Biological Activities of Terpenoid Compounds

Terpenoid compounds, a vast family of natural products derived from isoprene units, exhibit remarkable structural diversity spanning monoterpenes, sesquiterpenes, diterpenes and triterpenes. Across plant, fungal and marine sources, these metabolites have been shown to modulate an array of biological processes. Key activities include anti-inflammatory effects via inhibition of pro-inflammatory enzymes and cytokines; antimicrobial and antiparasitic actions driven by membrane disruption and interference with microbial signalling; antioxidant capacity through free-radical scavenging and upregulation of cellular defence pathways; and neuroprotective properties involving cholinesterase inhibition and protection against oxidative stress. Some triterpenoids have demonstrated potent anticancer activity by inducing apoptosis, cell-cycle arrest and inhibition of metastasis. Emerging research also highlights immunomodulatory, antiviral and cardioprotective roles, reflecting a broad potential for therapeutic development. These bioactivities underscore the global significance of terpenoids as lead structures for pharmaceuticals, agrochemicals and nutraceuticals.

Research from Nature Portfolio

Standardised screening of limonene-derived monoterpenes has clarified the structural features essential for anti-inflammatory potency. A comparative analysis of nine monoterpene analogues revealed that an oxygenated group at the C6 position conjugated to a double bond at C1 and an S configuration at C4 confer maximal inhibition of nitric oxide production in activated macrophages. The most potent compound significantly reduced expression of inducible nitric oxide synthase and interleukin-1β in both murine macrophages and human chondrocytes, suggesting promise for treating inflammation-related conditions such as osteoarthritis.

Biological Activities of Terpenoid Compounds publication trend

The graph below shows the total number of articles in biological activities of terpenoid compounds across all publications each year (not limited to Nature Index journals).

Technical terms

Terpenoid: A class of natural compounds built from isoprene units, encompassing monoterpenes, sesquiterpenes, diterpenes and triterpenes.

Monoterpene: A terpenoid composed of two isoprene units (C10), often volatile and bioactive.

Sesquiterpene: A terpenoid of three isoprene units (C15), many of which exhibit antimicrobial or anti-inflammatory activity.

Anti-inflammatory: The ability to reduce inflammation by inhibiting pro-inflammatory mediators or pathways.

Neuroprotective: Describing agents that safeguard nerve cells from damage or degeneration.

Structure-activity relationship (SAR): The analysis of how molecular modifications influence biological activity.

References

1. Standardised comparison of limonene-derived monoterpenes identifies structural determinants of anti-inflammatory activity. Scientific Reports (2020).
2. Molecular Mechanisms Underlying the Anti-Inflammatory Properties of (R)-(-)-Carvone: Potential Roles of JNK1, Nrf2 and NF-κB. Pharmaceutics (2023).
3. Synthesis of Carvone Derivatives and In Silico and In Vitro Screening of Anti-Inflammatory Activity in Murine Macrophages. International Journal of Molecular Sciences (2023).
4. S-(+)-Carvone, a Monoterpene with Potential Anti-Neurodegenerative Activity—In Vitro, In Vivo and Ex Vivo Studies. Molecules (2024).