Sorbicillinoid analogs with cytotoxic and selective anti-Aspergillus activities from Scytalidium album

摘要: As part of an ongoing project to explore filamentous fungi for anticancer and antibiotic leads, 11 compounds were isolated identified from organic extract the fungus Scytalidium album (MSX51631) using bioactivity-directed fractionation against human cancer cell lines. Of these, eight a series sorbicillinoid analogs (1–8), which four new (scalbucillin A (2), scalbucillin B (3), C (6) D (8)), two phthalides (9–10) one was naphthalenone (11). Compounds (1–11) tested in MDA-MB-435 (melanoma) SW-620 (colon) Compound 1 most potent with IC50 values 1.5 0.5 μM, followed by compound 5 2.3 2.5 μM at 72 h. showed 48-h value 3.1 μM when lymphocytic leukemia line OSU-CLL, while nearly identical had almost no activity this assay. selective equipotent Aspergillus niger minimum IC 0.05 0.04 μg ml−1 (0.20 0.16 μM), respectively. The vitro hemolytic sheep erythrocytes investigated found provoke 10% hemolysis 52.5 45.0 μg ml−1, respectively, indicative promising safety factor.