Bioactive Natural Products in Pharmacological Applications

Bioactive natural products encompass a vast array of specialised metabolites—alkaloids, flavonoids, terpenoids, lignans, glycosides and oxylipins—isolated from plants, microorganisms and marine organisms. These compounds serve as leads for drug discovery by modulating key biochemical targets, including enzymes, receptors and signalling pathways. Advances in structural elucidation, stereochemical analysis and synthetic modification have deepened our understanding of structure–activity relationships and enabled optimisation of potency, selectivity and pharmacokinetic properties. Globally, these natural products exhibit anti-inflammatory, antimicrobial, anticancer, neuroprotective and antidiabetic activities, underpinning their translation into therapeutics and functional foods. Challenges remain in sustainable sourcing, scalable production and rigorous in vivo validation, yet integration of modern analytical methods and biotechnological approaches continues to expand their pharmacological potential.

Research from Nature Portfolio

Chiral separation and stereochemical characterisation of enantiomeric neolignans from plant extracts have revealed distinct antioxidant profiles. High-performance chiral chromatography coupled with electronic circular dichroism has established absolute configurations and demonstrated potent free-radical scavenging activity for specific enantiomers, highlighting the importance of stereochemistry in bioefficacy. In parallel, isolation of novel prenylated flavonoids has uncovered selective antitumour agents that induce G0/G1 cell cycle arrest and caspase-mediated apoptosis in hepatocellular carcinoma models. Mechanistic studies indicate modulation of p38 and JNK branches of the mitogen-activated protein kinase pathway, while preclinical in vivo assays confirm tumour growth inhibition without overt toxicity, emphasising the promise of prenylated scaffolds for cancer chemotherapeutics.

Bioactive Natural Products in Pharmacological Applications publication trend

The graph below shows the total number of articles in bioactive natural products in pharmacological applications across all publications each year (not limited to Nature Index journals).

Technical terms

Enantiomer: One of two mirror-image forms of a chiral molecule, often exhibiting distinct biological activities.

Neolignan: A dimeric phenolic compound formed by oxidative coupling of monolignols, with diverse pharmacological properties.

Prenylated flavonoid: A flavonoid bearing a lipophilic prenyl group, enhancing cell membrane affinity and bioactivity.

Oxylipin: An oxygenated fatty acid derivative produced via enzymatic or non-enzymatic pathways, involved in signalling and defence responses.

Mitogen-activated protein kinase pathway: A cascade of protein kinases that transmits extracellular signals to regulate cell proliferation, differentiation and apoptosis.

References

1. Enantiomeric Lignans and Neolignans from Phyllanthus glaucus: Enantioseparation and Their Absolute Configurations. Scientific Reports (2016).
2. A new Prenylated Flavonoid induces G0/G1 arrest and apoptosis through p38/JNK MAPK pathways in Human Hepatocellular Carcinoma cells. Scientific Reports (2017).
3. Anti-Inflammatory, Neurotrophic, and Cytotoxic Oxylipins Isolated from Chaenomeles sinensis Twigs. Antioxidants (2023).
4. Identification of Small-Molecule Bioactive Constituents from the Leaves of Vaccinium bracteatum Confirms It as a Potential Functional Food with Health Benefits. Foods (2023).
5. Antibacterial Activity of Chalcone and Dihydrochalcone Compounds from Uvaria chamae Roots against Multidrug‐Resistant Bacteria. BioMed Research International (2018).