【摘要】 目的:从青藏高原地产中药材中筛选磷酸二脂酶4(PDE4)特异性抑制剂。方法:选取甘草、羌活、柴胡、大黄、红景天5种药材为试验对象,以PDE4特异性抑制剂Rolipram为阳性对照组,从猪中性粒细胞中提取PDE4进行PDE4活性实验。结果:5 mg/mL甘草、羌活、柴胡、大黄、红景天水提物、10μmol/L Rolipram组PDE4活性分别为6.8%、11.02%、11.07%、12.7%、18.7%、7.61%;抑制率分别为38.18%、0.02%、-0.47%、-15.21%、-69.66%、30.90%。与空白对照组PDE4活性相比较,甘草组P<0.05;红景天组P<0.001。与Rolipram组抑制率相比较,柴胡组P<0.05;大黄组P<0.01;红景天组P<0.001。甘草组对PDE4抑制率高于PDE4特异性抑制剂Rolipram。结论:5mg/mL甘草水提物能显著抑制PDE4活性,且高于PDE4特异性抑制剂Rolipram,5 mg/mL柴胡、羌活水提物对PDE4活性的影响不明显,5 mg/mL大黄水提物对PDE4的活性具有促进作用,5 mg/mL红景天对PDE4的活性具有极显著的促进作用。更多还原

【Abstract】 In order to select phosphodiesterase 4(PDE4)specific inhibitors from herbal medicines in Qinghai-Tibetan Plateau,five kinds of Qinghai-Tibetan Plateau herbal medicines(Radix Glycyrrhizae,Rhizoma Seu Radix Notopterygii,Radix Bupleuri,Radix Et Rhizoma Rhei,Radix Rhodiolae)were selected as the experimental group,and PDE4 specific inhibitor Rolipram was as positive control group.The experiment was conducted using PDE4 extracted from porcine neutrophil.The results showed that PDE4 activity of 5 mg/mL water extract of five herbal groups and Rolipram group was 6.8%,11.02%,11.07%,12.7%,18.7% and 7.61%,respectively;the inhibition rate was 38.18%,0.02%,-0.47%,-15.21%,-69.66%and 30.90%,respectively.The PDE4 activity of Radix Glycyrrhizae group(P<0.05)and Radix Rhodiolae group(P<0.001)were all different from that of blank control group.The inhibition rate of Radix Bupleuri group(P<0.05),Radix Et Rhizoma Rhei group(P<0.01) and Radix Rhodiolae group(P<0.001)were all different from that of Rolipram group.The inhibition rate of Radix Glycyrrhizae was higher than that of rolipram.Conclusion:5 mg/mL water extract of Radix Glycyrrhizae could significantly inhibit the activity of PDE4 which was superior to PDE4 specific inhibitor Rolipram,while the extract of Radix Bupleuri and Rhizoma Seu Radix Notopterygii had no obvious inhibition on the activity of PDE4.5 mg/mL water extract of Radix Et Rhizoma Rhei and Radix Rhodiolae had enhancement effect on the activity of PDE4 especially the latter.更多还原