十五烷
化学
立体化学
多重耐药
骨架(计算机编程)
P-糖蛋白
碳骨架
生物化学
解剖
医学
抗生素
作者
Lan-Jun Zhang,Pei-Zhi Huang,Ke-Jing Li,Yue-Yang Cao,Yue Sun,Wei-Jiao Feng,Yu-Xian Wang,Yi-Lin He,Le-Yuan Mi,Yan-Li Wei,Qi-Zhong Lai,Jian-Jun Chen,Kun Gao
标识
DOI:10.1016/j.bioorg.2023.106619
摘要
Three new diterpenoids with an unusual carbon skeleton, pedilanins A-C (1-3), and nine new jatrophane diterpenoids, pedilanins D-L (4-12), along with five known ones (13-17), were isolated from Pedilanthus tithymaloides. Compounds 1-3 characterize an unprecedented tricyclo[10.3.0.02,9]pentadecane skeleton. Compounds 4-8 are rare examples of the jatrophanes bearing a cyclic hemiketal substructure. Their structures were determined by an extensive analysis of HRESIMS, NMR, quantum-chemical calculation, DP4+ probability, and X-ray crystallographic data. In the bioassay, compounds 1-12 dramatically reversed multidrug resistance in cancer cells with the fold-reversals ranging from 17.9 to 396.8 at the noncytotoxic concentration of 10 μM. The mechanism results indicated that compounds 2 and 3 inhibited the P-glycoprotein (Pgp) transporter function, thus reversing the drug resistance.
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