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Open AccessArticle

Cytisine-Pterocarpan Derived Compounds: Biomimetic Synthesis and Apoptosis-Inducing Activity in Human Breast Cancer Cells

1
College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou 310014, China
2
Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals, Zhejiang University of Technology, Hangzhou 310014, China
*
Author to whom correspondence should be addressed.
Molecules 2018, 23(12), 3059; https://doi.org/10.3390/molecules23123059
Received: 26 October 2018 / Revised: 13 November 2018 / Accepted: 20 November 2018 / Published: 22 November 2018
Cytisine-pterocarpan derived compounds were biomimetically synthesized with (-)-cytisine and (-)-maackiain via a N,N-4-dimethyl-4-aminopyridine (DMAP)-mediated synthetic strategy in a mild manner. In the present study, tonkinensine B (4) was elaborated in good and high yields with the optimized reaction conditions. The in vitro cytotoxicity of compound 4 was evaluated against breast cancer cell lines and showed that 4 had a better cytotoxicity against MDA-MB-231 cells (IC50 = 19.2 μM). Depending on the research on cytotoxicities of 4 against RAW 264.7 and BV2 cells, it was suggested that 4 produced low cytotoxic effects on the central nervous system. Further study indicated that 4 demonstrated cytotoxic activity against MDA-MB-231 cells and the cytotoxic activity was induced by apoptosis. The results implied that the apoptosis might be induced by mitochondrion-mediated apoptosis via regulating the ratio of Bax/Bcl-2 and promoting the release of cytochrome c from the mitochondrion to the cytoplasm in MDA-MB-231 cells. View Full-Text
Keywords: cytisine-pterocarpan derived compounds; biomimetic synthesis; breast cancer; mitochondrion-mediated apoptosis cytisine-pterocarpan derived compounds; biomimetic synthesis; breast cancer; mitochondrion-mediated apoptosis
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MDPI and ACS Style

Peng, T.-T.; Sun, X.-R.; Liu, R.-H.; Hua, L.-X.; Cheng, D.-P.; Mao, B.; Li, X.-N. Cytisine-Pterocarpan Derived Compounds: Biomimetic Synthesis and Apoptosis-Inducing Activity in Human Breast Cancer Cells. Molecules 2018, 23, 3059.

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