摘要及百度翻译

摘要目的：建立杜仲炮制工艺的质量标准，研究盐炙前后杜仲中化学成分组群的变化特征，结合血清药物化学及体内代谢动力学阐明杜仲盐炙入肾的炮制机理。方法：采用UV、HPLC等分析方法建立盐制杜仲主要化学部位总含量，分析炮制过程对杜仲化学成分群组成结构的影响； 在此基础上，结合血清药物化学的研究方法，考察盐制杜仲在肾阳虚证模型大鼠的时空动态HPLC血清指纹图谱，在肾阳虚证模型大鼠肾组织的分布特征；测定血清中血清皮质醇、睾酮、雌二醇、环磷酸腺苷、环磷酸鸟苷、17-羟类固醇随时间变化情况。结果：（1）分别以芦丁、松脂醇二葡萄糖苷、谷氨酸、 D-葡萄糖为对照品，采用紫外分光光度法测定杜仲盐炙前后的总黄酮、总木脂素、氨基酸和多糖的含量，数据显示生品总黄酮的含量为2.76%，制品总黄酮含量为2.31%，炮制后含量明显下降（p<0.05）;生品总木质素的含量为 10.59%，制品总木脂素的含量为9.51%，炮制后含量明显下降（p<0.05）;生品氨基酸的含量为0.09%，制品氨基酸含量为0.12%，炮制后含量明显上升（p<0.05）;生品多糖的含量为0.26%，制品多糖的含量为0.36%，炮制后含量明显上升（p<0.05）。（2） 分别以京尼平酸、绿原酸、京尼平苷、松脂醇二葡萄糖苷为对照品，米用高效液相色谱法测定杜仲生品、盐炙品中京尼平苷酸、绿原酸、京尼平苷、松脂醇二葡萄糖苷的含量，数据分析显示，京尼平苷酸生品含量为 0.38%，制品含量为0.19%，炮制后含量明显下降（p<0.05）;绿原酸生品含量0.37%，为制品含量为0.29%，炮制后含量明显下降（p<0.05）;京尼平苷生品含量为0.24%，制品含量为0.20%，炮制后含量明显下降；松脂醇二葡萄糖苷生品含量为0.24%，制品含量为0.18%，炮制后含量明显下降。（3） 以氢化可的松造成肾阳虚模型，将杜仲生品及盐炙品灌胃给药，观察给药前后负重游泳时间、各脏器指数、血清中睾酮、雌二醇、环磷酸腺苷、环磷酸鸟苷、皮质醇和17-羟类固醇的变化，数据显示对于氢化可的松所致肾阳虚模型，模型与空白组比较有显著性差异（p<0.01）;盐炙杜仲与生品杜仲比较有显著性差异（p<0.05），给药组与模型组有显著性差异（p<0.05）;空白组与给药组无明显差异。取SD大鼠24只，随机分为6组，按成人用量的40倍量灌胃给予杜仲生品和盐制品浓缩液(浓度2.5g生药/mL/100g体重)，采用HPLC法测定入血成分，分析杜仲生品和盐制品化学成分的变化规律。结果显示，共有入血成分京尼平苷酸和松脂醇二葡萄糖苷，二者含量与液相测得数据变化规律类似，都是盐炙后成分略有减少；肝脏的分布京尼平苷酸含量变化不显著，而松脂醇二葡萄糖苷的含量盐炙后明显大于生品；肾脏的分布京尼平苷酸虽差异不大但二者吸收都较高，松脂醇二葡萄糖苷的吸收也是制品大于生品，吸收较高且差异显著。结论：结合各检测结果分析，杜仲炮制品总黄酮和总木脂素含量下降明显， 多糖与氨基酸显著上升，而HPLC检测结果显示京尼平苷酸、绿原酸、京尼平苷及松脂醇二葡萄糖苷含量都下降，只是下降程度不同；但药效学结果显示盐炙品效果优于生品；在血清药物化学成分中，入血成分京尼平苷酸和松脂醇二葡萄糖苷含量较高，且在肝脏和肾脏中分布盐炙品均大于生品；综合上述，有效成分的单项含量增加不能等同于药效结果的优劣，或者说入肾治疗肾阳虚的有效化学成分群不完全是文章中所述的全部，就本文而言，炮制后杜仲化学成分组群不论在质还是量上都发生了一定的改变，也在一定范围内迎合了本文所提出的化学成分配比关系的效应最大化假说，所以，以中医理论为指导，杜仲炮制是以各种炮制方法为间接手段，旨在使其化学成分组群在配比关系上达到最佳，从而发挥其入肾而治疗肾阳虚的最佳疗效。AbstractObjective:ToestablishthequalitystandardofEucommiaulmoidesOlivprocessed,studythevariationcharacteristicsofchemicalgroupafterstirfriedwithsaltwater.ClarifytheProcessingmechanismofEucommiaulmoidesOlivtransferintothekidneybyserumpharmaceuticalchemistryandpharmacokinetics.Methods:EstablishthetotalcontenttestingmethodofmainchemicalpartsofEucommiaulmoidesOlivbyUV,HPLCandotheranalysismethods,AnalysistheeffectofprocessingtothecompositionstructureofEucommiagroupchemical.Bythemethodofserumpharmacochemistry,westudiedthespatio-temporaldynamicsofHPLCserumfingerprintofEucommiaulmoidesOlivstirfriedwithsaltwater,andthedistributioncharacteristicsinrenaltissueininsufficiencyofkidney-YANGratmodel.Determinedthecontentvariationofserumcortisol,testosterone,estradiol,cAMP,cGMP,17-hydroxysteroid.Results:(1)Usingrutin,pinoresinoldiglucoside,glutamicacid,D-glucoseasstandardrespectively,testedthetotalflavonoids,totallignans,aminoacidandpolysaccharideofEucommiaulmoidesOlivbyUVmethod,testedthesamplesbeforestirfriedwithsaltandafterstirfriedwithsaltrespectively.Theresultsshowedthatcontentoftotalflavonoidswas2.76%intherawproducts,whilethecontentoftotalflavonoidswas2.31%afterprocessed.Thecontentdecreasedsignificantlyafterprocessed(P<0.05).Thecontentoftotallignanswas10.59%intherawproducts,thetotallignanscontentproductsis9.51%afterprocessed,Thecontentdecreasedsignificantlyafterprocessed(P<0.05).Thecontentofaminoacidsinrawproductswas0.09%,whilethecontentwas0.12%afterprocessed,Thecontentincreasedsignificantly(P<0.05).Thecontentofpolysaccharideinrawproductswas0.26%,whilethecontentwas0.36%afterprocessed,Thecontentincreasedsignificantly(P<0.05).Usinggeniposidicacid,chlorogenicacid,geniposide,pinoresinoldiglucosideasstandardrespectively,testedthecontentsoftheminbothrawproductandtheproductafterprocessed.Theanalysisshowed,thecontentofgeniposidicacidwas0.38%,whilethecontentoftheproductafterprocessedwas0.19%.Thecontentdecreasedsignificantlyafterprocessed(P<0.05);thecontentofchlorogenicacidinrawproductwas0.37%,astheproductafterprocessedwas0.29%.Thecontentdecreasedsignificantlyafterprocessed(P<0.05);thecontentofgeniposideinrawproductwas0.24%,whilethecontentofproductafterprocessedwas0.20%,Thecontentdecreasedsignificantlyafterprocessed.Thecontentofpinoresinoldiglucosideinrawproductwas0.24%,asthecontentofproductafterprocessedwas0.18%,Thecontentdecreasedsignificantlyafterprocessed.theinsufficiencyofkidney-YANGmodelwasbuiltwithhydrocortisone,therawmaterialandsaltfryingofEucommiaulmoidesOlivweretakenbyintragastricadministration,observethevariationoftheswimmingtime,Visceraindex,serumtestosterone,estradiol,cAMP,cGMP,cortisoland17-hydroxysteroidbeforeandafteradministration.Theresultshowed,forhydrogenationkidneyyangdeficiencymodelinducedbyhydrocortisone,therewassignificantdifferences(P<0.01)betweenmodelgroupandthecontrolgroup;comparedwiththerawEucommiaulmoidesOliv,theprocessedproductshowedsignificantlydifferent(P<0.05),thedruggroupandmodelgroupweresignificantlydifferent(P<0.05);controlgroupandadministrationgrouphadnoevidentdifferenee.(4)24SDratswererandomlydividedinto6groups,40timesofadultdosagewastakenbyintragastricadministration,boththerawEucommiaulmoidesOlivandprocessedproductconcentratedsolution(concentration2.5g/mL/100gbodyweight)wasexperiment.HPLCwasusedforthedeterminationofcomponentstransferintoblood,analysisthechemicalcompositionvariationofEucommiaulmoidesOlivrawmaterialsandofprocessedproducts.Theresultsshowedthat,thereweretwocomponentstransferintoblood,theyweregeniposidicacidandpinoresinoldiglucoside,thesecomponentschangesimilartotheHPLCresultstudiedbefore.Theybothdecreasedslightlyafterprocessed;contentofgeniposidicaciddistributedinliverdidnotchangesignificantly.ThecontentofpinoresinoldiglucosideofEucommiaulmoidesOlivthatstirfriedwithsaltwassignificantlygreaterthanrawproduct;geniposidicacidinrenaldistributionhaslittlediffereneebetweentherawproductandtheprocessedone,theabsorptionwerebothhigh.PinoresinoldiglucosideinkidneydistributenofEucommiaulmoidesOlivthatstirfriedwithsaltwasgreaterthanthecrudeproducttoo,theabsorptionwashighandthediffereneewassignificant.Conclusion:alltheresultshowed,thecontentoftotalflavonoidsandtotallignansofEucommiaulmoidesOlivProcessedproductshaveobviouslydecline,andPolysaccharideandandaminoacidhaveobviouslyrise.Ontheotherhand,thecontentofgeniposidicacid,geniposide,chlorogenicacid,pinoresinoldiglucosidehavedifferentlydecline.Also,thepharmacodynamicsstudyindicatedthat,theeffectoftheSaltroastproductisbetterthanthecrude,andthedistributionbothinliverandinkidney,theSaltroastproductaremorethanthecrude.Aboveall,theincreaseofonlyoneeffectivecomponent'sontentcannotindicatealltheefficacy,namely,theeffectivechemicalcompositions,treainginsufficieneyofkidney-YANGintothekidney,areincompletelyallincludedinthearticle.Inthisarticle,afterprocessed,theChemicalcompositionsofEucommiaulmoidesOlivbothqualityandquantityhavebeenchanged,whichinaccordaneewiththeEffectmaximizationhypothesisofchemicalcomposition,mentionedinthisarticle.So,GuidedbyTCMtheory,theprocessingmethodofEucommiaulmoidesOliviscombinedwithdifferentkindsofprocessingmethod,tomakethegroupsofchemicalcompositionincombinationachievetothebest,forthebestcurativeeffectthroughtreatinginsufficieneyofkidney-YANGintothekidney.AbstractObjective:toestablishthequalitystandardofEucommiaulmoidesOliverprocess,beforeandafterthestudyonsaltsunburnEucommiachemicalelementinthegroupcharacteristics,processingmechanismcombinedwithserumpharmaceuticalchemistryandpharmacokineticsofEucommiaulmoidesstirfriedwithsaltintothekidneytoelucidatethe.Methods:toestablishthemainchemicalpartsofEucommiaulmoidesOlivtotalcontentusingUV,HPLCandotheranalysismethods,analysisontheeffectofchemicalcompositionofprocessingEucommiagroupstructure;onthisbasis,combiningwiththeresearchmethodofserumpharmacochemistry,EucommiaulmoidesOlivonspatio-temporaldynamicsofHPLCserumfingerprintofkidneyyangdeficiencyratmodel,distributioncharacteristicsinrenaltissueofratswithkidneyyangdeficiencymodel;Determinationofserumcortisol,testosterone,estradiol,cyclicadenosinemonophosphate,cGMP,17-hydroxysteroidvariationwithtime.Results:(1)respectivelywithrutin,pinoresinolglucoside,glutamicacid,twoD-glucoseasstandard,thedeterminationoftotalflavonoidsofEucommiaulmoides,stirfriedwithsaltbeforeandafterthespectrophotometryoftotallignans,aminoacidandpolysaccharidecontentofUV,datadisplayscontentoftotalflavonoidswas2.76%,totalflavonoidsthecontentofproductis2.31%,afterprocessingcontentsignificantlydecreased(P<0.05);thecontentofcrudeligninwas10.59%,thetotallignanscontentproductsis9.51%,afterprocessingcontentsignificantlydecreased(P<0.05);contentofrawproductsofaminoacidswas0.09%,productaminoacidcontentwas0.12%,afterprocessingcontentincreasedsignificantly(P<0.05);studentscontentpolysaccharidewas0.26%,thecontentofpolysaccharidewas0.36%products,processedcontentincreasedsignificantly(P<0.05).respectivelytogeniposidicacid,geniposide,chlorogenicacid,pinoresinoltwoglucosideascontrolsample,usinghighperformaneeliquidcontentdeterminationEucommiarawmaterials,saltfryinggeniposidicacid,geniposide,chlorogenicacid,pinoresinoItwoglucosidechromatography,dataanalysisdisplay,geniposidicacidcontentis0.38%,productcontentis0.19%,afterprocessingcontentsignificantlydecreased(P<0.05);chlorogenicacidproductcontentof0.37%,astheproductwas0.29%,afterprocessingcontentsignificantlydecreased(P<0.05);genipinGanshengproductcontentis0.24%,thecontentofproducts0.20%,afterprocessingdecreasedtwo;pinoresinolglucosideproductcontentis0.24%,productcontentis0.18%,afterprocessingdecreased.withhydrocortisonecausesthekidneyyangdeficiencymodel,theEucommiarawmaterialsandsaltfryingintragastricadministration,observethechangebeforeandafteradministrationoftheswimmingtime,Visceraindex,serumtestosterone,estradiol,cyclicadenosinemonophosphate,cGMP,cortisoland17-hydroxysteroid,datadisplayforhydrogenationkidneyyangdeficiencyinducedbyhydrocortisonemodel,modelandthecontrolgrouphadsignificantdifferences(P<0.01);stirfriedwithsaltandcrudeEucommiaEucommiaulmoidesweresignificantlydifferent(P<0.05),druggroupandmodelgroupweresignificantlydifferent(P<0.05);controlgroupandadministrationgrouphadnoevidentdifferenee.24SDrats,wererandomlydividedinto6groups,accordingto40timesofadultdosagebyintragastricadministrationEucommiarawgoodsandsaltproductsconcentratedsolution(concentration2.5g//mL/100gbodyweight),usingHPLCmethodforthedeterminationofbloodcomponents,variationanalysisofEucommiarawmaterialsandchemicalcompositionofsaltproducts.Theresultsshowedthat,therewerebloodcomponentofgeniposidicacidandpinoresinolglucosidecontentoftwo,twoandtheliquidphasechangessimilartomeasureddata,areprocessedwithsaltcompositiondecreasedslightly;liverdistributiongeniposidicacidcontentdidnotchangesignificantly,andpinoresinolglucosidecontenttwostirfriedwithsaltwassignificantlygreaterthanproducts;renaldistributiongeniposidicacidhaslittledifferencebutthetwoabsorptionishigher,pinoresinoltwoglucosideabsorptionisgreaterthanthecrudeproducts,absorptionishigherandthedifferencewassignificant.Conclusion:combinedwiththeanalysisofthetestresultsoftotalflavonoidsofEucommiaulmoides,processed