Bavachinin analogues as agonists of pan-peroxisome proliferator-activated receptors
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Peroxisome proliferator-activated receptors (PPARs) agonists contribute to the regulation of glucose, lipid, and cholesterol metabolism and have emerged as key targets to treat metabolic syndrome. In our previous study, the natural compound bavachinin was found to have pan-PPAR agonist activity. In this study, five isoflavones, three isoflavanones, and five scaffold-hopping analogues of bavachinin were designed, synthesised, and evaluated through reporter gene assays for pan-PPAR agonist activity. The analogue 2-(4-hydroxyphenyl)-6-isopentenyl-7-methoxy-2,3-dihydroquinolin-4(1H)-one (21) was identified as a pan-PPAR agonist, exhibiting substantially higher PPAR α/β agonist activity and equal PPAR-γ agonist activity than does bavachinin.
KeywordsBavachinin Metabolic syndrome PPARs Reporter gene assays
This work was supported by the Excellent Academic Leaders Program of Shanghai (16XD1403500), the Shanghai Science and Technology Committee funding (16401902000) and the program of Shanghai E-Research Institute of Bioactive Constituents in Traditional Chinese Medicine.
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Conflict of interest
The authors declare that they have no conflict of interest.
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