Probing the Binding Sites of Antibiotic Drugs Doxorubicin and N-(trifluoroacetyl) Doxorubicin with Human and Bovine Serum Albumins 英文参考文献.docVIP

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Probing the Binding Sites of Antibiotic Drugs Doxorubicin and N-(trifluoroacetyl) Doxorubicin with Human and Bovine Serum Albumins 英文参考文献.doc

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Probing the Binding Sites of Antibiotic Drugs Doxorubicin and N-(trifluoroacetyl) Doxorubicin with Human and Bovine Serum Albumins 英文参考文献

ProbingtheBindingSitesofAntibioticDrugs DoxorubicinandN-(trifluoroacetyl)Doxorubicinwith HumanandBovineSerumAlbumins DanielAgudelo,PhilippeBourassa,JulieBruneau,GervaisBe′rube′,Eric′ Asselin,Heidar-AliTajmir-Riahi* De′partementdeChimie-Biologie,Universite′ duQue′beca` Trois-Rivie`res,Trois-Rivie`res(Que′bec),Canada Abstract Welocatedthebindingsitesofdoxorubicin(DOX)andN-(trifluoroacetyl)doxorubicin(FDOX)withbovineserumalbumin (BSA)andhumanserumalbumins(HSA)atphysiologicalconditions,usingconstantproteinconcentrationandvariousdrug contents. FTIR, CD and fluorescence spectroscopic methods as well as molecular modeling were used to analyse drug binding sites, the binding constant and the effect of drug complexation on BSA and HSA stability and conformations. Structural analysis showed that doxorubicin and N-(trifluoroacetyl) doxorubicin bind strongly to BSA and HSA via hydrophilic and hydrophobic contacts with overall binding constants of K DOX-BSA =7.8 (60.7)6103M21, KFDOX-BSA =4.8 (60.5)6103M21andKDOX-HSA=1.1(60.3)6104M21,KFDOX-HSA=8.3(60.6)6103M21.Thenumberofbounddrugmolecules per protein is 1.5 (DOX-BSA), 1.3 (FDOX-BSA) 1.5 (DOX-HSA), 0.9 (FDOX-HSA) in these drug-protein complexes. Docking studies showed the participation of several amino acids in drug-protein complexation, which stabilized by H-bonding systems.Theorderofdrug-proteinbindingisDOX-HSA.FDOX-HSA.DOX-BSA.FDOX.BSA.Drugcomplexationalters proteinconformationbyamajorreductionofa-helixfrom63%(freeBSA)to47–44%(drug-complex)and57%(freeHSA)to 51–40%(drug-complex)inducingapartialproteindestabilization.DoxorubicinanditsderivativecanbetransportedbyBSA andHSAinvitro. Citation:AgudeloD,BourassaP,BruneauJ,Be′rube′ G,AsselinE′,etal.(2012)ProbingtheBindingSitesofAntibioticDrugsDoxorubicinandN-(trifluoroacetyl) DoxorubicinwithHumanandBovineSerumAlbumins.PLoSONE7(8):e43814.doi:10.1371/journal.pone.0043814 Editor:DanielS.Sem,ConcordiaUniversityWisconsin,UnitedStatesofAmerica ReceivedJune8,2012;AcceptedJuly26