title: A novel carbazole derivative, BMVC: a potential antitumor agent and fluorescence marker of cancer cells.
abstract: We have investigated a novel compound, 3,6-bis[2-(1-methylpyridinium)vinyl]carbazole diiodide (BMVC), for inhibiting telomerase activity and distinguishing human lung H1299 and oral Ca9-22 cancer cells from lung IMR90 and skin Detroit-551 normal fibroblast cells. The telomeric repeat amplification protocol (TRAP) assay shows that the concentration of BMVC that inhibits 50% of the telomerase activity (IC50) is ca. 0.05 microM. On the other hand, the cell-viability assay indicates that the cytotoxicity was less than 15% to the H1299 and Ca9-22 cancer cells, and almost negligible to the MRC-5 and Detroit-551 normal cells after incubation with 0.5 microM BMVC for 72 h. The low concentration of 0.05 microM of BMVC can inhibit telomerase activity but does not have general toxic effects to normal cells, implying that BMVC is a promising telomerase inhibitor. Moreover, wide-field fluorescence images of 0.1 microM BMVC-treated cells show bright fluorescence spots in the nuclei of the most H1299 and Ca9-22 cancer cells. Interestingly, similar fluorescence spots are hardly observed in the nuclei of the IMR90 and Detroit-551 normal cells, implying that BMVC might be a useful marker to distinguish tumor cells and normal cells.
authors.affiliation: Institute of Atomic and Molecular Sciences, Academia Sinica, P. O. Box 23-166, Taipei, 106, Taiwan, Republic of China.
authors.forename: Cheng-Chung
authors.initials: CC
authors.lastname: Chang
authors.forename: I-Chun
authors.initials: IC
authors.lastname: Kuo
authors.forename: Jing-Jer
authors.initials: JJ
authors.lastname: Lin
authors.forename: Yu-Cheng
authors.initials: YC
authors.lastname: Lu
authors.forename: Chin-Tin
authors.initials: CT
authors.lastname: Chen
authors.forename: Hong-Tsun
authors.initials: HT
authors.lastname: Back
authors.forename: Pei-Jen
authors.initials: PJ
authors.lastname: Lou
authors.forename: Ta-Chau
authors.initials: TC
authors.lastname: Chang
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology; D015415:Biomarkers / Q000737:chemistry; D002227:Carbazoles / Q000737:chemistry* / Q000494:pharmacology; D045744:Cell Line, Tumor; D002478:Cells, Cultured; D004354:Drug Screening Assays, Antitumor / Q000379:methods; D015507:Drugs, Investigational / Q000737:chemistry / Q000494:pharmacology; D005456:Fluorescent Dyes / Q000737:chemistry; D006801:Humans; D008856:Microscopy, Fluorescence / Q000379:methods; D011726:Pyridinium Compounds / Q000737:chemistry* / Q000494:pharmacology
chemical_list: C486012:3,6-bis(1-methyl-4-vinylpyridium)carbazole diiodide; D000970:Antineoplastic Agents; D015415:Biomarkers; D002227:Carbazoles; D015507:Drugs, Investigational; D005456:Fluorescent Dyes; D011726:Pyridinium Compounds; C041514:carbazole