Pentacyclic Triterpenoid Acids in the Treatment of Breast Cancer.

Natalia Jankowska, Rostyslav Dudchak, Magdalena Podolak, Marcin Cybulski, Elisabetta Esposito, Olga Michalak, Krzysztof Bielawski, Anna Bielawska, Agnieszka Gornowicz

Journal: Molecules (Basel, Switzerland) 2026;31(18):

PMID: 42796494

Abstract

Despite increasing awareness about cancer, it still remains one of the biggest threats to human life. Breast cancer is among the most commonly diagnosed types of cancer. Pentacyclic triterpenoids are a group of plant compounds commonly known in traditional medicine due to their anti-inflammatory, antibacterial, antidiabetic, cardioprotective and anticancer effects. This review examined the potential of pentacyclic triterpenoid acids in the treatment of breast cancer, focusing on research from the past 15 years. Although the subject literature demonstrates that pentacyclic acids show anticancer activity, it also reveals their limitations such as low bioavailability, aqueous solubility, or high IC50 values. Therefore, to overcome these limitations, structural modifications, mostly at the C3 and C28 positions, were made, and several novel derivatives with oleanane, lupane and ursane skeletal types were synthesized. This review not only identified pentacyclic acids derivatives but also evaluated how structural modifications enhanced their biological activity and potential in breast cancer treatment. The findings revealed that even though the obtained derivatives enhanced anticancer potential against breast cancer, the main issues of bioavailability and solubility remain unsolved, suggesting that future research in synthesis should focus not only on improving cytotoxicity but also on the bioavailability of novel compounds.

Address: Department of Biotechnology, Medical University of Bialystok, 1 Kilińskiego Str., 15-089 Białystok, Poland.; Department of Synthesis and Technology of Drugs, Medical University of Bialystok, 1 Kilińskiego Str., 15-089 Białystok, Poland.; Chemistry Section, Pharmacy, Cosmetic Chemistry and Biotechnology Research Group, Łukasiewicz Research Network-Industrial Chemistry Institute, 8 Rydygiera Str., 01-793 Warsaw, Poland.; Department of Chemical, Pharmaceutical and Agricultural Sciences, University of Ferrara, Via Fossato di Mortara, 19-44121 Ferrara, Italy.
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