Modulation of the steroidogenic related activity according to the design of single-chain bovine FSH analogs

Asraf, Hila; Amsterdam, Abraham; Ben-Menahem, David

doi:10.1016/j.ygcen.2015.04.004

Cited by 5 publications

(1 citation statement)

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“…In HB4a cells, this effect is also found but in smaller proportions. Similar results were obtained by Asraf et al (2015) after exposing five different cell lines (AGS,HepG2,LoVo,Du145,and HT29) to monastrol (20-150 μM). They found that all cell lines showed an increase in the population of cells with 4n DNA content, with two phenotypes based on sensitivity to monastrol and levels of survivin: cells in mitotic arrest or a G1-like state.…”

Section: Discussionsupporting

confidence: 82%

Antiproliferative activity of monastrol in human adenocarcinoma (MCF-7) and non-tumor (HB4a) breast cells

Marques

Semprebon

Niwa

et al. 2016

Naunyn-Schmiedeberg's Arch Pharmacol

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Monastrol is an allosteric inhibitor of the mitotic kinesin Eg5 that exhibits an antiproliferative effect against several cell lines. We investigated the antiproliferative effect of monastrol on human breast adenocarcinoma cells (MCF-7) and mammary epithelial cells (HB4a, non-tumoral). Monastrol treatment decreased cell viability only in MCF-7 tumor cells. Real-time cell growth kinetic analysis showed a decrease in the proliferation of MCF-7 cells exposed to monastrol, while in the HB4a cells, only a concentration of 100 μM was able to induce this effect. In a cell cycle analysis, exposure of MCF-7 cells to monastrol led to an increased population of cells in both the G1 and G2/M phases. In HB4a cells, the proportion of cells in the G2/M phase was increased. Monastrol led to an increased mitotic index in both cell lines. Monastrol was not able to induce cell death by apoptosis in any of the cell lines studied. Gene expression analysis was performed to measure the mRNA levels of cell cycle genes, DNA damage indicator gene, and apoptotic related genes. Treatment with monastrol induced in MCF-7 cells a 5-fold increase in the mRNA levels of the CDKN1A gene, an inhibitor of CDKs related with cell cycle arrest in response a stress stimulus, and a 2-fold decrease in CDKN1C mRNA levels in HB4a cells. These results provide evidence that monastrol has a greater antiproliferative effect on MCF-7 tumor cells compared with non-tumor HB4a cells; however, no selective is observed.

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Section: Discussionsupporting

confidence: 82%