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Cardiovascular Pharmacology of Sinomenine: The Mechanical and Electropharmacological Actions

机译：青藤碱的心血管药理作用：机械和电药理作用

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Sinomenine is one of the alkaloids extracted from Chinese medical plant, Sinomenium acutum Rehder et Wilson. Sinomenine has been used for Rheumatoid arthritis as an anti-infl ammatory and immunomodulative drugs. We have so far been investigated the cardiovascular pharmacological actions of sinomenine. Sinomenine dilated NE (5 μM)-, KCl (60mM)- and PDB (300 nM)-induced vasoconstrictions. The pretreatment with nicardipine (0.1 μM), staurosporine (30 nM), L-NMMA (100 μM), indomethacin (10 μM) or propranolol signifi cantly attenuated the sinomenine-induced vasorelaxation. Therefore, these results indicate that sinomenine causes the vasorelaxation by the involvement with the inhibitions of Ca2+ current (ICa) and PK-C, β-adrenoceptor stimulation, and the activation of NO and PGI2 syntheses in endothelium. On the other hand, in the ventricular cardiomyocytes of guinea pig, sinomenine inhibits ICa and simultaneously decreases the delayed rectifi er K+ current (IK), resulting in the prolongation of action potential duration. Sinomenine also suppresses the dysrhysmias induced by triggered activities under the Ca2+ overload condition. Therefore, sinomenine may be expected as one of effective therapeutic drugs for heart failure and dysrhythmias, and may maintain the cardiovascular functions due to modulation of cardiac ionic channels and blood vessels.
机译：青藤碱是从中国药用植物青藤Rehder et Wilson提取的生物碱之一。青藤碱已被用作类风湿关节炎的抗炎药和免疫调节药物。迄今为止，我们已经研究了青藤碱的心血管药理作用。青藤碱使NE（5μM）-，KCl（60mM）-和PDB（300 nM）引起的血管收缩扩张。尼卡地平（0.1μM），十字孢碱（30 nM），L-NMMA（100μM），消炎痛（10μM）或普萘洛尔的预处理显着减弱了青藤碱诱导的血管舒张。因此，这些结果表明青藤碱通过抑制Ca 2+电流（ICa）和PK-C，β-肾上腺素受体刺激以及内皮中NO和PGI 2合成的激活而引起血管舒张。另一方面，在豚鼠的心室心肌细胞中，青藤碱抑制ICa并同时降低延迟整流K +电流（IK），从而导致动作电位持续时间延长。青藤碱还抑制Ca2 +超负荷条件下触发活动引起的肌萎缩。因此，青藤碱可望作为心力衰竭和心律不齐的有效治疗药物之一，并由于心脏离子通道和血管的调节而可维持心血管功能。

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