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Open AccessArticle

A Series of New Ligustrazine-Triterpenes Derivatives as Anti-Tumor Agents: Design, Synthesis, and Biological Evaluation

1
School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing 100102, China
2
Department of Pathology, Beijing University of Chinese Medicine, Beijing 100102, China
3
Center of Scientific Experiment, Beijing University of Chinese Medicine, Beijing 100102, China
4
School of Management, Beijing University of Chinese Medicine, Beijing 100102, China
*
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Academic Editor: Bing Yan
Int. J. Mol. Sci. 2015, 16(9), 21035-21055; https://doi.org/10.3390/ijms160921035
Received: 6 July 2015 / Revised: 22 July 2015 / Accepted: 23 July 2015 / Published: 2 September 2015
(This article belongs to the Section Biochemistry)
A series of novel ligustrazine-triterpenes derivatives was designed, synthesized and screened for their cytotoxicity against five cancer cell lines (Bel-7402, HepG2, HT-29, Hela, and MCF-7) and Madin-Darby canine kidney (MDCK). Current study suggested that most of the ligustrazine-triterpenes conjunctions showed better cytotoxicity than the starting materials. In particular, compound 4a exhibited better cytotoxic activity (IC50 < 5.23 μM) against Bel-7402, HT-29, MCF-7, Hela, and HepG2 than the standard anticancer drug cisplatin (DDP). The cytotoxicity selectivity detection revealed that 4a exhibited low cytotoxicity (IC50 > 20 μM) towards MDCK cells. A combination of fluorescence staining observation and flow cytometric analysis indicated that 4a could induce HepG2 cell apoptosis. Further studies suggested that 4a-induced apoptosis is mediated through depolarization of the mitochondrial membrane potential and increase of intracellular free Ca2+ concentration. In addition, the structure-activity relationships of these derivatives were briefly discussed. View Full-Text
Keywords: ligustrazine-triterpenes derivatives; cytotoxicity selectivity; combination principles; apoptosis ligustrazine-triterpenes derivatives; cytotoxicity selectivity; combination principles; apoptosis
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MDPI and ACS Style

Xu, B.; Chu, F.; Zhang, Y.; Wang, X.; Li, Q.; Liu, W.; Xu, X.; Xing, Y.; Chen, J.; Wang, P.; Lei, H. A Series of New Ligustrazine-Triterpenes Derivatives as Anti-Tumor Agents: Design, Synthesis, and Biological Evaluation. Int. J. Mol. Sci. 2015, 16, 21035-21055.

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