Active Carbohydrate Research Institute, Chongqing Key Laboratory of Inorganic Functional Materials, Chongqing Normal University, Chongqing, China.
Chem Biol Drug Des. 2019 Apr;93(4):539-543. doi: 10.1111/cbdd.13447. Epub 2018 Dec 19.
Epothilone, the macrolide compound produced by Sorangium cellulosum, has antitumor activity. Its anti-tumor mechanism is similar to that of paclitaxel, which promotes the polymerization of tubulin and induces apoptosis. Herein, 7-O-β-d-galactosyl-polyethylene glycol-epothilone B 6 was synthesized. It showed that the toxicity of the synthesized compound was 1/182 of the epothilone B. In addition, compound 6 also had significant anticancer activity under the action of enzyme.
埃坡霉素是一种由索拉金菌（Sorangium cellulosum）产生的大环内酯化合物，具有抗肿瘤活性。其抗肿瘤机制与紫杉醇类似，能促进微管蛋白聚合并诱导细胞凋亡。在此，我们合成了 7-O-β-d-半乳糖基-聚乙二醇-埃坡霉素 B6。结果表明，该合成化合物的毒性是埃坡霉素 B 的 1/182。此外，在酶的作用下，化合物 6 也具有显著的抗癌活性。
