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- Title
In vitro anticancer studies of a small library of cyclic lipopeptides against the human cervix adenocarcinoma HeLa cells.
- Authors
HMEDAT, ALI N.; MOREJÓN, MICJEL C.; RIVERA, DANIEL G.; PANTELIĆ, NEBOJŠA Đ.; WESSJOHANN, LUDGER A.; KALUĐEROVIĆ, GORAN N.
- Abstract
Various cyclic lipopeptides (CLPs, 23 compounds) were tested for their antitumor potential against human cervix adenocarcinoma HeLa cells. From the fast screening (tested concentrations: 0.01 and 10 μM) compound 10 ((12S,6S,10S,13S)-6-((R)-sec-butyl)-7-(2-(dodecylamino)-2-oxoethyl)-13-isopropyl-82-nitro-2,5,12,15-tetraoxo-4,7,11,14-tetraaza-1(1,2)-pyrrolidina-8(1,4)-benzenacyclopentadecaphane-10-carboxamide) was identified as active against HeLa cell line. The MTT 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide and CV (crystal violet) assays revealed at least five times higher cytotoxic potential of 10 (IC50 = 12.3±1.8 μM, MTT; 9.4±1.5 μM; CV) in comparison to control drug natural occurring CLP surfactin (IC50 = 64.9±0.8 μM, MTT; 76.2±1.6 μM; CV). The cell cycle analysis performed by DAPI (4',6-diamidino-2-phenylindole) assay indicated the involvement of apoptosis in HeLa cell death upon treatment with 10, which was confirmed by apoptosis assay (annexin V/PI). Furthermore, during this process caspase activation could be detected (ApoStat assay, immunocytochemistry caspase-3 analysis). The flow cytometry analysis did not display induction of autophagy as a possible death mechanism in HeLa cells upon 10 treatment. The current findings could be used to design more effective CLPs based on 10 structure as potential anticancer agents.
- Subjects
HELA cells; CELL death; CELL cycle; CELL analysis; IN vitro studies; GENTIAN violet; ADENOCARCINOMA
- Publication
Journal of the Serbian Chemical Society, 2024, Vol 89, Issue 4, p471
- ISSN
0352-5139
- Publication type
Article
- DOI
10.2298/JSC240109018H