Mantaj Julia, Rahman S M Abdur, Bokshi Bishwajit, Hasan Choudhury M, Jackson Paul J M, Parsons Richard B, Rahman Khondaker M
Institute of Pharmaceutical Science, King's College London, London SE1 9NH, UK.
Org Biomol Chem. 2015 Apr 7;13(13):3882-6. doi: 10.1039/c5ob00052a.
Crispene E, a new clerodane-type diterpene, inhibited STAT3 dimerization in a cell-free fluorescent polarisation assay and was found to have significant toxicity against STAT3-dependent MDA-MB 231 breast cancer cell line and selectively inhibited the expression of STAT3 and STAT3 target genes cyclin D1, Fascin and bcl-2. Molecular docking studies suggest the molecule inhibits STAT3 by interacting with its SH2 domain. The compound has been isolated from Tinospora crispa and characterized using standard spectroscopic techniques.
新克罗烷型二萜类化合物Crispene E在无细胞荧光偏振试验中抑制STAT3二聚化，并且发现其对STAT3依赖性MDA-MB 231乳腺癌细胞系具有显著毒性，还能选择性抑制STAT3及其靶基因细胞周期蛋白D1、丝状肌动蛋白和bcl-2的表达。分子对接研究表明该分子通过与其SH2结构域相互作用来抑制STAT3。该化合物已从毛叶锡生藤中分离出来，并采用标准光谱技术进行了表征。
