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1 | P a g e
Submitted By-
Mehrab Hossain Ayan
ID: 0242220011091084
Section: 28 B
Department of Pharmacy
Study on glycosides plays an important role in
new drug development
Submitted To-
Dr. Md. Sarowar Hossain
Associate Professor
Department of Pharmacy
Assignment on
Course Code: BPH 122
Course Title: Pharmacognosy-II
Date of Submission: 10 - 04 - 2023
2 | P a g e
Table of Contents
Introduction: ...........................................................................................................................................3
Study of glycosides:.................................................................................................................................3
1. Cardiac glycosides drug development ............................................................................................3
2. Alcoholic glycosides drug development..........................................................................................4
3. Steviol glycosides drug development .............................................................................................4
4. Thioglycosides drug development..................................................................................................4
5. Phenolic glycosides drug development ..........................................................................................4
6. Anthocyanins drug development....................................................................................................5
7. Cyanogenic glycosides drug development......................................................................................5
8. Anthraquinone drug development .................................................................................................5
9. Coumarin drug development..........................................................................................................6
10. Flavonoid glycosides drug development.....................................................................................6
11. Saponin drug development.........................................................................................................6
Conclusion...............................................................................................................................................7
3 | P a g e
Introduction:
Glycosides are compounds that are formed from the combination of a sugar molecule with
another type of molecule, such as a steroid or a flavonoid. They are found in a wide variety of
natural sources, including plants, animals, and microorganisms.
Glycosides have been shown to have a wide range of pharmacological activities, including anti-
inflammatory, antimicrobial, antitumor, and antiviral effects. They also have the potential to
be used as therapeutic agents for a variety of diseases, including diabetes, cardiovascular
disease, and cancer.
In drug development, glycosides are often used as lead compounds for the synthesis of new
drugs. Researchers can modify the structure of a glycoside to improve its pharmacological
properties, such as its solubility, bioavailability, and selectivity. This can lead to the
development of more effective and safer drugs.
In addition, glycosides are also important in drug discovery, where natural sources are screened
for new bioactive compounds. Many plants and other organisms produce glycosides as part of
their defense mechanisms, and these compounds can be isolated and tested for their
pharmacological activities.
Study of glycosides:
The study of glycosides is important in new drug development because many glycosides have
pharmacological properties that can be exploited for therapeutic purposes.
1. Cardiac glycosides
2. Alcoholic glycosides
3. Steviol glycosides
4. Thioglycosides
5. Phenolic glycosides
6. Anthocyanins
7. Cyanogenic glycosides
8. Anthraquinone
9. Coumarin
10. Flavonoid glycosides
11. Saponin
1. Cardiac glycosides drug development
Cardiac glycosides work by inhibiting the enzyme sodium-potassium ATPase, which
regulates the concentration of sodium and potassium ions inside and outside of heart muscle
cells. By blocking this enzyme, cardiac glycosides increase the concentration of calcium
ions inside the cells, which in turn increases the force of contraction of the heart muscle.
However, cardiac glycosides can be toxic at high doses, causing symptoms such as nausea,
vomiting, blurred vision, and heart arrhythmias. Therefore, they must be used with caution
and under the supervision of a qualified healthcare provider.
4 | P a g e
2. Alcoholic glycosides drug development
Alcoholic glycosides can have medicinal properties and are often used in traditional medicine.
However, they can also be toxic if consumed in large quantities. Therefore, it is important to
use caution when using products that contain alcoholic glycosides and to follow dosage
recommendations carefully.
3. Steviol glycosides drug development
While steviol glycosides are primarily used in the food industry, there has been some interest
in their potential use as a therapeutic agent. Research has suggested that these compounds may
have antioxidant, anti-inflammatory, and anti-cancer properties, among others.
However, to date, there has been limited drug development using steviol glycosides. This is
due in part to the fact that these compounds are primarily used as a food additive and have not
been extensively studied for use as a therapeutic agent. Additionally, the regulatory landscape
for developing natural products as drugs can be challenging.
That being said, there have been some promising preclinical studies using steviol glycosides as
a potential treatment for conditions such as diabetes, hypertension, and cancer. More research
is needed to fully understand the therapeutic potential of these compounds and to develop them
into safe and effective drugs.
4. Thioglycosides drug development
Thioglycosides are a class of compounds that have shown promising potential in drug
development. They are glycosides in which the oxygen atom of the glycosidic bond has been
replaced with a sulfur atom. This substitution imparts several unique properties to
thioglycosides, including enhanced stability, bioavailability, and metabolic resistance. As a
result, thioglycosides have been investigated for a variety of therapeutic applications, including
as anticancer, antiviral, and anti-inflammatory agents.
One of the main advantages of thioglycosides as drug candidates is their ability to selectively
target specific cells or tissues. This is due to the fact that many cell surface receptors and
enzymes are glycosylated, meaning they have sugar molecules attached to them.
Thioglycosides can be designed to mimic these sugar structures, allowing them to bind
specifically to the targeted receptor or enzyme. This targeted binding can lead to enhanced
therapeutic efficacy and reduced side effects.
Thioglycosides have also been shown to have broad-spectrum antiviral activity against a range
of viruses, including influenza, HIV, and hepatitis B and C. This is due in part to their ability
to inhibit the attachment and entry of the virus into host cells. Additionally, thioglycosides have
been investigated for their ability to inhibit viral replication and to stimulate the immune system
to fight off viral infections.
5. Phenolic glycosides drug development
The development of phenolic glycosides as drugs involves several stages, including
identification of potential compounds, isolation and purification of the compounds,
pharmacological evaluation, formulation development, and clinical trials.
5 | P a g e
Identification of potential phenolic glycosides can be done through various methods, such as
screening of natural sources, virtual screening, and structure-based design. Once potential
compounds have been identified, they are isolated and purified from natural sources, such as
plants or fungi.
Pharmacological evaluation involves testing the compounds for their efficacy and safety in
preclinical studies, such as in vitro assays and animal models. The most promising compounds
are then selected for formulation development, which involves developing the drug into a
suitable dosage form, such as a tablet or capsule.
6. Anthocyanins drug development
In recent years, there has been growing interest in the potential use of anthocyanins as
therapeutic agents in drug development. Some studies have suggested that anthocyanins may
have a range of pharmacological effects, including anti-cancer, anti-diabetic, and
neuroprotective activities.
However, more research is needed to fully understand the potential benefits of anthocyanins as
drugs, as well as any potential risks or side effects. Additionally, the development of
anthocyanin-based drugs may be challenging due to their complex chemical structures and
potential variability in composition depending on the source of the anthocyanins.
7. Cyanogenic glycosides drug development
There has been some interest in developing drugs based on cyanogenic glycosides. One
example is amygdalin, a cyanogenic glycoside found in the seeds of apricots, peaches, and
almonds. Amygdalin has been investigated as a potential anticancer agent, as it has been shown
to induce apoptosis (programmed cell death) in cancer cells. However, clinical trials have not
shown conclusive evidence of its effectiveness as a cancer treatment.
Another cyanogenic glycoside of interest is dhurrin, found in sorghum plants. Dhurrin has been
shown to have antimicrobial properties, inhibiting the growth of various bacteria and fungi. It
has also been investigated as a potential treatment for chronic pain, as it can activate opioid
receptors in the body.
8. Anthraquinone drug development
Here are some of the recent developments in anthraquinone drug development:
Cancer treatment: Anthraquinones have shown promising results in preclinical studies for the
treatment of different types of cancer, including breast, colon, lung, and liver cancer. Some of
the mechanisms of action that have been identified include inhibiting tumor cell growth,
inducing apoptosis, and suppressing angiogenesis. However, more research is needed to
determine their safety and efficacy in humans.
Anti-inflammatory agents: Anthraquinones have been shown to have anti-inflammatory
properties by inhibiting the production of inflammatory cytokines. They have potential in the
treatment of chronic inflammatory diseases such as rheumatoid arthritis, inflammatory bowel
disease, and psoriasis.
6 | P a g e
Antimicrobial agents: Anthraquinones have been shown to have antimicrobial activity against
a wide range of microorganisms, including bacteria, fungi, and parasites. They have potential
in the treatment of infections caused by drug-resistant pathogens.
Wound healing: Some anthraquinones have been shown to promote wound healing by
increasing the production of collagen and enhancing angiogenesis. They have potential in the
treatment of chronic wounds such as diabetic ulcers.
Neuroprotective agents: Anthraquinones have been shown to have neuroprotective effects by
reducing oxidative stress and inflammation in the brain. They have potential in the treatment
of neurodegenerative diseases such as Alzheimer's and Parkinson's disease.
9. Coumarin drug development
Recent studies have shown that some coumarin derivatives have potent antitumor activity,
making them potential candidates for cancer treatment. Other studies have investigated the use
of coumarin derivatives as anti-inflammatory agents for the treatment of conditions such as
arthritis.
There are also ongoing efforts to develop coumarin-based compounds as potential therapies for
neurodegenerative diseases such as Alzheimer's and Parkinson's. Coumarin has been shown to
have neuroprotective effects and may help prevent the buildup of amyloid-beta protein in the
brain.
10. Flavonoid glycosides drug development
Drug development efforts have focused on the isolation and synthesis of flavonoid glycosides,
as well as the identification of their molecular targets and mechanisms of action. Some of the
challenges in developing flavonoid glycosides as drugs include their low bioavailability and
rapid metabolism, as well as the need to optimize their pharmacokinetic and pharmacodynamic
properties.
One approach to overcome these challenges is to modify the structure of flavonoid glycosides
to improve their stability, solubility, and bioavailability. Another strategy is to use delivery
systems such as nanoparticles or liposomes to enhance their therapeutic efficacy and reduce
toxicity.
Several flavonoid glycosides have already been developed into drugs, including quercetin,
hesperidin, and rutin. These drugs have shown promise in preclinical and clinical studies for
their ability to target a variety of diseases, including cancer, diabetes, and inflammatory
disorders.
11. Saponin drug development
The development of saponin-based drugs is still in its early stages, but researchers are actively
exploring their potential as therapeutics. One approach is to modify the structure of naturally
occurring saponins to improve their efficacy and reduce toxicity. Another approach is to
synthesize saponin-like compounds that mimic the biological activity of natural saponins.
7 | P a g e
One area of research where saponins are being investigated is in the treatment of cancer. Some
saponins have been found to have cytotoxic effects on cancer cells, and they may be useful in
combination with other chemotherapy drugs.
Another area of interest is in the development of saponins as vaccine adjuvants. Saponins have
been shown to stimulate the immune system and enhance the immune response to vaccines.
Conclusion
Overall, the study of glycosides plays a vital role in the discovery and development of new
drugs, and ongoing research in this area has the potential to lead to important advances in
medicine.

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Study on glycosides plays an important role in new drug development

  • 1. 1 | P a g e Submitted By- Mehrab Hossain Ayan ID: 0242220011091084 Section: 28 B Department of Pharmacy Study on glycosides plays an important role in new drug development Submitted To- Dr. Md. Sarowar Hossain Associate Professor Department of Pharmacy Assignment on Course Code: BPH 122 Course Title: Pharmacognosy-II Date of Submission: 10 - 04 - 2023
  • 2. 2 | P a g e Table of Contents Introduction: ...........................................................................................................................................3 Study of glycosides:.................................................................................................................................3 1. Cardiac glycosides drug development ............................................................................................3 2. Alcoholic glycosides drug development..........................................................................................4 3. Steviol glycosides drug development .............................................................................................4 4. Thioglycosides drug development..................................................................................................4 5. Phenolic glycosides drug development ..........................................................................................4 6. Anthocyanins drug development....................................................................................................5 7. Cyanogenic glycosides drug development......................................................................................5 8. Anthraquinone drug development .................................................................................................5 9. Coumarin drug development..........................................................................................................6 10. Flavonoid glycosides drug development.....................................................................................6 11. Saponin drug development.........................................................................................................6 Conclusion...............................................................................................................................................7
  • 3. 3 | P a g e Introduction: Glycosides are compounds that are formed from the combination of a sugar molecule with another type of molecule, such as a steroid or a flavonoid. They are found in a wide variety of natural sources, including plants, animals, and microorganisms. Glycosides have been shown to have a wide range of pharmacological activities, including anti- inflammatory, antimicrobial, antitumor, and antiviral effects. They also have the potential to be used as therapeutic agents for a variety of diseases, including diabetes, cardiovascular disease, and cancer. In drug development, glycosides are often used as lead compounds for the synthesis of new drugs. Researchers can modify the structure of a glycoside to improve its pharmacological properties, such as its solubility, bioavailability, and selectivity. This can lead to the development of more effective and safer drugs. In addition, glycosides are also important in drug discovery, where natural sources are screened for new bioactive compounds. Many plants and other organisms produce glycosides as part of their defense mechanisms, and these compounds can be isolated and tested for their pharmacological activities. Study of glycosides: The study of glycosides is important in new drug development because many glycosides have pharmacological properties that can be exploited for therapeutic purposes. 1. Cardiac glycosides 2. Alcoholic glycosides 3. Steviol glycosides 4. Thioglycosides 5. Phenolic glycosides 6. Anthocyanins 7. Cyanogenic glycosides 8. Anthraquinone 9. Coumarin 10. Flavonoid glycosides 11. Saponin 1. Cardiac glycosides drug development Cardiac glycosides work by inhibiting the enzyme sodium-potassium ATPase, which regulates the concentration of sodium and potassium ions inside and outside of heart muscle cells. By blocking this enzyme, cardiac glycosides increase the concentration of calcium ions inside the cells, which in turn increases the force of contraction of the heart muscle. However, cardiac glycosides can be toxic at high doses, causing symptoms such as nausea, vomiting, blurred vision, and heart arrhythmias. Therefore, they must be used with caution and under the supervision of a qualified healthcare provider.
  • 4. 4 | P a g e 2. Alcoholic glycosides drug development Alcoholic glycosides can have medicinal properties and are often used in traditional medicine. However, they can also be toxic if consumed in large quantities. Therefore, it is important to use caution when using products that contain alcoholic glycosides and to follow dosage recommendations carefully. 3. Steviol glycosides drug development While steviol glycosides are primarily used in the food industry, there has been some interest in their potential use as a therapeutic agent. Research has suggested that these compounds may have antioxidant, anti-inflammatory, and anti-cancer properties, among others. However, to date, there has been limited drug development using steviol glycosides. This is due in part to the fact that these compounds are primarily used as a food additive and have not been extensively studied for use as a therapeutic agent. Additionally, the regulatory landscape for developing natural products as drugs can be challenging. That being said, there have been some promising preclinical studies using steviol glycosides as a potential treatment for conditions such as diabetes, hypertension, and cancer. More research is needed to fully understand the therapeutic potential of these compounds and to develop them into safe and effective drugs. 4. Thioglycosides drug development Thioglycosides are a class of compounds that have shown promising potential in drug development. They are glycosides in which the oxygen atom of the glycosidic bond has been replaced with a sulfur atom. This substitution imparts several unique properties to thioglycosides, including enhanced stability, bioavailability, and metabolic resistance. As a result, thioglycosides have been investigated for a variety of therapeutic applications, including as anticancer, antiviral, and anti-inflammatory agents. One of the main advantages of thioglycosides as drug candidates is their ability to selectively target specific cells or tissues. This is due to the fact that many cell surface receptors and enzymes are glycosylated, meaning they have sugar molecules attached to them. Thioglycosides can be designed to mimic these sugar structures, allowing them to bind specifically to the targeted receptor or enzyme. This targeted binding can lead to enhanced therapeutic efficacy and reduced side effects. Thioglycosides have also been shown to have broad-spectrum antiviral activity against a range of viruses, including influenza, HIV, and hepatitis B and C. This is due in part to their ability to inhibit the attachment and entry of the virus into host cells. Additionally, thioglycosides have been investigated for their ability to inhibit viral replication and to stimulate the immune system to fight off viral infections. 5. Phenolic glycosides drug development The development of phenolic glycosides as drugs involves several stages, including identification of potential compounds, isolation and purification of the compounds, pharmacological evaluation, formulation development, and clinical trials.
  • 5. 5 | P a g e Identification of potential phenolic glycosides can be done through various methods, such as screening of natural sources, virtual screening, and structure-based design. Once potential compounds have been identified, they are isolated and purified from natural sources, such as plants or fungi. Pharmacological evaluation involves testing the compounds for their efficacy and safety in preclinical studies, such as in vitro assays and animal models. The most promising compounds are then selected for formulation development, which involves developing the drug into a suitable dosage form, such as a tablet or capsule. 6. Anthocyanins drug development In recent years, there has been growing interest in the potential use of anthocyanins as therapeutic agents in drug development. Some studies have suggested that anthocyanins may have a range of pharmacological effects, including anti-cancer, anti-diabetic, and neuroprotective activities. However, more research is needed to fully understand the potential benefits of anthocyanins as drugs, as well as any potential risks or side effects. Additionally, the development of anthocyanin-based drugs may be challenging due to their complex chemical structures and potential variability in composition depending on the source of the anthocyanins. 7. Cyanogenic glycosides drug development There has been some interest in developing drugs based on cyanogenic glycosides. One example is amygdalin, a cyanogenic glycoside found in the seeds of apricots, peaches, and almonds. Amygdalin has been investigated as a potential anticancer agent, as it has been shown to induce apoptosis (programmed cell death) in cancer cells. However, clinical trials have not shown conclusive evidence of its effectiveness as a cancer treatment. Another cyanogenic glycoside of interest is dhurrin, found in sorghum plants. Dhurrin has been shown to have antimicrobial properties, inhibiting the growth of various bacteria and fungi. It has also been investigated as a potential treatment for chronic pain, as it can activate opioid receptors in the body. 8. Anthraquinone drug development Here are some of the recent developments in anthraquinone drug development: Cancer treatment: Anthraquinones have shown promising results in preclinical studies for the treatment of different types of cancer, including breast, colon, lung, and liver cancer. Some of the mechanisms of action that have been identified include inhibiting tumor cell growth, inducing apoptosis, and suppressing angiogenesis. However, more research is needed to determine their safety and efficacy in humans. Anti-inflammatory agents: Anthraquinones have been shown to have anti-inflammatory properties by inhibiting the production of inflammatory cytokines. They have potential in the treatment of chronic inflammatory diseases such as rheumatoid arthritis, inflammatory bowel disease, and psoriasis.
  • 6. 6 | P a g e Antimicrobial agents: Anthraquinones have been shown to have antimicrobial activity against a wide range of microorganisms, including bacteria, fungi, and parasites. They have potential in the treatment of infections caused by drug-resistant pathogens. Wound healing: Some anthraquinones have been shown to promote wound healing by increasing the production of collagen and enhancing angiogenesis. They have potential in the treatment of chronic wounds such as diabetic ulcers. Neuroprotective agents: Anthraquinones have been shown to have neuroprotective effects by reducing oxidative stress and inflammation in the brain. They have potential in the treatment of neurodegenerative diseases such as Alzheimer's and Parkinson's disease. 9. Coumarin drug development Recent studies have shown that some coumarin derivatives have potent antitumor activity, making them potential candidates for cancer treatment. Other studies have investigated the use of coumarin derivatives as anti-inflammatory agents for the treatment of conditions such as arthritis. There are also ongoing efforts to develop coumarin-based compounds as potential therapies for neurodegenerative diseases such as Alzheimer's and Parkinson's. Coumarin has been shown to have neuroprotective effects and may help prevent the buildup of amyloid-beta protein in the brain. 10. Flavonoid glycosides drug development Drug development efforts have focused on the isolation and synthesis of flavonoid glycosides, as well as the identification of their molecular targets and mechanisms of action. Some of the challenges in developing flavonoid glycosides as drugs include their low bioavailability and rapid metabolism, as well as the need to optimize their pharmacokinetic and pharmacodynamic properties. One approach to overcome these challenges is to modify the structure of flavonoid glycosides to improve their stability, solubility, and bioavailability. Another strategy is to use delivery systems such as nanoparticles or liposomes to enhance their therapeutic efficacy and reduce toxicity. Several flavonoid glycosides have already been developed into drugs, including quercetin, hesperidin, and rutin. These drugs have shown promise in preclinical and clinical studies for their ability to target a variety of diseases, including cancer, diabetes, and inflammatory disorders. 11. Saponin drug development The development of saponin-based drugs is still in its early stages, but researchers are actively exploring their potential as therapeutics. One approach is to modify the structure of naturally occurring saponins to improve their efficacy and reduce toxicity. Another approach is to synthesize saponin-like compounds that mimic the biological activity of natural saponins.
  • 7. 7 | P a g e One area of research where saponins are being investigated is in the treatment of cancer. Some saponins have been found to have cytotoxic effects on cancer cells, and they may be useful in combination with other chemotherapy drugs. Another area of interest is in the development of saponins as vaccine adjuvants. Saponins have been shown to stimulate the immune system and enhance the immune response to vaccines. Conclusion Overall, the study of glycosides plays a vital role in the discovery and development of new drugs, and ongoing research in this area has the potential to lead to important advances in medicine.