Aim: Bofutsushosan (BT) has been used to treat systemic inflammatory diseases, including obesity, according to an original Chinese prescription book written in 1172. The '-san' suffix of 'Bofutsushosan' means that BT is prescribed as a pulverized crude drug. Peroxisome proliferator-activated receptor (PPAR)γ is known to play a pivotal role in adipocyte differentiation and to downregulate the transcription of adipocytokine genes leading to an inflammatory response. Given that the 'san' formulation is important for the anti-inflammation effect, we compared the anti-obesity and anti-inflammatory effects of PPARγ induced by BT powder with those by BT extract. Methods: The PPARγ agonistic activity of the separate crude BT drug components was measured on enzyme-linked immunosorbent assay (ELISA). For in vivo studies, male mice of the C57BL/6 strain were fed a high-fat diet containing 6.4% BT extract or BT powder for 65 days. Results: Water extract prepared from the BT components Saposhnikoviae Radix, Zingiberis Rhizoma, Ephedra Herba, and Scutellariae Radix had strong PPARγ ligand activity on ELISA. BT powder produced a significant reduction in visceral fat weight in addition to increases in PPARγ mRNA expression and peroxidase activity in visceral fat. BT powder and BT extract considerably decreased fatty acid binding protein-4 (FABP4), although the difference was not statistically significant. Conclusion: Peroxidase catalyzes lipid peroxides. Oxidative stress and inflammation induce FABP4 expression. BT powder was a more effective anti-inflammatory agent than BT extract. Furthermore, FABP4 triggers the ubiquitination and subsequent proteasomal degradation of PPARγ. This suggests that decrease in PPARγ by FABP4 might be restored by treatment with BT powder.
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