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Int. J. Mol. Sci. 2015, 16(9), 21035-21055; doi:10.3390/ijms160921035

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
These authors contributed equally to this work.
*
Authors to whom correspondence should be addressed.
Academic Editor: Bing Yan
Received: 6 July 2015 / Revised: 22 July 2015 / Accepted: 23 July 2015 / Published: 2 September 2015
(This article belongs to the Section Biochemistry, Molecular and Cellular Biology)
View Full-Text   |   Download PDF [2631 KB, uploaded 2 September 2015]   |  

Abstract

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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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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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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