Marchantin C, a novel microtubule inhibitor from liverwort with anti-tumor activity both in vivo and in vitro.
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 G(2)/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.
Shi
Yan-qiu
YQ
School of Pharmaceutical Sciences, 44 Wen Hua Xi Road, Jinan, Shandong, China.
Zhu
Chang-jun
CJ
Yuan
Hui-qing
HQ
Li
Bo-qin
BQ
Gao
Jie
J
Qu
Xian-jun
XJ
Sun
Bin
B
Cheng
Yan-na
YN
Li
Song
S
Li
Xia
X
Lou
Hong-Xiang
HX
D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000494:pharmacology*; D001632:Bibenzyls / Q000494:pharmacology*; D002396:Catechols / Q000494:pharmacology*; D002455:Cell Division / Q000187:drug effects; D045744:Cell Line, Tumor; D004988:Ethers, Cyclic / Q000494:pharmacology*; D005260:Female; D016195:G2 Phase / Q000187:drug effects; D006801:Humans; D051379:Mice; D008807:Mice, Inbred BALB C; D008870:Microtubules / Q000187:drug effects* / Q000378:metabolism; D010647:Phenyl Ethers / Q000494:pharmacology*; D002583:Uterine Cervical Neoplasms / Q000188:drug therapy; D023041:Xenograft Model Antitumor Assays
D000972:Antineoplastic Agents, Phytogenic; D001632:Bibenzyls; D002396:Catechols; D004988:Ethers, Cyclic; D010647:Phenyl Ethers; C459129:marchantin C