Ischemia-reperfusion (I/R) injury is a complicated pathophysiological process, which is involved in calcium overload, free radical production, metabolic abnormalities, and inflammatory reaction. With the development of modern molecular biology, the expression and regulation of gene in myocardial I/R injury are focused on NF-κB.1Inflammatory reactions play an important role in I/R injury.2 TNF-α, an important inflammatory cytokine, is regulated by NF-κB and counteracts the activation of NF-κB. Sometimes, improper activation of NF-κB can induce excessive inflammatory responses and injury, so, modulation of NF-κB activation may dedicate a new target in alleviation of myocardial I/R injury.3Our previous studies have proved that Bai-hua Qian-hu (Peucedanum praeruptorum Dunn, BQ), a Chinese traditional plant had cardioprotective action in I/R animals.4 Its active ingredient Pd-Ia, a Ca2+-influx blocker5 and K+-channel opener,6 had similar effects. Meanwhile, it relieved inflammatory reaction and apoptosis in I/R myocardium through inhibition of interleukin-6 and Fas, bax, bcl-2 protein expression.7 However, the effects of BQ and Pd-Ia on the activation of NF-κB and the expression of TNF-α in I/R myocardium have not been clear yet. In this study, the effects of BQ and Pd-Ia on these two factors were investigated to further ascertain the molecular protective mechanism of BQ in I/R myocardium.