Monoterpene-Based Anticancer Therapeutics
Summary
Monoterpenes, a class of naturally occurring C₁₀ isoprenoids abundant in essential oils, have attracted considerable interest as leads for anticancer drug development. Their diverse structures—ranging from simple hydrocarbons such as limonene to oxygenated derivatives like perillyl alcohol and perillic acid—exhibit a spectrum of bioactivities, including induction of apoptosis, inhibition of cell proliferation and interference with key signalling pathways. Mechanisms of action encompass modulation of tubulin dynamics, disruption of membrane integrity, alteration of redox balance and inhibition of protein prenylation, which collectively impair tumour growth and metastasis. Advances in medicinal chemistry have yielded monoterpene hybrids and derivatives with enhanced potency and selectivity, while formulation strategies such as encapsulation in lipid-based nanocarriers have addressed issues of solubility and bioavailability. Clinical and pre-clinical studies underscore the ability of selected monoterpenes to overcome biological barriers, notably the blood-brain barrier, making them promising candidates for both systemic and intracranial malignancies. Continued exploration of structure-activity relationships and delivery platforms aims to translate these natural scaffolds into efficacious and safe anticancer therapeutics.
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Monoterpene-Based Anticancer Therapeutics publication trend
The graph below shows the total number of articles in monoterpene-based anticancer therapeutics across all publications each year (not limited to Nature Index journals).
Technical terms
Monoterpene: A natural C₁₀ isoprenoid compound found in essential oils, often exhibiting bioactive properties.
Tubulin polymerisation: The process by which tubulin proteins assemble into microtubules, essential for cell division and a target for anticancer agents.
Blood-brain barrier (BBB): A selective endothelial barrier that restricts passage of substances from the bloodstream into the central nervous system.
Prenylation: A post-translational lipid modification of proteins that facilitates membrane association and is critical for oncogenic signalling.
Lipid-based nanocarriers: Nanoscale delivery systems composed of lipids designed to enhance solubility, stability and targeted delivery of therapeutic agents.
References
- Investigation of Anticancer Properties of Monoterpene-Aminopyrimidine Hybrids on A2780 Ovarian Cancer Cells. International Journal of Molecular Sciences (2023).
- Incorporation of Perillyl Alcohol into Lipid-Based Nanocarriers Enhances the Antiproliferative Activity in Malignant Glioma Cells. Biomedicines (2023).
- The Monoterpenoid Perillyl Alcohol: Anticancer Agent and Medium to Overcome Biological Barriers. Pharmaceutics (2021).
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