Pharmacological Properties of Terpenoids in Cancer Biology
Summary
Terpenoids, a diverse class of naturally occurring organic compounds derived from isoprene units, have attracted considerable attention for their multifaceted roles in cancer prevention and therapy. Monoterpenes such as geraniol, limonene and perillyl alcohol exhibit cytotoxicity against malignant cells through induction of apoptosis, cell‐cycle arrest and inhibition of key pro-survival signalling pathways. Many terpenoids also display anti-angiogenic activity, suppressing vascular endothelial growth factor (VEGF)-mediated neovascularisation and reducing tumour perfusion. Their intrinsic antioxidant and anti-inflammatory properties further contribute to modulation of the tumour microenvironment, attenuating oxidative stress and chronic inflammation that support malignant progression. In addition, terpenoids can sensitize cancer cells to chemotherapeutic agents by downregulating drug-resistance transporters or altering xenobiotic-metabolising enzymes. Advances in formulation science, including nanoemulsions and lipid carriers, have improved the bioavailability and target delivery of poorly soluble terpenoids, enhancing in vivo efficacy. The confluence of these mechanisms underscores the global significance of terpenoids as cost-effective leads for novel anticancer regimens and adjuvant therapies.
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Pharmacological Properties of Terpenoids in Cancer Biology publication trend
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Technical terms
Terpenoid: A class of natural compounds built from isoprene units, exhibiting varied biological activities.
Monoterpene: A terpenoid containing two isoprene units (C10), often found in essential oils.
Apoptosis: Programmed cell death characterised by caspase activation and DNA fragmentation.
Angiogenesis: Formation of new blood vessels, a process exploited by tumours to secure nutrients and oxygen.
Transcription factor: A protein that binds DNA to regulate gene expression.
VEGF/VEGFR-2 signalling: A pathway in which vascular endothelial growth factor binds its receptor to promote angiogenesis.
E2F8: A member of the E2F transcription factor family involved in regulating the G2/M phase of the cell cycle.
References
- Geraniol Pharmacokinetics, Bioavailability and Its Multiple Effects on the Liver Antioxidant and Xenobiotic-Metabolizing Enzymes. Frontiers in Pharmacology (2018).
- Geraniol Suppresses Angiogenesis by Downregulating Vascular Endothelial Growth Factor (VEGF)/VEGFR-2 Signaling. PLOS ONE (2015).
- Geraniol suppresses prostate cancer growth through down‐regulation of E2F8. Cancer Medicine (2016).
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