Producción CyT
Libro de Resúmenes de la AAFE - Active principles present in Lepechinia meyenii ethanol extract as potential candidates for antiangiogenic drugs
Congreso
Autoría:
Alanis B.E. ; Ripani E.A. ; Laiolo J. ; Funes Chabán M. ; Vera D.M.A. ; CARPINELLA, MARIA CECILIA ; Joray M.B.Fecha:
2024Editorial y Lugar de Edición:
AAFEResumen *
Pathological angiogenesis is a common feature to a large number of human diseases. The limited efficacy of available treatments, their adverse effects and the development of resistance make it imperative to find new therapeutic agents. In this regard, natural products continue to play a significant role in drug discovery.This work studied the antiangiogenic activity of the ethanol extract of Lepechinia meyenii. Through chemical fractionation, three compounds were isolated. Tube formation assay using bovine aortic endothelial cells was the experiment of choice to assess antiangiogenic activity in vitro. Cell proliferation and cell migration were investigated through the MTT and the scratch assay, respectively. The inhibitory effect over the microsomal enzyme prostaglandin E2 synthase was studied by molecular and massive dynamic simulations. Cytotoxicity on peripheral blood mononuclear cells and erythrocyte cells was evaluated by means of MTT and hemolysis assay, respectively. In silico prediction of pharmacological properties was performed using the SwissADME online tool. Chemical fractionation of L. meyenii extract yielded the antiangiogenic compounds carnosic acid (1), carnosol (2) and rosmanol (3). Among these, 1 showed the strongest activity (IC50 = 5.7 M). No adverse effect was observed over cell proliferation, while this compound efficiently blocked cell migration. The isolated compounds did not show toxic effect on peripheral blood mononuclear cells and did not affect erythrocyte membrane integrity. Based on experimental evidence that supports mPGE2S-1 as the molecular target of 1, its inhibitory effect over this enzyme was further investigated. This work highlights the native flora of Argentina as a source of new antiangiogenic agents. As far as we know, there has been no previous description of the antiangiogenic activity of L. meyenii. These results position the isolated compounds as promising candidates for the development of new angiogenesis inhibitors. Información suministrada por el agente en SIGEVAPalabras Clave
INHIBIDORES DE ANGIOGENESISPLANTAS NATIVAS