Antitumor Effects of a Sesquiterpene Derivative from Marine Sponge in Human Breast Cancer Cells

• Main Authors: Li-Yuan Bai, Jui-Hsin Su, Chang-Fang Chiu, Wei-Yu Lin, Jing-Lan Hu, Chia-Hsien Feng, Chih-Wen Shu, Jing-Ru Weng
• Format: Article
• Language: English
• Published: MDPI AG 2021-04-01
• Series: Marine Drugs
• Subjects: ilimaquinone; sponge; cell cycle arrest; apoptosis; autophagy; breast cancer
• Online Access: https://www.mdpi.com/1660-3397/19/5/244

In this study, the anti-proliferative effect of ilimaquinone, a sesquiterpene derivative from the marine sponge, in breast cancer cells was investigated. Ilimaquinone inhibited the proliferation of MCF-7 and MDA-MB-231 breast cancer cells with IC₅₀ values of 10.6 μM and 13.5 μM, respectively. Non-tumorigenic human breast epithelial cells were less sensitive to ilimaquinone than breast cancer cells. Flow cytometric and Western blot analysis showed that ilimaquinone induced S-phase arrest by modulating the expression of p-CDC-2 and p21. Ilimaquinone induces apoptosis, which is accompanied by multiple biological biomarkers, including the downregulation of Akt, ERK, and Bax, upregulation of p38, loss of mitochondrial membrane potential, increased reactive oxygen species generation, and induced autophagy. Collectively, these findings suggest that ilimaquinone causes cell cycle arrest as well as induces apoptosis and autophagy in breast cancer cells.