SONG Chunmei, ZHANG Liang, LIANG Shengbin, QIAN Min, DU Bing, YU Yihua, LI Jianqi. SYNTHESIS OF FLUORESCENE LABELED PEPTIDE/POLY(ETHER-AMIDE)WITH TARGETING FUNCTION TO LIVER CANCER CELLS. [J]. Acta Polymerica Sinica (7):892-896(2010)
DOI:
SONG Chunmei, ZHANG Liang, LIANG Shengbin, QIAN Min, DU Bing, YU Yihua, LI Jianqi. SYNTHESIS OF FLUORESCENE LABELED PEPTIDE/POLY(ETHER-AMIDE)WITH TARGETING FUNCTION TO LIVER CANCER CELLS. [J]. Acta Polymerica Sinica (7):892-896(2010) DOI: 10.3724/SP.J.1105.2010.09287.
SYNTHESIS OF FLUORESCENE LABELED PEPTIDE/POLY(ETHER-AMIDE)WITH TARGETING FUNCTION TO LIVER CANCER CELLS
To develop and characterize a new cancer target gene delivery carrier
which could be used as potential blood pool magnetic resonance (MR)contrast agents
a novel FAM-AGKGTPSLETTPC-COOH/poly(ether-amide)(FAM-13/PEG/DTPA)copolymer (Ⅲ)with fluorescence probe was designed and obtained first from the reaction of the amino group terminated poly(ether-amide)(PEG/DTPA)copolymer ligand (Ⅱ)with heterobifunctional cross-linker m-maleimidobenzoyl-N-hydroxysuccinimide ester(MBS)(Step 2),and then Michael addition of CC double bond in MBS moiety with SH group in FAM-labeled hepatocarcinoma specific adhesin peptide
FAM-AGKGTPSLETTPC-(SH)-COOH(FAM-13)
in high yield(Step 3).Ⅱ was prepared by the reaction of diethylenetriamine pentaacetic acid dianhydrid(DTPAA)with amino group terminated PEG(Ⅰ)(Step 1).The two copolymers of Ⅱ and Ⅲ were characterized by 1H-NMR and 13C-NMR measurements.The liver tumor-specific identification and antigen localization of Ⅲ with the fluorescin-labeled FAM-13 peptide were performed under cellular level.Targeting properties of Ⅲ were tested on the normal cells and liver cancer cells
respectively.No fluorescence was observed on normal liver cells L-02
while strong yellowish green fluorescence was observed on the liver cancer cells BEL-7404.The property of FAM-13 peptide in Ⅲ for recognizing specifically the liver cancer cells was demonstrated.It was also demonstrated that the chemically synthesized Ⅲ with peptide FAM-13 still had the property for targeting on the surface membrane of liver cancer cells in vitro,thus further indicating that the specific targeting effect of the objective tissue was mediated by the peptides of Ⅲ insert into the cell membrane.It is evident that the Ⅲ with FAM-13 peptide would be an excellent candidate for the targeting therapy to hepatocarcinoma.So ligand molecules Ⅲ with targeting peptides can target hepatocellular carcinoma.Ligand Ⅲ is a promising candidate
which can be coordinated with Gd3+ ion to give the macromolecular contrast agent.To develop and characterize a new cancer target gene delivery carrier
which could be used as potential blood pool magnetic resonance (MR)contrast agents
a novel FAM-AGKGTPSLETTPC-COOH/poly(ether-amide)(FAM-13/PEG/DTPA)copolymer (Ⅲ)with fluorescence probe was designed and obtained first from the reaction of the amino group terminated poly(ether-amide)(PEG/DTPA)copolymer ligand (Ⅱ)with heterobifunctional cross-linker m-maleimidobenzoyl-N-hydroxysuccinimide ester(MBS)(Step 2),and then Michael addition of CC double bond in MBS moiety with SH group in FAM-labeled hepatocarcinoma specific adhesin peptide
FAM-AGKGTPSLETTPC-(SH)-COOH(FAM-13)
in high yield(Step 3).Ⅱ was prepared by the reaction of diethylenetriamine pentaacetic acid dianhydrid(DTPAA)with amino group terminated PEG(Ⅰ)(Step 1).The two copolymers of Ⅱ and Ⅲ were characterized by 1H-NMR and 13C-NMR measurements.The liver tumor-specific identification and antigen localization of Ⅲ with the fluorescin-labeled FAM-13 peptide were performed under cellular level.Targeting properties of Ⅲ were tested on the normal cells and liver cancer cells
respectively.No fluorescence was observed on normal liver cells L-02
while strong yellowish green fluorescence was observed on the liver cancer cells BEL-7404.The property of FAM-13 peptide in Ⅲ for recognizing specifically the liver cancer cells was demonstrated.It was also demonstrated that the chemically synthesized Ⅲ with peptide FAM-13 still had the property for targeting on the surface membrane of liver cancer cells in vitro,thus further indicating that the specific targeting effect of the objective tissue was mediated by the peptides of Ⅲ insert into the cell membrane.It is evident that the Ⅲ with FAM-13 peptide would be an excellent candidate for the targeting therapy to hepatocarcinoma.So ligand molecules Ⅲ with targeting peptides can target hepatocellular carcinoma.Ligand Ⅲ is a promising candidate
which can be coordinated with Gd3+ ion to give the macromolecular contrast agent.