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Eleven compounds were isolated from Poraqueiba sericea stems and identified as niga-ichigoside-F1 (1), trachelosperoside B1 (2), 4-epi-niga-ichigoside (7), 19α-hydroxyasiatic acid (3), myrianthic acid (4), hyptatic acid (5), trachelosperogenin B (6), arjunolic acid (8), and trachelosperogenin E (9), secologanoside (10) and secoxyloganin (11). Compounds 1–11 were tested for their antileishmanial activities against Leishmania infantum promastigotes, 1–6 and 8–11 were tested for their cytotoxic activities on fibroblasts, 1–3, 5–6, 8–11 were evaluated for their anti-elastase and anti-acetylcholinesterase assays activities by a spectrophotometric method and 1–2, 5 and 7–10 were tested using bioautography for their β-glucosidase. No antileishmanial activity was detected; compounds 1, 2 and 11 showed a moderate cytotoxic activity with IC50 17.7, 20.5 and 10.9 μg/mL, respectively; compounds 2, 8, 9 and 10 gave a percentage of inhibition ranging from 13 to 16% (at 50 μg/mL) and compounds 1 and 2 showed an inhibition zone on β-glucosidase and anti-acetylcholinesterase assays. [ABSTRACT FROM AUTHOR]

We identified 6-deoxy-homoDMDP as a potent inhibitor of chitin synthase (Ki=38?µM), displaying an uncompetitive inhibition pattern. Dual inhibition was also performed with the enzymatic reaction product uridine 5'-diphosphate in order to evaluate the concurrent effect of both inhibitors. An interaction coefficient a of 0.9 was found, revealing synergistic inhibition. [ABSTRACT FROM AUTHOR]