Hu Yuan, Guo Dai-Hong, Liu Ping, Rahman Khalid, Wang Dong-Xiao, Wang Bo
Department of Clinical Pharmacology and Pharmacy, Center of Pharmacy care Chinese PLA General Hospital, Beijing, China.
Pharmazie. 2009 Jan;64(1):53-7.
The aim of this study was to investigate (1) whether Rhodobryum roseum, a traditional Chinese medicine used to treat cardiac disease, can protect myocardium damage due to isoproterenol-induced injury, (2) whether the cardioprotective effect of the R. roseum extract is related to its antioxidant activity, and (3) to identify the active components of R. roseum using the oxidant-mediated injury in cardiomyocytes. R. roseum was extracted with 95% EtOH (RE-95), 50% EtOH (RE-50) and water (Re-H2O) and the rats were treated orally for 11 days at doses of 250 mg and 63 mg/kg respectively after cardiac necrosis was induced by administering ISO subcutaneously at a dose of 85 mg/kg body weight. Levels of marker enzymes (LDH, GOT and CK) were assessed in serum whilst the antioxidant parameters, superoxide dismutase (SOD), and malondialdehde (MDA) were assayed in heart homogenate. Significant myocardial necrosis, depletion of endogenous antioxidants and an increase in serum levels of marker enzymes was observed in ISO-treated animals when compared with the normal animals. The RE-50 elicited a significant cardioprotective effect by lowering the levels of serum marker enzymes, lipid peroxidation (MDA). To extend this work, we sought to investigate the antioxidant effects of the components of R. roseum, using the neonatal rat cardiomyocytes model of H2O2-induced oxidant injury. Among the four major components, piperine and methyl piperate significantly reduced the medium level of CK and LDH at a variety of dosages. Moreover, piperine and methyl piperate significantly attenuated 2',7'-dichlorofluorescein (DCF) fluorescence by 63.9% and 52.6%, respectively. The present findings demonstrate that the cardioprotective effects of extracted R. roseum in ISO-induced oxidative damage may be due to an augmentation of the endogenous antioxidants and inhibition of lipid peroxidation of the membranes. Moreover, its components piperine and methyl piperate exert significant protectective effects on cardiac myocytes.
（1）用于治疗心脏病的中药玫瑰藓是否能保护异丙肾上腺素诱导损伤所致的心肌损伤；（2）玫瑰藓提取物的心脏保护作用是否与其抗氧化活性有关；（3）利用心肌细胞中的氧化介导损伤来鉴定玫瑰藓的活性成分。用95%乙醇（RE-95）、50%乙醇（RE-50）和水（Re-H2O）提取玫瑰藓，在以85mg/kg体重皮下注射异丙肾上腺素诱导心脏坏死之后，分别以250mg和63mg/kg的剂量给大鼠口服给药11天。评估血清中标记酶（乳酸脱氢酶、谷草转氨酶和肌酸激酶）的水平，同时测定心脏匀浆中的抗氧化参数超氧化物歧化酶（SOD）和丙二醛（MDA）。与正常动物相比，在接受异丙肾上腺素治疗的动物中观察到明显的心肌坏死、内源性抗氧化剂的消耗以及血清中标记酶水平的升高。RE-50通过降低血清标记酶水平、脂质过氧化（MDA）产生了显著的心脏保护作用。为了拓展这项研究，我们试图利用过氧化氢诱导的氧化损伤新生大鼠心肌细胞模型来研究玫瑰藓各成分的抗氧化作用。在四种主要成分中，胡椒碱和胡椒酸甲酯在各种剂量下均显著降低了培养基中肌酸激酶和乳酸脱氢酶的水平。此外，胡椒碱和胡椒酸甲酯分别使2',7'-二氯荧光素（DCF）荧光显著减弱63.9%和52.6%。目前的研究结果表明，提取的玫瑰藓对异丙肾上腺素诱导的氧化损伤的心脏保护作用可能是由于内源性抗氧化剂的增加和膜脂质过氧化的抑制。此外，其成分胡椒碱和胡椒酸甲酯对心肌细胞具有显著的保护作用。
