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Article

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

by
Bing Xu
1,†,
Fuhao Chu
1,†,
Yuzhong Zhang
2,
Xiaobo Wang
3,
Qiang Li
1,
Wei Liu
4,
Xin Xu
1,
Yanyi Xing
1,
Jing Chen
1,
Penglong Wang
1,* and
Haimin Lei
1,*
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.
Int. J. Mol. Sci. 2015, 16(9), 21035-21055; https://doi.org/10.3390/ijms160921035
Submission received: 6 July 2015 / Revised: 22 July 2015 / Accepted: 23 July 2015 / Published: 2 September 2015
(This article belongs to the Section Biochemistry)
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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.
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.; et al. A Series of New Ligustrazine-Triterpenes Derivatives as Anti-Tumor Agents: Design, Synthesis, and Biological Evaluation. Int. J. Mol. Sci. 2015, 16, 21035-21055. https://doi.org/10.3390/ijms160921035

AMA Style

Xu B, Chu F, Zhang Y, Wang X, Li Q, Liu W, Xu X, Xing Y, Chen J, Wang P, et al. A Series of New Ligustrazine-Triterpenes Derivatives as Anti-Tumor Agents: Design, Synthesis, and Biological Evaluation. International Journal of Molecular Sciences. 2015; 16(9):21035-21055. https://doi.org/10.3390/ijms160921035

Chicago/Turabian Style

Xu, Bing, Fuhao Chu, Yuzhong Zhang, Xiaobo Wang, Qiang Li, Wei Liu, Xin Xu, Yanyi Xing, Jing Chen, Penglong Wang, and et al. 2015. "A Series of New Ligustrazine-Triterpenes Derivatives as Anti-Tumor Agents: Design, Synthesis, and Biological Evaluation" International Journal of Molecular Sciences 16, no. 9: 21035-21055. https://doi.org/10.3390/ijms160921035

APA Style

Xu, B., Chu, F., Zhang, Y., Wang, X., Li, Q., Liu, W., Xu, X., Xing, Y., Chen, J., Wang, P., & Lei, H. (2015). A Series of New Ligustrazine-Triterpenes Derivatives as Anti-Tumor Agents: Design, Synthesis, and Biological Evaluation. International Journal of Molecular Sciences, 16(9), 21035-21055. https://doi.org/10.3390/ijms160921035

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