title: Isolation of arginase inhibitors from the bioactivity-guided fractionation of Byrsonima coccolobifolia leaves and stems.
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.
authors: Departamento de Química, Universidade Federal de São Carlos , Rod. Washington Luís, Km 235, 13565-905 São Carlos, SP, Brazil.
authors: Lorena Ramos Freitas
authors: LR
authors: de Sousa
authors: Suelem Demuner
authors: SD
authors: Ramalho
authors: Marcela Carmen de Melo
authors: MC
authors: Burger
authors: Liliane
authors: L
authors: Nebo
authors: João Batista
authors: JB
authors: Fernandes
authors: Maria Fátima das Graças Fernandes
authors: MF
authors: da Silva
authors: Mônica Rosas da Costa
authors: MR
authors: Iemma
authors: Caroindes Julia
authors: CJ
authors: Corrêa
authors: Dulce Helena Ferreira
authors: DH
authors: de Souza
authors: Maria Inês Salgueiro
authors: MI
authors: Lima
authors: Paulo Cezar
authors: PC
authors: Vieira
mesh_terms: D001119:Arginase / Q000037:antagonists & inhibitors*; D001938:Brazil; D005419:Flavonoids / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D007891:Leishmania / Q000187:drug effects*; D029581:Malpighiaceae / Q000737:chemistry*; D015394:Molecular Structure; D018515:Plant Leaves / Q000737:chemistry; D018547:Plant Stems / Q000737:chemistry; D013329:Structure-Activity Relationship
chemical_list: D005419:Flavonoids; D001119:Arginase