喜树碱
细胞凋亡
多重耐药
污渍
A549电池
抑制性突触后电位
立体化学
化学
生物
生物化学
基因
神经科学
抗生素
作者
Yingze Yang,Mi Zhou,Dongni Wang,Xiangzhong Liu,Xiansheng Ye,Guanghui Wang,Ting Lin,Cuiling Sun,Rong Ding,Wenjing Tian,Haifeng Chen
标识
DOI:10.1021/acs.jnatprod.0c00986
摘要
Twelve undescribed jatrophane diterpenoids, euphpepluones A–L (1–12), together with seven known analogues (13–19), were isolated from the whole plant of Euphorbia peplus, and their structures were elucidated by spectroscopic studies. The absolute configurations of 1 and 4 were assigned by X-ray crystallographic analysis. All isolates were investigated for their inhibitory effects against the ATR-Chk1 pathway using a Western blotting assay. As a result, 1, 2, 5, 8, 10, and 16 were found to suppress the camptothecin (CPT)-induced phosphorylation of Chk1, indicating that these compounds inhibit the activation of the ATR-Chk1 pathway. A preliminary structure–activity relationship (SAR) study of the isolates was conducted. When compound 10 and CPT were combined, apoptosis was induced in A549 cells with PARP cleavage, while there was no apoptotic effect by treatment with CPT or 10 alone. The data obtained indicate that 10 potentiates the chemotherapeutic sensitivity of A549 cells to CPT.
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