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机构地区:[1]中国药品生物制品检定所
出 处:《中成药》2005年第3期297-300,共4页Chinese Traditional Patent Medicine
摘 要:目的研究苦参碱(matrineMT)、氧化苦参碱(oxymatrineOMT)、槐果碱(sophocarpineSC)、槐定碱(sophoridineSRI)4种苦豆子类生物碱对环氧化酶活性的影响。方法用LPS刺激小鼠腹腔巨噬细胞产生PGE2,放免法测定4种生物碱对给予外源性花生四烯酸AA后其产物PGE2的含量来反映生物碱对环氧化酶2(COX2)的影响;用A23187刺激小鼠腹腔巨噬细胞产生6KetoPGF1a,放免法测定4种生物碱对给予外源性花生四烯酸AA后其产物6KetoPGF1a含量反映生物碱对环氧化酶1(COX1)的影响。结果4种生物碱对COX1均有一定的抑制作用,且具有剂量效应关系。除MT外,其余3种生物碱对COX2均有明显的抑制作用,且具有良好的剂量效应关系。结论除MT为COX1选择性抑制剂外,其余三种苦豆子生物碱均具有COX2选择性抑制作用。AIM: To study the effect of the four alkaloids of Sophora Alopecuroides On cycloxygenase(COX) activities in vitro. METHODS: The effect of matrine, oxymatrine sophocarpine and sophoridine on COX2 and COX1 activity were evaluated by the content of Prostaglandin E_2(PGE_2) and 6-Keto-PGF_~1a , respectively. The PGE_2 came from exogenous AA in cultured mouse peritoneal macrophage supernatants induced by lipopolysaccharide(LPS) 1 ug·mL^-1 was measured with radioimmunoassay(RIA) method using ~ 3H-labelled PGE_2. The 6-Keto-PGF_~1a from exogenous AA in cultured mouse peritoneal macrophage supernatants induced by calcium ionophore A23187 1 μmol·L^-1 was measured with RIA method using^125 I-labelled 6-Keto-PGF_~1a . RESULTS: The COX2 activities were markedly inhibited in a dose dependent manner by oxymatrine, sophocarpine and sophoridine, Respectively. Excluding the sophoridine, all the other three alkaloids of Sophora Alopecuroids obviously suppressed the activities of COX1, respectively. CONCLUSION: The in vitro results show that oxymatrine, sophocarpine and sophoridine may have the significant specific inhibitory action for COX2, in contrase, matrine may be COX1 selective inhibitor.
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