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马兜铃酸与圆斑蝰磷脂酶A2的相互作用:其对酶活性和病理活性的影响。

Interaction of aristolochic acid with Vipera russelli phospholipase A2: its effect on enzymatic and pathological activities.

作者信息

Vishwanath B S, Gowda T V

机构信息

Department of Biochemistry, University of Mysore, India.

出版信息

Toxicon. 1987;25(9):929-37. doi: 10.1016/0041-0101(87)90155-3.

Abstract

Aristolochic acid, an alkaloid from the plant Aristolochia species, interacts with the major basic phospholipase A2 from Vipera russelli venom. It is an uncompetitive inhibitor with a Ki of 9.9 X 10(-4)M when phosphatidylcholine is used as substrate. The inhibition of direct and indirect hemolysis is higher compared to the inhibition of phosphatidylcholine hydrolysis. Edema-inducing activity of Vipera russelli phospholipase A2 is inhibited by aristolochic acid when injected either as a mixture or separately. Both i.m. and i.p. administration of aristolochic acid following phospholipase injection are equally effective in inhibiting edema. The alkaloid inhibits the edema-inducing activity as soon as it reaches the site, but does not aid in recovery. Aristolochic acid failed to inhibit other pathological activities of the enzyme.

摘要

马兜铃酸是一种从马兜铃属植物中提取的生物碱,它能与蝰蛇毒液中的主要碱性磷脂酶A2相互作用。当以磷脂酰胆碱作为底物时,它是一种非竞争性抑制剂,抑制常数Ki为9.9×10⁻⁴M。与对磷脂酰胆碱水解的抑制作用相比,其对直接和间接溶血的抑制作用更强。当马兜铃酸与蝰蛇磷脂酶A2混合注射或分别注射时,均可抑制蝰蛇磷脂酶A2的致水肿活性。在注射磷脂酶后,通过肌肉注射或腹腔注射马兜铃酸,在抑制水肿方面效果相同。该生物碱一旦到达作用部位就能抑制致水肿活性,但无助于恢复。马兜铃酸未能抑制该酶的其他病理活性。

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