Crispenes F and G, cis-Clerodane Furanoditerpenoids from Tinospora crispa, Inhibit STAT3 Dimerization

被引：20

作者：

Al Noman, Md. Abdullah ^{[1
]}

Hossain, Tasnova ^{[1
]}

Ahsan, Monira ^{[1
]}

Jamshidi, Shirin ^{[2
]}

Hasan, Choudhury Mahmood ^{[1
]}

Rahman, Khondaker Miraz ^{[2
]}

机构：

[1] Univ Dhaka, Dept Pharmaceut Chem, Dhaka 1000, Bangladesh

[2] Kings Coll London, Sch Canc & Pharmaceut Sci, 150 Stamford St, London SE1 9NH, England

来源：

JOURNAL OF NATURAL PRODUCTS | 2018年 / 81卷 / 02期

关键词：

TRANSCRIPTIONAL CONTROL; ANTIBACTERIAL ACTIVITY; SIGNAL TRANSDUCERS; GENETIC ALGORITHM; CANCER; TARGETS; CYTOTOXICITY; EXTRACTIVES; ACTIVATORS; DITERPENE;

D O I：

10.1021/acs.jnatprod.7b00377

中图分类号：

Q94 [植物学];

学科分类号：

071001 ;

摘要：

Two new cis-clerodane-type furanoditerpenes, crispenes F and G (1 and 2), together with seven known compounds, were isolated from the stems of Tinospora crispa. Crispenes F and G (1 and 2) inhibited STAT3 dimerization in a cell-free fluorescent polarization assay and were found to have significant cytotoxicity against a STAT3-dependent MDA-MB 231 breast cancer cell line, while being inactive in a STAT3-null A4 cell line. These two compounds share structural similarities with a previously reported STAT3 inhibitor, crispene E, isolated from the same plant. Molecular docking studies suggested that the molecules inhibit STAT3 by interacting with its SH2 domain.

引用

页码：236 / 242

页数：7

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