Isolation of Arginase Inhibitors from the Bioactivity-Guided Fractionation of Byrsonima coccolobifolia Leaves and Stems.

Journal of natural products

PubMedID: 24521209

de Sousa LR, Ramalho SD, Burger MC, Nebo L, Fernandes JB, da Silva MF, Iemma MR, Corrêa CJ, de Souza DH, Lima MI, Vieira PC. Isolation of Arginase Inhibitors from the Bioactivity-Guided Fractionation of Byrsonima coccolobifolia Leaves and Stems. J Nat Prod. 2014;.
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.