丹参活性成分生物可及性分析  

Bioaccessibility analysis of active components in Salvia miltiorrhiza

作　　者：赖莉 蒋正阳 冯宇鹏 罗国安[4] 谢媛媛 王淑美[1,2,3] LAI Li;JIANG Zheng-yang;FENG Yu-peng;LUO Guo-an;XIE Yuan-yuan;WANG Shu-mei(College of Traditional Chinese Medicine,Guangdong Pharmaceutical University,Guangzhou 510006,China;Guangdong Research Center for Quality Engineering Technology of Traditional Chinese Medicine,Guangzhou 510006,China;Key Laboratory of Digitalized Quality Evaluation Technology of Traditional Chinese Medicine,State Administration of Traditional Chinese Medicine,Guangzhou 510006,China;Department of Chemistry,Tsinghua University,Beijing 100084,China)

机构地区：[1]广东药科大学,广东广州510006 [2]广东省中药质量工程技术研究中心,广东广州510006 [3]国家中医药管理局中药数字化质量评价技术重点研究室,广东广州510006 [4]清华大学化学系,北京100084

出　　处：《药学学报》2022年第8期2435-2444,共10页Acta Pharmaceutica Sinica

基　　金：国家重点研发计划“中医药现代化研究”重点专项课题资助项目(2017YFC1700800);广东省大学生创新训练项目(S202010573050).

摘　　要：本研究采用超高效液相色谱(UHPLC)建立丹参中6个丹参酚酸类和4个丹参酮类成分同时定量分析的方法;采用半仿生方法对丹参进行体外模拟消化,探讨口服给药经胃肠消化转运过程中丹参有效成分含量比例的变化和生物可及性。结果表明,10个指标成分在相应浓度范围内均具有良好的线性关系,平均回收率在91.35%~105.65%;经过体外模拟消化后,丹参人工胃、肠液消化提取物化学成分种类无明显变化,丹酚酸B和迷迭香酸含量比例降低,原儿茶醛和丹参素的含量比例增加;在模拟胃液消化过程中,生物可及性由大到小依次为:丹参素(50.19%)>丹酚酸B(33.44%)>紫草酸(27.34%)>丹酚酸A(21.71%)>迷迭香酸(12.31%);在模拟肠液消化过程中,生物可及性由大到小依次为:15,16-二氢丹参酮Ⅰ(5.45%)>丹参酮Ⅰ(3.67%)>隐丹参酮(3.29%)>丹参酮ⅡA(3.01%)>丹酚酸A(2.39%)>紫草酸(1.57%)>丹酚酸B(1.02%)>丹参素(0.41%)>迷迭香酸(0.34%)。综上,本研究建立的UHPLC方法能准确、灵敏地同时测定丹参药材及提取物中6个丹参酚酸类和4个丹参酮类成分的含量,半仿生提取生物可及性研究结果表明在胃、肠液的作用下,丹参中并非所有成分均被消化,特别是迷迭香酸和丹酚酸B。因此,在丹参药材及其提取物质量研究中,质量标志物的选择及含量限度的确定均需同时考虑生物可及性。In this study,a method for simultaneous quantitative analysis of 6 salvianolic acids and 4 tanshinones in extracts of Salviae Miltiorrhizae Radix et Rhizoma was established by ultra-high performance liquid chromatography(UHPLC).The semi-biomimetic method was applied to simulate digestion process in vitro,to explore the digestion and transport characters of oral administration through the gastrointestinal tract,and to explain the content ratio changes and bioaccessibility of active ingredients in Salviae Miltiorrhizae Radix et Rhizoma.The results showed that the 10 index components have a good linear relationship in the corresponding concentration range,and the average recovery rate was 91.35%to 105.65%.After simulated digestion in vitro,types of chemical composition in simulated gastric fluid and simulated intestinal fluid digested extracts of Salviae Miltiorrhizae Radix et Rhizoma did not change significantly.While the content ratio of salvianolic acid B and rosmarinic acid decreased,and the content ratio of protocatechuic aldehyde and danshensu increased.In the simulated gastric fluid digestion extract of Salviae Miltiorrhizae Radix et Rhizoma,the order of bioaccessibility was:danshensu(50.19%)>salvianolic acid B(33.44%)>lithospermic acid(27.34%)>salvianolic acid A(21.71%)>rosmarinic acid(12.31%).In the simulated intestinal fluid digestion extract of Salviae Miltiorrhizae Radix et Rhizoma,the order of bioaccessibility was:15,16-dihydrotanshinoneⅠ(5.45%)>tanshinoneⅠ(3.67%)>cryptotanshinone(3.29%)>tanshinoneⅡA(3.01%)>salvianolic acid A(2.39%)>lithospermic acid(1.57%)>salvianolic acid B(1.02%)>danshensu(0.41%)>rosmarinic acid(0.34%).In conclusion,the UHPLC method established in this study can be applied for accurately and sensitively detecting the contents of 6 salvianolic acids and 4 tanshinones in Salviae Miltiorrhizae Radix et Rhizoma.The results of semi-biomimetic extraction showed that not all components were extracted with simulated gastric fluid and simulated intestinal fluid,especially rosmarinic aci

关 键 词：丹参 多指标定量分析 质量评价 半仿生提取 生物可及性 

分 类 号：R917[医药卫生—药物分析学]