Synthesis and evaluation of anticancer activity of quillaic acid derivatives: A cell cycle arrest and apoptosis inducer through NF-κB and MAPK pathways.

A series of quillaic acid derivatives with different substituents on the 28-carboxyl group were designed and synthesized. Five human cancer cell lines (HCT116, BEL7402, HepG2, SW620, and MCF-7) were evaluated for their antitumor activity in vitro. Some of the tested derivatives showed improved antiproliferative activity compared to the lead compound, quillaic acid. Among them, compound E (IC50 = 2.46 ± 0.44 μM) showed the strongest antiproliferative activity against HCT116 cells; compared with quillaic acid (IC50 > 10 μM), its efficacy against HCT116 cancer cells was approximately 4-fold higher than that of quillaic acid. Compound E also induces cell cycle arrest and apoptosis by modulating NF-κB and MAPK pathways. Therefore, the development of compound E is certainly valuable for anti-tumor applications. Copyright © 2022 Huang, Zhang, Deng, Wu, Guo, Lee, Chen, Shen, Jin and Quan.

Citation

Xing Huang, Chang-Hao Zhang, Hao Deng, Dan Wu, Hong-Yan Guo, Jung Joon Lee, Fen-Er Chen, Qing-Kun Shen, Li-Li Jin, Zhe-Shan Quan. Synthesis and evaluation of anticancer activity of quillaic acid derivatives: A cell cycle arrest and apoptosis inducer through NF-κB and MAPK pathways. Frontiers in chemistry. 2022;10:951713

PMID: 36157038

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