Research On Nuclide Labeling And Liver Targeting Of Angelica Sinensis Polysaccharide

Angelica sinensis of dried roots of angelica in umbrelliferae plant, is a famous traditional Chinese medicine in our country, known as the "party of nine to ten". The main active ingredient of Angelica polysaccharide, protect liver, spleen, blood and invigorate the circulation of pharmacological effects. Modern pharmacology study showed that Angelica Sinensis Polysaccharides?ASP? especially regulated glucolipid metabolism to various diseases, diseases of the cardiovascular system, anti- inflammatory, anti-tumor, lung function, immunity. In this study, the Angelica Sinensis Polysaccharide was obta ine d by water extraction, ac id-base deprote inization and alcohol-sinking, then isola ted a nd purifie d through dialysis and Se phade x G50, named ASP. In our research, radioactive-compound was given from chelating radionuclide technetium after modification ASP with small molecule, on this basis, to study the liver targeting effect, combining with galactose human serum albumin?NGA? competitive antagonist. Part? The preparation, purification, identification and stability study of radio-ASPASP was obtained by water extraction, acid-base deproteinization and alcohol-sinking, then isolated and purified through dialysis and Sephadex G50.Using ASP as material, reaction with diethylenetriaminepentaacetic dianhydride?DTPAA? and dialyzed against distilled water to give DTPA-ASP as intermediates. Take fresh Na99 mTc O4 eluent to radiolabel DTPA-ASP with trace Sn C l2, and ITLC chromatography technology were used to test rate of ^99mTc-DTPA-ASP, the PD-10 desalination column for purification, drawing outflow curve and testing the sugar content, and evaluated its stability of 1, 2, 4, 8 and 24 h in the PBS and serum. Part ? The ^99mTc-DTPA-ASP imaging in normal animal and research of its hepatic targeting effectsThe ^99mTc-DTPA-ASP subjected to single-photon emission-computed tomography?SPECT? imaging in normal BALB/c mice, SD rats and white rabbit. The normal BALB/c mice were injected with ^99mTc-DTPA-ASP via tail vein to assess the %ID/g of organization, including blood, brain, heart, lung, liver, spleen, stomach, small intestine, colo n, kidney, muscle and bone. To study the hepatic targeting of ASP, BALB/c mice were preinjected free NGA as inhibitor via tail vein, observation SPECT of antagonism group and biodistribution. The SPECT imaging, biodistribution and NGA competitive antagonism experiments showed that ASP had liver targeting mediated by NGA. Part ? The uptake studies of ^99mTc-DTPA-ASP in cancer cells and SPECT imaging in tumor-burdened nude miceIn order to study the biodistribution of ASP in tumor-burdened nude mice, this experiment had carried on the uptake and imaging e xperiments in vivo and vitro.The uptake of ^99mTc-DTPA-ASP in Hep G2 and PC3 with different time were given, and two tumor-burdened nude mice model were set up, to study the transplanted tumor model on the influence of ASP by SPECT imaging. According to the results, the uptake of ^99mTc-DTPA-ASP in Hep G2 and PC3 were not significant different, and tumor-burdened model did not affect the liver target of ASP.