In vitro and computational studies of natural products related to perezone as anti-neoplastic agents

Biochimie
Maricarmen Hernández-RodríguezRené Miranda Ruvalcaba

Abstract

Many natural phyto-products as perezone (Per) exhibit anti-cancer activities. Using experimental and computational studies, it was described that Poly ADP-ribose polymerase 1(PARP-1) inhibition and the induction of oxidative stress state explain the pro-apoptotic activity of Per. The aim of this study was to evaluate two phyto-products related to Per as anti-cancer agents: hydroxyperezone (OHPer) and its monoangelate (OHPer-MAng). These molecules were structurally characterized employing thermal analysis, IR spectrophotometry and X-ray diffraction techniques. The phyto-compounds evaluated in vitro in six cancer cell lines (K562, MCF-7, MDA-MB-231, HeLa, U373, A549) and non-malignant cells determinate their cytotoxicity, type of induced cell death, ability to avoid cell migration and changes at the redox status of the cell. Using, in vitro and computational studies provided the inhibition of PARP-1 and its potential binding mode. Cell proliferation assays demonstrated that OHPer-MAng treatment significantly induces apoptosis in triple negative breast cancer (TNBC) cell line (MDA-MB-231 IC50 = 3.53 μM), being particularly less cytotoxic to Vero cells (IC50 = 313.92 μM), human lymphocytes (IC50 = 221.46 μM) and rat endothelial cel...Continue Reading

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Citations

Nov 7, 2020·Drug Discovery Today·Samridhi Lal, Timothy J Snape
May 18, 2021·Chemistry & Biodiversity·Han ChenXiaoling Lu

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