五种原小檗碱型化合物对实验性耐缺氧及心律失常的作用
THE COMPARATIVE STUDIES ON THE ANTIHYFOXIC AND ANTIARRHYTHMIC EFFECT OF FIVE PROTO-BERBERINE COMPOUNDS
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摘要: 本文实验结果表明:(1)palmatine chloride(PC)、jatrorrhizinechloride(JC)25.6mg/kg I.P.对小鼠常压耐缺氧无保护作用,而同等剂量的13-methyl palmatine iodide(MPI)、berberine chloride(BC)、13-methyl berberineiodide(MBI)具有明显的保护作用。(2)BC、MBI、JC对氯仿引起的小鼠心室纤颤具有明显的保护作用,其ED_(50)±S.E.分别为14.91±0.104、16.46±0.059、15.84±0.122mg/kg,而PC、MPI则无作用。(3)静脉注射15mg/kg BC对乌头碱引起大鼠室纤具有明显保护作用,但对哇巴因引起的室性心律失常无明显保护作用。此外,讨论了该类药物结构与活性的关系。
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关键词:
- 抗心律失常 /
- 13—甲基小檗碱 /
- 小檗碱 /
- 13—甲基掌叶防己碱 /
- 耐缺氧
Abstract: The effects of antihypoxia and antiarrhythmia of five proto-compounds were studied. The results showed that an intraperitoneal dose of 25.6mg/kg of 13-methyl palmatine iodide(MPI), berberine chloride (BC) and 13-methyl berberine iodide (MBI) had significant protective effect on hypoxia in mice,but palmatine chloride (PC) and jatrorrhizine chloride (JC) had no such effect. It was also evident that the chloroform-induced arrhythmia in mice could be antagonised by BC. MBI and JC intraperitoneally, but compounds PC and MPI were ineffective. The ED50 of BC. MBI and JC antagonising the chloroforminduced arrhythmia in mice were 14.9±0.10. 16.5±O.06 and 15.8±0.12 mg/kg (x±S.E. ) respectively. BC was effective to antagonise the aconidine-induced ventricular fibrillation but had not any effect on arrhythmias induced by ouabain. The structure—activity relationship of five compounds were discussed. The groups at 13(R4). 2(R) and 3(R1) position of moiety seemed to be related to the antihypoxic and antiarrhythmic effects.-
Keywords:
- Antiarrhythmia /
- 13-Methyl berberine /
- Berberine /
- 13-Methyl palmatine /
- Antihypoxia
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