Natural products

Acetylsalicylic Acid (Aspirin)

Source: Salicin → salicylic acid → acetylsalicylic acid

Class: Salicylate

Mechanism: Irreversibly inhibits COX-1/COX-2 → ↓ prostaglandins/thromboxanes → analgesic, anti-inflammatory

Salicylic Acid

Class: Phenolic acid

Mechanism: COX inhibition (weak) → inflammation reduction → precursor to aspirin

Artemisinin

Source: Artemisia annua

Class: Sesquiterpene lactone

Mechanism: Heme-activated ROS formation → parasite protein/membrane damage → antimalarial

Avermectin

Source: Streptomycin avermitilis

Class: Macrocyclic lactone

Mechanism: Activates glutamate-gated Cl⁻ channels → paralysis → antiparasitic

Ivermectin

Class: Semi-synthetic avermectin derivative

Mechanism: Enhanced Cl⁻ channel activation → parasite paralysis → antiparasitic

Apoferretin encapsulation of MDAs

Biocompatible + stable → encapsulate cancer drugs

Tumour cells overexpress transferrin receptor 1 (TfR1) → bind/taken up via receptor-mediated endocytosis

Benefits: improved solubility, enhanced selectivity, reduced toxicity, controlled release

Berberine

Source: Coptis

Class: Isoquinoline alkaloid

Mechanism: AMPK activation → improved glucose and lipid metabolism → anti-diarrhoeal, DNA intercalation/efflux pump inhibition → antibacterial

Jerantinine A & B

Class: Aspidosperma alkaloids

Mechanism: Inhibit tubulin polymerisation ± PLK1 inhibition → mitotic arrest → anticancer

Cannabidiol (CBD)

Class: Phytocannabinoid

Mechanism: Multi-target modulation (TRPV1, 5-HT₁A; CB1 allosteric) → anticonvulsant, anti-inflammatory

Tetrahydrocannabinol (THC)

Class: Phytocannabinoid

Mechanism: Partial CB1 agonist → psychoactive effects → analgesia, antiemetic, appetite stimulation

Doxorubicin

Class: Anthracycline antibiotic

Mechanism: DNA intercalation + topoisomerase II inhibition → prevents DNA unwinding → ROS → DNA damage → anticancer (limitations: resistance and cardiotoxicity is dose-limiting)

Lanosterol

Class: Triterpenoid sterol

Mechanism: Cholesterol biosynthesis intermediate → sterol metabolism; biosynthetic precursor

Lovastatin

Source: Fungi secondary metabolite

Class: Polyketide (statin)

Mechanism: HMG-CoA reductase inhibition → ↓ cholesterol synthesis → reduces CVD risk

Mevastatin

Source: Semi-synthetic derivative of lovostatin

Class: Polyketide

Mechanism: HMG-CoA reductase inhibition → lipid lowering → prototype statin

Morphine

Source: Papaver somniferum

Class: Opioid alkaloid

Mechanism: μ-opioid receptor agonist → ↓ CAMP/Ca2+ → ↓ neurotransmitter release → CNS analgesia for severe pain relief (limitations: dependence, tolerance)

Paclitaxel

Source: Pacific yew bark

Class: Diterpenoid

Mechanism: β-tubulin binding → microtubule stabilisation → mitotic arrest → anticancer

Penicillin

Source: Penicillium

Class: β-lactam antibiotic

Mechanism: Inhibits PBPs (transpeptidases) → cell wall lysis → antibacterial

Quinine

Source: Cinchona bark

Class: Alkaloid

Mechanism: Blocks haemoglobin digestion → inhibits haemozoin formation → interferes with parasite growth and reproduction

Rapamycin (Sirolimus)

Class: Macrocyclic lactone

Mechanism: mTOR inhibition → ↓ T-cell proliferation → immunosuppressant; anticancer relevance

Resveratrol

Class: Polyphenol (stilbene)

Mechanism: Antioxidant + SIRT1 activation → cardioprotective; anti-inflammatory (preclinical)

Saponins

Name: Digitonin

Source: Foxglove

Class: Sapnonin = amphipathic glycosides: Aglycone region has fat soluble terpenoid. Glycone region has water soluble carbohydrate chain

Mechanism: Membrane disruption

Use: soaps/detergents, form foams

Name: Trabectedin

Source: tunicate Ecteinascidia turbinata

Class: tetrahydroquinoline alkaloids

Mechanism: produces ROS → binds DNA N2 minor groove → cleaves DNA → dsDNA breaks → triggers apoptosis → advanced soft tissue sarcoma

 

Atropine and Scopolamine

Name: Atropine and Scopolamine

Class: tropane alkaloids

Source: plants in the Solanaceae family

Target: muscarinic ACh receptor antagonists

Atropine: peripheral antimuscarinic effects → smooth muscle relaxation

Scopolamine: CNS-penetrant → sedation/anti-motion sickness effects