目的研究苦参碱抗炎机制和其抑制磷脂酶A2(PLA2)活性的作用.方法用[3H]花生四烯酸掺入大肠杆菌膜为底物检测细胞内外PLA2方法,测定了苦参碱对内毒素(LPS)造成的大鼠急性内毒素炎症时血清中分泌型磷脂酶A2(sPLA2)活性和外周血白细胞中胞浆型磷脂酶A2(cPLA2)活性的影响,同时用Fura2-AM作荧光指示剂检测胞内游离Ca2+浓度的变化,并通过大鼠足跖肿胀实验证实苦参碱的抗炎作用.结果在LPS介导的急性内毒素血症大鼠,30 mg/miL的苦参碱0.2 mLip 1 h对外周血sPLA2抑制效果最好,抑制率达(81.9±1.8)%,此时胞内cPLA2活性抑制率是(28.4±6.0)%,而Ca2+浓度是(157.10±20.56)nmol/L,比对照升高1 5.3%.足跖肿胀实验亦证明苦参碱对炎症有显著抑制作用.结论苦参碱是一种具有抗炎作用的新型PLA2抑制剂.

ObjectTo study the antiinf lammatory effect of matrine and its active mechanism. MethodsThe matrine effects on activities of secretory phospholipa se A2 (sPLA2) in peripheral serum and cytosolicphospholipase A2 ( cPLA2 ) in leucocyte were measured with Escherichia coli membrane incorporated by[3H] arachidonic acid as the substrate;the Ca2+ level of leucocyte was determined using Frua2-AM loading method, and the rat plantar swelling test was used to examine the antiinflammatory effect of matrine. ResultsOne hour after ip 30 mg /mL matrine,the inhibitory rate of sPLA2 activity was(81.9±1.8)%,cPLA2(28.4±6.0)%, while Ca2+ concent ration was(157.10± 20.56) nmol /L which was 15. 3% higherthan that of the control. Plantar swelling test showed that matrine had a significant anti-inflamma tory effect.Conclusion Matrine is a novel PLA2 inhibitor with anti-inflammatory effect.

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