A novel carbazole derivative, BMVC: a potential antitumor agent and fluorescence marker of cancer cells.
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.
Chang
Cheng-Chung
CC
Institute of Atomic and Molecular Sciences, Academia Sinica, P. O. Box 23-166, Taipei, 106, Taiwan, Republic of China.
Kuo
I-Chun
IC
Lin
Jing-Jer
JJ
Lu
Yu-Cheng
YC
Chen
Chin-Tin
CT
Back
Hong-Tsun
HT
Lou
Pei-Jen
PJ
Chang
Ta-Chau
TC
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
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