受体介导乳糖化重组人生长激素的肝靶向性

:2002203212;:2002209213:(39670861):(1972),(),,,154200211JournalofIsotopesVol.15No.4Nov.20021,2,3,1,2,4(1.,610041;2.,610041;3.,400010;4.,610041):(L2rhGH)131IL2rhGHrhGH,;125IL2rhGHrhGH:L2rhGH,76.8%,rhGH2;ASGP2R:(L2rhGH);;:R969.1:A:100027512(2002)0420197203(RecombinantHumanGrowthHormone,rhGH)(GrowthHormone,GH),Turners[1,2]GHIGH[3],rhGH,;,GHrhGH,rhGH,,(ASGP2R)[4]rhGH,L2rhGH,L2rhGH1(1):rhGH:;Na125I,Na131I(1000GBqöL):(2):C:Siemens;C:261(3):(),()():2211L-rhGHrhGHpH9.6140h;SephadexG250,LKB,2[5],,45L2rhGH212rhGHL-rhGH[6],SephadexG250,,98%0.22Lm2132.3.1131I2rhGH131I2L2rhGHNGA+131I2L2rhGH22.5kgSiemensBasicanC,131I2rhGH131I2L2rhGH,1ömin60min,1234510153060min2.5kg(NGA,ASGP2R),131I2L2rhGH,2.3.2131I2L2rhGH2kg,131I2L2rhGH,C2.3.3125I2L2rhGH125I2rhGH48(1624g,),16,3,8125I2L2rhGH,8125I2rhGH;125I2L2rhGH,13510153060120min,,,,7%3311131I2L2rhGH5min,,60min;3060min,,131I2rhGH,131I2L2rhGH,,,30min131I2L2rhGH131I2rhGHNGA+131I2L2rhGH11,131I2rhGH32.5%,131I2L2rhGH76.8%,2rhGHL2rhGHrhGHNGA131I2L2rhGH,131I2L2rhGH,5min25.0%NGAASGP2R,ASGP2R,,131I2L2rhGH312131I2L2rhGH,,ASGP2R313125I-L-rhGH125I-rhGH2323125I2L2rhGH125I2rhGH,23,125I2L2rhGH125I2rhGH,125I2rhGH(30min)T,,rhGHL2rhGH(P0.05),(P0.01)1131I-L-rhGH131I-rhGHNGA+131I-L-rhGH(min)öID%1234510153060131I2L2rhGH56.460.767.672.376.873.562.840.121.7131I2rhGH21.321.822.428.332.535.633.423.817.5NGA+131I2L2rhGH23.223.424.524.825.024.324.620.813.62125I-L-rhGH(xs,n=3)(min)öID%1351015306012023.797.398.281.104.440.84.810.684.861.889.320.348.980.634.420.430.730.290.540.80.210.060.330.060.260.060.580.050.510.220.220.074.751.763.851.112.560.152.530.332.530.432.770.652.350.701.541.0852.690.8163.872.3168.835.1565.221.3759.723.9921.671.089.910.475.200.380.370.090.410.050.210.010.330.080.210.020.440.100.490.100.260.067.861.589.460.9613.922.5210.691.607.991.564.630.272.320.111.330.502.800.633.400.592.230.433.330.573.390.809.780.779.480.777.050.75891153125I-rhGH(xs,n=3)(min)öID%1351015306012042.542.1823.240.0218.451.3311.022.1810.372.129.310.957.452.476.962.021.320.841.310.060.660.070.580.120.360.130.570.250.600.030.420.1416.421.4614.850.3912.50.129.491.439.002.946.930.664.710.213.241.5019.232.0324.361.9728.211.2235.972.7133.731.2312.161.315.960.903.950.440.490.020.520.030.420.110.770.160.470.160.800.220.610.120.650.0911.191.6820.281.9720.992.1518.424.8016.273.174.690.302.720.501.711.135.000.685.230.546.281.214.351.817.032.37.971.587.420.676.221.414(1)L2rhGH,ASGP2R,(2):rhGHL2rhGH,L2rhGH,(3)L2rhGHrhGH,,:[1],1[M]1:,199517379.[2]HoKY,KellyJj.RoleofGrowthHormoneinFlu2idHormostasis[J].HormRes,1991,36(Suppl1):4448.[3]BankeMb.GrowthHormoneTherapyinTurnerSyndrome[J].HormRes,1995,44(Suppl3):3541.[4]AshellG,GarfordJ.Carbonhyrate2SepecofilRe2ceptorsofLiver[J].AnnuRewBiochem,1982,51:531543.[5]DuboisM,GillesKA,HamiltonJK,etal.Col2orimetricMethodforDeterminationofSugarsandRelatedSubstance[J].AnalChem,1956,28(3):350356.[6]GreenwordFc,HunterWm,GloverJs.ThePre2parationof131I2LabledHumanGrowthHormoneofHGHSpecific[J].ActivityBiochemJ,1963,89:114123.TheLiverTaxisofReceptorMediatedLactosaminatedHumanGrowthHormoneCHENZe2lian1,LITong2ling2,HEJu2ying3,SHILin1,PANGQi2jie2,GUANChang2tian4(1.DepartmentofPharmcy,HuaxiHospitalofSichuanUniversity,Chengdu610041,China;2.SchoolofPharmacy,SichuanUniversity,Chengdu610041,China;3.DepartmentofPharmacy,XinanHospitaloftheThirdMilitaryMedicalUniversity,Chongqing400010,China;4.DepartmentofNuclearMedicine,HuaxiHospitalofSichuanUniversity,Chengdu610041,China)Abstract:Radiographyimagingisusedtoassesslivertaxismechanismofanti2dwarfismdruglac2tosaminatedhumangrowthhormone(L2rhGH).BothL2rhGHandrhGHlabelledwith131Iaretostudytheirbiodistributioninanimals(includingrabbits,cocksandrats).TheresultsshowthatL2rhGHisofspecifichepatictargetingproperty,andthemaximunhepaticconcertrationrateis76.8%,whichistwotimesofrhGH.Itshepaticbindingisreceptormediated.Keywords:lactosaminatedhumangrowthhormone(L2rhGH);hepatictargetingmechanism;recep2tormediatedproperty9914: