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1、AbstractTriptolide(TP)hasgoodanti-tumoractivityandanti-inflammatoryeffect,butitalsohasserioussideeffects,therebytheclinicalusewaslimited.Lowwatersolubilityandlowbioavailabilityarethetoxicityreason・Tosolvethisthornyproblem,ourresearchaimsatusingwater-solub
2、lepolymerasacarrier,prepareahigherlipid-watcrpartitioncoefficientprodrug-triptolidepolypeptide(TP-PAG)withoutaffectingitspharmacologicalactivity.Thisstudyincludesthefollowingfourparts:(1)EstablishtheanalyticalmethodsofTP-PAGTaketriptolideasthemeasurementi
3、ndicator,weestablishedthehighperformanceliquidchromatography(HPLC)methodtoanalyzeTP-PAGOptimalHPLCmethodconditionsare:themobilephase:acetonitrile-water(25:75);flowrateisLOmLmin4;detectionwavelengthis215nm.Triptolideshowedagoodlinearitywithinarangeof0.226〜
4、2.262mgmL_1,thelinearcurveisA=2803.5C+19167(r2=0.9998).Themethodisaccurateandsimple,showsgoodreproducibility,highsensitivity.(2)SynthesisofTP-PAGFirstly,wesynthesizedpolypeptidewithrawmaterialsofL-AspandL-Glu.Later,wecombinedpolypeptidewithTPtoformTP・PAGI
5、nordertogreatlyimproveproductyieldandpurity,weconductedorthogonalexperimentstofindouttheoptimalconditionofbenzylsynthesis.WcalsocharacterizedeachproductbyFTIRand"H・NMR,andtheresultsindicatedthatTP-PAGwassuccessfullysynthesized.(3)StabilityandactivityofTP-
6、PAGByTP-PAGstabilitystudyanditspreliminaryactivitystudyagainsttumorcells,wefoundthatTP-PAGsolubilityinwaterwas1.45g/100mL,andTP-PAGshowedgoodstabilityinpH6.8phosphatebuflersolution,pH7.4phosphatebufferanddistilledwate匚However,itcouldonlybestablein0.1mol/L
7、HC1for12hours,whichmeanthatitscontentwoulddecreaseafter12hours.ThepreliminaryactivitystudyagainsttumorcellsindicatedthatTP-PAGhasgoodinhibitionagainstthegrowthofhumanhepatomaBel7402cells.(4)PreparationandEvaluationofTP-PAGliposomesTaketheEncapsulationeffi
8、ciencyaskeyindicator,wcfoundthatthereverseevaporationmethodistheoptimalmethodtoprepareTP-PAGliposomesbycomparingfourpreparationmethodsandtheyareetherinjectionmethod,ethanolinjectionmethod,filmdispersion-fireeze-thaw
