1.Synthesis and animal imaging of 99mTc-hydrazinonicotinamide-folate as a new folate receptor-targeted tumor imaging agent.
Li-qin LIU ; Shi-zhen WANG ; Fang LI ; Bao TENG ; Ke-zhan WANG ; Fei-chan QIU
Acta Academiae Medicinae Sinicae 2006;28(6):786-789
OBJECTIVEThe synthesis, biodistribution, and animal imaging of 99mTc- hydrazinonicotinamide-folate (99mTc-HYNIC-Folate) were studied as a folate receptor-targeted tumor imaging agent.
METHODSHYNIC-Folate was synthesized by a muti-step reaction and radiolabeled with 99mTc using tricine and trisodium phenylphosphine-3, 3', 3"-trisulfonate (TPPTS) as coligands. The radiochemical purity and stability of 99mTc HYNIC-Folate was measured. The biodistributions of 99mTc-HYNIC-Folate in normal mice and tumor-bearing mice were detected. Whole-body gamma imaging was performed using an athymic mouse tumor xenograft model.
RESULTSThe ligand HYNIC-Folate was successfully synthesized and characterized by hydrogen nuclear magnetic resonance (1HNMR) and mass spectrometry (MS). The radiochemical purity of 99mTc-HYNIC-Folate was 96% under optimal conditions. Data from gamma scintigraphy and the biodistribution in tumor-bearing mice showed that 99mTc-HYNIC-Folate predominantly accumulated in tumor, its uptake rate per gram tissue alpham was 5. 620+/- 0. 753. The uptakes of 99mTc-HYNIC-Folate in the other non-target tissues were very low, except it was high in the kidneys ( am was 41. 959 +/-6. 759) .
CONCLUSION99mTc-HYNIC-Folate has the potential to be used as a noninvasive radiodiagnostic imaging agent for the detection of folate receptor-positive human cancers.
Animals ; Female ; Mice ; Mice, Inbred BALB C ; Mice, Inbred ICR ; Neoplasms, Experimental ; diagnostic imaging ; Organotechnetium Compounds ; chemical synthesis ; pharmacokinetics ; Radionuclide Imaging ; Radiopharmaceuticals ; chemical synthesis ; pharmacokinetics ; Tissue Distribution
2.Recombinant human pigment epithelium-derived factor inhibits the proliferation of the endothelial cells from blood vessels.
Bin YIN ; Fei-chan QIU ; Zhong-wei WEN ; Sheng-tao ZHU ; Jian-gang YUAN ; Bo-qin QIANG ; Xiao-zhong PENG
Acta Academiae Medicinae Sinicae 2005;27(3):295-299
OBJECTIVETo express and purify the recombinant human pigment epithelium-derived factor (PEDF) which inhibits the proliferation of the endothelium cells from blood vessel in E.coli.
METHODSPEDF gene was inserted into the prokaryotic expression vector pGEX-4T-2. The recombinant protein PEDF was expressed in E.coli BL-21, and purified by the GST Sepharose 4B affinity column. The recombinant human PEDF protein was identified by Western blot and mass spectrum. The biological activity of the recombinant human PEDF protein was measured by using MTT.
RESULTSThe 46 kDa recombinant human PEDF protein was obtained. It significantly inhibited the proliferation of the human umbilical vein cell line HUVEC.
CONCLUSIONThe recombinant human PEDF with anti-angiogenesis activity protein may be successfully purify through prokaryotic expression.
Angiogenesis Inhibitors ; pharmacology ; Apoptosis ; drug effects ; Base Sequence ; Cell Division ; drug effects ; Cells, Cultured ; Cloning, Molecular ; Endothelium, Vascular ; cytology ; Eye Proteins ; pharmacology ; Humans ; Molecular Sequence Data ; Nerve Growth Factors ; pharmacology ; Prokaryotic Cells ; metabolism ; Recombinant Proteins ; pharmacology ; Serpins ; pharmacology ; Umbilical Veins ; cytology
3.Bioluminescent imaging monitoring of a anti-angiogenesis therapeutic gene vasostatin in tumor cell PC3.
Jie-miao HU ; Fei-chan QIU ; Bin YIN ; Yan-hua GONG ; Jian-gang YUAN ; Bo-qin QIANG ; Shi-zhen WANG ; Xiao-zhong PENG
Acta Academiae Medicinae Sinicae 2007;29(3):312-317
OBJECTIVETo generate a sensitive tool for noninvasive monitoring of a therapeutic gene vasostatin.
METHODSWe fused the bioluminescent reporter gene firefly luciferase to the therapeutic transgene vasostatin and ensured that these two proteins would not interrupt each other and kept their own natural character.
RESULTSWe therefore examined clones of PC3 cells stably expressing fusion gene and positive controlfluc with bioluminescence. In vivo imaging of PC3-Fluc subcutaneous tumors showed that the mean tumor bioluminescence increased in animals over several weeks.
CONCLUSIONNoninvasive monitoring facilitates the detection of gene expression in vivo and in vitro.
Animals ; Calreticulin ; genetics ; metabolism ; Cell Line, Tumor ; Gene Transfer Techniques ; Genes, Reporter ; Humans ; Luciferases, Firefly ; genetics ; metabolism ; Luminescent Measurements ; Neoplasm Transplantation ; Peptide Fragments ; genetics ; metabolism ; Recombinant Fusion Proteins ; genetics ; metabolism