β-Sitosterol-2-hydroxypropyl-β-cyclodextrin inclusion complex: Characterization and inhibitory effect on adipogenesis in 3T3-L1 pre-adipocytes.

β-Sitosterol (Sit) has been used as a functional food additive. Among its many beneficial effects, this phytosterol plays a role in controlling obesity by inhibiting the adipogenesis process of pre-adipocytes. However, the highly lipophilic character of Sit limits its bioavailability. In the present study, 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) was used to form a complex with Sit, namely the Sit-HP-β-CD inclusion complex, and the inhibitory effect of this complex on adipogenesis in the 3T3-L1 pre-adipocyte cell line was investigated. The results of DSC, TLC, 1H NMR spectroscopy, and 2D ROESY showed that the Sit-HP-β-CD inclusion complex was successfully synthesized. In addition, the inhibitory effect of the Sit-HP-β-CD inclusion complex on adipogenesis was evaluated using the Oil Red O staining method and western blot analysis after a 14-day adipogenesis induction in 3T3-L1 pre-adipocytes. The results showed that the Sit-HP-β-CD inclusion complex had a higher efficiency than Sit in reducing intracellular lipid accumulation and the expression levels of PPARγ and FAS in 3T3-L1 cells, suggesting that the inhibitory effect on adipogenesis was improved by the formation of the Sit and HP-β-CD complex.