In vitro antileishmanial activity of hydroalcoholic extract, fractions, and compounds isolated from leaves of Piper ovatum Vahl against Leishmania amazonensis

Abstract

We assessed the biological activity of a crude extract, a mixture of several fractions, and a pure compound obtained from Piper ovatum Vahl against promastigote and amastigote forms of Leishmania amazonensis. The medicinal plant P. ovatum is used popularly as an anesthetic and anti-inflammatory. This study included the extraction process and bioassay-guided fractionation by the adsorption chromatography and Sephadex LH-20 method. A progressive increase in the antileishmanial effect was observed in the course of fractionation. The 50% inhibitory concentration (IC 50) for dichloromethane-ethyl acetate (1:1 v/v) fraction was 2.1 µg/ml and 24 µg/ml; mixture of piperovatine: piperlongumune (2:3) 0.9 µg/ml and 24 µg/ml; piperovatine (1) 9.5 µg/ml and 10 µg/ml; and piperlonguminine (2) 2.5 µg/ml and 9.0 µg/ml, for promastigote and amastigote forms, respectively. Cytotoxicity analysis indicated that these toxic concentrations were much higher for J774G8 macrophages and Vero cells than for the protozoans. The mixture of piperovatine: piperlongumune (2:3) showed important antiprotozoal activity against the amastigote and promastigote forms of L. amazonensis, and it produced morphological changes in promastigotes and amastigotes at 0.9 µg/ml and 24 µg/ml (50% growth inhibition concentration), respectively, including intense cytoplasmic vacuolization, mitochondrial swelling, and mitochondrial damage, as revealed by transmission electron microscopy.

Leishmanicidal Activity of Piper nigrum Bioactive Fractions is Interceded via Apoptosis In Vitro and Substantiated by Th1 Immunostimulatory Potential In Vivo

“…PNH and PNE at 200 mg/ kg bw rendered remarkable protection whereas partial recovery from disease was evident at 100 mg/kg bw dose. Despite several antileishmanial studies from numerous plants of the genus Piper ( Torres-Santos et al, 1999 ; Hermoso et al, 2003 ; Bodiwala et al, 2007 ; Sarkar et al, 2008 ; Flores et al, 2009 ; Rodrigues-Silva et al, 2009 ; Monzote et al, 2010 ; Cruz et al, 2011 ; Carrara et al, 2013 ), there are no reports on in vivo antileishmanial potential of P. nigrum extracts or pure compounds isolated from P. nigrum to the best of our knowledge. However, in vivo antileishmanial efficacy of PIP and its different formulations have been earlier reported.…”

Activity of Piperaceae extracts and fractions in the control of Phytomonas serpens

“…DMSo at the maximum concentration used (1%) did not interfere with parasite growth. RoDRIGUES-SILVA et al (2009) reported the in vitro activity of hydroalcoholic extract and fractions of Piper ovatum, against Leishmania amazonensis. A progressive increase in the antileishmanial effect was observed in the course of the fractionation.…”