2-Arylbenzo[b]furan derivatives as potent human lipoxygenase inhibitors

Li Lang, Ningning Dong, Deyan Wu, Xue Yao, Weiqiang Lu, Chen Zhang, Ping Ouyang, Jin Zhu, Yun Tang, Wei Wang, Jian Li, Jin Huang

Research output: Contribution to journalArticlepeer-review

10 Scopus citations


Human lipoxygenases (LOXs) have been emerging as effective therapeutic targets for inflammatory diseases. In this study, we found that four natural 2-arylbenzo[b]furan derivatives isolated from Artocarpus heterophyllus exhibited potent inhibitory activities against human LOXs, including moracin C (1), artoindonesianin B-1 (2), moracin D (3), moracin M (4). In our in vitro experiments, compound 1 was identified as the most potent LOX inhibitor and the moderate subtype selective inhibitor of 12-LOX. Compounds 1 and 2 act as competitive inhibitors of LOXs. Moreover, 1 significantly inhibits LTB4 production and chemotactic capacity of neutrophils, and is capable of protecting vascular barrier from plasma leakage in vivo. In addition, the preliminary structure–activity relationship analysis was performed based on the above four naturally occurring (1–4) and six additional synthetic 2-arylbenzo[b]furan derivatives. Taken together, these 2-arylbenzo[b]furan derivatives, as LOXs inhibitors, could represent valuable leads for the future development of therapeutic agents for inflammatory diseases.

Original languageEnglish (US)
Pages (from-to)98-105
Number of pages8
JournalJournal of Enzyme Inhibition and Medicinal Chemistry
StatePublished - Nov 4 2016
Externally publishedYes


  • 2-arylbenzo[b]furan
  • Anti-inflammation
  • Artocarpus heterophyllus
  • lipoxygenase
  • neutrophils

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery


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