2. Academic Validation
  3. NF-κB Inhibitory and Antibacterial Helvolic and Fumagillin Derivatives from Aspergillus terreus

NF-κB Inhibitory and Antibacterial Helvolic and Fumagillin Derivatives from Aspergillus terreus

  • J Nat Prod. 2020 Mar 27;83(3):730-737. doi: 10.1021/acs.jnatprod.9b01190.
Kh Ahammad Uz Zaman 1,  Zhenquan Hu 2 3,  Xiaohua Wu 1,  Shaobin Hou 4,  Jennifer Saito 4,  Tamara P Kondratyuk 1,  John M Pezzuto 1 5,  Shugeng Cao 1
Affiliations

Affiliations

  • 1 Department of Pharmaceutical Sciences, Daniel K. Inouye College of Pharmacy, University of Hawai'i at Hilo, Hilo, Hawaii 96720, United States.
  • 2 Warshel Institute for Computational Biology, The Chinese University of Hong Kong, Shenzhen, People's Republic of China.
  • 3 School of Chemistry and Materials Science, University of Science and Technology of China, Hefei, Anhui 230026, People's Republic of China.
  • 4 Advanced Studies in Genomics, Proteomics and Bioinformatics (ASGPB), University of Hawai'i at Manoa, Honolulu, Hawaii 96822, United States.
  • 5 Arnold & Mary Schwartz College of Pharmacy and Health Sciences, Long Island University, 75 DeKalb Avenue, Brooklyn, New York 11201-5497, United States.
PMID: 32163285 DOI: 10.1021/acs.jnatprod.9b01190
Abstract

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.

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