Hispidulin-7-O-Neohesperidoside from var. Attenuates the Production of Inflammatory Mediators in LPS-Induced Raw 264.7 Cells and HT-29 Cells.

BACKGROUND

Inflammatory bowel disease (IBD) is characterized by chronic inflammation of the gastrointestinal tract and involves secretion of inflammatory mediators. The flavone diglycoside hispidulin-7--neohesperidoside (HN) isolated from the methanolic extract of aerial parts of var. , but its pharmacologic activities, with the exception of alleviation of alcohol toxicity, have not been investigated to date.

OBJECTIVE

The aim of the present study was to investigate the anti-inflammatory activities of HN for the treatment of chronic inflammatory illnesses, including IBD.

MATERIALS AND METHODS

In lipopolysaccharide (LPS)-induced RAW264.7 cells and HT-29 cells, the effects of HN on cell viability and nitric oxide (NO) production were examined via MTT assay and the Griess reaction, respectively. The expression levels of interleukin (IL)-1α, IL-8, and tumor necrosis factor (TNF)-α and inducible nitric oxide synthase (iNOS) protein levels were measured by enzyme-linked immunosorbent assay and Western blotting, respectively.

RESULTS

HN concentration-dependently inhibited NO production in LPS-induced RAW 264.7 cells. Treatment with HN considerably downregulated the levels of the pro-inflammatory cytokines, IL-1β and TNF-α and the iNOS protein level in LPS-induced RAW 264.7 cells. Furthermore, HN inhibited the production of the chemotactic cytokine, IL-8, in LPS-induced HT-29 cells.

CONCLUSION

HN has potential as an anti-inflammatory agent to prevent and/or treat IBD.

SUMMARY

Hispidulin-7--neohesperidoside (HN) is flavone diglycoside isolated from the methanolic extract of aerial parts of . ussuriense.HN concentration-dependently inhibited NO production and considerably downregulated the levels of the proinflammatory cytokines, IL-1β and TNF-α, and the iNOS protein level in LPS-induced RAW 264.7 cells.HN inhibited the production of the chemotactic cytokine, IL-8, in LPS-induced HT-29 cells.HN has potential as an anti-inflammatory agent to prevent and/or treat IBD. IBD: Inflammatory bowel disease, HN: hispidulin-7--neohesperidoside, LPS: lipopolysaccharide, NO: nitric oxide, IL: interleukin, TNF: tumor necrosis factor, iNOS: inducible nitric oxide synthase, CD: Crohn's disease, UC: ulcerative colitis, RT: room temperature, DMEM: Dulbecco's modified Eagle's medium, FBS: fetal bovine serum, PBS: phosphate buffered saline, SDS: sodium dodecyl sulfate, PVDF: polyvinylidene difluoride, SD: standard deviation.