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<正>黄芩苷(baicalin,BG)及其苷元黄芩素(baicalein,B)(结构如图1)是由唇形科植物黄芩(Scutellariabaicalens Georgi)的干燥根中提取的一类黄酮类化合物,是黄芩的主要有效成分。两者具有相似的药理活性,包括抗炎[1]、抗氧化[2]、抗微生物[3]、抗HIV
Abstract:[1]Middleton E Jr,Kandasw ami C,Theoharides TC.The effects of plant flavonoids on mammalian cells:implications for inflammation,heart disease,and cancer[J].Pharmacol Rev,2000,52(4):673-751.
[2]Rice-Evans C.Flavonoid antioxidants[J].Curr Med Chem,2001,8(7):797-807.
[3]Kubo M,Kimura Y,Odani T,et al.Studies on Scutellaria radix.Part2:the antibacterial substance[J].Planta Med,1981,43(2):194-201.
[4]Wu JA,Attele AS,Zhang L,et al.Anti-HIV activity of medicinal herbs:usage and potenitial development[J].Am J Chin Med,2001,29(1):69-81.
[5]Lee MJ,Wang CJ,Tsai YY,et al.Inhitory effect of12-O-tetradecanoyphorbol-13-acetate-caused tumor promotion in benzo pyrene-initiated CD-1mouse skin by baicalein[J].Nutr Cancer,1999,34(2):185-191.
[6]Matsuzaki Y,Kurokawa N,Terai S,et al.Cell death in-duced by baicalein in human hepatocellular carcinoma cell lines[J].Jpn J Cancer Res,1996,87(2):170-177.
[7]Ikemoto S,Sugimura K,Yoshida N,et al.Antitumor effects of Scutellariae radix and its components baicalein,baicalin,and wogonin on bladder cancer cell lines[J].Urology,2000,55(6):951-955.
[8]Gao Z,Huang K,Yang X,et al.Free radical scavenging and antioxidant activities of flavonoids extracted from the radix of Scutellaria baicalensis Georgi[J].Biochim Biophys Acta,1999,1472(3):643-650.
[9]Akan T,Kawabata K,Yanagisaun E,et al.Baicalin,the predominant flavone glucuronide of scutellariae radix,is absorbed from the rat gastrointestinal tract as the aglycone and restored to its original form[J].J Pharm Pharmacol,2000,52(12):1563-1568.
[10]Lai MY,Hsiu SL,Tsai SY,et al.Comparison of metabolic pharmacokineties of baicalin and baicalein in rats[J].J Pharm Pharmacol,2003,55(2):205-209.
[11]刘太明,蒋学华.黄芩苷和黄芩素大鼠在体胃、肠的吸收动力学研究[J].中国中药杂志,2006,31(12):999-1001.
[12]Taiming L,Xuehua J.Investigation of the Absorption Mechanisms of Baicalin and Baicalein in Rats[J].J Pharm Sci,2006,95(6):1326-1333.
[13]Ng SP,Wang KY,Zhang L,et al.Evaluation of the first-pass glucurondation of selected flavones in gut by Caco-2monolayer model[J].J Pharm Sci,2004,8(1):1-9.
[14]Zhang L,Lin G,Chang Q,et al.Role of Intestinal first-pass metabolism of baicalein in its absorption process[J].Pharma Res,2005,22(7):1050-1058.
[15]Yee SY.In vitro permeability across Caco-2cells(colonic)can predict in vivo(small intestinal)absorption in man-fact or myth[J].Pharma Res,1997,14(6):763-766.
[16]Chen J,Lin H,Hu M.Metabolism of flavonoids via enter-ic recycling:role of intestinal disposition[J].J Pharmacol Exp Ther,2003,304(3):1228-1235.
[17]Hu M.,Chen J,Lin H.Metabolism of flavonoids via enter-ic recycling:mechanistic studies of disposition of apigenin in the Caco-2cell culture model[J].J Pharmacol Exp Ther,2003,307(1):314-321.
[18]Walle UK,Galijatovic A,Walle T.Transport of the flavonoid chrysin and its conjugated metabolites by the human intestinal cell line Caco-2[J].Biochem Pharmacol,1999,58(3):431-438.
[19]Akao T,Sakashita Y,Hamada M,et al.Enteric excretion of baicalein,a flavone of scutellariae radix,via glu-curonidation in rat:involvement of multidrug resistance-associated proteinl[J].Pharmal Res,2004,21(11):2120-2126.
[20]Zhang L,Lin G,Zuo Z,et al.Involvement of UDP-glu-curonosyl transferases in the extensive liver and intestinal first-pass metabolism of flavonoid baicalein[J].Pharma Res,2007,24(11):81-89.
[21]关小彬,叶玲,夏笔军,等.大鼠肝肠不同微粒体药物代谢酶对黄芩素葡糖醛酸酸化代谢物的影响研究[J].中国药房,2008,19(36):2811-2813.
[22]狄斌,冯年平,刘文英.复方双黄连与黄芩单方中黄芩苷在大鼠肠道菌群中代谢的比较[J].中国新药杂志,2005,14(1):89-93.
[23]Feng NP,Di B,Liu WY.Comparison of the metabolism of baicalin in rats orally administered with radix scutellariae extract and Shuang-Huang-Lian extract[J].Chem Pharm Bull(Tokyo),2005,53(8):978-983.
[24]Zuo F,Zhou ZM,Yan MZ,et al.Metabolism of constituents in huangqin-Tang,a prescription in traditional chinese medicine,by human intestinal flora biol[J].Biol Pharm Bull,2002,25(5):558-563.
[25]Xing J,Chen X,Sun Y,et al.Interaction of baicalin and baicalein with antibiotics in the gastrointestinal tract[J].J Pharm Pharmacol,2005,57(6):743-750.
[26]Abe K,Inoue O,Yumioka E.Biliary excretion of metabo-lites of baicalin and baicalein in rats[J].Chem Pharm Bull(Tokyo),1990,38(1):209-211.
[27]狄斌,冯年平,刘文英.复方双黄连颗粒与黄芩颗粒剂中黄芩苷在大鼠胆汁中代谢的比较研究[J].中国药科大学学报,2004,35(5):437-442.
[28]Lai MY,Hsiu SL,Chen CC,et al.Urinary pharmacoki-netics of baicalein,wogonin and their glycosides after oral administration of scutellariae radix in humans[J].Biol Pharm Bull,2003,26(1):79-83.
[29]狄斌,冯年平,刘文英.复方双黄连与黄芩提取物中黄芩苷代谢的比较研究[J].中国药学杂志,2005,40(2):127-130.
[30]Xing J,Chen X,Zhong D.Absorption and enterohepatic Circulation of baicalin in rats[J].Life Sci,2005,78(2):140-146.
[31]Liu J,Qiu L,Gao J,et al.Preparation,characterization and in vivo evaluation of formulation of baicalein with hy-droxypropyl-β-cyclodextrin[J].Int J Pharm,2006,312(1-2):137-143.
[32]龚明涛,虞丽芳,陈庆华,等.大鼠灌胃黄芩苷及其苷元黄芩素的药动学研究[J].中草药,2009,40(3):392-394.
[33]郭晓宇,杨琳,陈颖,等.黄芩素与黄芩苷大鼠体内药动学比较研究[J].中国药学杂志,2008,43(7):524-526.
基本信息:
中图分类号:R284
引用信息:
[1]许伯慧,严菲.黄芩苷及其苷元黄芩素体内过程的研究进展[J].南通大学学报(医学版),2010,30(03):220-223.
基金信息:
江苏省新药创新发展基金(0606038)