1. Two New Cytotoxic Maytansinoids Targeting Tubulin from Trewia nudiflora.
- Author
-
Lei, Chun, Li, Ya-Nan, Li, Jia-Nan, Zhou, Yu-Bo, Cui, Ming-Jun, Fu, Kai-Cong, Li, Jia, and Hou, Ai-Jun
- Subjects
THERAPEUTIC use of antineoplastic agents ,THERAPEUTIC use of plant extracts ,X-rays ,IN vitro studies ,NERVE tissue proteins ,APOPTOSIS ,CRYSTALLOGRAPHY ,TOXICITY testing ,MOLECULAR structure ,CELL lines ,SPECTRUM analysis - Abstract
Two new maytansinoids, N -methyltreflorine (1) and methyltrewiasine (2), were isolated from the dried fruits of Trewia nudiflora , together with three known congeners (3 – 5). Their structures were elucidated by spectroscopic methods, and the absolute configuration of 1 and 2 was determined by X-ray crystallographic analysis. Compounds 1 – 5 exhibited strong cytotoxicity against human tumor cell lines, including HeLa, MV-4 – 11, and MCF-7, with IC
50 values ranging from 0.12 to 11 nM. Compounds 1 and 4 also showed inhibitory activity against the MCF-7/ADR cell line with IC50 values of 13 and 28 nM, respectively. Compounds 1 and 2 significantly inhibited tubulin polymerization in vitro with IC50 values of 3.6 and 3.2 µM, respectively. [ABSTRACT FROM AUTHOR]- Published
- 2022
- Full Text
- View/download PDF