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丹参酮ⅡA是中药丹参中的主要活性成分,研究表明丹参酮ⅡA对缺血再灌注损伤具有保护作用.但丹参酮ⅡA的水溶性较差,限制了其临床应用.本研究以丹参酮ⅡA为对照,在大鼠缺血再灌注损伤模型上,评价丹参酮ⅡA与N-甲基-D-葡萄糖胺反应得到的一种新的水溶性的丹参酮ⅡA衍生物对心肌缺血再灌注损伤的保护作用与机制.结果表明,采用丹参酮ⅡA衍生物预处理能显著减少大鼠心肌缺血再灌注损伤引起的心肌炎症浸润及氧化损伤,减少乳酸脱氢酶(LDH)及丙二醛(MDA)的活性;降低核转录因子κB(NF-KB)的基因表达量;上调血红素氧合酶(HO-1)的基因表达;但对超氧化物歧化酶(T-SOD)的含量及SOD-1基因的表达量无显著调节作用.本研究结论表明丹参酮ⅡA衍生物具有保护心肌缺血再灌注损伤的作用,机制与其显著抑制炎症与氧化损伤有关.“,”Tanshinone ⅡA (TSⅡA) is the major bioactive constituent of Salvia miltiorrhiza Bunge,a Chinese herbal medicine,which has protective effects on myocardial ischemia/reperfusion (MIR) injury.However,the cardioprotective effects of TSⅡA as well as its clinical use were limited due to its poor water solubility.The objective of this study was to evaluate whether Tanshinone ⅡA derivative (TD),a new water soluble compound synthesized by TSⅡA and N-Methyl-D-Glucamine,had protective effects on MIR injury and what the related mechanism was.The cardioprotective effects of TD were evaluated and compared with TSIIA in a rat MIR model.The results show that pretreatment with TD significantly alleviated inflammatory infiltration and exhibited antioxidant effect in MIR injury by reducing the activity of lactate dehydrogenase (LDH) and malondialdehyde (MDA),decreasing expression of nuclear factor-κ-gene binding (NF-κB) and upregulating expression of heme oxygenase (HO-1),but having no effect on the content of total superoxide dismutase (T-SOD) and mRNA expression of superoxide dismutase (SOD-1).Thus,our study reveals that TD exerted significant protective effects on MIR injury through attenuating oxidative stress and inflammatory responses.