化学合成技术在中药新药开发中的应用

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1、5．合成的w3有与蜈蚣三七皂苷相似的抗肿瘤活性，从而证明中药内含有效成分的化学合成是可行的，亦有很好的操作性。关键词：W3；蜈蚣三七；中药资源；化学合成；增殖抑制作用；细胞凋亡率VAbstractChemosynthesistechniqueintheChineseherbalmedicinenewmedicinedevelopmentSpeciality：diagnosticsofTraditionalChineseMedicineAuthor：YifanLiaoTutor：JianxinHaoChineseherbalmedicineistheb

2、asicandcarrierofTraditionalChineseMedicinehealthcare，diseasesprevented．Chineseherbalmedicinehasawealthofsciencemeaningsandpracticalvalue．WiththerapidgrowthofhealthcarecauseandtheTraditionalChineseMedicineanddrugsheadforworldisbecomingclear,thereisaheavydemandonChineseherbalmedi

3、cineresources．Inthemeantime，thecontradictionbetweenthesupplyandrequirementisbecomingaculeateincreasingly．Weshouldeffectivelyprotect,rationallyexploitandeconomizeonthenaturalChineseherbalmedicinereSources．WugongSanqiisfromrhizomeofAnemoneflaccidaFr．Schmidtwhichisefficientattreat

4、ingrheumaticache，traumaticinjury．WeCanresolveresourcesshortagebymeansofchemosynthesis．IncontrastwiththewayofseparatingW3fromoriginalplants，chemosynthesishasmoreadvantagessuchassimplermethod，lowercost，shortertime，higherefficiencyandsuitedtocommercialprocess．W3Canbesynthesizedbyf

5、ivereportedcompoundsinaconvergenceprocess．Thepurityoffinallyproductisupto90％．Intheanti-tumorexperiment,drugsweredividedintosixgroups，totalsaponinsofWugongSanqigroup，W3group，oleanolicacidgroup，positiveVIdrugcontrolgroup，DMSOgroup，blankcontrolgroup．nleinhibitionratesofthecellgrow

6、thofcellsHepG2andcells卸巳LdeterminedbyusingMTTassays．After48hours，observedmorphologicalchangesofthesecellsandcellcycledistributionandapoptosisratewasanalyzedwithflowcytometry．Ultrastructuralofcellswereobservedbytransmissionelectronmicroscope．SPPS15．0softwarewasusedforstatistical

7、analysis．W’·‘·一一-‘lhemajorconclusions：1．InthisPaperthemethodofchemosynthesisWehaveadoptediseffectiveandfeasible．2．TheinhibitoryeffectofW3isgreaterthantotalsaponinsofWugongSanqiandoleanolicacid．NoinhibitionofcellsHELwithallthree．3．MorphologicalChanges(1ightandelectronmicroscope)

8、：W3moderatedosagegrouphasthebesteffecttokillcellsHepG2