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Marchantin C,a novel microtubule inhibitor from liverwort with anti-tumor activity both in vivo and in vitro
Authors:Yan-qiu Shi  Chang-jun Zhu  Hui-qing Yuan  Bo-qin Li  Jie Gao  Xian-jun Qu  Bin Sun  Yan-na Cheng  Song Li  Xia Li  Hong-Xiang Lou
Affiliation:1. School of Pharmaceutical Sciences, 44 Wen Hua Xi Road, Jinan, Shandong 250012, China;2. School of Medicine, Shandong University,44 Wen Hua Xi Road, Jinan, Shandong 250012, China
Abstract:Microtubules are long-standing targets in cancer chemotherapy. Previously, we reported that marchantin C triggers apoptosis of human tumor cells. We show here that marchantin C induced cell cycle arrest at G2/M phase in A172 and HeLa cells. In addition, marchantin C decreased the quantity of microtubules in a time- and dose-dependent manner in these cells. Exposure of purified bovine brain tubulin to marchantin C inhibited polymerization of gross tubulin in vitro. Moreover, marchantin C potently suppressed the growth of human cervical carcinoma xenografts in nude mice. Marchantin C-treated xenografts showed decreased microtubules, Bcl-2 and increased cyclin B1, Bax, caspase-3, indicating that marchantin C possess the same ability to induce microtubules depolymerization and tumor cell apoptosis in tumor-bearing mice as in vitro. In conclusion, marchantin C is a novel microtubule inhibitor that induces mitotic arrest of tumor cells and suppresses tumor cell growth, exhibiting promising antitumor therapeutic potential.
Keywords:Marchantin C   Macrocyclic bisbibenzyl   Microtubule inhibitor   Cell cycle arrest   Tumor cell apoptosis
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