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Abstract Title:

Dietary polyphenols rutin, taxifolin and quercetin related compounds target Leishmania amazonensis arginase.

Abstract Source:

Food Funct. 2019 Jun 19 ;10(6):3172-3180. PMID: 31134235

Abstract Author(s):

Edson Roberto da Silva, Simone Brogi, João Francisco Lucon-Júnior, Giuseppe Campiani, Sandra Gemma, Claudia do Carmo Maquiaveli

Article Affiliation:

Edson Roberto da Silva

Abstract:

Quercetin related compounds were tested against Leishmania amazonensis arginase, a potential target for the development of new approaches in treating leishmaniasis. The IC50 and kinetic analysis were performed to determine the dissociation constant Ki and the inhibition mechanism of the parasite's arginase enzyme. The best arginase inhibition was obtained from taxifolin (dihydroquercetin) with IC50 = 1.6± 0.1 μM. This study showed for the first time that rutin (IC50 = 10.4 ± 0.8 μM), and human metabolite quercetin-3-O-glucuronide (IC50 = 8.2 ± 0.4 μM), target L. amazonensis arginase. In addition, computational studies applying molecular docking simulations were performed to gain insight intothe molecular basis for arginase inhibition by the competitive inhibitors. Our results suggest that these compounds could be exploited to develop new approaches for treating leishmaniasis through molecular nutrition supplement in a drug-based therapy.

Study Type : In Vitro Study

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