Isolation of arginase inhibitors from the bioactivity-guided fractionation of Byrsonima coccolobifolia leaves and stems

  • J Nat Prod. 2014 Feb 28;77(2):392-6. doi: 10.1021/np400717m.
Lorena Ramos Freitas de Sousa  1 ,  Suelem Demuner Ramalho ,  Marcela Carmen de Melo Burger ,  Liliane Nebo ,  João Batista Fernandes ,  Maria Fátima das Graças Fernandes da Silva ,  Mônica Rosas da Costa Iemma ,  Caroindes Julia Corrêa ,  Dulce Helena Ferreira de Souza ,  Maria Inês Salgueiro Lima ,  Paulo Cezar Vieira
Affiliations
  • 1. Departamento de Química, Universidade Federal de São Carlos , Rod. Washington Luís, Km 235, 13565-905 São Carlos, SP, Brazil.
PMID: 24521209 DOI: 10.1021/np400717m
Abstract

Byrsonima coccolobifolia leaf and stem extracts were studied in the search for possible leishmanicidal compounds using Arginase (ARG) from Leishmania amazonensis as a molecular target. Flavonoids 1b, 1e-1g, 2a, 2b, and 2d-2f showed significant inhibitory activity, with IC50 values ranging from 0.9 to 4.8 μM. The kinetics of the most active compounds were determined. Flavonoids 1e, 1f, 2a, 2b, and 2e were characterized as noncompetitive inhibitors of ARG with dissociation constants (Ki) ranging from 0.24 to 3.8 μM, demonstrating strong affinity. Structure-activity relationship studies revealed some similarities in the structural features of Flavonoids related to ARG activity.

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