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Sulphated heparan sulfated for inhibiting cell proliferation

A technology of heparan sulfate and sulfate esterification, which is used in medical preparations containing active ingredients, organic active ingredients, antitumor drugs, etc., can solve the difficulty of preparing high-purity HS, has not been widely used, and the effect of natural HS is not significant And other issues

Inactive Publication Date: 2013-09-11
SHENZHEN HEPALINK PHARMA GRP CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Because it is difficult to prepare high-purity HS, and the effect of natural HS is not significant when used in tumor treatment, the use of HS to treat tumors has not been widely used at present.

Method used

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  • Sulphated heparan sulfated for inhibiting cell proliferation
  • Sulphated heparan sulfated for inhibiting cell proliferation
  • Sulphated heparan sulfated for inhibiting cell proliferation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] After freeze-drying the HS prepared by the reference patent "A Method for Purifying Heparan Sulfate from Heparin By-products", take 0.5g and dissolve it in 30mL of anhydrous DMF, fully swell, add 2.5g (CH 3 ) 3 N·SO 3 , The reaction was stirred at 80°C for 3h. After cooling to room temperature, clear the supernatant, dissolve the precipitate in distilled water, dialyze, freeze-dry, and dissolve it with 10% sodium hydroxide to prepare a 100 mg / mL solution, precipitate it with ethanol with a final concentration of 80%, and dry it. Sulfated HS is produced.

Embodiment 2

[0021] The molecular weight of the sulfated HS was determined by high performance liquid gel exclusion chromatography. The mobile phase is a mixed solution of 0.1mol / L ammonium acetate and 0.02% sodium azide, the molecular weight reference substance is heparin sodium (NIBSC code 07 / 324), and the tandem chromatographic column TSK Guard column (7.8mm×30cm), TSK SW xl4000 ( 7.8mm×30cm) and TSK SW xl3000 (7.8mm×30cm), column temperature 30°C, elution flow rate 0.6ml / min, differential refraction detector, temperature 30°C. GPC software draws the standard curve of heparin sodium reference substance molecular weight and retention time as: LogM w =1.09e +001 -5.06e -001 T+1.41e -002 T 2 -1.55e -004 T 3 (R 2 =9999). GPC software calculates the molecular weight M of sulfated HS w =27521Da, the molecular weight distribution is 2196~87845Da, the components with molecular weight greater than 24000Da account for 49.55%, and the components with molecular weight less than 8000Da acc...

Embodiment 3

[0023] Take a 96-well cell culture plate and add about 5×10 3Individual hepatoma cells (HepG2), in 5% CO 2 Cultivate in the incubator at 37°C for 12 hours, add DMEM medium containing 1 mg / mL and 0.1 mg / mL sulfated HS respectively; 2 Cultivate in an incubator for 48 hours, add 10 μL MTT to each well, incubate for 4 hours, absorb the medium, add 150 μL DMSO, shake well, and detect at 490 nm on an enzyme-linked immunosorbent analyzer, the absorbance value of the sample is A 1 , the absorbance of the blank is A 2 , inhibition rate (%)= . The inhibition rates of HepG2 by sulfated HS at concentrations of 1mg / mL and 0.1mg / mL were 47.12% and 41.53%.

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Abstract

A heparan sulfated derivative is prepared from heparan sulfated by sulphating. A preparation method comprises: swelling heparan sulfated by anhydrous dimethyl formamide, adding a sulfur trioxide-trimethylamine complex, heating for esterification, dissolving, dialyzing, freeze-drying precipitation components of the reactant by distilled water, then dissolving by sodium chloride solution, precipitating by ethanol, centrifuging, removing a supernatant, drying, and then obtaining sulphated heparan sulfated. The heparan sulfated derivative can inhibit activities of tumor cells and umbilical vein endothelial cell proliferation.

Description

technical field [0001] The invention relates to a sulfated heparan sulfate (Heparan Sulfated, HS), its preparation method and its application in inhibiting cell proliferation. Background technique [0002] HS is a complex polysaccharide compound widely present on the cell surface and in the extracellular matrix (ECM). Its structure is as figure 1 [Sanaullah Khan, Elizabeth Rodriguez, Rima Patel, Jayesh Gor, Barbara Mulloy, Stephen J. Perkins. The Solution Structure of Heparan Sulfate Differs from That of Heparin. J Biol Chem. 2011, 286(28): 24842–24854], of which Glucosamine residues can be modified by N-acetylation, N- and O-sulfation, and glucuronic acid residues can be isomerized to iduronic acid (IdoA) residues. [0003] Tumor invasion and metastasis are the most dangerous stages in the process of tumor occurrence and evolution, and they are also signs of malignant development of tumors. More than 80% of clinical cancer patients die from tumor invasion and metastasis. ...

Claims

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Application Information

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IPC IPC(8): C08B37/10A61K31/727A61P35/00
Inventor 金磊张攀黄洪马小来李锂
Owner SHENZHEN HEPALINK PHARMA GRP CO LTD
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