Natural product-based design, synthesis and biological evaluation of Albiziabioside A derivatives that selectively induce HCT116 cell death

Eur J Med Chem. 2016 May 4:113:92-101. doi: 10.1016/j.ejmech.2015.12.034.

Gaofei Wei ¹, Shanshan Cui ¹, Weijing Luan ¹, Shuai Wang ¹, Zhuang Hou ¹, Yongxiang Liu ¹, Yang Liu ², Maosheng Cheng ³

Affiliations

1 Key Laboratory of Structure-Based Drugs Design & Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
2 Key Laboratory of Structure-Based Drugs Design & Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, PR China. Electronic address: y.liu@syphu.edu.cn.
3 Key Laboratory of Structure-Based Drugs Design & Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, PR China. Electronic address: mscheng@syphu.edu.cn.

PMID: 26922223 DOI: 10.1016/j.ejmech.2015.12.034

Abstract

A series of Albiziabioside A coupled substituents of cinnamoyl derivatives were designed and synthesized. The synthesized compounds were screened for Anticancer activity against a panel of six human Cancer cell lines using a MTT assay. Synthetic derivatives showed excellent selectivity, as they were toxic against only HCT116 cell line. Some compounds exhibited better anti-cancer activity against HCT116 compared to positive controls, such as 5-fluorouracil and Albiziabioside A. Compound 8n was the most active derivative. Importantly, it was also found that the anti-proliferative activity of 8n could be attributed to the induction of cell cycle arrest and Apoptosis in HCT116 cells.

Keywords

Albiziabioside A; Anti-proliferative activities; Apoptosis; Cell cycle arrest; Cinnamoyl; Saponin.

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