1 research outputs found
Isolation of Arginase Inhibitors from the Bioactivity-Guided Fractionation of <i>Byrsonima coccolobifolia</i> Leaves and Stems
<i>Byrsonima coccolobifolia</i> leaf and stem extracts
were studied in the search for possible leishmanicidal compounds using
arginase (ARG) from <i>Leishmania amazonensis</i> as a molecular
target. Flavonoids <b>1b</b>, <b>1e</b>ā<b>1g</b>, <b>2a</b>, <b>2b</b>, and <b>2d</b>ā<b>2f</b> showed significant inhibitory activity, with IC<sub>50</sub> values ranging from 0.9 to 4.8 Ī¼M. The kinetics of the most
active compounds were determined. Flavonoids <b>1e</b>, <b>1f</b>, <b>2a</b>, <b>2b</b>, and <b>2e</b> were
characterized as noncompetitive inhibitors of ARG with dissociation
constants (<i>K</i><sub>i</sub>) ranging from 0.24 to 3.8
Ī¼M, demonstrating strong affinity. Structureāactivity
relationship studies revealed some similarities in the structural
features of flavonoids related to ARG activity