中草药及其活性成分对他克莫司药动学作用机制研究进展
摘要
<正>他克莫司(Tacrolimus,Tac)是从筑波链霉菌(Streptomycestsukubaensis)发酵液中提取的一种代谢产物,其与环孢素(Cyclosporine A,CsA)同属于钙调磷酸酶抑制药(Calcineurin inhibitors,CNIs)。其化学结构属23元环大环内酯类抗生素,具有高亲脂性和不溶于水的特性。该药主要通过抑制IL-2释
引文
[1]Krmer BK,Montagnino G,Krüger B,et al.Efficacy and safety of tacrolimus compared with ciclosporin-A in renal transplantation:7-year observational results[J].Transpl Int,2016,29(3):307-314.
[2]Oda K,Yamano K,Otsuka Y.In vitro-in vivo extrapolations to evaluate the effect of concomitant drugs on tacrolimus(FK506)exposure[J].Biopharm Drug Dispos,2015,36(5):265-274.
[3]常伟宇,辛华雯.中草药对孕烷X受体和组成型雄烷受体等核受体通路影响的研究进展[J].中国药师,2014,17(12):2127-2131.
[4]Tang JT,Andrews LM,van Gelder T,et al.Pharmacogenetic aspects of the use of tacrolimus in renal transplantation:recent developments and ethnic considerations[J].Exp Opin Drug Metab Toxicol,2016,12(5):555-565.
[5]Stefanovi C'NZ,Cvetkovi C'TP,Jevtovi C-Stoimenov'TM,et al.Investigation of CYP 3A5 and ABCB1 gene polymorphisms in the longterm following renal transplantation:Effects on tacrolimus exposure and kidney function[J].Exp Ther Med,2015,10(3):1149-1156.
[6]Shi S,Klotz U.Drug interactions with herbal medicines[J].Clin Pharmacokinet,2012,51(2):77-104.
[7]Di Lorenzo C,Ceschi A,Kupferschmidt H,et al.Adverse effects of plant food supplements and botanical preparations:a systematic review with critical evaluation of causality[J].Br J Clin Pharmacol,2015,79(4):578-592.
[8]Khodaie L,Sadeghpoor O.Ginger from ancient times to the new outlook[J].Jundishapur J Nat Pharm Prod,2015,10(1):e18402.
[9]Lete I,AlluéJ.The effectiveness of ginger in the prevention of nausea and vomiting during pregnancy and chemotherapy[J].Integr Med Insights,2016,11:11-17.
[10]Egashira K,Sasaki H,Higuchi S,et al.Food-drug interaction of tacrolimus with pomelo,ginger,and turmeric juice in rats[J].Drug Metab Pharmacokinet,2012,27(2):242-247.
[11]Qiu JX,Zhou ZW,He ZX,et al.Estimation of the binding modes with important human cytochrome P450 enzymes,drug interaction potential,pharmacokinetics,and hepatotoxicity of ginger components using molecular docking,computational,and pharmacokinetic modeling studies[J].Drug Des Devel Ther,2015,9:841-866.
[12]Zhang W,Lim LY.Effects of spice constituents on P-glycoproteinmediated transport and CYP3A4-mediated metabolism in vitro[J].Drug Metab Dispos,2008,36(7):1283-1290.
[13]Mukkavilli R,Gundala SR,Yang C,et al.Modulation of cytochrome P450 metabolism and transport across intestinal epithelial barrier by ginger biophenolics[J].PLo S One,2014,9(9):e108386.
[14]Jiang X,Williams KM,Liauw WS,et al.Effect of ginkgo and ginger on the pharmacokinetics and pharmacodynamics of warfarin inhealthy subjects[J].Br J Clin Pharmacol,2005,59(4):425-432.
[15]Young HY,Liao JC,Chang YS,et al.Synergistic effect of ginger and nifedipine on human platelet aggregation:a study in hypertensive patients and normal volunteers[J].Am J Chin Med,2006,34(4):545-551.
[16]Chiang HM,Chao PD,Hsiu SL,et al.Ginger significantly decreased the oral bioavailability of cyclosporine in rats[J].Am JChin Med,2006,34(5):845-855.
[17]Le PM,Mc Cooeye M,Windust A.Application of UPLC-QTOF-MSin MS(E)mode for the rapid and precise identification of alkaloids in goldenseal(Hydrastis canadensis)[J].Anal Bioanal Chem,2014,406(6):1739-1749.
[18]Chen S,Wan L,Couch L,et al.Mechanism study of goldenseal-associated DNA damage[J].Toxicol Lett,2013,221(1):64-72.
[19]蔡明志,陈凯,范星,等.盐酸小檗碱引起他克莫司血药浓度升高1例分析[J].实用医药杂志,2014,31(2):156-157.
[20]Hou Q,Han W,Fu X.Pharmacokinetic interaction between tacrolimus and berberine in a child with idiopathic nephrotic syndrome[J].Eur J Clin Pharmacol,2013,69(10):1861-1862.
[21]Gurley BJ,Swain A,Hubbard MA,et al.Supplementation with goldenseal(Hydrastis canadensis),but not kava kava(Piper methysticum),inhibits human CYP3A activity in vivo[J].Clin Pharmacol Ther,2008,83(1):61-69.
[22]Etheridge AS,Black SR,Patel PR,et al.An in vitro evaluation of cytochrome P450 inhibition and P-glycoprotein interaction with goldenseal,Ginkgo biloba,grape seed,milk thistle,and ginseng extracts and their constituents[J].Planta Med,2007,73(8):731-741.
[23]Lu Y,Chen DF.Analysis of Schisandra chinensis and Schisandra sphenanthera[J].J Chromatogr A,2009,1216(11):1980-1990.
[24]Jang MK,Nam JS,Kim JH,et al.Schisandra chinensis extract ameliorates nonalcoholic fatty liver via inhibition of endoplasmic reticulum stress[J].J Ethnopharmacol,2016,185:96-104.
[25]He JL,Zhou ZW,Yin JJ,et al.Schisandra chinensis regulates drug metabolizing enzymes and drug transporters via activation of Nrf2-mediated signaling pathway[J].Drug Des Devel Ther,2014,9:127-146.
[26]Sun Z,Ren M,Wu Q,et al.Co-administration of Wuzhi capsules and tacrolimus in patients with idiopathic membranous nephro-pathy:clinical efficacy and pharmacoeconomics[J].Int Urol Nephrol,2014,46(10):1977-1982.
[27]Lai Q,Wei J,Mahmoodurrahman M,et al.Pharmacokinetic and nephroprotective benefits of using Schisandra chinensis extracts in a cyclosporine A-based immune-suppressive regime[J].Drug Des Devel Ther,2015,9:4997-5018.
[28]Xin HW,Wu XC,Li Q,et al.Effects of Schisandra sphenanthera extract on the pharmacokinetics of tacrolimus in healthy volunteers[J].Br J Clin Pharmacol,2007,64(4):469-475.
[29]Jiang W,Wang X,Xu X,et al.Effect of Schisandra sphenanthera extract on the concentration of tacrolimus in the blood of liver transplant patients[J].Int J Clin Pharmacol Ther,2010,48(3):224-229.
[30]Xin HW,Li Q,Wu XC,et al.Effects of Schisandra sphenanthera extract on the blood concentration of tacrolimus in renal transplant recipients[J].Eur J Clin Pharmacol,2011,67(12):1309-1311.
[31]Wang K,Qu QS,Zhang YX,et al.Effects of Wuzhi capsule on blood concentration of tacrolimus after renal transplantation[J].JBiol Regul Homeost Agents,2016,30(1):155-159.
[32]Qin XL,Yu T,Li LJ,et al.Effect of long-term co-administration of Wuzhi tablet(Schisandra sphenanthera extract)and prednis-one on the pharmacokinetics of tacrolimus[J].Phytomedicine,2013,20(3-4):375-379.
[33]Wei H,Tao X,Di P,et al.Effects of traditional chinese medicine Wuzhi capsule on pharmacokinetics of tacrolimus in rats[J].Drug Metab Dispos,2013,41(7):1398-1403.
[34]Wang B,Yang S,Hu J,et al.Multifaceted interaction of the traditional Chinese medicinal herb Schisandra chinensis with cytochrome P450-mediated drug metabolism in rats[J].J Ethnopharmacol,2014,155(3):1473-1482.
[35]Qin XL,Bi HC,Wang XD,et al.Mechanistic understanding of the different effects of Wuzhi Tablet(Schisandra sphenanthera extract)on the absorption and first-pass intestinal and hepatic metabolism of Tacrolimus(FK506)[J].Int J Pharm,2010,389(1-2):114-121.
[36]Qin XL,Chen X,Zhong GP,et al.Effect of Tacrolimus on the pharmacokinetics of bioactive lignans of Wuzhi tablet(Schisandra sphenanthera extract)and the potential roles of CYP3A and P-gp[J].Phytomedicine,2014,21(5):766-772.
[37]Qin XL,Chen X,Wang Y,et al.In vivo to in vitro effects of six bioactive lignans of Wuzhi tablet(Schisandra sphenanthera extract)on the CYP3A/P-glycoprotein-mediated absorption and metabolism of tacrolimus[J].Drug Metab Dispos,2014,42(1):193-199.
[38]Russo E,Scicchitano F,Whalley BJ,et al.Hypericum perforatum:pharmacokinetic,mechanism of action,tolerability,and clinical drug-drug interactions[J].Phytother Res,2014,28(5):643-655.
[39]Süntar I,Oyard O,Akkol EK,et al.Antimicrobial effect of the extracts from Hypericum perforatum against oral bacteria and biofilm formation[J].Pharm Biol,2016,54(6):1065-1070.
[40]Bolley R,Zülke C,Kammerl M,et al.Tacrolimus-induced nephrotoxicity unmasked by induction of the CYP3A4 system with St John's wort[J].Transplantation,2002,73(6):1009.
[41]Mai I,St9rmer E,Bauer S,et al.Impact of St John's wort treatment on the pharmacokinetics of tacrolimus and mycophenolic acid in renal transplant patients[J].Nephrol Dial Transplant,2003,18(4):819-822.
[42]Hebert MF,Park JM,Chen YL,et al.Effects of St.John's wort(Hypericum perforatum)on tacrolimus pharmacokinetics in healthy volunteers[J].J Clin Pharmacol,2004,44(1):89-94.
[43]Godtel-Armbrust U,Metzger A,Kroll U,et al.Variability in PXR-mediated induction of CYP3A4 by commercial preparations and dry extracts of St John's wort[J].Naunyn Schmiedebergs Arch Pharmacol,2007,375(6):377-382.
[44]Komoroski BJ,Zhang S,Cai H,et al.Induction and inhibition of cytochromes P450 by the St John's wort constituent hyperforin in human hepatocyte cultures[J].Drug Metab Dispos,2004,32(5):512-518.
[45]王红勋.枳实与枳壳的现代药理与临床应用研究[J].中国卫生标准管理,2014,5(16):39-40.
[46]Stohs SJ,Preuss HG,Shara M.A review of the human clinical studies involving Citrus aurantium(bitter orange)extract and its primary protoalkaloid p-synephrine[J].Int J Med Sci,2012,9(7):527-538.
[47]Lin SP,Wu PP,Hou YC,et al.Different influences on tacrolimus pharmacokinetics by coad ministrations of zhi ke and zhi shi in rats[J].Evid Based Complement Alternat Med,2011,2011:751671.
[48]Wang MJ,Hou YC,Tsai SY,et al.Effects of coad ministrations of unripe fruits and ripe peels of Citrus aurantium on cyclosporine pharmacokinetics in rats[J].J Food Drug Anal,2007,15(3):265-270.
[49]Allison TL.Immunosuppressive therapy in transplantation[J].Nurs Clin North Am,2016,51(1):107-120.
[50]Vanhove T,Annaert P,Kuypers DR.Clinical deter minants of calcineurin inhibitor disposition:a mechanistic review[J].Drug Metab Rev,2016,48(1):88-112.
[2]Oda K,Yamano K,Otsuka Y.In vitro-in vivo extrapolations to evaluate the effect of concomitant drugs on tacrolimus(FK506)exposure[J].Biopharm Drug Dispos,2015,36(5):265-274.
[3]常伟宇,辛华雯.中草药对孕烷X受体和组成型雄烷受体等核受体通路影响的研究进展[J].中国药师,2014,17(12):2127-2131.
[4]Tang JT,Andrews LM,van Gelder T,et al.Pharmacogenetic aspects of the use of tacrolimus in renal transplantation:recent developments and ethnic considerations[J].Exp Opin Drug Metab Toxicol,2016,12(5):555-565.
[5]Stefanovi C'NZ,Cvetkovi C'TP,Jevtovi C-Stoimenov'TM,et al.Investigation of CYP 3A5 and ABCB1 gene polymorphisms in the longterm following renal transplantation:Effects on tacrolimus exposure and kidney function[J].Exp Ther Med,2015,10(3):1149-1156.
[6]Shi S,Klotz U.Drug interactions with herbal medicines[J].Clin Pharmacokinet,2012,51(2):77-104.
[7]Di Lorenzo C,Ceschi A,Kupferschmidt H,et al.Adverse effects of plant food supplements and botanical preparations:a systematic review with critical evaluation of causality[J].Br J Clin Pharmacol,2015,79(4):578-592.
[8]Khodaie L,Sadeghpoor O.Ginger from ancient times to the new outlook[J].Jundishapur J Nat Pharm Prod,2015,10(1):e18402.
[9]Lete I,AlluéJ.The effectiveness of ginger in the prevention of nausea and vomiting during pregnancy and chemotherapy[J].Integr Med Insights,2016,11:11-17.
[10]Egashira K,Sasaki H,Higuchi S,et al.Food-drug interaction of tacrolimus with pomelo,ginger,and turmeric juice in rats[J].Drug Metab Pharmacokinet,2012,27(2):242-247.
[11]Qiu JX,Zhou ZW,He ZX,et al.Estimation of the binding modes with important human cytochrome P450 enzymes,drug interaction potential,pharmacokinetics,and hepatotoxicity of ginger components using molecular docking,computational,and pharmacokinetic modeling studies[J].Drug Des Devel Ther,2015,9:841-866.
[12]Zhang W,Lim LY.Effects of spice constituents on P-glycoproteinmediated transport and CYP3A4-mediated metabolism in vitro[J].Drug Metab Dispos,2008,36(7):1283-1290.
[13]Mukkavilli R,Gundala SR,Yang C,et al.Modulation of cytochrome P450 metabolism and transport across intestinal epithelial barrier by ginger biophenolics[J].PLo S One,2014,9(9):e108386.
[14]Jiang X,Williams KM,Liauw WS,et al.Effect of ginkgo and ginger on the pharmacokinetics and pharmacodynamics of warfarin inhealthy subjects[J].Br J Clin Pharmacol,2005,59(4):425-432.
[15]Young HY,Liao JC,Chang YS,et al.Synergistic effect of ginger and nifedipine on human platelet aggregation:a study in hypertensive patients and normal volunteers[J].Am J Chin Med,2006,34(4):545-551.
[16]Chiang HM,Chao PD,Hsiu SL,et al.Ginger significantly decreased the oral bioavailability of cyclosporine in rats[J].Am JChin Med,2006,34(5):845-855.
[17]Le PM,Mc Cooeye M,Windust A.Application of UPLC-QTOF-MSin MS(E)mode for the rapid and precise identification of alkaloids in goldenseal(Hydrastis canadensis)[J].Anal Bioanal Chem,2014,406(6):1739-1749.
[18]Chen S,Wan L,Couch L,et al.Mechanism study of goldenseal-associated DNA damage[J].Toxicol Lett,2013,221(1):64-72.
[19]蔡明志,陈凯,范星,等.盐酸小檗碱引起他克莫司血药浓度升高1例分析[J].实用医药杂志,2014,31(2):156-157.
[20]Hou Q,Han W,Fu X.Pharmacokinetic interaction between tacrolimus and berberine in a child with idiopathic nephrotic syndrome[J].Eur J Clin Pharmacol,2013,69(10):1861-1862.
[21]Gurley BJ,Swain A,Hubbard MA,et al.Supplementation with goldenseal(Hydrastis canadensis),but not kava kava(Piper methysticum),inhibits human CYP3A activity in vivo[J].Clin Pharmacol Ther,2008,83(1):61-69.
[22]Etheridge AS,Black SR,Patel PR,et al.An in vitro evaluation of cytochrome P450 inhibition and P-glycoprotein interaction with goldenseal,Ginkgo biloba,grape seed,milk thistle,and ginseng extracts and their constituents[J].Planta Med,2007,73(8):731-741.
[23]Lu Y,Chen DF.Analysis of Schisandra chinensis and Schisandra sphenanthera[J].J Chromatogr A,2009,1216(11):1980-1990.
[24]Jang MK,Nam JS,Kim JH,et al.Schisandra chinensis extract ameliorates nonalcoholic fatty liver via inhibition of endoplasmic reticulum stress[J].J Ethnopharmacol,2016,185:96-104.
[25]He JL,Zhou ZW,Yin JJ,et al.Schisandra chinensis regulates drug metabolizing enzymes and drug transporters via activation of Nrf2-mediated signaling pathway[J].Drug Des Devel Ther,2014,9:127-146.
[26]Sun Z,Ren M,Wu Q,et al.Co-administration of Wuzhi capsules and tacrolimus in patients with idiopathic membranous nephro-pathy:clinical efficacy and pharmacoeconomics[J].Int Urol Nephrol,2014,46(10):1977-1982.
[27]Lai Q,Wei J,Mahmoodurrahman M,et al.Pharmacokinetic and nephroprotective benefits of using Schisandra chinensis extracts in a cyclosporine A-based immune-suppressive regime[J].Drug Des Devel Ther,2015,9:4997-5018.
[28]Xin HW,Wu XC,Li Q,et al.Effects of Schisandra sphenanthera extract on the pharmacokinetics of tacrolimus in healthy volunteers[J].Br J Clin Pharmacol,2007,64(4):469-475.
[29]Jiang W,Wang X,Xu X,et al.Effect of Schisandra sphenanthera extract on the concentration of tacrolimus in the blood of liver transplant patients[J].Int J Clin Pharmacol Ther,2010,48(3):224-229.
[30]Xin HW,Li Q,Wu XC,et al.Effects of Schisandra sphenanthera extract on the blood concentration of tacrolimus in renal transplant recipients[J].Eur J Clin Pharmacol,2011,67(12):1309-1311.
[31]Wang K,Qu QS,Zhang YX,et al.Effects of Wuzhi capsule on blood concentration of tacrolimus after renal transplantation[J].JBiol Regul Homeost Agents,2016,30(1):155-159.
[32]Qin XL,Yu T,Li LJ,et al.Effect of long-term co-administration of Wuzhi tablet(Schisandra sphenanthera extract)and prednis-one on the pharmacokinetics of tacrolimus[J].Phytomedicine,2013,20(3-4):375-379.
[33]Wei H,Tao X,Di P,et al.Effects of traditional chinese medicine Wuzhi capsule on pharmacokinetics of tacrolimus in rats[J].Drug Metab Dispos,2013,41(7):1398-1403.
[34]Wang B,Yang S,Hu J,et al.Multifaceted interaction of the traditional Chinese medicinal herb Schisandra chinensis with cytochrome P450-mediated drug metabolism in rats[J].J Ethnopharmacol,2014,155(3):1473-1482.
[35]Qin XL,Bi HC,Wang XD,et al.Mechanistic understanding of the different effects of Wuzhi Tablet(Schisandra sphenanthera extract)on the absorption and first-pass intestinal and hepatic metabolism of Tacrolimus(FK506)[J].Int J Pharm,2010,389(1-2):114-121.
[36]Qin XL,Chen X,Zhong GP,et al.Effect of Tacrolimus on the pharmacokinetics of bioactive lignans of Wuzhi tablet(Schisandra sphenanthera extract)and the potential roles of CYP3A and P-gp[J].Phytomedicine,2014,21(5):766-772.
[37]Qin XL,Chen X,Wang Y,et al.In vivo to in vitro effects of six bioactive lignans of Wuzhi tablet(Schisandra sphenanthera extract)on the CYP3A/P-glycoprotein-mediated absorption and metabolism of tacrolimus[J].Drug Metab Dispos,2014,42(1):193-199.
[38]Russo E,Scicchitano F,Whalley BJ,et al.Hypericum perforatum:pharmacokinetic,mechanism of action,tolerability,and clinical drug-drug interactions[J].Phytother Res,2014,28(5):643-655.
[39]Süntar I,Oyard O,Akkol EK,et al.Antimicrobial effect of the extracts from Hypericum perforatum against oral bacteria and biofilm formation[J].Pharm Biol,2016,54(6):1065-1070.
[40]Bolley R,Zülke C,Kammerl M,et al.Tacrolimus-induced nephrotoxicity unmasked by induction of the CYP3A4 system with St John's wort[J].Transplantation,2002,73(6):1009.
[41]Mai I,St9rmer E,Bauer S,et al.Impact of St John's wort treatment on the pharmacokinetics of tacrolimus and mycophenolic acid in renal transplant patients[J].Nephrol Dial Transplant,2003,18(4):819-822.
[42]Hebert MF,Park JM,Chen YL,et al.Effects of St.John's wort(Hypericum perforatum)on tacrolimus pharmacokinetics in healthy volunteers[J].J Clin Pharmacol,2004,44(1):89-94.
[43]Godtel-Armbrust U,Metzger A,Kroll U,et al.Variability in PXR-mediated induction of CYP3A4 by commercial preparations and dry extracts of St John's wort[J].Naunyn Schmiedebergs Arch Pharmacol,2007,375(6):377-382.
[44]Komoroski BJ,Zhang S,Cai H,et al.Induction and inhibition of cytochromes P450 by the St John's wort constituent hyperforin in human hepatocyte cultures[J].Drug Metab Dispos,2004,32(5):512-518.
[45]王红勋.枳实与枳壳的现代药理与临床应用研究[J].中国卫生标准管理,2014,5(16):39-40.
[46]Stohs SJ,Preuss HG,Shara M.A review of the human clinical studies involving Citrus aurantium(bitter orange)extract and its primary protoalkaloid p-synephrine[J].Int J Med Sci,2012,9(7):527-538.
[47]Lin SP,Wu PP,Hou YC,et al.Different influences on tacrolimus pharmacokinetics by coad ministrations of zhi ke and zhi shi in rats[J].Evid Based Complement Alternat Med,2011,2011:751671.
[48]Wang MJ,Hou YC,Tsai SY,et al.Effects of coad ministrations of unripe fruits and ripe peels of Citrus aurantium on cyclosporine pharmacokinetics in rats[J].J Food Drug Anal,2007,15(3):265-270.
[49]Allison TL.Immunosuppressive therapy in transplantation[J].Nurs Clin North Am,2016,51(1):107-120.
[50]Vanhove T,Annaert P,Kuypers DR.Clinical deter minants of calcineurin inhibitor disposition:a mechanistic review[J].Drug Metab Rev,2016,48(1):88-112.