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8-Chrysoeriol, as a potential BCL-2 inhibitor triggers apoptosis of SW1990 pancreatic cancer cells.

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.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Zhang Y,Li Z,Min Q,Palida A,Zhang Y,Tang R,Chen L,Li H

doi

10.1016/j.bioorg.2018.01.042

subject

Has Abstract

pub_date

2018-04-01 00:00:00

pages

478-484

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(17)30883-0

journal_volume

77

pub_type

杂志文章

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