Abstract
Twenty fangchinoline derivatives were synthesized from the natural product fangchinoline, and their anticancer activities on human breast cancer MDA-MB-231 cell line, human prostate cancer PC3 cell line, human melanoma WM9 cell line and human leukaemia HEL and K562 cell lines were evaluated. The biological result showed that those derivatives exhibited potent activities on inhibiting cancer cell growth, and the structure-activity relationships were investigated. Among them, compound 4g, which was protected by benzoyl group in 7-phenolic position and nitrified in 14-position, showed impressive inhibition on all 5 cancer cell lines, especially WM9 cell line, with an IC50 value of 1.07 µM. Further mechanistic studies demonstrated that compound 4g may induce cancer cell death by apoptotic means. These research results suggested that compound 4g could be a lead for the further development toward an anticancer agent against human melanoma WM9 in the future.
Highlights
Cancer is one the most crucial public health concerns across the world
Melanoma is another aggressive human cancer, the incidence of which has dramatically increased during the past decades, racial difference varies the risk of developing this kind of cancer [3]
Natural products play an important role in the context of anti-cancer drug discovery
Summary
Cancer is one the most crucial public health concerns across the world. Based on the estimation of the World Health Organization (WHO), 8.8 million people died from cancer in 2015, occupying 16.7%of all global death [1]. Cancer is one the most crucial public health concerns across the world. Based on the estimation of the World Health Organization (WHO), 8.8 million people died from cancer in 2015, occupying 16.7%. According to the world cancer report, breast cancer has the highest incidence among women (43.3 per 100,000) while prostate cancer has the second-highest among men Chemotherapy remains one of the most important methods for cancer treatment [5,6]. Natural products play an important role in the context of anti-cancer drug discovery. Fangchinoline and tetrandrine (Figure 1) are two bisbenzylisoquinoline alkaloids isolated from a Chinese traditional herb Stephaniae tetrandra S. Many bioactivities have been discovered since fangchinoline and tetrandrine were isolated as two of the main active ingredients in Molecules 2017, 22, 1923; doi:10.3390/molecules22111923 www.mdpi.com/journal/molecules
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