Publication | Open Access
Verbascoside Inhibits Promastigote Growth and Arginase Activity of <i>Leishmania amazonensis</i>
57
Citations
29
References
2016
Year
Antiparasitic AgentVisceral LeishmaniasisParasite GenomicsMolecular PharmacologyMedicinal ChemistryBiosynthesisLeishmania DonovaniArginase InhibitionLeishmania AmazonensisInhibitory ActivityParasitologyArginase ActivityBiochemistryParasitic ProtozoaPharmacologyNatural SciencesMicrobiologyHost ResistanceMedicineDrug Discovery
Verbascoside (1) is a phenylethanoid glycoside that has antileishmanial activity against Leishmania infantum and Leishmania donovani. In this study, we verified the activity of 1 on Leishmania amazonensis and arginase inhibition. Compound 1 showed an EC50 of 19 μM against L. amazonensis promastigotes and is a competitive arginase inhibitor (Ki = 0.7 μM). Docking studies were performed to assess the interaction of 1 with arginase at the molecular level. Arginase is an enzyme of the polyamine biosynthesis pathway that is important to parasite infectivity, and the results of our study suggest that 1 could be useful to develop new approaches for treating leishmaniasis.
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