4 research outputs found
Evaluation of Cuspidaria pulchra and its Isolated Compounds Against Schistosoma mansoni Adult Worms
The present study has investigated the chemical composition of the bioactive EtOAc fraction of Cuspidaria pulchra aerial parts, as well as its schistosomicidal activities against Schistosoma mansoni adult worms in vitro. To this end, the crude ethanol extract obtained from the aerial parts of C. pulchra (Bignoniaceae) was partitioned with n-hexane, EtOAc, and n-BuOH. The EtOAc fraction was purified by preparative HPLC, which afforded 3,4-dihydroxybenzaldehyde (1), p-coumaric acid (2), p-hydroxybenzoic acid (3), ursolic acid (4), and oleanolic acid (5). The bioassay results indicated that the crude ethanol extract and the EtOAc fraction at 100 µg/mL killed the adult schistosomes in vitro. Compounds 1 and 3 at 100 µm were only able to separate coupled S. mansoni adult worms
Lipoxygenase inhibitory activity of <i>Cuspidaria pulchra</i> and isolated compounds
<div><p>This work evaluated the <i>in vitro</i> inhibitory activity of the crude ethanolic extract from the aerial parts of <i>Cuspidaria pulchra</i> (Cham.) L.G. Lohmann against 15-lipoxygenase (15-LOX). The bioassay-guided fractionation of the <i>n</i>-butanol fraction, which displayed the highest activity, led to the isolation of three compounds: caffeoylcalleryanin (<b>1</b>), verbascoside (<b>2</b>) and 6-hydroxyluteolin-7-<i>O</i>-β-glucoside (<b>3</b>). Assessment of the ability of the isolated compounds to inhibit 15-LOX revealed that compounds <b>1</b>, <b>2</b> and <b>3</b> exerted strong 15-LOX inhibitory activity; IC<sub>50</sub> values were 1.59, 1.76 and 2.35 μM respectively. The XTT assay showed that none of the isolated compounds seemed to be significantly toxic.</p></div
Schistosomicidal Activity of Alkyl-phenols from the Cashew Anacardium occidentale against Schistosoma mansoni Adult Worms
Bioassay-guided
study of the ethanol extract from the cashew Anacardium
occidentale furnished cardol triene (<b>1</b>), cardol diene (<b>2</b>), anacardic acid triene (<b>3</b>), cardol monoene (<b>4</b>), anacardic acid diene
(<b>5</b>), 2-methylcardol triene (<b>6</b>), and 2-methylcardol
diene (<b>7</b>). 1D- and 2D-NMR experiments and HRMS analysis
confirmed the structures of compounds <b>1</b>–<b>7</b>. Compounds <b>2</b> and <b>7</b> were active
against Schistosoma mansoni adult worms
in vitro, with LC<sub>50</sub> values of 32.2 and 14.5 μM and
selectivity indices of 6.1 and 21.2, respectively. Scanning electron
microscopy of the tegument of male worms in the presence of compound <b>7</b> at 25 μM after 24 h of incubation showed severe damage
as well as peeling and reduction in the number of spine tubercles.
Transmission electron microscopy analyses revealed swollen mitochondrial
membrane, vacuoles, and altered tegument in worms incubated with compound <b>2</b> (25 μM after 24 h). Worms incubated with compound <b>7</b> (25 μM after 24 h) had lysed interstitial tissue,
degenerated mitochondria, and drastically altered tegument. Together,
the results indicated that compound <b>7</b> presents promising
in vitro schistosomicidal activity