硫酸软骨素

硫酸软骨素结构式副作用CLINICALSTUDIESHAVENOTIDENTIFIEDANYSIGNIFICANTSIDEEFFECTSOROVERDOSESOFCHONDROITINSULFATE,WHICHSUGGESTITSLONGTERMSAFETY临床研究没有发现任何硫酸软骨素的明显副作用，即使服用过量，这表明其长期食用的安全性。（HATHCOCKJN,SHAOARISKASSESSMENTFORGLUCOSAMINEANDCHONDROITINSULFATEREGULATORYTOXICOLOGYANDPHARMACOLOGY,2007477883）临床试验THESTUDYALSOFOUNDCHONDROITINSULFATETOHAVEASIGNIFICANTEFFECTINREDUCINGJOINTSWELLING,EFFUSION,ORBOTH研究发现，硫酸软骨素，以减少关节肿胀，积液，或两者有显着效果。（CLEGGDO,REDADJ,HARRISCL,KLEINMA,ODELLJR,HOOPERMM,BRADLEYJD,BINGHAMCO3RD,WEISMANMH,JACKSONCG,LANENE,CUSHJJ,MORELANDLW,SCHUMACHERHRJR,ODDISCV,WOLFEF,MOLITORJA,YOCUMDE,SCHNITZERTJ,FURSTDE,SAWITZKEAD,SHIH,BRANDTKD,MOSKOWITZRW,WILLIAMSHJ2006“GLUCOSAMINE,CHONDROITINSULFATE,ANDTHETWOINCOMBINATIONFORPAINFULKNEEOSTEOARTHRITIS“NEWENGLJMED3548795808DOI101056/NEJMOA052771PMID16495392）IN2007,AREVIEWBYBRUYEREETALABOUTGLUCOSAMINEANDCHONDROITINSULFATEFORTHETREATMENTOFKNEEANDHIPOSTEOARTHRITISCONCLUDESTHATBOTHPRODUCTSACTASVALUABLESYMPTOMATICTHERAPIESFOROSTEOARTHRITISDISEASEWITHSOMEPOTENTIALSTRUCTUREMODIFYINGEFFECTS2007年，BRUYERE等人关于氨基葡萄糖和硫酸软骨素治疗膝关节和髋关节骨关节炎的结论是，这两种物质存在潜在的骨骼重建效果，从而对治疗骨关节疾病有着重要价值。（BRUYEREO,REGINSTERJYGLUCOSAMINEANDCHONDROITINSULFATEASTHERAPEUTICAGENTSFORKNEEANDHIPOSTEOARTHRITISDRUGSAGING,2007247573580）ATPRESENT,OARSIOSTEOARTHRITISRESEARCHSOCIETYINTERNATIONALISRECOMMENDINGCHONDROITINSULFATEASTHESECONDMOSTEFFECTIVETREATMENTFORMODERATECASESOFOSTEOARTHRITIS目前，OARSI（国际骨关节炎研究协会）建议硫酸软骨素作为中度骨关节炎的第二个最有效的治疗方法（ZHANGW,MOSKOWITZRWOARSIRECOMMENDATIONSFORTHEMANAGEMENTOFHIPANDKNEEOSTEOARTHRITIS,PARTICRITICALAPPRAISALOFEXISTINGTREATMENTGUIDELINESANDSYSTEMATICREVIEWOFCURRENTRESEARCHEVIDENCEACTIVITYOSTEOARTHRITISANDCARTILAGE,200715981999）LIKEWISE,THEEUROPEANLEAGUEAGAINSTRHEUMATISMEULARSUPPORTSTHEUSEFULNESSOFCHONDROITINSULFATEINTHEMANAGEMENTOFKNEEOSTEOARTHRITISANDGRANTSTHEHIGHESTLEVELOFEVIDENCE,1A,ANDSTRENGTHOFTHERECOMMENDATION,A,TOTHISPRODUCT同样，欧洲风湿病防治联合会（EULAR）支持硫酸软骨素对膝关节骨性关节炎治疗的有效性，并给予其最高的支持和建议水平。（JORDANKM,RECOMMENDATIONSARDENNKEULAR2003“ANEVIDENCEBASEDAPPROACHTOTHEMANAGEMENTOFKNEEOSTEOARTHRITISREPORTOFATASKFORCEOFTHESTANDINGCOMMITTEEFORINTERNATIONALCLINICALSTUDIESINCLUDINGTHERAPEUTICTRIALSESCISIT“ANNRHEUMDIS621211451155DOI101136/ARD2003011742PMC1754382PMID14644851HTTP/WWWPUBMEDCENTRALNIHGOV/ARTICLERENDERFCGITOOLPMCENTREZ172733）（CONTEA,DEBERNARDIM,PALMIERIL,LUALDIP,MAUTONEG,RONCAGMETABOLICFATEOFEXOGENOUSCHONDROITINSULFATEINMANARZNEIMITTELFORSCHUNG19914176872）（CONTEA,VOLPIN,PALMIERIL,BAHOUSI,RONCAGBIOCHEMICALANDPHARMACOKINETICASPECTSOFORALTREATMENTWITHCHONDROITINSULFATEARZNEIMITTELFORSCHUNG19954591825）（PALMIERIL,CONTEA,GIOVANNINIL,LUALDIP,RONCAGMETABOLICFATEOFEXOGENOUSCHONDROITINSULFATEINTHEEXPERIMENTALANIMALARZNEIMITTELFORSCHUNG19904031923）MULTIPLEDOSESOF800MGINPATIENTSWITHOSTEOARTHRITISDONOTALTERTHEKINETICSOFCHONDROITINSULFATETHEBIOAVAILABILITYOFCHONDROITINSULFATERANGESFROM15TO24OFTHEORALLYADMINISTEREDDOSEMOREPARTICULARLY,ONTHEARTICULARTISSUE,RONCAETAL19REPORTEDTHATCHONDROITINSULFATEISNOTRAPIDLYABSORBEDINTHEGASTROINTESTINALTRACTANDAHIGHCONTENTOFLABELEDCHONDROITINSULFATEISFOUNDINTHESYNOVIALFLUIDANDCARTILAGE在患者的骨关节炎处，800毫克的多剂量不会改变硫酸软骨素的动力学。硫酸软骨素的生物利用度范围为口服剂量的15至24。尤其是，对关节组织显示出其独特性，RONCA等19报道，硫酸软骨素在胃肠道吸收并不迅速，并且在滑液和软骨中发现了高含量标记的硫酸软骨素。（RONCAF,PALMIERIL,PANICUCCIP,RONCAGANTIINFLAMMATORYACTIVITYOFCHONDROITINSULFATEOSTEOARTHRITISCARTILAGE19986SUPPLA1421）作用机制THEEFFECTOFCHONDROITINSULFATEINPATIENTSWITHOSTEOARTHRITISISLIKELYTHERESULTOFANUMBEROFREACTIONSINCLUDINGITSANTIINFLAMMATORYACTIVITY,THESTIMULATIONOFTHESYNTHESISOFPROTEOGLYCANSANDHYALURONICACID,ANDTHEDECREASEINCATABOLICACTIVITYOFCHONDROCYTESINHIBITINGTHESYNTHESISOFPROTEOLYTICENZYMES,NITRICOXIDE,ANDOTHERSUBSTANCESTHATCONTRIBUTETODAMAGECARTILAGEMATRIXANDCAUSEDEATHOFARTICULARCHONDROCYTESARECENTREVIEWSUMMARIZESDATAFROMRELEVANTREPORTSDESCRIBINGTHEBIOCHEMICALBASISOFTHEEFFECTOFCHONDROITINSULFATEONOSTEOARTHRITISARTICULARTISSUES硫酸软骨素对骨关节炎患者的影响是综合效应的结果，包括其抗炎活性，刺激蛋白多糖和透明质酸的合成，通过抑制蛋白水解酶、一氧化氮和其他损伤软骨基质并导致关节软骨细胞死亡的物质的合成，从而减少软骨细胞的分解代谢。最近的一项调查总结了有关报告的数据，描述了硫酸软骨素对骨性关节炎的关节组织影响的生化基础。（MONFORTJ,PELLETIERJP,GARCIAGIRALTN,MARTELPELLETIERJBIOCHEMICALBASISOFTHEEFFECTOFCHONDROITINSULFATEONOSTEOARTHRITISARTICULARTISSUESANNRHEUMDIS2007DOI101136/ARD2006068882）RECENTLY,NEWMECHANISMSOFACTIONHAVEBEENDESCRIBEDFORCHONDROITINSULFATEINANINVITROSTUDY,CHONDROITINSULFATEREDUCEDTHEIL1INDUCEDNUCLEARFACTORKBNFBTRANSLOCATIONINCHONDROCYTES21最近，已有硫酸软骨素新作用机制的描述。在体外研究中，硫酸软骨素减少了软骨细胞IL1诱导的核因子KB（NFB的）的易位。（JOMPHEC,GABRIACM,HALETM,HEROUXL,TRUDEAULE,DEBLOISD,MONTELLE,VERGESJ,DUSOUICHPCHONDROITINSULFATEINHIBITSTHENUCLEARTRANSLOCATIONOFNUCLEARFACTO