高霞;刘璇;陈彦;王莹;贾晓斌;
GAO Xia;LIU Xuan;CHEN Yan;WANG Ying;JIA Xiao-bin;Key Laboratory of New Type Drug Administration System of Traditional Chinese Medicines of Jiangsu Provincial Academy of Chinese Medicine,Key Laboratory of Drug Release System of Oral Traditional Chinese Medicine Preparations under State Administration of Traditional Chinese Medicine;Nanjing University of Chinese Medicine;

• 1:江苏省中医药研究院中药新型给药系统重点实验室
• 2:国家中医药管理局中药口服制剂释药系统重点研究室
• 3:南京中医药大学
• 4:江苏省中医药研究院中药新型给药系统重点实验

摘要(Abstract)：

该文旨在研究淫羊藿总黄酮在体外水解酶作用下的生物转化过程。主要采用蜗牛酶水解淫羊藿总黄酮,用HPLC测定总黄酮中主要黄酮的转化。数据结果显示已知主要黄酮成分淫羊藿苷,朝藿定A,朝藿定B,朝藿定C都在1~2 h内分别完全转化为宝藿苷Ⅰ,箭藿苷A,箭藿苷B和鼠李糖基淫羊藿次苷Ⅱ,随着水解时间的延长,各转化产物被继续水解。因此可得出结论,蜗牛酶在37℃,pH 6.0的Hank's平衡盐溶液中,2 h内能将淫羊藿主要总黄酮转化为次级苷或苷元,且其酶解产物与肠道代谢产物相一致。
This study aims to investigate the biotransformation of Epimedium brevicornu flavonoids under the effect of hydrolytic enzymes in vitro. Snailase was mainly used to hydrolyze E. brevicornu flavonoids,and HPLC was used to determine the content of the main flavonoids in E. brevicornu flavonoids. The data results showed that the main known flavonoids included icariin,epimedin A,epimendin B and epimendin C,which were completely transformed into baohuoside I,sagittatoside A,sagittatoside B and 2″-O-rhamnosylicariside II in 1-2 h,respectively. Their transformed products were continuously hydrolyzed over time. In conclusion,snailase could transform E. brevicornu flavonoids into secondary glycoside or aglycone under 37 ℃ in pH 6. 0 HBSS balanced salt solution in 2 h. Moreover,its enzymatic hydrolysates were consistent with intestinal metabolites.

关键词(KeyWords)： 淫羊藿总黄酮;蜗牛酶;生物转化
Epimedium brevicornu flavonoids;snailase;biotransformation

Abstract:

Keywords:

基金项目(Foundation): 国家自然科学基金项目(81173557);; 江苏省中医药领军人才专项(LJ200913);; 江苏省“333人才培养工程”项目(BRA2011219)

作者(Author): 高霞;刘璇;陈彦;王莹;贾晓斌;
GAO Xia;LIU Xuan;CHEN Yan;WANG Ying;JIA Xiao-bin;Key Laboratory of New Type Drug Administration System of Traditional Chinese Medicines of Jiangsu Provincial Academy of Chinese Medicine,Key Laboratory of Drug Release System of Oral Traditional Chinese Medicine Preparations under State Administration of Traditional Chinese Medicine;Nanjing University of Chinese Medicine;

Email:

DOI:

参考文献(References)：

• [1]王霄旸,谢人明,孙文基.淫羊藿属药用植物黄酮类化合物的研究进展[J].中药药理与临床,2010,26(5):171.
• [2]于霄,宋静,熊志立,等.一测多评法测定淫羊藿中朝藿定A、朝藿定B、朝藿定C及淫羊藿苷的含量[J].中国中药杂志,2010,35(24):3310.
• [3]陈彦,贾晓斌,Hu Ming,等.Caco-2细胞单层研究淫羊藿黄酮类成分的吸收转运[J].中草药,2009,40(2):220.
• [4]Chen Y,Wang J Y,Jia X B,et al.Role of intestinal hydrolase in the absorption of prenylated flavonoids present in Yinyanghuo[J].Molecules,2011,16:1336.
• [5]陈彦,贾晓斌,谭晓斌,等.大鼠在体肠灌流模型研究淫羊藿不同黄酮苷的吸收代谢[J].中国中药杂志,2009,34(22):2928.
• [6]贾晓斌,兰雪莲,陈彦,等.淫羊藿黄酮类成分抗骨质疏松作用及其机制研究进展[J].中国药房,2010,21(3):269.
• [7]杨乾栩,刘艳秋,王莉,等.基于模型群体分析的淫羊藿抗骨质疏松活性成分筛选研究[J].药学学报,2012,47(9):1205.
• [8]Wang Y,Harvey C B,Hollox E J,et al.The genetically programmed down-regulation of lactase in children[J].Gastroenterology,1998,114:1230.
• [9]Bacsi K,Kosa J P,Balla B,et al.The decreased activity of lactase phlorizin hydrolase and bone mineral density in postmenopausal women[J].J Bone Miner Res,2007,22:186.
• [10]崔莉,张振海,孙娥,等.柚皮苷-羟丙基-β-环糊精包合物酶解制备柚皮素工艺的研究[J].中国中药杂志,2012,37(3):310.
• [11]贾东升,贾晓斌,薛璟,等.蜗牛酶转化淫羊藿苷制备淫羊藿苷元的研究[J].中国中药杂志,2010,35(7):857.
• [12]平其能.中药成分的胃肠道转运与剂型设计[M].北京:化学工业出版社,2010:32.
• [13]陈彦,贾晓斌,谭晓斌,等.大鼠肠道水解酶对淫羊藿黄酮苷的处置影响[J].中国中药杂志,2010,45(7):516.
• [14]Chen Y,Wang J Y,Jia X B,et al.Role of intestinal hydrolase in the absorption of prenylated flavonoids present in Yinyanghuo[J].Molecules,2011,16:1336.