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.
Maquiaveli, C.C., Lucon Júnior, J.F., Brogi, S., Campiani, G., Gemma, S., Vieira, P.C., et al. (2016). Verbascoside Inhibits Promastigote Growth and Arginase Activity of Leishmania amazonensis. JOURNAL OF NATURAL PRODUCTS, 79(5), 1459-63-1463 [10.1021/acs.jnatprod.5b00875].
Verbascoside Inhibits Promastigote Growth and Arginase Activity of Leishmania amazonensis
BROGI, SIMONE;CAMPIANI, GIUSEPPE;GEMMA, SANDRA;
2016-01-01
Abstract
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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https://hdl.handle.net/11365/995547
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