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Terpenoids: Emerging Natural Modulators for Reversing ABC Transporter-Mediated Multidrug Resistance in Cancer
Lanfei Ma1, Dina Mahemuti1, Yuanhong Lan1
1School of Pharmaceutical Science, Institute of Materia Medica, College of Life Science and Technology, Xinjiang University, Urumqi 830017, China.
Pharmaceuticals (Basel, Switzerland)
|January 28, 2026
Summary
Terpenoids, natural compounds from plants, show promise as a fourth generation of multidrug resistance (MDR) reversal agents. They exhibit low toxicity and multi-targeting capabilities, offering advantages over synthetic MDR reversers.
Area of Science:
- Pharmacology and Natural Product Chemistry
- Cancer Biology and Therapeutics
- Drug Resistance Mechanisms
Background:
- Multidrug resistance (MDR) is a major obstacle in cancer chemotherapy, leading to treatment failure and disease recurrence.
- Current MDR reversal agents face limitations due to toxicity and pharmacokinetic issues.
- Natural products, particularly terpenoids, are emerging as promising fourth-generation MDR reversal agents due to their favorable profiles.
Purpose of the Study:
- To systematically review the inhibitory activities of various terpenoids against ABC transporter proteins.
- To explore the mechanisms by which terpenoids reverse drug resistance, including efflux pump inhibition and signaling pathway modulation.
- To identify lead terpenoid compounds with translational potential for MDR reversal therapy.
Main Methods:
- In vitro and in vivo studies evaluating terpenoid activity against ABC transporter proteins.
- Analysis of terpenoid effects on key signaling pathways (PI3K-AKT, Nrf2, NF-κB) involved in MDR.
- Identification and characterization of specific terpenoid structures with potent MDR reversal properties.
Main Results:
- Terpenoids demonstrate significant inhibitory activity against ABC transporter proteins, effectively blocking drug efflux.
- Specific terpenoids, such as oleanolic acid and β-caryophyllene, show high target specificity and multi-mechanistic effects.
- Lead compounds like BBA, sooneuphanone D, Conferone, and dihydro-β-agarofuran derivatives exhibit potent MDR reversal activity with low toxicity.
Conclusions:
- Terpenoids represent a promising class of MDR reversal agents with advantages over traditional synthetic compounds.
- Further research is needed to address challenges like low bioavailability and optimize structure-activity relationships for clinical translation.
- Nano-delivery, structural modifications, and combination strategies are proposed to enhance the clinical applicability of terpenoids in cancer therapy.
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