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  • Title: [In vitro inhibitory effect of dibenzoxanthene CY-B12 on proliferation of tumor cell lines and its possible mechanisms].
    Author: Pu XX, Jiang GF, Chen Y, Xu ZL, Xian LJ.
    Journal: Ai Zheng; 2005 Dec; 24(12):1442-7. PubMed ID: 16351789.
    Abstract:
    BACKGROUND & OBJECTIVE: CY-B12, a new dibenzon-xanthene, has been synthesized recently. This study was to investigate the in vitro antiproliferative activity of CY-B12 and its possible mechanisms. METHODS: The inhibitory effects of CY-B12 on proliferation of gastric carcinoma cell line MGC803, nasopharyngeal carcinoma cell line CNE-2, oral epithelial carcinoma cell line KB-3-1, and lung cancer cell line Glc82 were assessed by MTT assay. Cell cycle distribution and apoptosis were detected by flow cytometry (FCM). Apoptotic morphology of CNE-2 cells was observed under fluorescent microscope after Hoechst33258 staining. The expression of cell cycle-related proteins Cdc25C, Cdc2, and Cyclin B1 were measured by Western blot. DNA damage was detected by single cell gel electrophoresis (SCGE). RESULTS: CY-B12 obviously inhibited the proliferation of MGC803, CNE-2, KB-3-1, and Glc82 cells; the IC(50) values were 7.51, 9.58, 8.84, and 15.99 micromol/L, respectively. After treatment of CY-B12, CNE-2 cells were arrested at G(2)/M phase; chromatin condensation, apoptotic bodies, and sub-G1 peak were observed in CNE-2 cells. The protein expression of Cdc25C in CNE-2 cells was down-regulated by CY-B12 in a dose-dependent mannerû whereas Cyclin B1 and Cdc2 were up-regulated by low dose of CY-B12, and down-regulated by high dose of CY-B12. CY-B12 induced DNA damage in CNE-2 cells in a dose-dependent manner. CONCLUSION: CY-B12 has potent in vitro antiproliferative activity, which may be exerted through breaking DNA, down-regulating cell cycle-related protein Cdc25C, and inducing cell cycle arrest and apoptosis.
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