| Literature DB >> 29454280 |
Yiwen Zhang1, Zhimei Li2, Qiuxia Min2, Abulizi Palida3, Yiyuan Zhang2, Ruotian Tang4, Lixia Chen5, Hua Li6.
Abstract
8-Chrysoeriol, a bioactive flavanoid, was firstly identified to bind directly to BCL-2 as BH3 mimetics by structure-based virtual ligand screening. And 3D docking model revealed the molecular basis of 8-Chrysoeriol targeting to BCL-2. The interaction between 8-Chrysoeriol and BCL-2 was further confirmed using Microscale Thermophoresis (MST) technique. Meanwhile, high expression level of antiapoptotic protein BCL-2 was detected in SW1990 pancreatic cancer cells and 8-Chrysoeriol showed obvious proapoptosis effect against SW1990 in vitro. Collectively, the results showed that 8-Chrysoeriol as a natural dietary product potentially targeting to BCL-2 could serve as a lead compound for SW1990 pancreatic cancer therapy.Entities:
Keywords: BCL-2 inhibitor; BH3 mimetics; SW1990 pancreatic cancer
Mesh:
Substances:
Year: 2018 PMID: 29454280 DOI: 10.1016/j.bioorg.2018.01.042
Source DB: PubMed Journal: Bioorg Chem ISSN: 0045-2068 Impact factor: 5.275