Although valerenic
acid (VA) is an important marker compound for
quantitative assessment of Valeriana officinalis products, little is known about its potential effects on adipocytes.
We investigated the effects of VA on adipocyte differentiation, adiponectin
production, and glucose uptake using 3T3-L1 adipocytes. The results
showed that VA promoted adipocyte differentiation and increased the
gene expression of adipogenesis and glucose uptake-related proteins,
including peroxisome proliferator-activated receptor gamma (PPARγ),
cytosine-cytosine-adenosine-adenosine-thymidine enhancer binding protein
alpha (C/EBPα), adiponectin, and glucose transporter 4 (GLUT4).
Additionally, cell cultures treated with VA had elevated adiponectin
secretion and glucose uptake. The PPARγ luciferase assay indicated
VA as a partial agonist of PPARγ, while the analysis using its
antagonist, GW9662, and a docking simulation between PPARγ and
VA revealed the binding site of VA as likely adjacent to the Ω
loop pocket of PPARγ. Taken together, these results demonstrate
that VA acts as a PPARγ partial agonist to promote adipocyte
differentiation, adiponectin production, and glucose uptake.