【摘要】 临床报道丹参酮Ⅱ-A磺酸钠（T）对冠心病心绞痛和胸闷症状有一定疗效,并能改善缺血性心电图。药理研究证明,具有抗钙和抗钙调蛋白（CaM）作用。本文进一步研究了T对正常的和异丙基肾上腺素（Isp）兴奋的家兔心肌线粒体摄取⁴⁵Ca²⁺的影响。本文制备的心肌线粒体经透射和扫描电镜检查证明形态和内部结构均正常。线粒体蛋白在0.1mg/ml以下时其钙摄取与浓度呈线性关系。Isp10^-6mol/L可使线粒体钙摄取提高20±5％。T在10μg/ml时对正常的和Isp兴奋的线粒体摄取钙的抑制率分别为61.2±3.9％和54.2±5.1％。已知大剂量Isp可引起心肌线粒体钙超载和细胞坏死。戊脉安可减少以上病理性损害。本文结果表明T也具有类似戊脉安的保护心肌的作用。更多还原

【Abstract】 Sodium Tanshinone II-A sulfonate (T) is a water soluble derivative of Tan-shinone II-A which was isolated from Salvia miltiorrhiza. Given to coronary patients, T relieved the anginal pain and the feeling of chest tightness, and improved the ischemic alterations in the electro-cardiogram. Recently it was reported that the mechanism of action of T seemed to be similar to that of verapamil as a calcium antagonist and anti-CaM drug. This paper reports the effect of T on normal and isoprenaline stimulated mitochondrial Ca-uptake of myocardium of rabbit.Myocardial mitochondria were isolated from rabbit hearts by differential cen-trafugation and suspended in a medium containing 10mmol/L KCI, 10mmol/L EDTA and 0.5% bovine serum albumin. The freshly isolated mitochondria were fixed for transmission electron microscopy and scanning electron microscopy. Mitochon-drial Ca2+ accumulation was measured by the Millipore filtration method.Our results showed that below 100μg/ml concentration of mitochondria protein, Ca-uptake increases linearly with increase in mitochondria protein. Isoprenaline (10M) caused elevation of mitochondrial Ca-uptake by 20 @0.5%. T inhibited Ca uptake in metochondria. At low concentration of T, below 10 μg/ml, the concentration-inhibition curve for normal and isoprenaline stimulated Ca-uptake of mitochondria were both straight line. The maximal inhibition of T for both normal and isoprenaline stimalated Ca-uptake in mitochondria were 61.2@3.9% and 54.2 @5.1% respectively. It is well known that at high dose level isoprenaline is capable of inducing massive myocardial necrosis (infarct-like lesions), and the intra-cellular calcium concentrations increased after ischemia is paralleled by the calcium content of isolated mitochondria as well as by the impairment in myocardial cell function reflected by mechanical performance of the ventricle, Verapamil and other Ca antagonists may prevent the Ca overload and structural damage. Our results suggest that T may act as Ca antagonist similar to that of verapamil and can even protect hypoxic and ischemic hearts against additional Ca-induced myocardial fibre damage and necrosis.更多还原