新化合物甲胺鳶尾素對麻醉犬急性心肌缺血的保護作用   全文下載

Protective Effect of Methylamine Irisolidone, a Novel Compound, on Acute Myocardial Ischemia in Anesthetized Dogs

近來我們的研究結果表明葛花?，從傳統中藥葛花中提取的一種化合物，對實驗性心肌缺血具有保護作用，但是這種化合物必須在?-β- 環糊精助溶下才能使用，后者用于靜脈注射爭議較大。甲胺鳶尾素是葛花?經結構修飾得到的新化合物，水溶性較好。本文研究了甲胺鳶尾素對麻醉犬急性心肌缺血的影響。結果表明，甲胺鳶尾素80.0 mg/kg 劑量組給藥後240 分鐘可明顯減輕麻醉犬急性心肌缺血梗塞面積，降低血清乳酸脫氫?（LDH）和肌酸激?同工?（CK-MB）水平。由此可見，新化合物甲胺鳶尾素對麻醉犬冠狀動脈前降枝結紮所致的心肌缺血具有明顯保護與改善作用，其機制可能與抑制LDH 和CK-MB 釋放，穩定心肌細胞膜，改善心肌微循環和能量代謝有關。

Kakkalide, a compound obtained from a traditional Chinese medicine Puerariae flos, has been shown significant anti-ischemia activity in animal experiments recently. However, the solubility of the compound need to be enhanced with hydroxypropyl-β- cyclodextrin, which is a strong controversial solution adjuvant via intravenous administration. Methylamine irisolidone is a structurally modified kakkalide with good solubility in the water. In this study, the effect of this new compound on acute myocardial ischemia in dogs was investigated. The results showed that methylamine irisolidone (80 mg/kg, i.v) could reduce the myocardial infarct areas in dogs with myocardial infarction. The serum lactate dehydrogenase (LDH) activity and MB isoenzyme of creatine kinase (CK-MB) were suppressed by methylamine irisolidone after 240 min of administration. These results suggested that methylamine irisolidone exerts the protective effects on myocardial ischemia injury, which may be due to its function of inhibiting LDH and CK-MB releasing, stabilizing myocardial cell membrane and improving myocardial microcirculation and metabolism.