AI Article Synopsis
- Heterocyclic organobismuth compounds have shown strong potential as antimicrobial and antitumor agents, particularly those with eight-membered rings versus those with six-membered rings.
- Bi-chlorodibenzo[c,f][1,5]thiabismocine (Compound 3) causes G/M arrest by inhibiting tubulin polymerization in HeLa cells, while N-tert-butyl-bi-chlorodibenzo[c,f][1,5]azabismocine (Compound 1) demonstrates even greater cytotoxic effects against cancer cells.
- Research indicates that Compound 1 effectively inhibits cell growth and induces mitotic arrest, whereas Compound 5 exhibits limited antitumor activity, highlighting the importance of the compound
Article Abstract
We previously showed that heterocyclic organobismuth compounds have excellent antimicrobial and antitumor potential. These compounds structurally consist of either six- or eight-membered rings. Previous research has shown that bi-chlorodibenzo[c,f][1,5]thiabismocine (Compound 3), an eight-membered ring, induced G/M arrest via inhibition of tubulin polymerization in HeLa cells. Additionally, N-tert-butyl-bi-chlorodi-benzo[c,f][1,5]azabismocine (Compound 1), another eight-membered ring, exhibited higher cytotoxicity than Compound 3 against several cancer cell lines, including HeLa and K562. Finally, bi-chlorophenothiabismin-S,S-dioxide (Compound 5), a six-membered ring, exhibited lower antitumor activity than eight-membered ring compounds. In this study, we investigated the antimitotic activity of Compounds 1 and 5 in HeLa cells. At low concentrations, (0.1 and 0.25 μM), Compound 1 inhibited cell growth and arrested the cell cycle in mitosis. However, 0.5 μM Compound 1 exhibited no antimitotic activity. Conversely, Compound 5 weakly inhibited cell growth and did not markedly arrest the cell cycle. Flow cytometry showed that Compound 1 arrested the cell cycle at G/M, resulting in apoptosis. Compound 1 inhibited tubulin polymerization as revealed by a cell-free assay, and both Compounds 1 and 3 inhibited microtubule spindle formation and chromosome alignment during prometaphase. These results suggest that eight-membered ring-containing organobismuth compounds can induce mitotic arrest by perturbing spindle dynamics.
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| http://dx.doi.org/10.1016/j.tiv.2018.03.007 | DOI Listing |
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