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Bupleurum falcatum L. is employed in oriental medicine in Korea. This root has been used for anti-inflammatory, anti-pyretic, and anti-hepatotoxic effects in the treatments of common cold, fever, and hepatitis. One of major bioactive compounds of Radix Bupleuri is the saikosaponin a (SSNa). However, little is known concerning the effects of SSNa on obesity associated with a state of low-grade inflammation. Consequently, this study was conducted to determine the inhibition of the inflammation pathway of SSNa in obesity. MTT assay was conducted for cytotoxicity and viability; nuclear and cytoplasmic fractions were extracted from adipocytes for translocation of nuclear factor-κB cells (NF-κB); nitric oxide (NO) production and secretion using Griess reagent; reverse transcription-polymerase chain reaction (RT-PCR) and immunoblotting for mRNA and protein levels associated with inflammation in the hypertrophied adipocytes. The results revealed that SSNa significantly decreased the expression of tumor necrosis factor-α (TNFα), interleukin (IL)-1β and IL-6 as proinflammatory cytokines, compared to that of non-treated control cells. Inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) as inflammatory factors were reduced by treatment of these cells with SSNa and also suppressed NO production. Phosphorylation of IκBα was inhibited and translocation of NF-κB was suppressed via the ERK pathway in response to SSNa treatment. In conclusion, the results demonstrated that SSNa can inhibit the expression of inflammatory-associated genes in hypertrophied 3T3-L1 adipocytes and is a potent inhibitor of NF-κB activation. Thus these results suggest that SSNa is a novel therapeutic agent against that can be used against obesity-associated inflammation.

Saikosaponin a, an active compound of Radix Bupleuri, attenuates inflammation in hypertrophied 3T3-L1 adipocytes via ERK/NF-κB signaling pathways