Tanshinol borneol ester (DBZ) is a novel experimental compound that consists of two chemical structural units from danshensu and borneol. It exhibits efficacious anti-ischemic and anti-atherosclerosis activities in rats. A fecal metabolomics based on Liquid Chromatography-Mass Spectrometry combined with clinical histopathology and blood lipid estimation was employed to assess the efficacy and the metabolic changes caused by administration of DBZ in atherosclerotic rats. There were the typical pathological features of atherosclerosis and significantly increased levels of TC, TG and LDL-C in the atherosclerotic rat group. Nevertheless, atherosclerotic rats administered both DBZ (at a dose of 40 mg kg(-1)) and simvastatin (at a dose of 20 mg kg(-1)) showed good therapeutic effects. The results of the metabolomics studies showed that 55 differential metabolites such as sebacic acid, enterodiol, nonanedioic acid, dodecanedioic acid, cholic acid, 13(S)-HPODE, deoxycholic acid, some phosphatidylglycerol and phosphatidic acids were found, indicating that abnormal metabolism occurred in the pathways of fatty acid oxidation, linoleic acid metabolism, bile acid biosynthesis and glycerophospholipid metabolism in atherosclerotic rats. Compared to those in the model group, the contents of 41 differential metabolites showed a tendency to recover to a healthy level after DBZ administration. Metabolomics studies suggested that DBZ exhibited good treatment efficacy against atherosclerosis by adjusting disturbed metabolic pathways related to atherosclerosis. This study could provide an experimental basis for DBZ's application to act as a candidate drug with anti-atherosclerosis activity.

目的 采用高效液相色谱-四级杆-飞行时间串联质谱(HPLC-Q-TOF-MS/MS)法对广枣醇提物的主要化学成分进行分析鉴定.方法 采用回流提取法制备广枣醇提物,以Agilent TC-C18(4.6mm×250 mm,5μm)柱为分析柱,并以0.2％甲酸-甲醇溶液为流动相,流速0.7 mL/min,柱温30℃,进样量25 μL,进行梯度洗脱;质谱采用电喷雾离子源,毛细管电压4.0 kV,干燥器流速10.0 L/min,干燥器温度350℃,雾化器压力35.0 psi(1 psi=6 894.8 Pa),正负离子模式下扫描采集数据,并对各主要色谱峰进行归属.结果 通过正负离子质谱信息及元素组成分析,并结合相关文献和对照品数据对照,共鉴定出42种化合物,主要为氨基酸类、有机酸类及黄酮类,其中首次在广枣中发现的成分有17种.结论 HPLC-Q-TOF-MS/MS兼具色谱的高分离特性和质谱的高灵敏度双重优势,能对广枣的主要化学成分进行定性分析,可为广枣药效物质的基础研究提供依据.

目的 建立同时测定血浆中丹参素(DSS)、原儿茶酸(PA)及羟基红花黄色素A(HSYA)的HPLC分析方法,研究丹红注射液主要酚酸类成分DSS、PA以及HSYA在正常和寒凝血瘀大鼠中药代动力学行为.方法 正常及寒凝血瘀模型大鼠各6只,尾静脉注射丹红注射液.采用HPLC法检测给药后2、5、10、15、20、25、30、40、50、60、90 min时血浆中DSS、PA以及HSYA的浓度,流动相为0.2％甲酸水(A)_甲醇(B),梯度洗脱,梯度波长检测:280 nm(0～40 min),402 nm(40～60min).DAS 3.0软件计算药代动力学参数.结果 DSS和PA呈现二室开放模型,HSYA呈现三室模型.与正常组相比,模型大鼠体内DSS、PA和HSYA的达峰浓度Cmax、DSS的分布半衰期t1/2α、PA和HSYA的消除半衰期t12α(t12γ)和药时曲线下面积AUC以及总表观分布容积V均增大(P＜0.05);PA和HSYA的分布半衰期t1/2α和DSS药时曲线下面积AUC均降低(P＜0.05).结论 在寒凝血瘀病理模型下,DSS在体内分布减慢,生物利用度降低;PA和HSYA的分布加快,消除减慢,表观分布容积增大,生物利用度增加,更能发挥好疗效.