butyrolactone-i and terrein

The marine fungus, Aspergillus flavipes (MTCC 5220), was isolated from the pneumatophore of a mangrove plant Acanthus ilicifolius found in Goa, India. The crude extract of A. flavipes was found to show anti-inflammatory activity. It blocked interleukin-6 (IL-6) and tumor necrosis factor-α (TNF-α) production in lipopolysaccharide (LPS)-activated THP-1 cells with IC

Topics: 4-Butyrolactone; Anti-Inflammatory Agents; Aspergillus; Biological Products; Cyclopentanes; Humans; Interleukin-6; Lipopolysaccharides; THP-1 Cells; Tumor Necrosis Factor-alpha

The compounds terrein (1), butyrolactone I (2), and butyrolactone V (3) were isolated from the ethyl acetate extract (EtOAc) of the endophytic fungus Aspergillus terreus-F7 obtained from Hyptis suaveolens (L.) Poit. The extract and the compounds presented schistosomicidal activity against Schistosoma mansoni; at 100 µg/mL for EtOAc extract, 1297.3 µM for compound 1, 235.6 µM for compound 2, and 454.1 µM for compound 3, they killed 100% of the parasites after 72 h of treatment. Compounds 1, 2, and 3 exerted moderate leishmanicidal activity against Leishmania amazonensis (IC

Topics: 4-Butyrolactone; Animals; Anthelmintics; Antineoplastic Agents; Antiprotozoal Agents; Aspergillus; Cell Line, Tumor; Cell Proliferation; Cell Survival; Cyclopentanes; Endophytes; Furans; Humans; Hyptis; Lactones; Leishmania; MCF-7 Cells; Schistosoma

Breast cancer cells express ABCG2 transporters, which mediate multidrug resistance. Discovering a novel compound that can suppress ABCG2 expression and restore drug sensitivity could be the key to improving breast cancer therapeutics. In the current work, one new nor-neolignan, asperjinone (1), as well as 12 other known compounds, was isolated from Aspergillus terreus. The structure of the new isolate was determined by spectroscopic methods. Among these isolates, terrein (2) displayed strong cytotoxicity against breast cancer MCF-7 cells. Treatment with terrein (2) significantly suppressed growth of ABCG2-expressing breast cancer cells. This suppressive effect was achieved by inducing apoptosis via activating the caspase-7 pathway and inhibiting the Akt signaling pathway, which led to a decrease in ABCG2-expressing cells and a reduction in the side-population phenotype.

Topics: Antineoplastic Agents; Aspergillus; ATP Binding Cassette Transporter, Subfamily G, Member 2; ATP-Binding Cassette Transporters; Breast Neoplasms; Caspase 7; Cyclopentanes; Drug Screening Assays, Antitumor; Female; Humans; Lignans; Molecular Structure; Neoplasm Proteins; Nuclear Magnetic Resonance, Biomolecular; Proto-Oncogene Proteins c-akt; Taiwan

Chloroform and ethyl acetate extracts of Aspergillus fischeri TISTR 3272 showed good growth inhibitory activity on Mimosa pigra and Echinochloa crus-galli. Bioassay-directed fractionation of the active extracts led to the isolation of five known compounds, (+)-terrein (1), (-)-6-hydroxymellein (2), two diketopiperazines (cyclo-(S-Pro-S-Leu) (3) and cyclo-(S-Pro-S-Val) (4)) and butyrolactone I (5). Compounds 2-5 were reported for the first time in this fungus. Their structural determinations were based on analyses of spectroscopic data and their weed growth inhibitory effects were assessed.

Topics: 4-Butyrolactone; Aspergillus; Cyclopentanes; Diketopiperazines; Echinochloa; Herbicides; Isocoumarins; Mimosa; Molecular Structure; Ochratoxins; Peptides, Cyclic