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Purpose  To investigate the effects of icariin, a major constituent of flavonoids isolated from the herb  Epimedium , on cigarette smoke (CS) induced inflammatory responses  in vivo  and  in vitro .    Methods    In vivo , BALB/c mice were exposed to smoke of 15 cigarettes for 1 h/day, 6 days/week for 3 months and dosed with icariin (25, 50 and 100 mg/kg) or dexamethasone (1 mg/kg).  In vitro , A549 cells were incubated with icariin (10, 50 and 100 µM) followed by treatments with CSE (2.5%).    Results  We found that icariin significantly protected pulmonary function and attenuated CS-induced inflammatory response by decreasing inflammatory cells and production of TNF-α, IL-8 and MMP-9 in both the serum and BALF of CS-exposed mice and decreasing production of TNF-α and IL-8 in the supernatant of CSE-exposed A549 cells. Icariin also showed properties in inhibiting the phosphorylation of NF-κB p65 protein and blocking the degradation of IΚB-α protein. Further studies revealed that icariin administration markedly restore CS-reduced GR protein and mRNA expression, which might subsequently contribute to the attenuation of CS-induced respiratory inflammatory response.    Conclusion  Together these results suggest that icariin has anti-inflammatory effects in cigarette smoke induced inflammatory models  in vivo  and  in vitro , possibly achieved by suppressing NF-κB activation and modulating GR protein expression.

Icariin Ameliorates Cigarette Smoke Induced Inflammatory Responses via Suppression of NF-κB and Modulation of GR In Vivo and In Vitro