NF-κB Inhibitory and Antibacterial Helvolic and Fumagillin Derivatives from Aspergillus terreus
| Autor: | Shugeng Cao, Jennifer Saito, Shaobin Hou, Xiaohua Wu, John M. Pezzuto, KH Ahammad Uz Zaman, Tamara P. Kondratyuk, Zhenquan Hu |
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| Rok vydání: | 2020 |
| Předmět: |
Pharmacology
biology Stereochemistry Organic Chemistry Pharmaceutical Science NF-κB Nuclear magnetic resonance spectroscopy Inhibitory postsynaptic potential biology.organism_classification Analytical Chemistry chemistry.chemical_compound Complementary and alternative medicine Mauna kea chemistry Drug Discovery Ic50 values medicine Molecular Medicine Moiety Aspergillus terreus Fumagillin medicine.drug |
| Zdroj: | Journal of Natural Products. 83:730-737 |
| ISSN: | 1520-6025 0163-3864 |
| DOI: | 10.1021/acs.jnatprod.9b01190 |
| Popis: | Two new helvolic acid analogues (1 and 2) and one new fumagillin derivative containing an octahydroisobenzofuran moiety (3), together with four known compounds (4-7), were isolated from an Aspergillus terreus, isolated from soil collected from Mauna Kea, the highest mountain in Hawaii. Compound 4 was recorded in SciFinder with a CAS Registry Number of 1379525-35-5, but it was not documented in the cited reference (ACS Chem. Biol. 2012, 7, 137). The structures of compounds 1-4 were elucidated by NMR spectroscopy and HRMS and ECD analysis. Compounds 5 and 6 showed significant inhibitory activity against NF-κB with IC50 values of 2.7 ± 2.6 and 6.5 ± 0.8 μM, respectively. Compounds 1 and 2 were active against S. aureus with MICs of 6.25 and 6.25 μg/mL, respectively, while compound 5 inhibited E. coli with an MIC of 3.12 μg/mL. |
| Databáze: | OpenAIRE |
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