Podcast
Questions and Answers
What percentage of drugs approved between 1981 and 2006 that were derived from natural products?
What percentage of drugs approved between 1981 and 2006 that were derived from natural products?
- 25%
- 10%
- 45% (correct)
- 75%
Which of the following is considered a direct natural product derived from plants?
Which of the following is considered a direct natural product derived from plants?
- Ciprofloxacin
- Ibuprofen
- Paclitaxel (correct)
- Metformin
What is the main reason for the focus on plant-based chemicals for drug discovery?
What is the main reason for the focus on plant-based chemicals for drug discovery?
- They have a higher potency than synthetic drugs.
- They are perceived as safer and more effective. (correct)
- They have fewer side effects overall.
- They are cheaper to produce.
Which compound is primarily derived from the opium poppy?
Which compound is primarily derived from the opium poppy?
Which plant is known for producing Artemisinin, effective against multidrug-resistant malaria?
Which plant is known for producing Artemisinin, effective against multidrug-resistant malaria?
What type of properties do flavonoids exhibit?
What type of properties do flavonoids exhibit?
What is the typical failure rate for drug leads even in late clinical trials?
What is the typical failure rate for drug leads even in late clinical trials?
What type of drugs have been derived from plant polysaccharides?
What type of drugs have been derived from plant polysaccharides?
Which of the following alkaloids is derived from Galanthus nivalis and is used to treat Alzheimer's disease?
Which of the following alkaloids is derived from Galanthus nivalis and is used to treat Alzheimer's disease?
Which of the following is NOT a characteristic of compounds derived from plants?
Which of the following is NOT a characteristic of compounds derived from plants?
What type of drug is apomorphine classified as?
What type of drug is apomorphine classified as?
What is the fate of approximately one in ten thousand screened compounds?
What is the fate of approximately one in ten thousand screened compounds?
Which plant is the primary source of Dronabinol and Cannabidiol?
Which plant is the primary source of Dronabinol and Cannabidiol?
Berberine, a compound with various health benefits, is isolated from which plant?
Berberine, a compound with various health benefits, is isolated from which plant?
What is one of the major challenges in drug discovery mentioned in the context of traditional herbal medicine?
What is one of the major challenges in drug discovery mentioned in the context of traditional herbal medicine?
What approach is used to study plant-based medicinal compounds for their utility as drugs?
What approach is used to study plant-based medicinal compounds for their utility as drugs?
Which of the following statements about artemisinin is accurate?
Which of the following statements about artemisinin is accurate?
Which compound is a synthetic second-generation derivative used for treating hepatitis?
Which compound is a synthetic second-generation derivative used for treating hepatitis?
What does the term 'hybrid molecules' refer to in drug discovery?
What does the term 'hybrid molecules' refer to in drug discovery?
Which region is noted for meeting half its healthcare demand through traditional herbal medicine?
Which region is noted for meeting half its healthcare demand through traditional herbal medicine?
What is a major limitation of single-target drug approaches?
What is a major limitation of single-target drug approaches?
What is one of the risks of harvesting medicinal plants mentioned?
What is one of the risks of harvesting medicinal plants mentioned?
Which of the following is a potential consequence of over-exploiting medicinal herbs?
Which of the following is a potential consequence of over-exploiting medicinal herbs?
What approach is suggested to prevent the extinction of medicinal plants?
What approach is suggested to prevent the extinction of medicinal plants?
What type of effects can curcumin have on different molecular targets?
What type of effects can curcumin have on different molecular targets?
What is the primary purpose of systems pharmacology in drug discovery?
What is the primary purpose of systems pharmacology in drug discovery?
What is the estimated percentage of artemisinin found in the dry weight of the plant?
What is the estimated percentage of artemisinin found in the dry weight of the plant?
Which of the following describes a consideration needed when using transgene technology?
Which of the following describes a consideration needed when using transgene technology?
How does the complexity of diseases challenge drug development?
How does the complexity of diseases challenge drug development?
What is the consequence of the limited number of effective compounds from natural products?
What is the consequence of the limited number of effective compounds from natural products?
Study Notes
Plant-Based Drugs
- Approximately 70,000 plant species have been screened for medicinal properties.
- Many antitumor drugs (e.g., paclitaxel, camptothecin) are plant-derived.
- About 8 out of 10 drugs for infections, cardiovascular disease, cancer, or immunosuppression are plant-derived or derivatives.
- Only about 1 in 10,000 screened compounds are proven safe and effective.
- Many drug leads fail in late-stage clinical trials.
- Plant-based chemicals are often considered safer and more effective than synthetic alternatives.
Plant-Based Drug Types
- Polysaccharides: Have immunomodulatory/immunostimulatory effects (e.g., Ganoderma lucidum, Cordyceps sinensis, Açaà fruit).
- Flavonoids: Found in most plants, with diverse bioactive properties. Have a heterocyclic ring structure (aromatic and benzopyran rings). Examples include flavones, isoflavones, flavonols, flavonones, and xanthones.
- Proteins: From some herbs used as natural protein supplements for convalescents.
- Alkaloids: Found in various plants and have diverse applications.
- Morphine and aspirin are derived from natural sources (opium poppy and willow bark, respectively).
- Artemisinin (from Artemisia annua), used for multidrug-resistant malaria; silymarin (from Silybum marianum) for liver disease; galantamine (from Galanthus nivalis) for Alzheimer's.
- Apomorphine (semi-synthetic morphine derivative) for Parkinson's, Tiotropium (atropine derivative) for COPD;
- Cannabis sativa yields dronabinol and cannabidiol for pain relief; Capsicum annuum yields capsaicin for pain relief.
- Nitisinone is a derivative of Leptospermone (from Callistemon citrinus), used to treat antityrosinaemia; -Alkaloids are finding reapplication as nitric oxide activators for obesity and atherosclerosis prevention.
- Other compounds: Bicyclol (synthetic derivative of a compound from Schisandra chinensis) for hepatitis B treatment. Schisandra chinensis fruit contains schisandrin C and compounds with anti-steatotic effects. Curcumin (from turmeric) has multiple molecular targets with various bioactivities (anticancer, antiviral, antiarthritic, etc.).
Traditional Herbal Medicine (THM)
- THM is used extensively for primary healthcare in China and India.
- THM data, gained over decades, can contribute to more successful plant-derived drug discovery.
- Indian THM is heavily documented in Ayurveda, providing information on various compounds such as alkaloids from Rauwolfia serpentina, psoralens, alkaloids from Holarrhena antidysenterica, guggulsterons, bacosides from Bacopa monnieria, piperidines, curcumins, lignans, glycosides, polyphenols, and steroidal lactones.
- Berberine (from goldthread; Coptis chinensis) has potent antibiotic and anti-inflammatory properties and is used for various conditions.
- Modern technology is being used for quality control and standardization of THM products.
- Over 100 billion USD is being spent globally on herbal drug discovery.
- China has ~1,500 patented THM products; ~8,400 in clinical trials, and ~13,000 herbs used.
Plant Harvesting Concerns
- Overharvesting of medicinal plants (e.g., Cypripedium pubescens, Trillium erectum, Aletris farinose) threatens several species.
- Up to 70% of endangered plants in China are medicinal.
- Herb farming and agrotechnology are important for sustainability.
Drug Discovery Challenges
- Single-target approaches fail to account for complex human physiology and the multiple factors affecting diseases.
- Multi-target effects of some compounds can be beneficial or dangerous.
- The ADMET (absorption, distribution, metabolism, excretion, and toxicity) approach is critical to evaluating any plant-derived compound for drug efficacy.
Future Directions
- Modern technology aids quality control and standardization of plant-derived drugs.
- Hybrid molecules linking different drug molecules could lead to novel treatments.
- Research is attempting to overcome the bioavailability issues of some plant-derived compounds.
- Plant-based and synthetic drugs are being brought under the same regulatory umbrella.
- Complementary alternative medicine (CAMTs) are gaining recognition for the use of plant-derived drugs.
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