np9b01190_si_001.pdf (1.29 MB)
NF-κB Inhibitory and Antibacterial Helvolic and Fumagillin Derivatives from Aspergillus terreus
journal contribution
posted on 2020-03-12, 16:05 authored by KH Ahammad
Uz Zaman, Zhenquan Hu, Xiaohua Wu, Shaobin Hou, Jennifer Saito, Tamara P. Kondratyuk, John M. Pezzuto, Shugeng CaoTwo 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.