Digoxin from foxglove:
Cardiac glycoside (terpenoid).
High dose: vomiting, cardiac arrest, death.
Low dose: treats congestive heart failure (CHF) and edema.
Morphine from opium poppy:
Alkaloid (nitrogenous compound).
Highly addictive; caused Opium Wars.
Overdose: respiratory failure, death.
Relieves severe pain as a CNS depressant.
Fossil records: Neanderthals used early versions of penicillin and aspirin.
Written documents: Sumerian clay tablets (4000 years old), Papyrus Ebers (ancient Egyptian medicine).
Still used by 60% of the world population.
Accounts for >40% of China's pharmaceutical market.
Annual turnover >190 billion yuan.
Governmental funding: TCM inheritance, innovation, internationalization, modernization, and standardization to identify bioactive compounds.
Produce physiological effects in living cells and tissues.
Many are secondary metabolites (terpenoids, phenolics, nitrogenous compounds) produced under stress.
Caused by Plasmodium spp., transmitted by female Anopheles mosquito.
Alkaloid from fever tree bark.
Antimalarial effect discovered in the 17th century.
Kills Plasmodium in bloodstream.
Tonic water: soda & sugar mask bitter taste.
Extraction from bark causes deforestation.
Terpenoid from sweet wormwood.
Kills Plasmodium effectively with fewer side effects; also shows anti-inflammatory & anti-cancer effects.
Artemisinin-based Combination Therapy (ACT) completes clearance and hinders resistance.
Production:
Extraction: inconsistent harvest, long lead time, low yield (0.01 – 0.8%).
Total synthesis: Short lead time, but low yield & high cost.
Semi-synthesis: Medium lead time, High cost.
Biosynthesis: Higher yield ,Under development.
Malignant tumor with abnormal cell growth & potential to spread.
Caused by genetic mutation: hyperactive oncogenes, inactive tumor suppressor or DNA repair genes.
Alkaloid from Madagascar periwinkle.
Antimitosis by preventing microtubule formation.
Very low yield (<0.0003%) from extraction.
Semi-synthesis from 2 natural precursors.
Terpenoid from Pacific yew bark.
Antimitosis by preventing microtubule disassembly.
Broader anticancer activity & less cytotoxic effect.
Production:
Extraction: low yield and slow growth.
Total synthesis: complicated steps, low yield, high cost.
Semi-synthesis: abundant precursors, high yield.
Biosynthesis: pathway not fully understood, low & unstable yield.
Extraction: growth rate, bioactive compound concentration.
Total synthesis: chirality (R vs S).
Semi-synthesis: suitable precursor.
Biosynthesis: optimal conditions, potential contamination.
Other considerations: usage & demand, chemical complexity, cost effectiveness.
Cytoprotective Effect 20(S)−Rg3$$20(S)-Rg3$$ on Benzo[a]pyrene-Induced DNA Damage
Medicinal Plants & Natural Drug Molecules