Marchantin C,a novel microtubule inhibitor from liverwort with anti-tumor activity both in vivo and in vitro |
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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 |
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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 |
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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. |
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Keywords: | Marchantin C Macrocyclic bisbibenzyl Microtubule inhibitor Cell cycle arrest Tumor cell apoptosis |
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