<p>Peroxisome proliferator-activated receptor γ (PPARγ) is a transcriptional factor and key regulatory element in glucose and lipid metabolism. We have attempted to determine the structure–activity relationship between flavonoids as PPARγ agonists through a literature search. To compare results from different studies and methods, we have recalculated them to the percentage of positive control (%<sub>PC</sub>). We have also described various methods used to determine PPARγ agonists. The most promising PPARγ agonists are isoflavones, namely 4'-fluoro-7-hydroxyisoflavone (<b>4</b>; %<sub>PC</sub> = 710.3%). The results presented in this review could be used for further semisynthetic modifications of flavonoids to enhance their PPARγ agonistic activity.</p>

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Structure activity relationship of flavonoids as PPARγ agonists

  • Jakub Treml,
  • Daniela Nykodýmová,
  • Peter Kubatka

摘要

Peroxisome proliferator-activated receptor γ (PPARγ) is a transcriptional factor and key regulatory element in glucose and lipid metabolism. We have attempted to determine the structure–activity relationship between flavonoids as PPARγ agonists through a literature search. To compare results from different studies and methods, we have recalculated them to the percentage of positive control (%PC). We have also described various methods used to determine PPARγ agonists. The most promising PPARγ agonists are isoflavones, namely 4'-fluoro-7-hydroxyisoflavone (4; %PC = 710.3%). The results presented in this review could be used for further semisynthetic modifications of flavonoids to enhance their PPARγ agonistic activity.