丹酚酸B药理活性及药物动力学探究进展.docVIP

丹酚酸B药理活性及药物动力学探究进展【摘要】 目的:拓宽对丹酚酸B的研究视野以及提升对其的研究水平。方法查阅大量国内外文献,总结、提炼和阐明丹酚酸B的研究前景。结果:丹酚酸B具有显著的心脏、脑、肝、肾保护作用及促进溃疡面愈合等药理活性。丹皮酚大鼠灌胃体内药代动力学过程符合二室模型,配伍应用可使丹酚酸B的AUC降低,表观分布容积和清除率增加。结论:丹酚酸B作为有效中药分子用于开发治疗心血管疾病药物具有良好前景,探讨其分子中药组方的药理活性及其药代动力学特征,对于创制分子中药,促进中药现代化具有重要意义。 【关键词】 丹酚酸B;药理活性;药物动力学;中药分子;分子中药;中医药 【中图分类号】 R392.5【文献标识码】 B【文章编号】 1007-8517(2009)24-0051-01 Pharmacological Action and Pharmacokinetics of Salvianolic acidB HuaLi??1 Si-wang Wang??1 Bang-le Zhang??2 ??1 Institute of Materia Medica, ??2 Department of Pharmaceutics, School of Pharmacy,the Fourth Military Medical University,Xi?an 710032,China. Abstract:Objective To enlargh the research sight and promote increasing the level of study on salvianolic acidB. Methods The research prospect of Salvianolic acidB were summarizedand clarifiedby reveiwing a vast amount of literature at home and abroad. ResultsSalvianolic acid B have protective effect inheart, brain, liver,kidneyand other pharmacological activity.Atwo-compartment model could describe the pharmacokinetics of Salvianolic acid B in ratafter intrfteragastricadministration. The combination can decrease the AUC value and increase the Vd and CL ofSalvianolic acid B. ConclusionSalvianolic acid B have a good prospect ofdevelopmentfor cardiovascular diseaseas a Active Molecule of Chinese Medicinal Materials(AMCMM). Study for the pharmacological action and pharmacokinetics of MolecularMedicine(MM)produced with AMCMM have the important instruction significance fordiscovering and advancingmodernizationof Traditional Chinese Medicine(TCM). Key words:salvianolic acidB,pharmacological action, pharmacokinetics, AMCMM, MM, TCM 0 引言 丹酚酸B(Salvianolic acidB,Sal B)系丹参的水溶性有效成分,属酚酸类化合物,在丹参的功效作用中占有重要地位。2005版《中国药典》已将其列为丹参及丹参中成药的药效指标成分[1]。丹酚酸B为三分子丹参素与一分子咖啡酸缩合而成,是一低聚体型化合物,分子式C36H36O16,相对分子量718.59。丹酚酸B结构中含多个酚羟基,具有较强抗氧化性,目前研究认为其是丹参水溶性物质中药理活性最强的成分。 1 药理作用 1.1 对心脏的保护作用内皮素(Endothelin,ET)是迄今为止所知作用最强、作用时间持久的缩血管多肽,对心血管系统有重要的调节作用[2]。当心肌缺血再灌注时,血液及缺血组织中ET含量明显升高。一氧化氮(NO)为