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: [email protected].
  • 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: [email protected].
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.