynamic stability, and morphology using Transmission Electron Microscopy. SNEDDS of Amomum compactum essential oil was successfully formulated to SNEDDS using 10% of Amomum compactum essential oil, 10% of virgin coconut oil, 65.71% of Tween 80, and 14.29% of PEG 400. The characterization result showed the percent transmittance 99.37 ± 0.06, emulsification time 46.38 ± 0.61 s, the average droplet size 13.97 ± 0.31 nm with PI 0.06 ± 0.05, zeta potential −28.8 to −45.9 mV, viscosity 187.5 ± 0 mPa·s, passed the thermodynamic stress tests, and indicated spherical shape. The study revealed that the formulation has increased solubility and stability of Amomum compactum essential oil.
Design expert software assisted development and evaluation of cefpodoxime pro...Makrani Shaharukh
Cefpodoxime Proxetil is third generation, broad-spectrum Cephalosporin Antibiotic & it has an oral bioavailability of only 50% and biological half life 2 h so to improve it’s bioavailability sustain release matrix formulation was designed. Sustained release matrix tablets of Cefpodoxime Proxetil prepared by direct compression method based on combination of natural Acacia gum & Karaya gum polymers. 32 full factorial designs optimization study was carried out by using Design Expert Software to find the effect of independent variables, i.e., Acacia gum (X1) and Karaya gum (X2) concentration on dependent variables i.e., Hardness & % CDR. The drug excipient mixtures were subjected to preformulation studies. The tablets were subjected to physicochemical studies, in-vitro drug release, kinetic studies and stability studies. FTIR and DSC studies shown there was no interaction between drug and polymers. Matrix tablet of Cefpodoxime Proxetil were formulated well in term of hardness 5.07 ± 0. 5.93 ± 0.03 kg/cm2, thickness 2.25 ± 0.1 mm to 3.33 ± 0.3 mm, weight variation were within limits. In-vitro release studies show that almost 90 % of drug was release from all the formulation were within 12 h. Formulation F5 selected as a optimized one since it showed optimum hardness & sustained drug release within 12 h in comparison to other formulation. The F5 optimized formulations were subjected to stability studies and shown there were no significant changes in drug content, physicochemical parameters and release pattern. 32 full factorial design optimization technique was successfully used in this research work. Developed matrix tablets of Cefpodoxime Proxetil produced a sustained and effective drug release over a prolonged time frame that led to greater therapeutic efficacy.
Spectrophotometric Estimation of Dronedarone Hydrochloride in Pharmaceutical ...Jing Zang
An accurate and precise UV spectrophotometric method with multivariate calibration technique for the determination of dronedarone hydrochloride in pharmaceutical dosage forms has been described. The term multivariate calibration refers to the process of constructing a mathematical model that relates a property such as content or identity to the absorbance of a set of known reference samples at more than one wavelength. Dronedarone shows maximum wavelength at 288 nm using methanol as a solvent and obeyed Beer’s law in the linear range of 10-35μg/ml. The present method was found to be accurate, precise, and can be successfully used for quantitative estimation of dronedarone in drug and tablet dosage form compare to other complex techniques.
ANTIMICROBIAL AND ANTIFUNGAL OF SOME NEW SEMISYNTHETIC TERPENOID DERIVATIVES ...Jing Zang
The synthesis of a series of euphorbol derivatives is described, starting from euphorbol isolated from fresh latex of Euphorbia resinifera Berg. Their structures have been established on the basis of spectral data. All compounds were evaluated for antibacterial activities against Escherichia coli and Staphyloccus aureus strains and antifungal activity against Candida albicans and Aspergillus niger strains by using serial dilution method. `
This presentation deals with they proposal of my M Pharm research project topic briefly. It consist of various areas which needs to answer during the course of project.
Preparation, In Vitro and In Vivo Characterization of Solid Dispersions of La...iosrphr_editor
The IOSR Journal of Pharmacy (IOSRPHR) is an open access online & offline peer reviewed international journal, which publishes innovative research papers, reviews, mini-reviews, short communications and notes dealing with Pharmaceutical Sciences( Pharmaceutical Technology, Pharmaceutics, Biopharmaceutics, Pharmacokinetics, Pharmaceutical/Medicinal Chemistry, Computational Chemistry and Molecular Drug Design, Pharmacognosy & Phytochemistry, Pharmacology, Pharmaceutical Analysis, Pharmacy Practice, Clinical and Hospital Pharmacy, Cell Biology, Genomics and Proteomics, Pharmacogenomics, Bioinformatics and Biotechnology of Pharmaceutical Interest........more details on Aim & Scope).
IJERA (International journal of Engineering Research and Applications) is International online, ... peer reviewed journal. For more detail or submit your article, please visit www.ijera.com
This presentation deals with the brief study of functionalized graphene oxide nanoparticles for the delivery of model anticancer drug. It represents benefits of targeted drug delivery over the conventional drug delivery,
It is one of the remingtons journal club seminar which is part of masters degree progam in pharmacy.
Intranasal delivery of drug loaded thiolated co-polymeric microparticles for...Gaurav Patil
E-Presentation at Two days 15th Indo-US virtual International Conference
on “Global advances in Pharmaceutical and Allied Science”
In collaboration with
APP Gujarat State branch, AAP American International branch,
AAP Pharmedu Healthcare Manag Division
Present study deals with the preliminary study of Glycine Max Ethanol Extract (GMEE). GMEE stacks more macro and micro nutrients with many pharmacological and nutraceutical standards. GMEE was preliminary screened by simple test methods and instrumentation methods such as RP-HPLC, IR and GC-MS. The obtained results from IR predicted the presence of different functional groups such as OH, CH2, C=O, C-O and cyclic ring. While, the RP-HPLC and GC-MS profiles of GMEE predicted the presence of lipids, polyphenols, alkaloids and flavonoids in the extract.
Combined effects of PEGylation and particle size on uptake of PLGA particles ...Nanomedicine Journal (NMJ)
Abstract
Objective:
At the present study, relationship between phagocytosis of PLGA particles and combined effects of particle size and surface PEGylation was investigated.
Materials and Methods:
Microspheres and nanospheres (3500 nm and 700 nm) were prepared from three types of PLGA polymers (non-PEGylated and PEGylation percents of 9% and 15%). These particles were prepared by solvent evaporation method. All particles were labeled with FITC-Albumin. Interaction of particles with J744.A.1 mouse macrophage cells, was evaluated in the absence or presence of 7% of the serum by flowcytometry method.
Results:
The study revealed more phagocytosis of nanospheres. In the presence of the serum, PEGylated particles were phagocytosed less than non-PEGylated particles. For nanospheres, this difference was significant (P<0/05) and their uptake was affected by PEGylation degree. In the case of microsphere formulation, PEGylation did not affect the cell uptake. In the serum-free medium, the bigger particles had more cell uptake rate than smaller ones but the cell uptake rate was not influenced by PEGylation.
Conclusion:
The results indicated that in nanosized particles both size and PEgylation degree could affect the phagocytosis, but in micron sized particles just size, and not the PEGylation degree, could affect this.
Physicochemical Properties of Gelatin Extracted from Buffalo Hide Pretreated ...UniversitasGadjahMada
The acid pretreatment of collagen molecules disrupts their crosslinks and assists in the release of acid-soluble proteins, fats, and other components. Generally, to achieve optimum extraction efficiency, strong acids may be used at a lower acid concentration compared to weak acids. This study aimed to determine the yield and physicochemical properties of gelatins extracted from buffalo hides pretreated with different acids. Hides were extracted with hydrochloric, citric, and acetic acids at concentrations of 0.3, 0.6, 0.9, 1.2, and 1.5 M. A completely randomized design and the least significant difference test were used in the experimental design, and all measurements were performed in triplicate. The highest yield (29.17%) was obtained from pretreatment with 0.9 M HCl. The gel strength did not differ significantly (p>0.05) according to acid type (280.26-259.62 g Bloom), and the highest viscosity was obtained from the 0.6 M citric acid pretreatment. All the gelatins contained α- and β-chain components and several degraded peptides (24-66 kDa). The color and Fourier-transform infrared spectrum of the gelatin extracted using 0.9 M HCl were similar to those of commercial bovine skin gelatin. In general, the physicochemical properties of the gelatin complied with the industry standard set by the Gelatin Manufacturers Institute of America, revealing that buffalo hide could serve as a potential alternative source of gelatin.
Self-nanoemulsifying drug delivery system (SNEDDS) of Amomum compactum essent...UniversitasGadjahMada
The main purpose of this study was to formulate and to characterize a self-nanoemulsifying drug delivery systems of cardamom (Amomum compactum) essential oil. The optimum formula was analyzed using a D-Optimal mixture designed by varying concentrations of oil component (Amomum compactum essential oil and virgin coconut oil), Tween 80, and polyethylene glycol 400 (PEG 400) (v/v) using a Design Expert® Ver. 7.1.5. Emulsification time and transmittance were selected as responses for optimization. The optimum formula was characterized by droplet size, zeta potential, viscosity, thermodynamic stability, and morphology using Transmission Electron Microscopy. SNEDDS of Amomum compactum essential oil was successfully formulated to SNEDDS using 10% of Amomum compactum essential oil, 10% of virgin coconut oil, 65.71% of Tween 80, and 14.29% of PEG 400. The characterization result showed the percent transmittance 99.37 ± 0.06, emulsification time 46.38 ± 0.61 s, the average droplet size 13.97 ± 0.31 nm with PI 0.06 ± 0.05, zeta potential −28.8 to −45.9 mV, viscosity 187.5 ± 0 mPa·s, passed the thermodynamic stress tests, and indicated spherical shape. The study revealed that the formulation has increased solubility and stability of Amomum compactum essential oil.
Design expert software assisted development and evaluation of cefpodoxime pro...Makrani Shaharukh
Cefpodoxime Proxetil is third generation, broad-spectrum Cephalosporin Antibiotic & it has an oral bioavailability of only 50% and biological half life 2 h so to improve it’s bioavailability sustain release matrix formulation was designed. Sustained release matrix tablets of Cefpodoxime Proxetil prepared by direct compression method based on combination of natural Acacia gum & Karaya gum polymers. 32 full factorial designs optimization study was carried out by using Design Expert Software to find the effect of independent variables, i.e., Acacia gum (X1) and Karaya gum (X2) concentration on dependent variables i.e., Hardness & % CDR. The drug excipient mixtures were subjected to preformulation studies. The tablets were subjected to physicochemical studies, in-vitro drug release, kinetic studies and stability studies. FTIR and DSC studies shown there was no interaction between drug and polymers. Matrix tablet of Cefpodoxime Proxetil were formulated well in term of hardness 5.07 ± 0. 5.93 ± 0.03 kg/cm2, thickness 2.25 ± 0.1 mm to 3.33 ± 0.3 mm, weight variation were within limits. In-vitro release studies show that almost 90 % of drug was release from all the formulation were within 12 h. Formulation F5 selected as a optimized one since it showed optimum hardness & sustained drug release within 12 h in comparison to other formulation. The F5 optimized formulations were subjected to stability studies and shown there were no significant changes in drug content, physicochemical parameters and release pattern. 32 full factorial design optimization technique was successfully used in this research work. Developed matrix tablets of Cefpodoxime Proxetil produced a sustained and effective drug release over a prolonged time frame that led to greater therapeutic efficacy.
Spectrophotometric Estimation of Dronedarone Hydrochloride in Pharmaceutical ...Jing Zang
An accurate and precise UV spectrophotometric method with multivariate calibration technique for the determination of dronedarone hydrochloride in pharmaceutical dosage forms has been described. The term multivariate calibration refers to the process of constructing a mathematical model that relates a property such as content or identity to the absorbance of a set of known reference samples at more than one wavelength. Dronedarone shows maximum wavelength at 288 nm using methanol as a solvent and obeyed Beer’s law in the linear range of 10-35μg/ml. The present method was found to be accurate, precise, and can be successfully used for quantitative estimation of dronedarone in drug and tablet dosage form compare to other complex techniques.
ANTIMICROBIAL AND ANTIFUNGAL OF SOME NEW SEMISYNTHETIC TERPENOID DERIVATIVES ...Jing Zang
The synthesis of a series of euphorbol derivatives is described, starting from euphorbol isolated from fresh latex of Euphorbia resinifera Berg. Their structures have been established on the basis of spectral data. All compounds were evaluated for antibacterial activities against Escherichia coli and Staphyloccus aureus strains and antifungal activity against Candida albicans and Aspergillus niger strains by using serial dilution method. `
INFLUENCE OF DEMOGRAPHIC FACTORS ON PAIN KILLER USAGE AND ADDICTION SYMPTOMSJing Zang
Pain killers have been a necessity for humans since their skin has been laden with pain receptors to signal them against any invasion or unusual going on in the body.This pain when exceeds the limits of tolerance has to be alleviated to reduce suffering. Since ancient times numerous natural substances like herbs and oils have been used to relieve pain, but in modern era more refined ways to relieve pain have been discovered that exactly target the precise pain. This research identifies the factors that govern painkiller usage and addiction and the people who, in majority fall prey to pleasures of pain killers. The research was carried out through a questionnaire and results were statistically analyzed by fishers exact test. Males, employed people, non medics and graduates are most attracted to pain killers and are susceptible to long term addiction. The reasons for these people falling prey to pain killers are work load, mental stress and physiological responses to the drug. These factors can be managed through proper intervention by health professionals. The role of friends and family too here cannot be ignored.
Formulation Development and In Vitro Evaluation of Microsponge Drug Delivery ...YogeshIJTSRD
A Microsponge Delivery System MDS is patented, highly cross linked, porous, polymeric microspheres that can entrap wide range of actives and then release them onto the skin over a time and in response to trigger. It is a unique technology for the controlled release of topical agents and consists of microporous beads, typically 10 25 microns in diameter, loaded with active agent. In this study, Ketoconazole microsponges were prepared by using quasi emulsion solvent diffusion method. The microsponges thus prepared, were evaluated for production yield, loading efficiency, particle size analysis, in vitro release study of microsponges, and stability. Hence, the present work concluded that MDS has a great potential in topical delivery of drugs like Ketoconazole, with added advantage of reduction in irritation profile due to the controlled release and possible enhancement in the activity due to amorphization of the drug. Vilas S. Bhagat | Sanjay R. Arote "Formulation Development and In-Vitro Evaluation of Microsponge Drug Delivery System of Antifungal Drug" Published in International Journal of Trend in Scientific Research and Development (ijtsrd), ISSN: 2456-6470, Volume-5 | Issue-3 , April 2021, URL: https://www.ijtsrd.com/papers/ijtsrd39870.pdf Paper URL: https://www.ijtsrd.com/pharmacy/pharmaceutics/39870/formulation-development-and-invitro-evaluation-of-microsponge-drug-delivery-system-of-antifungal-drug/vilas-s-bhagat
Microbial Production Of Alkaline Proteases And Evaluation Of Its Performances...Shafkat Shamim Rahman
A high alkaline protease producing bacterial strain was isolated and identified a local soil sample. The organism was gram positive and forms spore during adverse condition in the growth medium. After various tests it was suggested and the features agreed with the description of Bacillus subtilis. It was also identified as B. subtilis with 99.9% identity by API 50 CHB. The enzyme hydrolyses a number of proteins including azocasein which suggests that it is an extracellular alkaline protease. The experimentally determined isoelectric point was 5.1 and the optimal enzyme activity was at 60°C and at pH 8.5. The esterase preferentially hydrolyzed short-chain fatty acids. Native enzyme preparations typically showed a Michaelis constant (Km) and Vmax of 0.40mM and 12,200 U mg)-1, respectively. This microbial enzyme was partially purified by ammonium sulfate fractionation, dialysis, DEAE cellulose chromatography and electrophoretic analysis. Enzyme purity was tested by SDS-PAGE. Quantitative estimation has shown that 40mL of culture supernatant could dehair 2×1 cm of leather completely in 9 hours. In future the tanneries will use a combination of chemical and enzymatic processes. In practical applications, protease is a useful enzyme for promoting the hydrolysis of proteins and showing significant industrial applications.
The bioactive phytochemicals in Gouania longipetala was determined using GCMS analysis. The
extract was prepared using Soxhlet`s extraction method and concentrated at 35oC in hot air oven. GCMS
analyzes phytochemicals in plant by demonstrating the structures of the chemical compounds in it. The gas
chromatogram showed the presence of eight phytochemicals. The molecular mass of the phytochemicals were
established based on the molecular ion in the mass spectra. Identification of the phytochemicals was based on
comparison with National Institute of Standards and Technology (NIST) database. The identified
phytochemicals with their peak area percentages are 11,14-octadecadienoic acid (1.72%), Hexadecanoic acid
also known as Palmitic acid (19.86%), 9,11-octadecadienoic acid (1.33%), 9,12,15-Octadecatrien-1-ol (2.92%),
9-Octadecenoic acid (56.40%), Ethyl palmitate (9.42%), 17-carboxyheptadec-9-en-1-ylium (1.70%) and
Glutaric acid, isobutyl 2-nitrophenyl ester (6.65%). These identified compounds exhibited the following
bioactivities; inhibition of uric acid, urine acidifiers, amino acid decarboxylase activity, arachidonic acid
inhibitor, oligosaccharide provider, decrease endothelial leukocyte and platelet adhesion . Gouania longipetala
therefore contain active phytochemicals that may be beneficial in pharmacognosy. We recommend further work
to be done on its isolation and synthesis.
Abstract:
The Chronopharmacotherapy the drug administration is synchronised with circadian rhythms Formulation development of Microspheres is more reliable formulation as compare to single type dosage formulation due to it avoids dose dumping, as per required drug release profile is achieved For microspheres many polymers are used such as albumin, gelatine, starch, Eudragit, Polyacrylamide (“PAM”) these material loading capacity is high. Micro sponges which are Spherical are called as micro-balloons. Due to its hollow structure it shows good floating properties. In these systems use of Carbon-dioxide (CO2) as gas generating system which are used for floating purpose. The objective of present investigation is to prepared and evaluate a floating pulsatile drug delivery system of Aceclofenac. The strategy adopted for microspheres containing Aceclofenac as a material were prepared by emulsion solvent diffusion technique. Drug and polymer were mixed in dichloromethane and ethanol at 1:1 ratio. The drug and polymer solution were poured in water 50% W/V polyvinyl alcohol maintained at 30-40 C and the solution was stir at 500rpm using mechanical stirrer, The microspheres obtain were washed repeatedly with water until free from poly vinyl alcohol. The developed formulations were evaluated yield of floating microspheres particle size and shape, drug entrapment efficiency in-vitro evolution of floating ability, in-vitro drug release study. On the basis of these evolution parameters it was found that optimised floating pulsatile release formulation F7 showed higher drug entrapment efficiency floating time 6.8 minutes and the drug and polymer 32 1:3 ratio the particle size was increased.
Key Words: Chronopharmacotherapy, Floating pulsatile drug delivery, Aceclofenac.
FORMULATION AND CHARACTERISATION OF TRANSDERMAL PATCHES OF PERINDOPRILSriramNagarajan19
Transdermal drug delivery system (TDDS) has been an increased interest in the drug administration via the skin for both local therapeutic effects on diseased skin (topical delivery) as well as for systemic delivery of drugs. The skin as a site of drug delivery, has a number of significant advantages over many other routes of drug administration, including the ability to avoid problems of gastric irritation, pH and emptying rate effects, avoid hepatic first-pass metabolism thereby increasing the bioavailability of drug, reduce the risk of systemic side effects by minimizing plasma concentrations compared to oral therapy, provide a sustained release of drug at the site of application; rapid termination of therapy by removal of the device or formulation, the reduction of fluctuations in plasma levels of drugs, and avoid pain associated with injections. The transdermal delivery can also eliminate pulsed entry into the systemic circulation, which might often cause undesirable side effects. Main objective of formulating the transdermal system was to prolong the drug release time, reduce the frequency of administration and to improve patient compliance. In the present study, five formulations were prepared using single polymer in different ratios, along with plasticizers and penetration enhancer. Finally it was concluded that Some formulations show formation of brittle patch due to insufficient amount of polymer and in some patches texture of patch is not elegant due to plasticizer concentration for patch preparation. So by increasing concentration of polymer and plasticizer, finally formulation-5 was considered as optimized formula for preparing transdermal patch of Perindopril, where it shown best drug release profile.
Formulation and In-Vitro Evaluation of Fluconazole Loaded Microsponge Gel For...iosrjce
IOSR Journal of Pharmacy and Biological Sciences(IOSR-JPBS) is a double blind peer reviewed International Journal that provides rapid publication (within a month) of articles in all areas of Pharmacy and Biological Science. The journal welcomes publications of high quality papers on theoretical developments and practical applications in Pharmacy and Biological Science. Original research papers, state-of-the-art reviews, and high quality technical notes are invited for publications.
Formulation and Evaluation of Liquisolid Compact of Etoricoxib for Solubility...ijpsmjournal
Liquisolid compact technique is a novel concept for delivery of drug through oral route. This
approach of delivering drug is mostly suitable for lipophilic drug and poorly or water insoluble drugs. The
main objective of present study was to increase the solubility of water in soluble BSc class II drug etoricoxib.
Etoricoxib is alipophilic drug that is practically insoluble in water and exhibit an excessively slow dissolution
rate in class II compound in biopharmaceutics classification system. The liquid solid compacts were prepared
using PEG 400 as non volatile solvent, microcrystalline cellulose as carrier, aerosil 200 as coating material
and Sodium starch glycolate was used as super disintegrating agent. Several formulations of liquid solid
compacts having different drug concentration in PEG 400 (non volatile solvent) with varying ratio of career
to coating material were prepared. The liquid solid compacts were evaluated for Bulk characterization, Flow
properties, solubility studies, drug content, FTIR studies, DSC studies and in vitro drug release studies. The
saturated solubility studies and in vitro drug release studies shows that the increase in solubility of drug and
enhanced drug release rate in liquisolid compacts compared to pure drug. The Formulation F5 andF4 is
considered as best formulation as it has shown highest drug release in short time (1 hr). Our studies showed
that the solubility of the drug can be significantly enhanced with increase in the carrier content there is
increase in the solubility resulting and enhanced drug release rate.
Identification of Bioactive Compounds in the acetone extract of Daedalea eleg...AI Publications
Daedalea elegans is a Nigerian wild (non-edible) higher fungus with great potentials in the pharmaceutical, textile, cosmetics and food industry. This current study investigates the bioactive compounds that can be found in the acetone extract of D. elegans using Gas Chromatography-Mass Spectrometry (GC-MS). There were twenty-eight compounds identified to be present in the acetone extract of the fungi under study and these are Benzoic acid (0.40%), Nonanoic acid (0.14%), Oxetane, 2,2,4-trimethyl- (0.28%), n-Decanoic acid (0.09%), Phthalimide (0.44%) Dodecanoic acid (0.24%), E-2-Hexenyl benzoate (0.21%), 2,4-Difluorobenzene, 1-benzyloxy- (0.16%), Tetratetracontane (0.55%), Isopropylphosphonic acid, fluoroanhydryde (0.28%), Benzene, (1-methylundecyl)- (0.21%), Tetradecanoic acid (0.76%), Cyclohexanepropanol, .alpha.,2,2,6-tetrame (0.56%), Pentadecanoic acid (0.71%), E-2-Hexenyl benzoate (0.32%), Pentadecanoic acid (0.97%), 1-Decanol, 2-hexyl- (0.46%), 9-Tetradecenal, (Z) (1.67), n-Hexadecanoic acid (23.59%) is the second most abundant, Phthalic acid, butyl undecyl ester (1.08%), Eicosanoic acid (0.79%), 9,12-Octadecadienoic acid (Z,Z)- (44.64%) was the highest in quantity, Octadecanoic acid (6.98%), Bis(2-ethylhexyl) phthalate (2.64%), 2,2,4-Trimethyl-3-(3,8,12,16-tetramethyl-heptadeca-3,7,11,15-tetraenyl)-cyclohexanol (1.95%), 9(11)-Dehydroergosteryl benzoate (8.37%), 9(11)-Dehydroergosteroltosylate (1.28%), 4,6-Decadienal, 8-ethyl-10-[4-hydroxy-8-(2-hydroxypropyl)-3,9 (0.22%). These compounds possess activities which includes but not limited to cancer chemotherapy, antifeedant against pine weevil, antifungi agent in topical therapeutic preparation, anti-inflammatory, immunomodulatory, anti-convulsant, antioxidants, hypocholesterolemic, anti-androgenic, nematicide, analgesic, intermediate for food-grade additives, lubricants, greases, rubber, dyes and plastic, antineoplastic agent, biosynthesis of prostaglandins and cell membrane to mention a few. This study has been able to show that D. elegans is a good source of bioactive compounds with great potentials that can be harnessed in various industries.
Molecular docking studies of abelmoschus esculentus for anti diabetics and a...Jing Zang
Okra (Abelmoschus esculentus (L) Moench) or bhendi also known as ladies finger is an important vegetable crop in India, and African regions. Abelmoscus esculentus having the medicinal property of anti inflammatory , anti diabetics, anti oxidant activities . In this studies we are going to analysis the anti diabetics and anti inflammatory property of Abelmoscus esculentus by using molecular docking studies. Diabetics is a major cause of death and the number of new cases, as well as the number of individuals living with Diabetics, is expanding continuously. Now a days It is one of the most common diseases in the worldwide .Foot ulceration remains a major health problem for diabetic patients and has a major impact on the cost of diabetes treatment. One major complication of diabetes is foot ulceration, which occurs in as many as 15–25% of type 1 and type 2 diabetic patients over their lifetimes. The phytochemicals of Abelmoscus esculentus are analysed and optimized with the Arguslab to investigate the interactions between the target compounds and the amino acid residues of the Mafa and Mmp9. All the compound have shown binding pose between from – 3.25 to -7.95 and -7.95 into -11.40 out of ten compound . [E,E] Farenesal with Mafa protein and gossypol with Mmp9 protein show best ligand energy -10.55 and -8.88 Kcal/mol with 1 and 1 hydrogen bond of distance is 3.0 and 2.3 respectively .
Molecular docking studies of gloriosa superba for anti cancer and anti tuberc...Jing Zang
Gloriosa superba is a medicinal plant generally found in western parts of Tamilnadu and kerala in India. Gloriosa superba having the medicinal property of anticancer, antibacterial, antifungal, anti Tuberculosis and mutagenic activities. In this studies we are going to analysis the anti cancer and anti tuberculosis property of Gloriosa superba by using molecular docking studies. Cancer is a major cause of death and the number of new cases, as well as the number of individuals living with cancer, is expanding continuously. Cervical cancer is one of the most common cancers among women worldwide . Tuberculosis is a common and often deadly infectious disease caused by mycobacteria , usually Mycobacterium tuberculosis in humans. Tuberculosis usually attacks the lungs but can also affect other parts of the body. The phytochemicals of Gloriosa superba are analysed and optimized with the Arguslab to investigate the interactions between the target compounds and the amino acid residues of the E7 and DAHP. All the compound have shown binding pose between from – 3.25 to -7.95 and -7.95 into -11.40 out of ten compound .Chrysophanic acid with E7 protein and Colchicine with DAHP protein show best ligand energy -9.52049 and -7.47679Kcal/mol with 1 and 3 hydrogen bond of distance is 2.3 and 2.2,2.9 and 3.2 respectively .
A systemic review on antibiotic use evaluation in paediatricsJing Zang
Drug utilization is the marketing, distribution, prescription, and use of drug in a society, with special emphasis on the resulting medical, social and economic consequences. Antibiotics are valuable discoveries of modern medicine and their definitive and or appropriate use has led to a decline in the morbidity and mortality associated with various infectious diseaseswhile inappropriate use of antibiotics can increase morbidity, mortality, patient cost and bacterial antibiotic resistance.Antimicrobial agents are among the most commonly prescribed drug in Paediatrics. Because of an overall rise in health care costs, lack of uniformity in drug prescribing and the emergence of antibiotic resistance, monitoring and control of antibiotic use are of growing concern and strict antibiotic policies should be warranted. The caution use for antimicrobial agents is very important as their unavailability or resistance can be life threatening. Irrational drug use is a common practice in developing countries. In India, clinician often prescribe three or four drugs to treat the most trivial conditions for the sake of satisfying the patients need to receive drugs or the drug sellers need for profit. Thus drug use evaluation studies are required for all drugs in general and particularly for antibiotics.
A review on medicinal properties of Camel milkJing Zang
Many research findings proved that Camel milk is closer to human milk than any other milk. It is often easily digested by lactose-intolerant individuals. It is rich in healthy vitamins and minerals, especially B vitamins, vitamin C and iron. The lactoferrin in camel milk has antibacterial, antiviral and anti-tumor properties. It contains disease-fighting immunoglobulins which are small in size, allowing penetration of antigens and boosting the effectiveness of the immune system. It is a rich source of insulin and also it containing approximately 52 units of insulin in each liter of camel milk, making it a great treatment option for Type 1 or Type 2 diabetics as well as Gestational Diabetes. This review focused on the medicinal properties of camel milk which will be more useful to generate value added products formation from camel milk.
Formulation and Evaluation of Solid dispersion for Dissolution Enhancement of...Jing Zang
Nifedipine, a calcium channel blocker antihypertensive drug, is a poorly water soluble drug and belongs to BCS class II. The objective of the research work was to formulate and optimize solid dispersions (SDs) of a poorly water soluble drug, nifedipine, with sodium starch glycollate, croscarmellose sodium, eudragit E-100. Solid dispersions were prepared by solvent evaporation techniques in different weight ratios of polymers. The results indicated that homogeneous or heterogeneous conditions during the preparation methods employed governed the internal structures of the polymer matrices while retaining the drug in an amorphous form. The physical mixtures and solid dispersions were subjected to drug content and dissolution test. The best formulation, nifedipine with croscarmellose sodium in 1:7 ratio, among all was further adsorbed on neusilin US2 to form ternary mixture. The increased dissolution was achieved by more than 70percent and 30percent comparatively to the nifedipine API and marketed product respectively. The tablet dosage form prepared from ternary mixture was stable at stressed conditions 40±2°C and 75±5% RH. The release kinetics of drug from formulation and marketed product follows peppas model. The similar factor f2 was within limit for the product at stressed conditions with the product at room temperature at the same time.
Glucose lowering potential of hydromethanolic extract of RauwolfiaJing Zang
The objective of the present study was to evaluate the phytochemistry, acute toxicity and glucose lowering potential of hydromethanolic roots extract (HMREt) of Rauwolfia serpentina. The qualitative analysis of HMREt showed the presence of many important phyto-constituents except anthraquinones, carbohydrates and saponins whereas quantitatively it found rich in total phenols. In acute toxicity study, orally administrated HMREt from 5-250 mg/ kg was observed safe and non-sedative while its doses from 500-2500 mg/kg were found sedative and induced mortalities (17-100%) within 4 hours of administration. The median lethal dose (LD50) of same extract was calculated as 1412.54 mg / kg (log LD50 = 3.15 mg/ kg) from log doses verses probit graph. The HMREt in doses of 50, 100 and 150 mg/kg induced significant percent decrease in blood glucose level at 30, 60 and 120 minutes in normo-hyperglycemic test mice as compared to control and negative control groups (p<0.05). The results concluded that HMREt has glucose lowering potential either by developing glucose tolerance or by pancreatic action in normo-hyperglycemic mice.
Nutritive and Anti-nutritive composition of Wild grown Canavalia gladiata seedsJing Zang
The wild Canavalia gladiata seeds were widely distributed in Nupeland, North Central Nigeria. It was obtained and processed by decoating, sun drying and grinding into powder. Using petroleum ether (40-60oC), the fats was extracted, the protein content, ash content, crude fibre, moisture, carbohydrate with respective values of 3.60±0.14, 11.1±0.83, 4.25±0.11, 3.39±0.27, 5.85±0.47 and 72.3±0.08 % as well as the mineral contents were determined using standard methods. The mineral composition determined from the C. gladiata seeds shows higher values of potassium, zinc, iron and calcium 25.15±0.03, 25.89±0.27, 18.3±0.14 and 17.25±0.49 mg/100 g respectively. This seed analyzed contains low yield of anti-nutritional contents which suggested that, it could be safe for human consumption since it fell below the lethal dose limit. The sample contains reasonable amount of essential and non-essential amino acids with yield varying between 48 and 52%. The presence of unsaturated and saturated fatty acids in the C. gladiata was 96 and 4% respectively. The higher percentage of unsaturated fatty acid present makes this seed desirable for consumption by the person with heart diseases. In addition, from the data obtained this oil becomes attractive options for commercial purposes since it is suitable for the manufacture of soaps, lubricating oil, candles as well as pharmaceutical industries.
Pharmacovigilance in South Africa: Undocumented undergraduate training and pr...Jing Zang
Pharmacovigilance is a clinical discipline that is gaining more and more attention worldwide and in Africa. The rolling out of large scale programs on HIV/AIDS, tuberculosis and malaria has heightened the need to step up efforts to have pharmacovigilance concepts to be operationalized in clinical practice. A quick search in PubMed and Google Scholar and a review of available literature was conducted in order to establish whether medical, nursing and pharmacy undergraduate students are taught pharmacovigilance concepts and skills for effective practice. It seems that there is a paucity of data on the undergraduate training in pharmacovigilance in South Africa. It may be that there might be inadequate training on pharmacovigilance during undergraduate training of medical, nursing and pharmacy students in South Africa. More studies are needed to document the views and experiences of South African students and healthcare professionals on training and practice of pharmacovigilance.
Black Seed (Nigella sativa) Possess Bioactive Compounds Act as Anti-Helicobac...Jing Zang
ABSTRACT
Gastrointestinal associated problems are physiological processes effects almost every individual at some stage of their life. Among the various plants studied previously Nigella sativa possess numerous therapeutic properties including its anti-ulcer potential. This seed carries significant anti-ulcer properties arbitrated by antimicrobial activities specifically against gastric damage induced by Helicobacter pylori. Evidence is available supporting the utilization of NS and its bioactive components in a daily diet for health improvement. This review is envisioned to emphasis on the curative role of NS and to provide an evidence for being a functional food to protect from a range of malaises. An attempt is also made to emphasize aspects that need further investigations for it to be use in clinics in future.
In vitro enzyme inhibition studies on new sulfonamide derivatives of 4-tosyl ...Jing Zang
Sulfonamides are considered to be pharmaceutically important class of compounds. In the present work, N-(2,4-dimethylphenyl)-4-toluenesulfonamide (3) was synthesized by the reaction of 2,4-dimethylaniline (1) and 4-tosyl chloride (2; 4-methylbenzenesulfonyl chloride) using 10% aqueous Na2CO3 solution as reaction medium. At the second step, the synthesized molecule 3 was made to react with different alkyl/aralkyl halides (4a-o) to yield the target compounds, 5a-o, using N,N-dimethylformamide (DMF) as reaction medium and lithium hydride as an activator. The synthesis of all the compounds was verified by spectral techniques using IR, 1H-NMR and EIMS; and further examined for their anti-enzymatic activities. The synthesized compound 5f represented a suitable inhibitory potential against α-glucosidase and lipoxygenase enzymes.
In vitro sun screening activity of Sri Lankan orthodox black tea (Camellia Si...Jing Zang
Currently, there is demand for the development of herbal sunscreen formulations to suppress harmful effects of UV rays. In this regard, this study, was conducted to investigate the sun screen potential of Sri Lankan Orthodox black tea (made from buds and top most leaves of Camellia sinensis L plant) using three grades (Dust No:1, Broken Orange Pekoe and Orange Pekoe) using UV spectroscopic technique and Mansur equation. Sun Protection Factor (SPF) value was determined using 20% aqueous extracts (Black tea brews). The results revealed that all three tea samples had markedly high absorbance values (1.4 to 4.2) at 290-320 nm range and SPF values above 15 which are considered as the threshold value for good sunscreen. The SPF value of Dust No:1, B.O.P.F and O.P were respectively 36, 23 and 22. This is a novel finding for Sri Lankan black tea. It is concluded that Sri Lankan black tea, especially, Dust No: 1 can function as an efficient sunscreen agent and has great promise to be developed as cheap, safe and effective topical botanical sunscreen acting via multiple mechanisms (considering its other reported bioactivities).
HPTLC determination of carotenoid profile in the leaf and bark samples of lor...Jing Zang
Influence of host plants on the carotenoid profile of Loranthus longiflorus leaf and bark samples collected from Casuarina equisetifolia and Ficus religiosa host trees were determined by HPTLC method. The methanol extract of L. longiflorus leaf samples obtained from C. equisetifolia host trees showed 9 compounds while it was 8 compounds in the leaf samples collected from F. religiosa host tree. Among the compounds, 5 and 3 compound in each sample, respectively, was identified as carotinoids while the others were unknown. Four compounds from each leaf samples collected from C. equisetifolia (peak no. 4- 6 & 8) and F. religiosa (peak no. 1-3 & 6) host trees showed similar Rf values (0.15, 0.19, 0.23 & 0.53, respectively). Similarly, the methanol extract of L. longiflorus bark sample collected from C. equisetifolia and F. religiosa host trees contained 8 compounds each. Of these compounds only 3 from each sample was identified as carotenoids whereas others were unknown and none of these compounds showed any similar Rf values. One compound from leaf and park samples of L. longiflorus collected from C. equisetifolia (peak no. 6 & 4) and F. religiosa (peak no. 4 & 3) showed similar Rf values (0.23 & 0.26), respectively.
Antinociceptive and Diuretic Activities of Tagetes erecta LinnJing Zang
In the present investigation, the possible antinociceptive and diuretic activities of methanolic extract of Tagetes erecta has been tested in animal models. The methanol extract of both aerial part and root of the plant exhibited significant antinociceptive activity at higher dose (400 mg/kg body weight) in Swiss albino mice. The root extract was found to reduce the writhing more effectively than that of aerial part which is comparable to that produced by aminopyrine, used as standard drug. In addition, crude whole plant extract was also showed efficient diuresis at higher dose 400 mg/kg tested. Diuretic activity was proved by the electrolyte loss ratio (Na+/K+ excretion ratio) and we used furosemide as the reference.
PREVAILENCE OF MIGRIANE IN A LOW INCOME COMMUNITY OF KARACHIJing Zang
Migraine is the most common problem affecting large population, with prevalence frequency 10-12 %. This study was conducted to evaluate the prevalence of migraine in a low income community in Karachi from June-Oct, 2013. Three hundred and seven participants were involved in this study. For this purpose cross-sectional community based questionnaire was designed in accordance with the diagnostic criteria given by International Headache Society. Data collection was carried out by personal visit to patients and through clinics. It was observed that females (65.5%) are more affected from migraine then male. 32.9% housewives reported that they are suffering from migraine. This medical problem is common among youngsters (38.1%) than old citizens. Employees working in different organizations (39.7%), were found to be mostly affected from migraine then self employed persons. Majority of the migraine patients (41%) reported that they are suffering from common symptoms including: photophobia, phonophobia, nausea, vomiting etc. Dietary habits of individuals were found to be closely associated with migraine such as use of caffeine, chocolate are prominent; and their use is common among 75% patients cumulatively. It was evaluated that certain disease conditions i.e. stress (33.6%), depression (22.1%) and anxiety (18.9%) are more common among sufferers of migraine.
ANTIDIABETIC POTENTIAL OF MEMECYLON TERMINALE DALZ EXTRACTS IN ALLOXAN INDUCE...Jing Zang
Memecylon terminale Dalz is an endemic plant that is exclusively present in the Western Ghat region of Southern India. The traditional healers in this region have been using this plant extract to cure disorders such as dysentery, diabetes, diarrhea, piles, haemoptysis, menorrhagia and shown to possess carminative stomachic astringent property. The present study was carried out to evaluate the hypoglycemic activity of different extracts of M. terminale Dalz in alloxan induced diabetic rats. Chloroform and methanolic extracts of M. terminale Dalz leaves were screened for hypoglycemic activity in alloxan induced diabetes in Swiss albino rats. The lipid profile was also examined in diabetic rats administered with these extracts. The efficacy of these extracts was also analyzed for their ability to inhibit α-glucosidase and α-amylase. Of the two extracts, chloroform extract (500 mg/kg body weight) showed dose dependent decrease in blood glucose level which was comparable to that of control after 24 h of extract administration. On the other hand, chloroform extract also showed good lipid profile that was comparable with standard drug. As compared to chloroform extract, the methanolic extract showed good inhibition of α-amylase and α-glucosidase enzyme activity. The results of our study indicate that M. terminale Dalz plant possesses significant protective effects against alloxan induced diabetes. However, detailed structure function analysis of active ingredients of the extract is needed to be validated.
How to Build a Module in Odoo 17 Using the Scaffold MethodCeline George
Odoo provides an option for creating a module by using a single line command. By using this command the user can make a whole structure of a module. It is very easy for a beginner to make a module. There is no need to make each file manually. This slide will show how to create a module using the scaffold method.
it describes the bony anatomy including the femoral head , acetabulum, labrum . also discusses the capsule , ligaments . muscle that act on the hip joint and the range of motion are outlined. factors affecting hip joint stability and weight transmission through the joint are summarized.
This slide is special for master students (MIBS & MIFB) in UUM. Also useful for readers who are interested in the topic of contemporary Islamic banking.
Introduction to AI for Nonprofits with Tapp NetworkTechSoup
Dive into the world of AI! Experts Jon Hill and Tareq Monaur will guide you through AI's role in enhancing nonprofit websites and basic marketing strategies, making it easy to understand and apply.
How to Add Chatter in the odoo 17 ERP ModuleCeline George
In Odoo, the chatter is like a chat tool that helps you work together on records. You can leave notes and track things, making it easier to talk with your team and partners. Inside chatter, all communication history, activity, and changes will be displayed.
Executive Directors Chat Leveraging AI for Diversity, Equity, and InclusionTechSoup
Let’s explore the intersection of technology and equity in the final session of our DEI series. Discover how AI tools, like ChatGPT, can be used to support and enhance your nonprofit's DEI initiatives. Participants will gain insights into practical AI applications and get tips for leveraging technology to advance their DEI goals.
June 3, 2024 Anti-Semitism Letter Sent to MIT President Kornbluth and MIT Cor...Levi Shapiro
Letter from the Congress of the United States regarding Anti-Semitism sent June 3rd to MIT President Sally Kornbluth, MIT Corp Chair, Mark Gorenberg
Dear Dr. Kornbluth and Mr. Gorenberg,
The US House of Representatives is deeply concerned by ongoing and pervasive acts of antisemitic
harassment and intimidation at the Massachusetts Institute of Technology (MIT). Failing to act decisively to ensure a safe learning environment for all students would be a grave dereliction of your responsibilities as President of MIT and Chair of the MIT Corporation.
This Congress will not stand idly by and allow an environment hostile to Jewish students to persist. The House believes that your institution is in violation of Title VI of the Civil Rights Act, and the inability or
unwillingness to rectify this violation through action requires accountability.
Postsecondary education is a unique opportunity for students to learn and have their ideas and beliefs challenged. However, universities receiving hundreds of millions of federal funds annually have denied
students that opportunity and have been hijacked to become venues for the promotion of terrorism, antisemitic harassment and intimidation, unlawful encampments, and in some cases, assaults and riots.
The House of Representatives will not countenance the use of federal funds to indoctrinate students into hateful, antisemitic, anti-American supporters of terrorism. Investigations into campus antisemitism by the Committee on Education and the Workforce and the Committee on Ways and Means have been expanded into a Congress-wide probe across all relevant jurisdictions to address this national crisis. The undersigned Committees will conduct oversight into the use of federal funds at MIT and its learning environment under authorities granted to each Committee.
• The Committee on Education and the Workforce has been investigating your institution since December 7, 2023. The Committee has broad jurisdiction over postsecondary education, including its compliance with Title VI of the Civil Rights Act, campus safety concerns over disruptions to the learning environment, and the awarding of federal student aid under the Higher Education Act.
• The Committee on Oversight and Accountability is investigating the sources of funding and other support flowing to groups espousing pro-Hamas propaganda and engaged in antisemitic harassment and intimidation of students. The Committee on Oversight and Accountability is the principal oversight committee of the US House of Representatives and has broad authority to investigate “any matter” at “any time” under House Rule X.
• The Committee on Ways and Means has been investigating several universities since November 15, 2023, when the Committee held a hearing entitled From Ivory Towers to Dark Corners: Investigating the Nexus Between Antisemitism, Tax-Exempt Universities, and Terror Financing. The Committee followed the hearing with letters to those institutions on January 10, 202
This presentation includes basic of PCOS their pathology and treatment and also Ayurveda correlation of PCOS and Ayurvedic line of treatment mentioned in classics.
Safalta Digital marketing institute in Noida, provide complete applications that encompass a huge range of virtual advertising and marketing additives, which includes search engine optimization, virtual communication advertising, pay-per-click on marketing, content material advertising, internet analytics, and greater. These university courses are designed for students who possess a comprehensive understanding of virtual marketing strategies and attributes.Safalta Digital Marketing Institute in Noida is a first choice for young individuals or students who are looking to start their careers in the field of digital advertising. The institute gives specialized courses designed and certification.
for beginners, providing thorough training in areas such as SEO, digital communication marketing, and PPC training in Noida. After finishing the program, students receive the certifications recognised by top different universitie, setting a strong foundation for a successful career in digital marketing.
MATATAG CURRICULUM: ASSESSING THE READINESS OF ELEM. PUBLIC SCHOOL TEACHERS I...NelTorrente
In this research, it concludes that while the readiness of teachers in Caloocan City to implement the MATATAG Curriculum is generally positive, targeted efforts in professional development, resource distribution, support networks, and comprehensive preparation can address the existing gaps and ensure successful curriculum implementation.
Macroeconomics- Movie Location
This will be used as part of your Personal Professional Portfolio once graded.
Objective:
Prepare a presentation or a paper using research, basic comparative analysis, data organization and application of economic information. You will make an informed assessment of an economic climate outside of the United States to accomplish an entertainment industry objective.
2. Resmi et al., World J Pharm Sci 2013; 1(3): 72-80
73
with Intel Core Duo processor T6500 2.1 GHz, 800
MHz FSB, operating system Windows VistaTM
Home Basic, a hard disk capacity of 320 GB, and
RAM memory 2 GB.
The software used in this study was
SwissPDBViewer v.4.01 which was downloaded
from http://www.expasy.org. ChemOffice 2004
software (by Cambridge Soft Corporation 2003
downloaded from www.cambridgesoft.com).
Portable HyperChem Release 8.0.7 (by Hypercube
Incorporation downloaded from
http://www.hyper.com 2007). Ligand Explorer
Viewer v.3.8 application was data on line from
(http://www.pdb.org/pdb/explore). Program v.4.0.1
ArgusLab downloaded from
http://www.arguslab.com and AutoDockTools
v.3.05 software package program in MGLTools
v1.5.4 (Molecular Graphics Laboratory, The
Scripps Research Institute in 2009 downloaded
from http://mgltools . scripps.edu).
Materials: Three-dimensional structure of the
enzyme tyrosinase which crystallized with kojik
acid with 2.3 Å resolution (PDB code: 3NQ1) by
Sendovski et al. [8] and α-MSH by Giblin et al. [9]
(PDB code: 1B0Q) . Both the 3D structure was
obtained from the data base on line Protein Data
Bank (www.pdb.org). Two-and three-dimensional
structure of curcumin, demethoxycurcumin,
xanthorrizol and acid kojik drawn using the
program package ChemOffice ChemDraw Ultra
2004 that Chem3D Ultra 8.0.3 and 8.0.3.
Method: The study began with the preparation of
ERα (PDB code: 1A52) obtained from the Protein
Data Bank (www.pdb.org). This was done by
downloaded data from the Protein Data Bank Erα,
reduction ERα chains into monomeric form using
SwissPDBViewer v4.01, analysis binding pocket
by Ligand Explorer Viewer bond in the Protein
Data Bank (www.pdb.org) and Q-SiteFinder,
analysis of ligand-receptor interactions with the
Ligand Explorer Viewer in the Protein Data Bank
(www.pdb.org). Next, preparation of ligand
curcumin, demethoxycurcumin, xanthorrizol and
Kojik acid with 3D ChemBio package v.12.0.2
Free Trial and HyperChem v8.0. Professional
Edition. The preparation was done by making the
structure of 2D and 3D using ChemBio program
package 3Ddengan v.12.0.2 Free Trial,
optimization of geometry with HyperChem
software v8.0. Professional Edition and analysing
of molecular properties with QSAR Properties on
the program HyperChem v8.0. Professional
Edition.
To make sure that the AutoDockVina program
used was valid, the model structure was overlayed
with a ligand that had been crystallized using
program HyperChem v8.0. Professional Edition,
redocking ligands had been crystallized into ERα
binding pockets using the program AutoDock Vina
and analysing of validation data.
Further, docking of curcumin, demethoxy
curcumin, xanthorrizol and Kojik acid, enzyme
tyrosinase, and α-MSH using AutoDock Vina
program and last, interpretation of obtained data.
RESULTS AND DISCUSSION
Results Preparation of Ligand Curcumin,
Demethoxycurcumin, Xanthorrizol and Acid
kojik with software ChemOffice 2004 and
Portable HyperChem Release 8.0.7: The first
step in the preparation of the ligand was making a
two-dimensional structure which was then
converted into three-dimensional structures with
ChemDraw Ultra program Chem3D Ultra v8.0.3
and v8.0.3 in Chemoffice program package 2004.
Three-dimensional structure then optimized
geometry to obtain the most stable conformation.
Conformational changes before and after optimized
shown in Fig. 1.
The next step was the analysis of the characteristic
of the ligand using Portable HyperChem Release
8.0.7 software. Ligand analysis results shown in
Table 1.
Principle Lipinski's Rule of Five [10] was used as
a reference to determine the effectiveness of the
theoretical and bioavaibilitas of an oral drug that
was used. Principle Lipinski's Rule of Five is the
first compound mass not more than 500 dalton.
Mass owned by curcumin, demethoxycurcumin,
xanthorrizol and kojik acid had met the criteria as
oral medications which could produce an effect.
Requirements Lipinski's Rule of Five others were
reviewing the physical properties of a compound
was the value of the partition coefficient (cLogP).
Partition coefficient is the ratio of fat solubility
concentration values with the concentration in the
water. cLogP was the calculation of the partition
coefficients obtained by using the software
HyperChem Release 8.0.7 Portable. cLogP showed
lipophilicity of a compound. Partition coefficient of
both curcumin, demethoxycurcumin, xanthorrizol
and kojik acid oral drug met the criteria according
to Lipinski's Rule of Five, which was under five
and less than minus two. Negative sign on the
coefficient of curcumin and kojik acid showed that
the two compounds were hydrophilic. This means
that these compounds would easily be dissolved in
water or body fluids so that the process of
distribution to achieve the longer the cell
3. Resmi et al., World J Pharm Sci 2013; 1(3): 72-80
74
membranes. Unlike the cLogP xanthorrizol which
had close to 5. This suggested that xanthorrizol had
the ability to penetrate the cell membrane was
higher than the other compounds because it was
more lipophilic which xanthorrizol more soluble in
fat than in water or body fluids.
All four compounds have the volume varies. If
viewed from the volume sac active enzyme
tyrosinase (320 Å ³) and α-MSH (43 Å ³), the four
compounds would be difficult to get into the bag
off in full because the volume was greater than the
volume of the bag. Thus, all four of these
compounds into the coffers of active only in part.
Moreover, the principle of Lipinski's Rule of Five
can also be used as a reference to assess the
feasibility of the chemical properties of drug
compounds with the oral. Chemical properties are
taken into account by this principle is the number
of donors and acceptors of hydrogen bonds. Based
on the principle of Lipinski's Rule of Five, a
compound can be medication by mouth if it has a
maximum of five donors and a maximum of 10
acceptors of hydrogen bonds. Curcumin has two
donors and six acceptor hydrogen bonds.
Demethoxycurcumin has two donors and five
acceptor hydrogen bonds. Xanthorrizol have one
donor who also serves as an acceptor of hydrogen
bonds, while the acid kojik have two donors and
four acceptors of hydrogen. The fourth of these
compounds meet the criteria according to the
principles Lipinski's Rule of Five. Number of
donor and acceptor bonding is one of the capital of
the interaction between the five compounds with
amino acids making up the bag off the enzyme
tyrosinase and α-MSH. These atoms provide the
ability for four to interact with sac active through
hydrogen bonding. Hydrogen bond is a bond
between the H atom that has a partial positive
charge with other atoms that are electronegative
and has a lone pair with octets complete, such as O,
N, and F [11]. Overall, the four compounds is
compliant with the rules of Lipinski's Rule of Five,
so it can be said that all four of these compounds
have bioavaibilitas good to be preparation orally.
In addition, curcumin and demethoxycurcumin
have 2 ring aromatics, xanthorrizol only have one
ring aromatic while the kojik acid have no ring
aromatics. Ring aromatic donating properties of
non-polar to a compound. In addition, the ring
aromatics can donate interaction van der Waals
with the amino acids making up the bag off the
enzyme tyrosinase enzyme and α-MSH.
Results of Tyrosinase Enzyme Preparation
(PDB code: 3NQ1) and alpha-melanocyte
stimulating hormone (α-MSH) (PDB code:
1B0Q) were obtained from the Protein Data
Bank: Data enzymes that have been downloaded
from the Protein Data Bank was reduced to a single
chain. Chain used was a chain of the enzyme
tyrosinase. Ligand Explorer Viewer Tool was used
to analyze the amino acids making up the active
enzyme tyrosinase bag and α-MSH. Analysis done
by record amino acids located around kojik acid
and Rhenium atom during crystallization. On the
enzyme tyrosinase, there weree 6 amino acids were
around kojik acid, namely Gly196, Phe197,
Gly200, Pro201, Asn205, Arg209, whereas in α-
MSH contained four amino acids, namely Cys1,
Arg5, Trp6, and Cys7.
To see more precisely the active enclave on a
receptor, used Q Site Finder application.
Active enzyme tyrosinase bag on light blue area
(site 1) with a volume of 320 Å where all the
constituent amino acids in the enzyme tyrosinase
active sac contained on exploler ligand for Q Site
Finder (Table 2).
Similarly, the enzyme tyrosinase, active sac of α-
melanocyte stimulating hormone (α-MSH) were in
light blue area (site 1) with a volume of 43 Å ³. All
the amino acids making up the active α-MSH sac
contained on exploler ligand for Q Site Finder
(Table 3).
In addition, through the Site Q finder can be known
coordinates (x, y, z) of a bag activated receptor. On
the enzyme tyrosinase, the minimum coordinates
were (-19, -28, -3) and maximum coordinates (-1, -
5, 14). Minimum coordinates (-6, -7, -3) and
maximum coordinates (7, 4, 9) for the active α-
MSH bag.
On the enzyme tyrosinase, there is no hydrogen
bonding between the kojik acid and the enzyme
tyrosinase but there is a bond with hydrophobic
amino acids Phe197, Pro201, and Asn205.
Similarly, the enzyme tyrosinase, bonding pouch α-
melanocyte stimulating hormone (α-MSH) do not
form hydrogen bonds with rhenium atom. In
addition, the alpha-MSH α there is a hydrophobic
bond. This is because an atom of rhenium is not a
compound that has a hydrogen bond donor or
acceptor which allows for better interaction with
the receptor through hydrogen bonding and
hydrophobic bonding.
Results Validation Program v3.05
AutoDockTools in MGLTools Program Package
v1.5.2 with Re-Docking Inhibitor crystallized to
enzyme Tyrosinase Pouch: For the validation
process initially made two-and three-dimensional
kojik acid structure. The three-dimensional
4. Resmi et al., World J Pharm Sci 2013; 1(3): 72-80
75
structure was then optimized geometry with AM1
and PM3 methods. The AM1 buildup result better
than PM3 method (AM1 method produces 0.07 Å
RMSD whereas the PM3 method gave 0.8 Å ).
These results indicate that the AM1 method is
better used than PM3. RMSD values showed
similarities with the model structure crystalliser.
Stacking the AM1 method produces models kojik
acid structure similar to the crystal structure kojik
acid. That is, kojik acid can be used to validate the
model program AutoDockTools v3.05.
Value of RMSD (Root Mean Square Deviation) re-
docking kojik acid on tyrosinase worth 1:30 Å.
Because the value of the results of re-docking
RMSD less than 2 Å, then AutoDock v.3.05
software used in this study has been proven valid.
Docking Simulation results Curcumin,
Demethoxycurcumin, Xanthorrizol and Acid
kojik Using v3.05 AutoDockTools Program and
Data Interpretation Results: In the docking
simulation, run used 10 times run with grid points
at 40 x 40 x 40. Formation intended to limit the
grid box, so that other atoms or other parts of the
receptor are not necessary, do not interfere with the
process of docking calculations. Docking
simulations on the enzyme tyrosinase using the
same grid coordinates with re-docking grid box
which wass placed in the middle position of the
ligand, which was at position -12 584, -24 146,
8417 (x, y, z) in Cartesian coordinates.
Interaction energy or free energy is the energy
required for a ligand can enter into binding pockets
and interact with the receptor. The negative sign
indicates that the three compounds curcumin and
others can interact spontaneously with the enzyme
tyrosinase. Curcumin can interact with the enzyme
tyrosinase through the hydrogen bonds and van der
Waals bonding. The hydrogen bonding between the
O atom in curcumin with H atoms in the amino
acid Val218 (1.886 Å). Hydrogen bond is a bond
between the H atom has a partial positive charge
with another atom that is electronegative and has a
lone pair with complete octets, such as O, N, and F
[11]. According Siswandono and Soekardjo [12],
an amino acid which is about 4 - 6A will form van
der Waals interactions. Curcumin forming van der
Waals bonds with several amino acids on
tyrosinase namely Val217 (4,393 Å), Pro201
(4,908 Å), and Gly216 (5,528 Å). Curcumin had
the inhibition constants (Ki) of 1520 µm. This
value was smaller than the value of Ki kojik acid.
This indicated that the strength of the bond
between the curcumin with the tyrosinase enzyme
was stronger than kojik acid. This is evident from
the value of 0.0 µm Ki kojik acid. Ki kojik worth
0.0 M acid, this might due to AutoDockTools
v3.05 software used was not able to detect large Ki
values.
In contrast to curcumin, demethoxycurcumin
interact with the enzyme tyrosinase only through
van der Waals bonding. The absence of hydrogen
bonds in this interaction suggests that the ability to
bind to demethoxycurcumin for tyrosinase smaller
than curcumin. It can be seen from
demethoxycurcumin interaction energy greater than
curcumin. Demethoxycurcumin forming van der
Waals bonds with several amino acids on
tyrosinase which Met184 (5,383 Å), Gly200 (4,014
Å), Pro201 (4,442 Å), Asn205 (4,957 Å), Gly216
(5,396 Å), Val217 (4,527 Å). Demethoxycurcumin
has a Ki value of 5650 µm. This value is greater
than Ki curcumin. Showed inhibition constants of
affinity ligand-receptor binding. Low Ki value
indicates that the ligand has a higher strength than
the Ki values were higher (weaker bond strength).
A good values range of Ki is 10-6
-10-12
M. When
ligands bound to the receptor too powerful, the
ligand will be difficult excreted from the body and
the ability to cause an activity is inhibited, but
when the ligand binds weakly to the receptors, the
ligands will be easily removed before generating an
activity.
Similarly, curcumin, xanthorrizol interact with the
enzyme tyrosinase through the hydrogen bonds and
van der waals interactions. Hydrogen bonds occur
between atoms H on xanthorrizol with O atoms in
the amino acids Asn205 (1.899Å). Xanthorrizol
bonding van der Waals with some amino acids on
tyrosinase which Glu158 (5,757 Å), Phe197 (4,303
Å), Gly200 (4313 Å), Pro201 (5,315 Å), and
Arg209 (4,931 Å). Xanthorrizol has a Ki of 1040
lm. This value is smaller than the kojik acid. Means
of interaction xanthorrizol with tyrosinase stronger
than the acid kojik. Research of Batubara et al.,
(2010) showed that the extract of turmeric
(Curcuma xanthorrhiza) has activity in inhibiting
the enzyme tyrosinase with IC50 of 267.3 ± 6.1 mg /
mL. This value indicates that the concentration
needed to inhibit the enzyme tyrosinase is quite
large. With the value of Ki owned curcumin,
demethoxycurcumin and xanthorrizol showed that
doses in vivo are needed to inhibit the enzyme
tyrosinase larger but smaller than the kojik acid.
At the protein α-MSH, curcumin interacts through
3 hydrogen bonds and Van der Waals interactions.
The hydrogen bonding between the O atoms
contained in curcumin with H atoms contained in
amino acids Cys1 (1,986 Å), His3 (1.733 Å), and
Arg5 (2,204 Å). Curcumin makes three hydrogen
bonds have a high enough affinity to bind to α-
5. Resmi et al., World J Pharm Sci 2013; 1(3): 72-80
76
MSH. It can be seen from the interaction energy of
-5.49 kcal / mol. Number of hydrogen bonds
formed in the ligand-receptor interaction depends
on the presence of atomic H, O, N, or S ligands
which are located around the H atom acts as a
hydrogen bond donor, while O atoms, N, and S acts
as a hydrogen bond acceptor.
According to Bohm and Schneider [13], the range
of hydrogen bond distances are good docking
simulation results are 1.72-2.85 Å. The four
compounds had bond distances in the range, in
other words that the four compounds had a
hydrogen bond distance corresponding
requirements so that they could interact with either
the tyrosinase enzyme through hydrogen bonding.
Curcumin formed van der Waals bond with the
amino acids in α-MSH with DPN4 (4,645 Å) and
Cys7 (4,571 Å). Van der Waals interaction is the
force of attraction between molecules or atoms are
not charged and is located adjacent to the bond
strength of 0.5-1 kcal / mol [11]. According
Siswandono and Soekardjo [12], amino acids that
are about 4-6A will form van der Waals
interactions. Although the van der Waals bonds are
weak, but the sum of van der Waals bonding is a
substantial binding factor, especially for
compounds with high molecular weight. Van der
Waals interactions also give effect to the lipid
solubility of the ligand. The more the van der
Waals interaction that happens it will be easier
ligand is soluble in lipid ligands that can penetrate
the cell membrane to be able to bind to the
receptor. Curcumin has a Ki of 10000 lm. This
value is smaller than the Ki kojik acid. It means
that the bond between the curcumin-enzyme
tyrosinase is stronger than kojik acid.
Demethoxycurcumin have a smaller interaction
energy compared with curcumin, xanthorrizol and
kojik acid. This suggests that demethoxycurcumin
has a higher affinity than the other three
compounds, so demethoxycurcumin more easily
interact with amino acids in the active α-MSH sac.
Demethoxycurcumin interact with α-MSH via 2
hydrogen bonds and van der Waals interactions.
Hydrogen bonds are formed from the O atom to
atom H demethoxycurcumin on His3 amino acids
(2,074 Å) and Arg5 (2.008 Å).
Demethoxycurcumin forming van der Waals bonds
with several amino acids that Cys1 (4.413Å), Glu2
(5,084 Å), DPN4 (4.781Å), and Cys7 (4.400 Å).
Xanthorrizol can interact with α-MSH via 2
hydrogen bonds and van der Waals interactions.
Hydrogen bonds are formed between atoms O on
xanthorrizol with H atoms in the amino acid Trp6
(1.730 Å) and Cys7 (1.780 Å) and van der Waals
bonding with some amino acids are Cys1, Glu2,
His3, DPN4, and Arg5 which has a distance
between 4-6 Å. Unlike the other compounds, 4
kojik acid has hydrogen bonding, but still has a
lower affinity compared with the three compounds.
Kojik acid forming van der Waals interactions with
amino acids Cys1 (4,208 Å) and DPN4 (5,572 Å).
This suggests that the weak acid bound kojik with
α-MSH. It can be seen from the Ki value and the
value of the bond energy is greater than the other
three compounds.
Curcumin, demethoxycurcumin, and xanthorrizol
have a smaller interaction energy than kojik acid
which is a compound synthesis. So it can be said
that all three of these compounds have a high
affinity to bind with the amino acids making up the
active enzyme tyrosinase bag and α-MSH. All three
of these compounds are able to interact as
inhibitors that can later suppress the production of
melanin. This indicates that these three compounds
may provide pharmacological effects as skin
whitening agent as an alternative to the use of acid
kojik [14], who have carcinogenic effects.
Our similar works on indication of
pharmacological effects based on docking
procedure has been published elsewhere [15, 16]
CONCLUSION AND RECOMMENDATION
Based on the research it can be concluded that
curcumin, demethoxycurcumin, and xanthorrizol
spontaneously interact with amino acids in the
active enzyme tyrosinase sac and α-MSH. On the
enzyme tyrosinase, the easiest interaction occurs in
xanthorrizol because the low energy interactions.
Xanthorrizol interact through via the formation of
hydrogen bonds with the amino acids Asn205 and
van der Waals interactions with amino acids
Glu158, Phe197, Gly200, Pro201, and Arg209. On
α-MSH, demethoxycurcumin interact easiest
because the low energy interactions through the
formation of two hydrogen bonds with the amino
acid His3, and Arg5 and form van der Waals
interactions with amino acids Cys1, Glu2, DPN4,
and Cys7. This indicates that these compounds
have a high potential to be used as a bleaching
agent candidates (whitening agent) as an alternative
to the use of kojik acid which have carcinogenic
effects. It is suggested that further in-vivo research
on curcumin, demethoxycurcumin and xanthorrizol
to know the best compounds that have a lower dose
with the highest activity as a skin whitening agent
(skin whitening agent).
6. Resmi et al., World J Pharm Sci 2013; 1(3): 72-80
77
Fig. 1 Three-dimensional structure before and after optimization
(a) curcumin, (b) demethoxycurcumin, (c) kojik acid and (d) xanthorrizol
(a) (b)
Figure 2. Active enclave (a) the enzyme tyrosinase
and (b) α-MSH using Q Site Finder application
(a) (b)
(c) (d)
Fig.3 Docking results in active enzyme tyrosinase pocket
(a) curcumin, (b) demethoxycurcumin (c) xanthorrizol, and (d) kojik acid
8. Resmi et al., World J Pharm Sci 2013; 1(3): 72-80
79
Table 3. Amino acid constituent Pouch Active α-MSH
No
Amino
acids
Ligan
Exsploler
Viewer
Qsite
Finder
1 Cys1 √ √
2 Arg5 √ √
3 Trp6 √ √
4 Cys7 √ √
5 Lys8 - √
Table 4. Top Score Against Enzyme Docking Results tyrosinase
Compound
Parameter
EIa
Kib
Hydrogen bond
Hydrogen
bond
distancec
Amino
acids
residue
Curcumin -6.45 1520
O-KMNH-
Val218
1.886
Phe197,Gly200,
Pro201,Asn205,
Arg209,Gly216,
Val217,Val218
Demethoxy-
curcumin
-6.34 5650 - -
Phe197,Met184,
Gly200, Pro201,
Asn205,Arg209,
Gly216, Val217
Xanthorrizol -6.63 1040
H-XNTO-
Asn205
1.899
Glu158, Gly196,
Phe197, Gly200,
Pro201, Asn205,
Arg209
Kojik acid -3.93 0.0
H-KJK O-
Glu158
H-KJK O-
Asn205
1.780
2.036
Glu158, Gly196,
Phe197, Gly200,
Pro201, Asn205,
Arg209
Note : a
Interaction energy (kcal/mole) obtained from the results of three times the value of the best
repetition docking, b
Inhibition constants (µM) and c
Hydrogen bond distance (Å)
Table 5. Top Score Docking Results Against α-MSH
Compound
Parameter
EIa
Kib
Hydrogen bond
Hydrogenc
bond
distance
Amino acids
residue
Curcumin -5.49 10000
O-KMNH-Cys1
O-KMNH-His3
O-KMNH-Arg5
1.986
1.733
2.204
Cys1, Glu2,
His3,DPN4,
Arg5, Cys7
Demethoxy-
curcumin
-5.95 0.0
O-DKMNH-His3
O-DKMNH-Arg5
2.074
2.008
Cys1, Glu2,
His3,DPN4,
Arg5,Trp6,
Cys7
Xanthorrizol -5.36 7080
O-XNTH-Trp6
O-XNT H-Cys7
1.730
1.780
Cys1,Glu2,
His3,DPN4,
9. Resmi et al., World J Pharm Sci 2013; 1(3): 72-80
80
Arg5,Trp6,
Cys7
Kojik acid -4.06 0.0
O-KJK H-Arg5
O-KJK H-Trp6
O-KJK H-Cys7
H-KJK O-Lys8
1.884
2.018
2.211
1.865
Cys1,DPN4,
Arg5, Trp6,
Cys7, Lys8
Note : a
Interaction energy (kcal/mol) obtained from the results of three times the value of the best repetition
docking, b
Inhibition constants (µM) and c
Hydrogen bond distance (Å)
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