Isolation, in vitro antidiabetic, antioxidant activity and molecular docking studies of pentacyclic triterpenoids from Syzygium alternifolium (wt.) Walp bark
The document describes the isolation and characterization of two pentacyclic triterpenoids, friedelin and 3β-friedelinol, from the stem bark of Syzygium alternifolium. The compounds were tested for their antidiabetic and antioxidant activities. Friedelin and 3β-friedelinol showed significant inhibition of α-glucosidase and α-amylase enzymes, decreasing plasma glucose levels and demonstrating antidiabetic effects. They also exhibited antioxidant properties by scavenging free radicals in the DPPH inhibition assay. Molecular docking studies confirmed the binding of friedelin and 3β-friedelinol to α-glucosidase and
Isolation, in vitro antidiabetic, antioxidant activity and molecular docking ...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.
ABSTRACT- Secondary metabolites or phytochemicals from plants have eminent pharmacological activities such as
anti-oxidative, anti-allergic, antibiotic, hypoglycaemic and anti-carcinogenic. These secondary metabolites protect the
cells from the damage caused by unstable molecules known as free radicals. They can inhibit oxidation of free radicals in
both human body and food system. Food industry uses both natural and synthetic antioxidants to extend shelf life of
products. But the application of synthetic antioxidant has been limited due to its carcinogenicity. Recently research is
being focused on fruit materials, which are considered rich source of antioxidant compounds. In this study the
phytoconstituents of seed extracts of two varieties of Cucumis melo L, namely Cucumis melo cantalupensis and Cucumis
melo reticulatus, were studied for their antioxidant property by DPPH free radical scavenging method. In this
investigation, chloroform, petroleum ether, acetone, aqueous and ethanolic extracts of the fruit seed were made using cold
extraction process. Phytochemical study reveals that anthroquinones, quinines, cardiac glycosides, terpenoids, phenols and
steroids were present in aqueous extract of both the samples. The total phenolic content of their seed extracts were found
to be 8.8 mg GAE/g of dry sample and 9.2 mg GAE/g of dry sample respectively. The phenolic content was found to be
linearly proportional to the antioxidant ability of the samples.
Key-words- Cucumis melo cantalupensis, Cucumis melo reticulates, DPPH, Antioxidant, Phenolic content,
Phytochemicals
Protective effects of commelina benghalensis linn (root) extract on ethanol i...IJSIT Editor
The present study was undertaken to investigate the protective effect and possible mechanism of
alcoholic (AlE) and aqueous extract (AqE) from Commelina benghalensis root (CB) on EtOH-induced hepatic
injury in Wistar rat. Hepatotoxic parameters studied in vivo include serum transaminases (AST, and ALT),
ALP, bilirubin, protein, lipid profile (Cholesterol, triglyceride, VLDL and HDL) and level of antioxidants
together with histopathological examination. Liv 52® was used as a reference hepatoprotective agent
(5ml/kg-1b.w.). AlE and AqE (200 mg/kg-1b.w.) on oral administration decreased the level of AST, ALP, ALT,
bilirubin, cholesterol, triglyceride, VLDL, MDA and increased the level of protein, HDL and antioxidants (SOD,
GSH and CAT) in rats being treated with ethanol (EtOH). Pentobarbitone -induced sleeping time study was
carried out to verify the effect on microsomal enzymes Histopathological observations confirmed the
beneficial roles of MF against EtOH-induced liver injury in rats. Possible mechanism may involve their
antioxidant activity
In vitro antioxidant, antimicrobial and cytotoxic activities of the various e...Akhil Gupta
The present study was designed to investigate antioxidant, antimicrobial and cytotoxic potential of pet ether, chloroform and methanol extracts of Ganoderma lucidum available in Bangladesh.
Present study deals with the investigation of hepatoprotective activity of Tephrosia purpurea Linn stem. Powdered stem was extracted with methanol and subjected for the preliminary phytochemical screening. Acute toxicity study of the extract was carried out following OECD guidelines 423 and found safe upto the dose 2000 mg/kg, p.o. Hepatoprotective activity of extract was evaluated against CCl induced hepatotoxicity in Wistar albino rats. Rats were divided into five groups containing 4 6 mice per group. Group 1 animals were administered with vehicle only, Group II animals were administered with CCl (1.4 ml/kg p.o.) to induced hepatotoxicity, 4 group III animals were administered with silymarin (25 mg/kg) for 7 days and CCl (1.4 ml/kg p.o.) on fifth day, group IV and V animals were administered with 4 methanol extract of T. purpurea stem at 75 and 150 mg/kg, po respectively for 7 days and CCl (1.4 ml/kg p.o.) on fifth day of treatment schedule. Biochemical 4 parameters (SGPT, SGOT, ALP, total bilirubin and direct bilirubin) were assessed in all the experimental animals. Phytochemical investigation of methanol extract of T. purpurea stem revealed the presence of flavanoids, phytosterols, alkaloids and proteins. Methanol extract of T. purpurea stem was exhibited dose dependant hepatoprotective activity comparable to that of silymarin.
Isolation, in vitro antidiabetic, antioxidant activity and molecular docking ...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.
ABSTRACT- Secondary metabolites or phytochemicals from plants have eminent pharmacological activities such as
anti-oxidative, anti-allergic, antibiotic, hypoglycaemic and anti-carcinogenic. These secondary metabolites protect the
cells from the damage caused by unstable molecules known as free radicals. They can inhibit oxidation of free radicals in
both human body and food system. Food industry uses both natural and synthetic antioxidants to extend shelf life of
products. But the application of synthetic antioxidant has been limited due to its carcinogenicity. Recently research is
being focused on fruit materials, which are considered rich source of antioxidant compounds. In this study the
phytoconstituents of seed extracts of two varieties of Cucumis melo L, namely Cucumis melo cantalupensis and Cucumis
melo reticulatus, were studied for their antioxidant property by DPPH free radical scavenging method. In this
investigation, chloroform, petroleum ether, acetone, aqueous and ethanolic extracts of the fruit seed were made using cold
extraction process. Phytochemical study reveals that anthroquinones, quinines, cardiac glycosides, terpenoids, phenols and
steroids were present in aqueous extract of both the samples. The total phenolic content of their seed extracts were found
to be 8.8 mg GAE/g of dry sample and 9.2 mg GAE/g of dry sample respectively. The phenolic content was found to be
linearly proportional to the antioxidant ability of the samples.
Key-words- Cucumis melo cantalupensis, Cucumis melo reticulates, DPPH, Antioxidant, Phenolic content,
Phytochemicals
Protective effects of commelina benghalensis linn (root) extract on ethanol i...IJSIT Editor
The present study was undertaken to investigate the protective effect and possible mechanism of
alcoholic (AlE) and aqueous extract (AqE) from Commelina benghalensis root (CB) on EtOH-induced hepatic
injury in Wistar rat. Hepatotoxic parameters studied in vivo include serum transaminases (AST, and ALT),
ALP, bilirubin, protein, lipid profile (Cholesterol, triglyceride, VLDL and HDL) and level of antioxidants
together with histopathological examination. Liv 52® was used as a reference hepatoprotective agent
(5ml/kg-1b.w.). AlE and AqE (200 mg/kg-1b.w.) on oral administration decreased the level of AST, ALP, ALT,
bilirubin, cholesterol, triglyceride, VLDL, MDA and increased the level of protein, HDL and antioxidants (SOD,
GSH and CAT) in rats being treated with ethanol (EtOH). Pentobarbitone -induced sleeping time study was
carried out to verify the effect on microsomal enzymes Histopathological observations confirmed the
beneficial roles of MF against EtOH-induced liver injury in rats. Possible mechanism may involve their
antioxidant activity
In vitro antioxidant, antimicrobial and cytotoxic activities of the various e...Akhil Gupta
The present study was designed to investigate antioxidant, antimicrobial and cytotoxic potential of pet ether, chloroform and methanol extracts of Ganoderma lucidum available in Bangladesh.
Present study deals with the investigation of hepatoprotective activity of Tephrosia purpurea Linn stem. Powdered stem was extracted with methanol and subjected for the preliminary phytochemical screening. Acute toxicity study of the extract was carried out following OECD guidelines 423 and found safe upto the dose 2000 mg/kg, p.o. Hepatoprotective activity of extract was evaluated against CCl induced hepatotoxicity in Wistar albino rats. Rats were divided into five groups containing 4 6 mice per group. Group 1 animals were administered with vehicle only, Group II animals were administered with CCl (1.4 ml/kg p.o.) to induced hepatotoxicity, 4 group III animals were administered with silymarin (25 mg/kg) for 7 days and CCl (1.4 ml/kg p.o.) on fifth day, group IV and V animals were administered with 4 methanol extract of T. purpurea stem at 75 and 150 mg/kg, po respectively for 7 days and CCl (1.4 ml/kg p.o.) on fifth day of treatment schedule. Biochemical 4 parameters (SGPT, SGOT, ALP, total bilirubin and direct bilirubin) were assessed in all the experimental animals. Phytochemical investigation of methanol extract of T. purpurea stem revealed the presence of flavanoids, phytosterols, alkaloids and proteins. Methanol extract of T. purpurea stem was exhibited dose dependant hepatoprotective activity comparable to that of silymarin.
Healing Effects of Hydroalcoholic Extract of Guava (Psidium guajava) Leaf on ...Dr. Anuj S Parihar
Oral mucositis (OM) is a common inflammatory complication among cancerous patients as an adverse effect of chemotherapy and radiotherapy. The aim of this study is to evaluate the healing effects of hydroalcoholic extract of Psidium
Guajava leaf on oral induced mucositis induced by 5-fluorouracil using histopathologic and tissue antioxidative markers assessment in male dark brown rats. In a prospective randomized double blind animal study, OM was induced in 64 male dark brown rats that allocated in 4 groups by 5-FU (60 mg/kg) on days 0, 5, and 10 of the study. The cheek pouch was scratched with a sterile needle on once daily on days 3 and 4. Starting from day 12, gel base, topical form and 600 mg/kg dietry form of hydroalcoholic extract of Psidium Guajava leaf were administered per day. Pouch histopathology score, superoxide dismutase, glutathione peroxidase, total antioxidant capacity were evaluated on day 14 and 18. DPPH scavenging activity and total phenolic content also were measured. Histopathology scores of mucositis were lower in the systemic and topical treatment groups than the gel base and control groups (P<0.05). Higher activities of SOD, GPX and TAC were detected in the topical and systemic treatment groups in comparison to the others (P<0.05). The extract was rich in total phenolic content as antioxidant. The use of extract of Psidium Guajava leave may be associated with reduced intensity of OM, increased concentration of SOD, GPX and TAC on induced
OM in dark brown rats undergoing 5-FU consumption.
Phytochemical Evaluation and Antioxidant Activity of Holarrhena pubescens Wal...BRNSS Publication Hub
The selected medicinal plant Holarrhena pubescens Wall. ex G.Don belongs to the family Apocynaceae, and it was collected in hillock of Muthu Malai hill in Coimbatore, Tamil Nadu. In the present study, preliminary phytochemical screening of H. pubescens a medicinal plant was carried out. Qualitative phytochemical analysis of these plants confirms the presence of various secondary metabolites such as steroids, tannins, alkaloids, and phenols. The results suggest that the phytochemical properties for curing various ailments possess potential anti-inflammatory, antimicrobial, and antioxidant and leads to the isolation of new and novel compounds. Gas chromatography-mass spectrometry analysis showed the existence of various compounds with different chemical structures. The presence of various bioactive compounds confirms the application of H. pubescens for various ailments by traditional practitioners. However, isolation of individual phytochemical constituents may proceed to find a novel drug. Extracts from H. pubescens showed varying antioxidant (free radical scavenging) activities when compared to Vitamin C, and the results suggest that the antioxidant activity of H. pubecens may contribute to their claimed medicinal property.
The Effect Of Roselle Extract (Hibiscus Sabdariffa Linn.) On Blood Glucose ...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).
Background: Dennentia tripetalla (Pepper Fruit) belongs to the Annonaceae family and is abundant in Nigeria. Its
fruit in folklore medicine is used for treatment of varying ailments. While ample research evidence exists on the
plants fruit and seed, no current study exists on the toxicological profile of the plant leaves.
Methods: qualitative and quantitative phytochemicals and In vitro antioxidant assays were carried out using
standard methods. The acute toxicity study indicates that the LD50 was higher than 2000 mg/Kg body weight. Subchronic
toxicity studies was carried out using five groups of rats. Group 1 served as control, 2–5 received 100 mg/
Kg, 200 mg/Kg, 500 mg/Kg and 1000 mg/Kg body weight orally for 28 days.
Results: Post-administration biochemical analysis indicates there was increased weight in rats administered 100
mg/kg and 200 mg/kg while it reduced in the 500 mg/kg group. Significant elevations of liver function markers
were reported for 200 mg/kg and 500 mg/kg respectively. Serum and hepatic protein profiles remained unaltered.
Renal function analysis revealed elevated serum urea and creatinine for 200 and 500 mg/kg groups, elevated serum
Na+ and Ca+ and reduced serum Cl− for the 500 mg/Kg group. Elevated Kidney K+ and Ca+ levels, reduced Cl−
were significantly observed in 500 mg/Kg group. Significant rise in hepatic and renal lipid peroxidation was
observed in 200 and 500 mg/Kg groups. There were observed disarmament of the antioxidant defense systems
occasioned by rise and drop in tissue (hepatic, renal, testes, heart) Superoxide dismutase (SOD), Catalase (Cat),
Glutathione-s-transferase (GST), Glutathione peroxidase (GPx) activities in the test groups relative to control.
Histopathological examination indicated architectural aberrations at 500 and 1000 mg/kg.
Conclusions: It concluded that the plant had significant phytochemical and antioxidant properties of medical
interest and possessed toxic properties in rats when administered at a dose above 200 mg/Kg over a prolonged
period of time.
Hepatoprotective Effect of Cestrum parqui L. aerial parts and Phytochemical ...Jing Zang
This study deals with the investigation of hepatoprotective effect of 70% methanolic extract from Cestrum parqui aerial parts and determination of the bioactive components of the plant. The hepatoprotective effect of Cestrum parqui methanol extract (100, 500, 1000 mg/kg) was analysed on carbon tetrachloride (CCl4)-induced acute liver injury. The administration of a single dose of 40% CCl4 (1ml/kg b.w.) causes an increase in the activities of serum alanine aminotransferase (ALT) and aspirate aminotransferase (AST) enzymes and so pretreated orally of a dose from Cestrum parqui methanol extract (100, 500, 1000 mg/kg) and silymarin (200 mg/kg) for three consecutive days prior to The administration of a single dose of CCl4 significantly prevented the increase in the activities of these enzymes. Histological analysis showed that Cestrum parqui methanol extract at doses of 500 and 1000 mg/kg and silymarin reduced the incidence of liver lesions including vacuole formation, neutrophil infiltration and necrosis of hepatocytes induced by CCl4. The extract cause a negative result on the antioxidative enzymes, superoxide dismutase (SOD), glutathione peroxidase (GPx), glutathione reductase (GRd) and decreased malondialdehyde (MDA) level in liver, as compared to those in the CCl4-treated group and this suggests that the hepatoprotective activity of the extract is due to the antioxidant effect of the extract. Phytochemical analysis of the methanol extract from Cestrum parqui aerial parts showed that it contained different phytoconstituents, flavonoids, tannins, saponins, alkaloids, terpenes and carbohydrates.
This is an Engg Biotechnology project based on medicinal plant i.e singapore cherry or jamaican cherry tree (scientific name Muntingia calabure ), we did in 2013 in GMIT college Davangere, karanataka, India. i have complete project detail what we did..,
This study was conducted to detect the presence of some active compounds in the extract of Alhagi maurorum plant, which was extracted by soxhlet using methanol as a solvent. The chemical survey showed the presence of glycosides, tannins, alkaloids and phenolic in the studied plant.The anti-inflammatory activity of the plant extract had been studied in vitro by two methods , albumin denaturation inhibition test and hemolysis stimulated by heating test and results showed the effectiveness of the Alhagi maurorum plant extract with compared to standard medicine (Aspirin) and negative control groups.
ANTI - INFLAMMATORY ACTIVITY OF LEAVES OF JATROPHA GOSSYPIFOLIA L.Raju Sanghvi
BY HRBC MEMBRANE STABILIZATION METHOD, Introduction, Preparation of extracts, Chemicals and instruments, In vitro anti – inflammatory activity, Acute oral toxicity study, Discussion
Formulation and Biological Evaluation of Some Selected Medicinal Plants for A...BRNSS Publication Hub
Objective: The aim of the paper is to assess the anti-inflammatory potential of three medicinal plants using two rat models. Materials and Methods: Soxhlet extraction approaches utilized to separate the constituents of interest. Quantitative analysis has been performed to determine the total phenolic and flavonoid content. Three plants extract employed for the ointment formulation by addition of the extract of Artocarpus heterophyllus (AH), Murraya koenigii (MK), and Punica granatum (PG) in polyethylene glycol (PEG) ointment base, a blend of PEG 600 and PEG 4000, and ratio 7:3, respectively. Two rat models based on chemical induced animals employed for the anti-inflammatory potential. Results and Discussion: All three plants including AH Lam., MK Linn., and PG Linn. extracted for the major component and have shown the gallic acid and quercetin as major component for flavonoid and phenol content. The ointment formulation F3 has showed maximum inhibition (80.95%) at 50 mg/kg dose of carrageenan-induced edema and 83.33% inhibition at 100 mg/kg dose. The ointment formulation F3 has showed maximum inhibition (78.57%) at 50 mg/kg dose of histamine persuade edema and 83.33% inhibition at 100 mg/kg dose. F3 ointment formulation is better than the F2 and F1 formulation in inhibition and in all phases showing its reserve of kinins as well as arachidonic acid. Conclusion: Quantitative and pharmacological evaluation indicated that ointment formulations of AH, MK, and PG have exploit for anti-inflammatory activity. The normal extract has shown the least activity but ointment formulations have shown the better result. The ointment formulations containing plant extracts in 10% amount have better wound healing potential.
Protective Effect of Alysicarpus Monilifer L., Against CCl4 induced Hepatotox...ijtsrd
Alysicarpus monilifer L. is a widely used plant in the north coastal districts of Andhra Pradesh, India, has been used in indigenous system of medicine. The roots are used for the treatment of leprosy and urinary troubles. The decoction of roots is prescribed for cough. The boiled leaves are used as purgative. The herb is credited with anti- pyretic, anti- periodic and expectorant properties, febrifuge and also recommended for cutanious scabies and boils and to cure pain. Acute toxicity tests were conducted as per OECD guidelines on Alysicarpus monilifer L. whole plant. The hydro-alcoholic extract of the aerial parts at 200 mg/kg, 400 mg/kg and 800 mg/kg b.w., was tested in Carbon tetrachloride (CCl4) induced hepatotoxicity of rats followed by histopathological examination of the isolated livers of the control and the treated groups . The potential effects in protecting liver function by reducing the elevated levels of various serum biochemical parameters in a dose dependent manner, reducing oxidative stress, and histopathological alterations in the rat model of CCl4 “induced liver damage was demonstrated. The results showed significant protective effect against CCl4 induced hepatotoxicity in albino rats. The study on qualitative phytochemical screening also identified some important bioactive phytochemical principles such as steroids, triterpenoids, saponins, flavonoids, tannins, carbohydrates and glycosides in this plant which were also validated as antioxidants and biologically active phytoconstituents. This report of hepatoprotective activity of Alysicarpus monilifer L. throws light on attenuation of hepatotoxic effects of CCl4 challenged rats by membrane stabilization through antioxidation K. Manikya Kumari | V. Padmaja"Protective Effect of Alysicarpus Monilifer L., Against CCl4 induced Hepatotoxicity in Albino Rats" Published in International Journal of Trend in Scientific Research and Development (ijtsrd), ISSN: 2456-6470, Volume-1 | Issue-4 , June 2017, URL: http://www.ijtsrd.com/papers/ijtsrd114.pdf http://www.ijtsrd.com/biological-science/botany/114/protective-effect-of-alysicarpus-monilifer-l-against-ccl4-induced-hepatotoxicity-in-albino-rats/k-manikya-kumari
Anti-diabetic potentials of Sorbaria tomentosa Lindl. Rehder: Phytochemistry ...RaktimavaDasSarkar
Original Artcle by Falak Naz, Muhammad Zahoor, Muhammad Ayaz, Muhammad Ashraf, Asif Nawaz, Amal Alotaibi.
Presentation prepared by Raktimava Das Sarkar
IOSR Journal of Pharmacy (IOSRPHR), www.iosrphr.org, call for paper, research...iosrphr_editor
IOSR Journal of Pharmacy (IOSRPHR), www.iosrphr.org, call for paper, research paper publishing, where to publish research paper, journal publishing, how to publish research paper, Call for research paper, international journal, publishing a paper, call for paper 2012, journal of pharmacy, how to get a research paper published, publishing a paper, publishing of journal, research and review articles, Pharmacy journal, International Journal of Pharmacy, hard copy of journal, hard copy of certificates, online Submission, where to publish research paper, journal publishing, international journal, publishing a paper
Healing Effects of Hydroalcoholic Extract of Guava (Psidium guajava) Leaf on ...Dr. Anuj S Parihar
Oral mucositis (OM) is a common inflammatory complication among cancerous patients as an adverse effect of chemotherapy and radiotherapy. The aim of this study is to evaluate the healing effects of hydroalcoholic extract of Psidium
Guajava leaf on oral induced mucositis induced by 5-fluorouracil using histopathologic and tissue antioxidative markers assessment in male dark brown rats. In a prospective randomized double blind animal study, OM was induced in 64 male dark brown rats that allocated in 4 groups by 5-FU (60 mg/kg) on days 0, 5, and 10 of the study. The cheek pouch was scratched with a sterile needle on once daily on days 3 and 4. Starting from day 12, gel base, topical form and 600 mg/kg dietry form of hydroalcoholic extract of Psidium Guajava leaf were administered per day. Pouch histopathology score, superoxide dismutase, glutathione peroxidase, total antioxidant capacity were evaluated on day 14 and 18. DPPH scavenging activity and total phenolic content also were measured. Histopathology scores of mucositis were lower in the systemic and topical treatment groups than the gel base and control groups (P<0.05). Higher activities of SOD, GPX and TAC were detected in the topical and systemic treatment groups in comparison to the others (P<0.05). The extract was rich in total phenolic content as antioxidant. The use of extract of Psidium Guajava leave may be associated with reduced intensity of OM, increased concentration of SOD, GPX and TAC on induced
OM in dark brown rats undergoing 5-FU consumption.
Phytochemical Evaluation and Antioxidant Activity of Holarrhena pubescens Wal...BRNSS Publication Hub
The selected medicinal plant Holarrhena pubescens Wall. ex G.Don belongs to the family Apocynaceae, and it was collected in hillock of Muthu Malai hill in Coimbatore, Tamil Nadu. In the present study, preliminary phytochemical screening of H. pubescens a medicinal plant was carried out. Qualitative phytochemical analysis of these plants confirms the presence of various secondary metabolites such as steroids, tannins, alkaloids, and phenols. The results suggest that the phytochemical properties for curing various ailments possess potential anti-inflammatory, antimicrobial, and antioxidant and leads to the isolation of new and novel compounds. Gas chromatography-mass spectrometry analysis showed the existence of various compounds with different chemical structures. The presence of various bioactive compounds confirms the application of H. pubescens for various ailments by traditional practitioners. However, isolation of individual phytochemical constituents may proceed to find a novel drug. Extracts from H. pubescens showed varying antioxidant (free radical scavenging) activities when compared to Vitamin C, and the results suggest that the antioxidant activity of H. pubecens may contribute to their claimed medicinal property.
The Effect Of Roselle Extract (Hibiscus Sabdariffa Linn.) On Blood Glucose ...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).
Background: Dennentia tripetalla (Pepper Fruit) belongs to the Annonaceae family and is abundant in Nigeria. Its
fruit in folklore medicine is used for treatment of varying ailments. While ample research evidence exists on the
plants fruit and seed, no current study exists on the toxicological profile of the plant leaves.
Methods: qualitative and quantitative phytochemicals and In vitro antioxidant assays were carried out using
standard methods. The acute toxicity study indicates that the LD50 was higher than 2000 mg/Kg body weight. Subchronic
toxicity studies was carried out using five groups of rats. Group 1 served as control, 2–5 received 100 mg/
Kg, 200 mg/Kg, 500 mg/Kg and 1000 mg/Kg body weight orally for 28 days.
Results: Post-administration biochemical analysis indicates there was increased weight in rats administered 100
mg/kg and 200 mg/kg while it reduced in the 500 mg/kg group. Significant elevations of liver function markers
were reported for 200 mg/kg and 500 mg/kg respectively. Serum and hepatic protein profiles remained unaltered.
Renal function analysis revealed elevated serum urea and creatinine for 200 and 500 mg/kg groups, elevated serum
Na+ and Ca+ and reduced serum Cl− for the 500 mg/Kg group. Elevated Kidney K+ and Ca+ levels, reduced Cl−
were significantly observed in 500 mg/Kg group. Significant rise in hepatic and renal lipid peroxidation was
observed in 200 and 500 mg/Kg groups. There were observed disarmament of the antioxidant defense systems
occasioned by rise and drop in tissue (hepatic, renal, testes, heart) Superoxide dismutase (SOD), Catalase (Cat),
Glutathione-s-transferase (GST), Glutathione peroxidase (GPx) activities in the test groups relative to control.
Histopathological examination indicated architectural aberrations at 500 and 1000 mg/kg.
Conclusions: It concluded that the plant had significant phytochemical and antioxidant properties of medical
interest and possessed toxic properties in rats when administered at a dose above 200 mg/Kg over a prolonged
period of time.
Hepatoprotective Effect of Cestrum parqui L. aerial parts and Phytochemical ...Jing Zang
This study deals with the investigation of hepatoprotective effect of 70% methanolic extract from Cestrum parqui aerial parts and determination of the bioactive components of the plant. The hepatoprotective effect of Cestrum parqui methanol extract (100, 500, 1000 mg/kg) was analysed on carbon tetrachloride (CCl4)-induced acute liver injury. The administration of a single dose of 40% CCl4 (1ml/kg b.w.) causes an increase in the activities of serum alanine aminotransferase (ALT) and aspirate aminotransferase (AST) enzymes and so pretreated orally of a dose from Cestrum parqui methanol extract (100, 500, 1000 mg/kg) and silymarin (200 mg/kg) for three consecutive days prior to The administration of a single dose of CCl4 significantly prevented the increase in the activities of these enzymes. Histological analysis showed that Cestrum parqui methanol extract at doses of 500 and 1000 mg/kg and silymarin reduced the incidence of liver lesions including vacuole formation, neutrophil infiltration and necrosis of hepatocytes induced by CCl4. The extract cause a negative result on the antioxidative enzymes, superoxide dismutase (SOD), glutathione peroxidase (GPx), glutathione reductase (GRd) and decreased malondialdehyde (MDA) level in liver, as compared to those in the CCl4-treated group and this suggests that the hepatoprotective activity of the extract is due to the antioxidant effect of the extract. Phytochemical analysis of the methanol extract from Cestrum parqui aerial parts showed that it contained different phytoconstituents, flavonoids, tannins, saponins, alkaloids, terpenes and carbohydrates.
This is an Engg Biotechnology project based on medicinal plant i.e singapore cherry or jamaican cherry tree (scientific name Muntingia calabure ), we did in 2013 in GMIT college Davangere, karanataka, India. i have complete project detail what we did..,
This study was conducted to detect the presence of some active compounds in the extract of Alhagi maurorum plant, which was extracted by soxhlet using methanol as a solvent. The chemical survey showed the presence of glycosides, tannins, alkaloids and phenolic in the studied plant.The anti-inflammatory activity of the plant extract had been studied in vitro by two methods , albumin denaturation inhibition test and hemolysis stimulated by heating test and results showed the effectiveness of the Alhagi maurorum plant extract with compared to standard medicine (Aspirin) and negative control groups.
ANTI - INFLAMMATORY ACTIVITY OF LEAVES OF JATROPHA GOSSYPIFOLIA L.Raju Sanghvi
BY HRBC MEMBRANE STABILIZATION METHOD, Introduction, Preparation of extracts, Chemicals and instruments, In vitro anti – inflammatory activity, Acute oral toxicity study, Discussion
Formulation and Biological Evaluation of Some Selected Medicinal Plants for A...BRNSS Publication Hub
Objective: The aim of the paper is to assess the anti-inflammatory potential of three medicinal plants using two rat models. Materials and Methods: Soxhlet extraction approaches utilized to separate the constituents of interest. Quantitative analysis has been performed to determine the total phenolic and flavonoid content. Three plants extract employed for the ointment formulation by addition of the extract of Artocarpus heterophyllus (AH), Murraya koenigii (MK), and Punica granatum (PG) in polyethylene glycol (PEG) ointment base, a blend of PEG 600 and PEG 4000, and ratio 7:3, respectively. Two rat models based on chemical induced animals employed for the anti-inflammatory potential. Results and Discussion: All three plants including AH Lam., MK Linn., and PG Linn. extracted for the major component and have shown the gallic acid and quercetin as major component for flavonoid and phenol content. The ointment formulation F3 has showed maximum inhibition (80.95%) at 50 mg/kg dose of carrageenan-induced edema and 83.33% inhibition at 100 mg/kg dose. The ointment formulation F3 has showed maximum inhibition (78.57%) at 50 mg/kg dose of histamine persuade edema and 83.33% inhibition at 100 mg/kg dose. F3 ointment formulation is better than the F2 and F1 formulation in inhibition and in all phases showing its reserve of kinins as well as arachidonic acid. Conclusion: Quantitative and pharmacological evaluation indicated that ointment formulations of AH, MK, and PG have exploit for anti-inflammatory activity. The normal extract has shown the least activity but ointment formulations have shown the better result. The ointment formulations containing plant extracts in 10% amount have better wound healing potential.
Protective Effect of Alysicarpus Monilifer L., Against CCl4 induced Hepatotox...ijtsrd
Alysicarpus monilifer L. is a widely used plant in the north coastal districts of Andhra Pradesh, India, has been used in indigenous system of medicine. The roots are used for the treatment of leprosy and urinary troubles. The decoction of roots is prescribed for cough. The boiled leaves are used as purgative. The herb is credited with anti- pyretic, anti- periodic and expectorant properties, febrifuge and also recommended for cutanious scabies and boils and to cure pain. Acute toxicity tests were conducted as per OECD guidelines on Alysicarpus monilifer L. whole plant. The hydro-alcoholic extract of the aerial parts at 200 mg/kg, 400 mg/kg and 800 mg/kg b.w., was tested in Carbon tetrachloride (CCl4) induced hepatotoxicity of rats followed by histopathological examination of the isolated livers of the control and the treated groups . The potential effects in protecting liver function by reducing the elevated levels of various serum biochemical parameters in a dose dependent manner, reducing oxidative stress, and histopathological alterations in the rat model of CCl4 “induced liver damage was demonstrated. The results showed significant protective effect against CCl4 induced hepatotoxicity in albino rats. The study on qualitative phytochemical screening also identified some important bioactive phytochemical principles such as steroids, triterpenoids, saponins, flavonoids, tannins, carbohydrates and glycosides in this plant which were also validated as antioxidants and biologically active phytoconstituents. This report of hepatoprotective activity of Alysicarpus monilifer L. throws light on attenuation of hepatotoxic effects of CCl4 challenged rats by membrane stabilization through antioxidation K. Manikya Kumari | V. Padmaja"Protective Effect of Alysicarpus Monilifer L., Against CCl4 induced Hepatotoxicity in Albino Rats" Published in International Journal of Trend in Scientific Research and Development (ijtsrd), ISSN: 2456-6470, Volume-1 | Issue-4 , June 2017, URL: http://www.ijtsrd.com/papers/ijtsrd114.pdf http://www.ijtsrd.com/biological-science/botany/114/protective-effect-of-alysicarpus-monilifer-l-against-ccl4-induced-hepatotoxicity-in-albino-rats/k-manikya-kumari
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Anti-diabetic potentials of Sorbaria tomentosa Lindl. Rehder: Phytochemistry ...RaktimavaDasSarkar
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Presentation prepared by Raktimava Das Sarkar
IOSR Journal of Pharmacy (IOSRPHR), www.iosrphr.org, call for paper, research...iosrphr_editor
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Antidiabetic and Cytoprotective Effect of Ethanolic Extract of SalaciaNitida ...IOSRJPBS
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Natural remedies from medicinal plants are considered to be effective and safe alternative treatment for liver injury. The present study was conducted to evaluate the hepatoprotective activity of methanolic extract of whole plant of Pulicaria wightiana in wistar rats. The studies were conducted using the two popular inducing agents Paracetamol (2 g/kg, p.o.) in 1% NaCMC and Carbon tetrachloride (1 ml/kg). Silymarin (100 mg/kg, p.o.) was used as reference drug in the respective models. The effect was estimated by measuring the enzymatic levels and histo- pathological studies. The methanolic extract of whole plant of Pulicaria wightiana has shown very significant hepatoprotection against both Paracetamol and CCl4 - induced hepatotoxicity study models in wistar rats. This was evidenced by marked reduction in marker enzymes in serum. Histopathological studies also confirmed the hepatoprotective nature of the extract
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.
ABSTRACT- The invitro anti-inflammatory activity of various solvent fractions of Parkia biglobosa fruit bark was investigated using human red blood cell membrane stabilization, heat-induced hemolysis and protein denaturation methods. All the extracts of P. biglobosa fruit bark showed a concentration dependent increase in anti-inflammatory activity. The anti-inflammatory activity of the crude extract (60.8%, 58.3%, 78.2%) and last remaining aqueous extract (61.1%, 54.1%, 77.2%) have the maximum membrane stabilization, protection against hemolysis and albumin denatura-tion respectively which was comparable to Diclofenac sodium (61.4%, 60.6%, 100%) at 400μg/ml concentration. This study suggests that P. biglobo-sa fruit bark posses enough potential to reduce inflammation, hence directs the importance of further research and development of novel anti-inflammatory agents. Key words- Invitro anti-inflammatory, fruit bark, HRBC membrane stabilization, hemolysis, protection
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Pharmaceutical industries are still in the hunt of effective scavengers for free radicals from the unexplored
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belief that 'Green Medicine' is safe and more dependable than the costly synthetic drugs, which have adverse side effects.
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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).
Research on Diabetes and hepatotoxicity in wistar rat By Nitin Kale final 24...NitinKale46
Thyroid hormone is the hormone that’s mainly responsible for controlling the speed of your body’s metabolism. In infants, thyroid hormone is critical for brain development. Your thyroid, a small, butterfly-shaped gland located at the front of your neck under your skin, makes and releases thyroid hormone. It’s a part of your endocrine system.A naturally occurring coumarin called Scopoletin (SPl) has been found to have anti-inflammatory, anti-diabetic, anti-microbial, and anti-cancer characteristics. Scopoletin has been proposed to act through the antioxidant Nrf2 pathway, the pro-inflammatory NF-B pathway, the Stat-3 pathway, the hypoxia signalling pathway, the Wnt-ꞵ signalling pathway, the Notch signalling pathway, the autophagy pathway, the hypoxia signalling pathway, and other signalling pathways, depending on the cell type, organ, experimental model, and disease studied
DOI: 10.21276/ijlssr.2016.2.3.16
ABSTRACT- The present research article was described about the hypotriglycerdemic activity of Withania coagulans
bud extract. Withania coagulans Dunal belonging to the family Solanaceae is a small bush which is widely spread in
South Asia. The biological activity of with anolides from Withania coagulans has antihyperglycaemic activity and the
plant is commonly called as Indian cheese maker due to the milk coagulation characteristics of the bud. The present study
was to investigate preliminary studies shows satisfactory result. The chromatographic studies like TLC, HPTLC and
HPLC show good spot. HPTLC shows maximum height and area of 18.83%.HPLC shows maximum peak at 1.867
minutes having area coverage of 87.4%.The free radical scavenging activity of chloroform fraction (CF) of a crude drug
shows 510μg/ml of scavenging activity. The IC50 value for MTT assay was found to be 84.7μg/ml. The GLUT4 study
shows significant uptake of glucose. PPAR gamma activity regulation of glucose disposal and insulin sensitivity in the
skeletal muscles shows concentration dependence response using standard Pioglitazone. The bud of Withania coagulants
will be a promising medicine for more ailments.
Key-words- Withania coagulants, Hypotriglycerdemic, HPLC, HPTLC, GLUT-4, MTT assay
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This pdf is about the Schizophrenia.
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Isolation, in vitro antidiabetic, antioxidant activity and molecular docking studies of pentacyclic triterpenoids from Syzygium alternifolium (wt.) Walp bark
1. IOSR Journal of Pharmacy and Biological Sciences (IOSR-JPBS)
e-ISSN: 2278-3008, p-ISSN:2319-7676. Volume 10, Issue 6 Ver. II (Nov - Dec. 2015), PP 22-27
www.iosrjournals.org
DOI: 10.9790/3008-10622227 www.iosrjournals.org 22 | Page
Isolation, in vitro antidiabetic, antioxidant activity and molecular docking
studies of pentacyclic triterpenoids from Syzygium alternifolium (wt.) Walp
bark
N.V.L Suvarchala Reddy Va,b
, M. Akhilac
, C.V.S Subrahmanyamd
,
G. Trimurtulue
,N.M. Raghavendrac,f
a, d
Depatment of Pharmacology, GokarajuRangaraju College of Pharmacy, Osmania University,
Hyderabad, India
b
Jawaharlal Nehru Technololgical University, Hyderabad, India
c
Depatment of Pharmaceutical Chemistry, GokarajuRangaraju College of Pharmacy, Osmania University, Hyderabad, India
e
LailaNutraceuticals, Vijayawada, India
f
Department of Applied Pharmacology, FundaçãoOswaldo Cruz, Rio de Janeiro, Brasil
Abstract: Diabetes mellitus type 2 is a metabolic disorder characterized by hyperglycemia including insulin resistance and
relative lack of insulin. Type 2 diabetes is expected to reduce ten-year-shorter life expectancy. In this research article, we
have isolated two terpenoids from the stem bark of Syzygium alternifoliumby column chromatography.The isolated
compounds were identified as friedelin and 3β-friedelinol terpenoids by 1H-NMR, 13C-NMR, and Mass spectroscopy.
Isolated compounds were screened for in vitro enzyme inhibition assays against α-glucosidase & α-amylase; and were found
decrease plasma glucose level significantly showing antidiabetic activity. Isolated compounds also exhibited significant
radical scavenging antioxidant activity by DPPH inhibition assay. The results of in vitro experimentation were confirmed by
the molecular docking studies of the isolated terpenoids on α-glucosidase and α-amylase enzymes.The present
researchreveals the antidiabetic and antioxidant activity of isolated terpenoids from stem bark of Syzygium alternifolium
against diabetes mellitus type 2 disorders.
Keywords:α-glucosidase,α-amylase, DPPH,Syzygiumalternifolium, terpenoids and docking
I. Introduction
Type 2 diabetes is a public health problem that is characterized by tissue resistance to insulin combined with a
relative deficiency in insulin secretion [1,2,]. On the other hand, diminished glucose-induced insulin secretion with shrinkage
in pancreatic cell mass will ultimately lead to postprandial hyperglycemia [3]. Postprandial hyperglycemia is an independent
risk factor for cardiovascular disease, stroke and mortality; it initiates a cascade of pro-atherogenic and pro-thrombotic events
[4]. Oxidative stress is also considered to be the major cause in the development of type-II diabetes. In 2011, about 366
million people suffered with diabetes globally and this is expected to increase to 552 million by 2030 [5]. One recent study by
ICMR-INDIA reported that about 62.4 million type-II diabetic people are from India. This statistics are expected to increase
to 101 million by the year 2030 [6].
Currently, the methods used for treating the various types of diabetes can be classified into oral hypoglycemic drugs
and insulin injection therapy. However, in taking these hypoglycemic drugs, patients still encounter serious side effects, such
as abdominal distention, abdominal pain, diarrhea, gastrointestinal spasmodic pain, constipation, bowel gurgling, nausea,
vomiting, anorexia, fatigue, headache, dizziness, skin itching and others.An effective inhibition of α-glucosidase enzyme
(preventing postprandial hyperglycemia) and α-amylase (antioxidant activity) is a good strategy for the prevention or
treatment of Type 2 diabetes, hypolipoproteinemia and obesity.
Plant-based products have been determined to function in the regulation pathophysiological signaling pathways in
diabetes and exhibit anti-diabetic activity [7,8]. The hypoglycemic effect of some herbal extracts have been established in
human and animal models of type-II diabetics and some of the conventional drugs have been derived from the active
molecules of these herbs. For example, metformin a less toxic and potent oral hypoglycemic was developed from plant
galgeaofficinals[9]. Among natural compounds, pentacyclic triterpenoids (PTs) are a class of pharmacologically active and
structurally rich metabolites which are reported to act on glucose metabolism [10]. PTs may exert their glucose-lowering
effect through multi-target pathways, including α-amylase, α-glucosidase, glycogen phosphorylase, Akt/protein kinase B,
protein tyrosine phosphatase 1B, insulin receptor, the membrane G protein-coupled receptor, glucocorticoid receptor, 11b-
hydroxysteroid dehydrogenase, glyceraldehyde-3-phosphate dehydrogenase and glycerol-3-phosphate dehydrogenase.
Syzygiumalternifolium(Wt.) Walp. (Myrtaceae) is an endemic aromatic tree, distributed in Assam and Andhra
Pradesh, states of India. Locally it is known as mogi/movi. The plant parts were used traditionally as a medicine to cure
various diseases viz., tender shoots and fruits for dysentery, seeds for diabetes and stem bark was used to treat gastric ulcers
[11]. In the present study, we isolated the active constituents from stem bark of Syzygium alternifolium. Isolated compounds
were identified as friedelin and 3β-friedelinol pentacyclic terpenoids. Isolated PTs were screened for antioxidant and
antidiabetic activities by in vitro DPPH inhibition assay, α-amylase and α-glucosidaseenzyme inhibition biochemical assays.
Furthermore, the mechanism of action of the isolated PTs was explored by molecular docking analysis.
2. Isolation, in vitro antidiabetic, antioxidant activity and molecular docking studies of pentacyclic…
DOI: 10.9790/3008-10622227 www.iosrjournals.org 23 | Page
II. Materials And Methods
2.1 Plant material
The bark of Syzygium alternifolium was collected in the month of November 2011 from Seshachalam hills of
Tirupati, Andhra Pradesh. The botanical identity of the plant was confirmed with the help of botanist, Department of Botany,
S. V. University, Tirupati, Andhra Pradesh, India.
2.2 Extraction
The bark of Syzygium alternifolium was chopped into small pieces, cleaned, powdered, air-dried, sieved (mesh size
= 40) and stored in air tight container at room temperature. The powdered plant material (2 kg) was then extracted
sequentially with methanol (MeOH) using soxhlet extractor. The extract (329 gm) was concentrated to dryness using rotary
evaporator. The yield of methanol extract was found to be 16.45% respectively.
2.3 Isolation
Isolated compounds were identified as terpenoids by positive Liebermann’s Burchardt test and Salkowski test.The
stem bark (2 kg) of the Syzygium alternifolium bark was refluxed with methanol of three hours. After refluxing the bark with
methanol, the total filtrate was concentrated to dryness in vacuum at 40 °C leaving behind the methanolic extract (329 gm).
The bark methanol extract of Syzygium alternifolium was partitioned with hexane and ethyl acetate. The respective solubles
were separated. 310 gm of methanol extract was partitioned with 1:4 ratio of hexane solvent (1200 ml) by refluxing for two
hours. The obtained residue was further fractionated with ethyl acetate: hexane (1:4), followed by column chromatography.
The column was packed with silica gel (100-120). 5 g of hexane extract was taken and adsorbed with 15 g of silica gel. The
column was filled with 50 g of silica gel. The bed volume for the column is 100 ml. The fraction was further
chromatographed to give compound 1 (170 mg) and compound 2 (100 mg).
2.4 Biological assays
2.4.1In vitro inhibition of intestinal α-glucosidase enzyme
An inhibitory α-glucosidase activity was performed according to the method by Feng[12]. In this method inhibition
of α-glucosidase enzyme was determined spectrophotometrically in a 96-well microtiter plate which is based on p-
nitrophenyl-α-D-glucopyranoside (PNPG) as a substrate. Everything considered the test samples (Compound 1and 2) 120 μl
each was mixed with 20 μl of enzyme solution [0.8 U/ml α-glucosidase in 0.01 M potassium phosphate buffer]. The whole
mixture was preincubated at 37 °C prior to initiation of the reaction by incorporating the substrate. After the preincubation
period of 15 min, 20 μl PNPG solutions [5.0 mM PNPG in 0.1 M potassium phosphate buffer (pH 6.8)] was incorporated and
then incubated at 37 °C. To terminate the reaction after 15 min of incubation, 80 μl of 0.2 M Na2CO3 in 0.1 M potassium
phosphate buffer was added to the microtiter plate. The percentage inhibition of α-glucosidase activity was determined by
measuring the absorbance of the resultant mixture was recorded at 405 nm.
2.4.2In vitro inhibition of bacterial α-amylase enzyme
The α-amylase inhibitory activity of isolated compounds from Syzygium alternifolium bark, was performed
according to the method of Wan [13]. Samples acarbose (ALD) were mixed and pre-incubated in 20 mM sodium phosphate
buffer (pH 6.7) for 5 min at 37 °C. After that the volume of reaction mixture was made up to 2 ml by incorporation of 1 ml of
2% (w/v) starch dissolved in the buffer, and the whole reaction mixture was incubated for 5 min at 37 °C. After the
incubation, 1 ml of di-nitro salicylic acid (DNS) color reagent was incorporated and kept in boiling water bath precisely for 5
min. Then, the temperature of this mixture was decreased to room temperature by cooling it on ice and added another 6 ml of
deionized water. α-Amylase inhibitory activity was determined by measuring the absorbance of the mixture at 540 nm.
2.4.3 Spectrophotometric DPPH inhibition assay
Antioxidant capacities of compounds 1, 2 were assessed by DPPH free radical scavenging assay [14]. This method
is based on decline of relatively stable radical DPPH to the development of non-radical form in the presence of hydrogen
donating test samples. The test samples depict antioxidant activity by the diminution in purple colored DPPH to the yellow
colored diphenylpicryl hydrazine derivatives. In this method, 2 mL of 0.1 mmol/L solution of DPPH in methanol was blended
with 1 mL of each compound 1 and 2. The different mixtures were incubated at room temperature in a dark room for 30 min.
The absorbance was measured at 517 nm and percentage inhibition of radical scavenging was determined.
2.4.4 Molecular docking analysis
Mode of inhibition of compounds 1 (friedelin) and 2 (3β–friedelinol) on the α-glucosidase enzyme was further
assessed by molecular docking analysis using ligand fit of GLIDE software from Schrodinger Inc[15]. The protein α-
glucosidase (Pdb Code: 3W37) and α-amylase (Pdb Code: 2QV4) was downloaded from Protein Data Bank (PDB). These
proteins were prepared by filling the missing loops and missing side chains using protein preparation wizard application of
Schrodinger drug design software (Maestro 9.1). The proteins were further processed by removing nonreactive water
molecules, and ligand molecules other than crystal ligand. The ionized proteins having the lowest penalty were energy
minimized using the optimized potential for liquid simulations 2005 force field incorporated in the Impref tool of Glide
programme. Then the grid was generated in the processed protein by excluding the crystal ligand in the active site using
receptor grid generation tool of Glide programme (van der Waals radius scaling factor was limited to 1.0 with a partial charge
cut off of 0.25). The chemical structures of compounds 1 (friedelin) and 2 (3β–friedelinol) and acarbose was drawn using
ChemBioDraw software. The ligands (Acarbose, Fredeline and Fredelinol) were subjected to Ligprep simulations to generate
energy minimized 3D structures (300 steps) by investigating tautomeric, stereo chemical, and ionization variations. The
ligprepout ligands were docked flexibly in the protein grids using Glide-extra precision (XP) simulations [16]. Energies of
3. Isolation, in vitro antidiabetic, antioxidant activity and molecular docking studies of pentacyclic…
DOI: 10.9790/3008-10622227 www.iosrjournals.org 24 | Page
residues within 12 Å of grid were used for simulations. Poses having coulomb-vdw energy greater than 0.0 kcal/mol and
poses having RMS deviation 0.5Å were discarded. Finally the interactions were scored based on non-bonded interactions.
III. Results And Discussion
3.1 Chemistry
The hexane-Et2O (1:1, v/v) extracts of the root barks of stem bark of Syzygium alternifolium was subjected to
multiple chromatographic steps, involving vacuum liquid chromatography, medium-pressure liquid chromatography and
preparative TLC, on silica gel to yield two friedelane-type triterpenoids. The structures of the new compounds 1–2(Table 1)
were deduced as described below.
3.1.1 Compound 1
The compound 1 was obtained as white crystalline powder with a melting point of 259 °C,Rf(cm) 0.71 (solvent
system-hexane: ethyl acetate) (8:2). The molecular formula of compound 1 was shown to be C30H50O based on the positive
ion LC-MS [m/z 427.5 (M+H)+
and 449.4 (M+Na) +
] analysis. The IR spectrum showed bands at 2972, 2945 (CH3
asymmetric and symmetric stretching); 2895, 2870 (CH2 asymmetric and symmetric stretching); 1714 (OH stretching), 1454,
1386, 1246 (C=C aromatic skeletal bands). In the 1
H-NMR spectrum (CDCl3, 400 MHz) quartet signal integrating for one
proton at (δ 2.40q) assigned to H-4. The resonances of eight methyls δ 0.72 (s, 3H, H-24), 0.87 (s, 3H, H-25), 0.87 (d, 3H,
J=6.5Hz, H-23), 0.94 (s, 3H, H-30), 1.01 (s, 3H, H-29), 1.003 (s, 3H, H-27), 1.005 (s, 3H, H-26) and 1.18 (s, 3H, H-28).
Eleven methylene protons showed multiplet signals at δ2.2 and 2.30 (H-2); δ1.956 and1.75 (H-1); δ1.70 and 1.58 (H-6:);
δ1.58 and1.55 (H-7); δ1.54 and1.50 (H-11); δ1.45 and1.43 (H-12); δ1.40 and1.39 (H-15); δ δ1.40 and1.39 (H-16); δ1.35
and1.32 (H-19); δ1.29 and1.28 (H-21); and δ 1.25 and 1.20 (H-22). The remaining three methine protons were seen as
multiplets at δ 1.28 (3H, J = 6.5Hz, H-8, H-10 and H-18). The 13
C-NMR spectrum of compound 1 indicated the presence of
30 carbon resonances. The DEPT spectrum indicated the presence of carbonyl at δ 213.07 including seven quaternary
carbons, four CH carbons, ten CH2 carbons and eight CH3 carbons. Since the molecular formula indicative six units of
unsaturation, this compound 1 was concluded to be pentacyclic triterpene with a ketone group. The presence of signals due to
one secondary and seven quaternary methyls in the 1
H-NMR spectrum suggested the friedelane skeleton. The 1
Hand 13
C-
NMR spectral data of compound 1 indicates that it belongs to was identified as Friedelin. The identification of friedelin was
confirmed by comparison of the reported spectral data with compound [17].
3.1.2 Compound 2
The compound 2 was obtained as white crystalline powder having a melting point of 294 °C, Rf(cm) 0.71(solvent
system-hexane: ethyl acetate) (8:2). The molecular formula of compound 2 was shown to be C30H52O based on the positive
ion LC-MS [m/z 428.4(M)+
and 429.3 (M+H)+
] analysis. The IR spectrum showed bands at 3473 (OH stretching),3003
(aromatic CH stretching), 2978, 2943 (CH3asymmetric and symmetric stretch), 2872, 2837 (CH2 asymmetric and symmetric
stretch) and 1477, 1384 (aromatic C=C skeletal bands). The 1
H NMR spectrum (CDCl3, 400 MHz) gave a peak at δ 3.73
which corresponds to H-3. In the HMBC spectrum C-1 showed correlations with H-3 and H-10. H-3 resonated at δ 3.73, ddJ
= 10.8, 4.6 Hz, the HMBC correlations and this chemical shift value allowed us to place the hydroxyl functionality at this
position (C-3). The resonances of eight methyls δ 0.85 (s, 3H, H-25), 0.93 (s, 3H, H-24), 1.06 (s, 6H, H-29, H-30), 0.99 (d,
3H, H-23), 1.00 (s, 3H, H-27), 1.01 (s, 3H, H-26), 1.16 (s, 3H, H-28). Eleven methylene protons showed multiplet signals at
δ1.90 and 1.75 (H-2); δ1.85 and1.70 (H-1); δ1.53 and 1.50 (H-6:); δ1.51 and1.49 (H-7); δ1.47 and1.39 (H-11); δ1.45 and1.43
(H-12); δ1.43 and1.39 (H-15); δ1.42 and1.38 (H-16); δ1.36 and1.34 (H-19); δ1.35 and1.33 (H-21); and δ 1.24 and 1.19 (H-
22). Out of remaining four methine protons, methine proton showed multiplet at δ 1.55 (m, J= 6.0Hz, H-4), while others were
seen at 1.25-1.32 (3H, J = 6.8Hz, H-8, H-10 and H-18).H-10 resonated at δ 1.25, ddJ=6.8 Hz the multiplicity, dd was due to a
coupling of this proton with H-1 proton. C-3 (δ- 72.20) showed correlations with H-2 and H-23. These correlations and the
chemical shift value supported to phase the hydroxyl functionality at C-3 and methyl a group (C-23) at C-4. Further, in the
1D proton NMR spectrum, the methyl group at C-23 split in to a doublets, which was due to the coupling of these methyl
protons with H-4 and fits the characteristic of this methyl group (C-23) at C-4. C-4 showed correlation with H-2, H-23 and H-
24 and the quaternary carbon C-3 showed correlations with H-1, H-3, H-6 and H-24. These correlations supported the
attachment of C-23 methyl group at C-4 and C-24 methyl group at C-5. The methyl protons at H-26 showed correlations with
C-12, C-13, C-14 and C-18. These correlations allowed us to place the C-26 methyl group at C-13 and C-27 methyl a group
at C-14 respectively. The methyl protons at H-28 showed correlations with C-16, C-17, C-18 and C-22. These correlations
allowed us to place C-28 methyl group at C-17. Finally, C-29 showed correlations with H-19, H-21 and H-30; H-30 showed
correlations with H-19, H-21 and H-29. C-20 showed correlations with H-19, H-21, H-29 and H-30; C-21 showed
correlations with H-22,H-29 and H-30 all these correlations supported the attachment of both C-29 and C-30 methyl groups
to the same carbon at C-20 and the compound is an oleane type triterpenoid. The β orientation of the hydroxyl group at C-3
was confirmed by comparing the proton coupling between H-3 and H-4 and H-2 confirms the stereochemistry.
The 13
C-NMR spectrum of 2 indicated the presence of 30 carbon resonances. The DEPT spectrum indicated the
presence of six quaternary carbons, five CH carbons, eleven CH2 carbons and eight CH3 carbons; one of the carbons
resonated at δ72.8 and indicative of presence of hydroxyl group.These data of compound 2 had good agreements with the
reported data of 3β–friedelinol[18].
3.1.3 Biological evaluation
Pentacyclic triterpenoids (PTs) have been reported as naturally occurring active constituents having regulatory
action on glucose metabolism by many biochemical mechanisms including inhibition of α-glucosidase and α-amylase. α-
glucosidases is membrane bound enzyme integrated in the epithelium of the small intestine and is implicated for the last step
of carbohydrate hydrolysis to create absorbable monosaccharide. Starch is the main dietary carbohydrate cause of glucose and
4. Isolation, in vitro antidiabetic, antioxidant activity and molecular docking studies of pentacyclic…
DOI: 10.9790/3008-10622227 www.iosrjournals.org 25 | Page
diabetic complications depends upon the rate and extent of digestion of glucose from starch by the pancreatic α-amylase and
intestinal α-glucosidase [19]. Disaccharides and oligosaccharides are broken down by the pancreatic α-amylase, followed by
intestinal α-glucosidase enzyme which catabolizes disaccharides into glucose [20].The isolated terpenoidscompounds were
evaluated for the inhibitory activity against α-glucosidase and α-amylase protein. Table 2 shows the inhibitory activity of
terpenoidsagainst α-glucosidase and α-amylase in the percentage inhibition at 10-50µM concentration. Compound 2 (3β–
friedelinol) inhibited the enzymes α-glucosidase and α-amylase with 15.57 and 36.35 percentage respectively and compound
1 (fredelin) inhibited the enzymes α-glucosidase and α-amylase with 10.4 and 23.04 percentage respectively. These
terpenoids have shown better antidiabetic activity than marketed α-glucosidase inhibitor acarbose, which showed the
inhibition of 9.46 percentages against both α-glucosidase and α-amylase. These results were in agreement to the in vitro α-
glucosidase inhibition of terpenoids as per reported literature [10,21]. Antioxidants have been known to exert the protective
effects against the oxidative damage and are associated with reduced risk of chronic diseases such as inflammation, diabetes,
carcinogenesis and atherosclerosis [21,22,23]. Isolated PTs when investigated for their efficacy in scavenging free radicals
through DPPH inhibition assay; Compound 2 (3β–friedelinol) was found to have better antioxidant activity, followed by
compound 1 (fredeline) (Table 3).
3.1.4 Molecular Modeling
In this research work, we also sought to give in silico evidence for the binding interaction of isolated compounds 1
(Fredeline) and 2 (3β–friedelinol) against α-glucosidase and α-amylase enzymes. The interactions were scored based on non-
bonded interactions such as lipophilic pair term, hydrophobic enclosure reward, hydrogen bonding, and electrostatic rewards
(Table 4 and Table 5). As expected, compounds 1 and 2 were shown to have efficient antagonism of α-glucosidase and α-
amylase enzymes. Acarbose is a tetrasaccharide possessing multiple free hydroxyl groups capable of forming numerous polar
interactions with the active site of protein.While, compounds 1 (fredeline) and 2 (3β–friedelinol) being non polar in nature,
exhibited enhanced hydrophobic interactions to inhibit α-glucosidase and α-amylase enzymes (Fig 1 and Fig 2). With α-
glucosidase enzyme (Pdbcode: 3W37), compounds 1 (fredeline) and 2 (3β–friedelinol) possess hydrophobic interactions with
Phe476, Trp432, Ile 358, Trp329, Phe601, Ala602 aminoacids. The hydrophobic interaction in acarbose were comparitively
less (Phe 476, Trp432, Met470, Phe601) than polar hydrogen bonding interactions(His626, Asp357(2), Asp568, Arg552,
Asp232). With α-amylase protein (Pdb code: 2QV4), the polar interaction are due to the hydroxyl group of 3β–friedelinol
with Hie305 amino acid. The non-polar interactions of compounds 1 and 2 were found to be with Glu60, Trp58, Leu165,
Val107, Ala106 aminoacids. Acarbose also possess similar interactions with additional hydrogen bonding with various amino
acids (Asp300, Arg195, Glu233, Thr163, and Gln63).
IV. Conclusion
In summary, we report the isolation and characterization of Friedelin and 3β–Friedelinol pentacyclic terpenoids
from the stem bark of Syzygium alternifolium. To our knowledge nobody has reported the identification of these two PTs
from Syzygium alternifolium. The isolated compounds 1 (fredeline) and 2 (3β–friedelinol) PTs showed a showed significant
inhibition of α-glucosidase, α-amylase and DPPH indicating the reduction in high blood glucose level as well as the reduction
in the formation of ROS (Reactive Oxygen Species). Inhibition of these enzymes by compounds 1 (fredeline) and 2 (3β–
friedelinol) was further supported by the molecular docking analysis. Therefore, these properties would be of therapeutic
benefit in insulin resistant states. Future research will be carried out in this direction.
Acknowledgements
We are grateful to the management of GokarajuRangaraju College of Pharmacy, Hyderabad and Laila
Nutraceuticals, Vijayawada for their support and cooperation.
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Table 1: Structural details of isolated compounds from the bark of Syzygiumalternifolium
Compound code Chemical structure IUPAC name Common names
Compound 1
2
3
4
5
10
1
6
7
8
9 14
13
12
11
15
16
17
18
22
21
20
19
O
23
24
25
27
28
26
30 29
(4R,4aS,6bR,8aR,12bS,14aS)-
octadecahydro-4,4a,6b,8a,11,11,12b,14a-
octamethylpicen-3(4H,6bH,14bH)-one
Friedelin
Compound 2
2
3
4
5
10
1
6
7
8
9 14
13
12
11
15
16
17
18
22
21
20
19
HO
23
24
25
27
28
26
30 29
(3S,4R,4aS,6bR,8aR,12bS,14aS)-
docosahydro-4,4a,6b,8a,11,11,12b,14a-
octamethylpicen-3-ol
3β–Friedelinol
Table 2: In vitro enzyme inhibition activity against α- glucosidase and α-amylase
α-Glucosidase α-Amylase
Compound IC50 value ± SEM IC50 value ± SEM
Compound 1 10.40 ± 0.12** 23.04 ± 0.34*
Compound 2 15.57 ± 0.23** 36.35 ± 0.21**
Acarbose 09.46 ± 0.02 09.46 ± 0.02
SEM = Standard Error Mean; **p < 0.001, ***p < 0.0001
Table 3: Inhibition of radical scavenging activity by DPPH assay
Samples IC50 value ± SEM
Compound 1 20.5*** ± 0.39
Compound 2 30.5*** ± 0.22
Ascorbic acid 17.3 ± 1.10
SEM = Standard Error Mean; ***p < 0.0001
Table 4: Scoring Data (kcal/mol) of Glide-XP Docking of Schrodinger (Maestro 9.1) against α-amylase enzyme(PDB
Code: 2QV4)
Ligand Docking Scorea
Lipophilic EvdWb
H-Bondc
Electrod
RotPenale
Acarbose -12.37 -3.87 -4.80 -1.95 0.10
Compound 2 -6.05 -3.27 -0.68 -0.13 0.00
Compound 1 -5.43 -2.93 0.00 -0.01 0.00
a
An estimate of ligand- α-amylase binding energy; b
Lipophilic van der Walls interactions of ligand- α-amylase complex; c
Hydrogen-bonding term; d
Electrostatic interactions of ligand- α-amylase complex; e
Rotational penalty causing the decreased
ligand-protein interactions.
6. Isolation, in vitro antidiabetic, antioxidant activity and molecular docking studies of pentacyclic…
DOI: 10.9790/3008-10622227 www.iosrjournals.org 27 | Page
Table 5: Scoring Data (kcal/mol) of Glide-XP Docking of Schrodinger (Maestro 9.1) against α-glucosidase enzyme
(PDB Code: 3W37)
Ligand Docking Scorea
Lipophilic EvdWb
H-Bondc
Electrod
RotPenale
Acarbose -10.5 -1.94 -4.87 -2.00 0.00
Compound 1 -3.28 -1.17 0.00 -0.12 0.00
Compound 2 -3.57 -1.36 -0.70 -0.11 0.00
a
An estimate of ligand- α-amylase binding energy; b
Lipophilic van der Walls interactions of ligand- α-amylase complex; c
Hydrogen-bonding term; d
Electrostatic interactions of ligand- α-amylase complex; e
Rotational penalty causing the decreased
ligand-protein interactions.
Fig. 1 Superimposition of compound 1, compound 2 and acarbose (line forms) in the
binding site of α-amylase (PDB Code: 2QV4).
Fig. 2 Overlay view of compounds 1, 2 and acarbose (stick forms) in α-glucosidase binding
pocket surrounded by non-polar amino acids (space fill form) (PDB Code: 3W37).