Abstract
Two new butyrolactones: aspernolides F (6) and G (7), together with three stigmasterol derivatives: (22E, 24R)-stigmasta-5,7,22-trien-3-beta-ol (1), stigmast-4-ene-3-one (2), and stigmasta-4,6,8(14), 22-tetraen-3-one (3), two meroterpenoids: terretonin A (4) and terretonin (5), and a butyrolactone derivative: butyrolactone VI (8) have been isolated from the endophytic fungus Aspergillus terreus isolated from the roots of Carthamus lanatus (Asteraceae). Their structures were determined by spectroscopic means (1D, 2D NMR, and HRESIMS), as well as optical rotation measurement and comparison with literature data. The isolated compounds were evaluated for their anti-microbial, antimalarial, anti-leishmanial, and cytotoxic activities. Compound 1 displayed a potent activity against MRSA and C. neoformans with IC50 values of 0.96 mu g/mL and 4.38 mu g/mL, respectively compared to ciprofloxacin (IC50 0.07 mu g/mL) and amphotericin B (IC50 0.34 mu g/mL), respectively. While, 6 showed good activity against C. neoformans (IC50 5.19 mu g/mL) and mild activity against MRSA (IC50 6.39 mu g/mL). Moreover, 1 and 2 exhibited very good anti-leishmanial activity towards L. donovani with IC50 values of 4.61 and 6.31 mu g/mL, respectively and IC90 values of 6.02 and 16.71 mu g/mL, respectively. (C) 2015 Phytochemical Society of Europe. Published by Elsevier B. V. All rights reserved.