Using molecular docking screening for identifying hyperoside as an inhibitor of fatty acid binding protein 4 from a natural product database

Yan Wang, Huang Quan Lin, Chu Ying Xiao, Wai Kit Law, Jian Shu Hu, Tsz Ming Ip, David Chi Cheong Wan

Research output: Contribution to journalArticlepeer-review

5 Scopus citations

Abstract

The inhibition of fatty acid binding protein 4 (FABP4) by using small molecules could potentially provide therapeutic opportunities for metabolic disorders treatment. According to the results of our in-house virtual screening on the herbal molecules database, this study reports flavonols as an ideal scaffold for FABP4 inhibitors development. Among the popular flavonols examined, we identified hyperoside as a promising FABP4 inhibitor. Identical to the well-known FABP4 inhibitor BMS309403, hyperoside induced lipid accumulation and upregulated peroxisome proliferator-activated receptor γ (PPARγ) protein expression during the adipocyte differentiation process. Furthermore, both PPARγ antagonist and FABP4 overexpression attenuated hyperoside-induced adipogenesis, indicating that hyperoside promoted adipogenesis in adipocytes via the FABP4/PPARγ pathway. We anticipate hyperoside to be a promising, novel FABP4 inhibitor for antidiabetic drug development.

Original languageEnglish (US)
Pages (from-to)159-170
Number of pages12
JournalJournal of Functional Foods
Volume20
DOIs
StatePublished - Jan 1 2016

Keywords

  • Adipogenesis
  • Fatty acid binding protein 4 inhibitor
  • Flavonols
  • Hyperoside

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