<i>In Vitro</i> and <i>In Vivo</i> Evaluation of the Antischistosomal Activity of Polygodial and 9-Deoxymuzigadial Isolated from <i>Drimys brasiliensis</i> Branches

<i>In Vitro</i> and <i>In Vivo</i> Evaluation of the Antischistosomal Activity of Polygodial and 9-Deoxymuzigadial Isolated from <i>Drimys brasiliensis</i> Branches

In the present study, the hexane extract from branches of <i>Drimys brasiliensis</i> (Winteraceae) displayed potent activity against <i>Schistosoma mansoni</i> parasites (100% mortality of the worms at 200 μg/mL). Bioactivity-guided fractionation afforded, in addition to the...

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Bibliographic Details
Main Authors: Eric Umehara, Rayssa A. Cajas, Gabriel B. Conceição, Guilherme M. Antar, Adriano D. Andricopulo, Josué de Moraes, João Henrique G. Lago
Format: Article
Language:English
Published: MDPI AG 2025-01-01
Series:Molecules
Subjects:
antischistosomal activity
polygodial
9-deoxymuzigadial
<i>Drimys brasiliensis</i>
schistosomiasis
Online Access:https://www.mdpi.com/1420-3049/30/2/267
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Summary:In the present study, the hexane extract from branches of <i>Drimys brasiliensis</i> (Winteraceae) displayed potent activity against <i>Schistosoma mansoni</i> parasites (100% mortality of the worms at 200 μg/mL). Bioactivity-guided fractionation afforded, in addition to the previously reported bioactive sesquiterpene 3,6-epidioxy-bisabola-1,10-diene, two chemically related drimane sesquiterpenes—polygodial (<b>1</b>) and 9-deoxymuzigadial (<b>2</b>). The anti-<i>S. mansoni</i> effects for compounds <b>1</b> and <b>2</b> were determined in vitro, with compound <b>1</b> demonstrating significant potency (EC<sub>50</sub> value of 10 μM for both male and female worms), while <b>2</b> was inactive. Cytotoxicity assays against Vero cells revealed no toxicity for either compound (CC<sub>50</sub> > 200 μM). Additionally, an in silico analysis was conducted using the SwissADME platform for <b>1</b>, revealing that this natural sesquiterpene exhibited adherence to several ADME parameters and no PAINS violations. Finally, in vivo studies with <i>S. mansoni</i>-infected mice treated with compound <b>1</b> demonstrated a 44.0% reduction in worm burden, accompanied by decreases in egg production of 71.8% in feces and 69.5% in intestines. These findings highlight the potential of polygodial (<b>1</b>) as a promising prototype for schistosomiasis treatment.
ISSN:1420-3049

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