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Sulfation derivative of dendrobium stem polysaccharide and preparation method and application of sulfation derivative

A Dendrobium nobile, sulfation technology, applied in the direction of medical preparations containing active ingredients, drug combinations, pharmaceutical formulas, etc., can solve the problems of lack of specificity, small toxic and side effects, etc., and achieve a significant anti-angiogenesis effect

Active Publication Date: 2019-01-04
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Tumor is one of the main diseases that cause human death, and there is still a lack of therapeutic drugs with strong specificity, good curative effect, and small side effects

Method used

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  • Sulfation derivative of dendrobium stem polysaccharide and preparation method and application of sulfation derivative
  • Sulfation derivative of dendrobium stem polysaccharide and preparation method and application of sulfation derivative
  • Sulfation derivative of dendrobium stem polysaccharide and preparation method and application of sulfation derivative

Examples

Experimental program
Comparison scheme
Effect test

preparation Embodiment 1

[0033] Preparation Example 1 Preparation of Dendrobium nobile polysaccharide

[0034] Take the dried stems of Dendrobium nobile, degrease with 95% ethanol for 1 week, and dry naturally at room temperature after degreasing. After drying, 5 kg of dried stems of Dendrobium nobile were extracted with boiling water, adding 40 L of water each time for 4 hours, and the sugar content of the extract was detected by the sulfuric acid-phenol method until the sugar reaction was not obvious. Each extract was combined, concentrated to a small volume, and dialyzed against running water for 2 days. The dialyzed inner solution was concentrated to a small volume, centrifuged to remove the precipitate, and the supernatant was added with 4 times the volume of 95% ethanol to settle under stirring, and stood at 4°C overnight. Use the principle of siphon to suck out the settled supernatant, centrifuge the remaining small amount of solution and the mixed solution of the precipitate, wash the precipi...

preparation Embodiment 2

[0036] The preparation of the sulfated derivative (hereinafter referred to as sulfated polysaccharide) of preparation example 2 Dendrobium nobile polysaccharide

[0037] Weigh 100 mg of Dendrobium nobile polysaccharide and place it in a stoppered round bottom flask (25 mL) and dry overnight in a vacuum desiccator. Suspend the dried polysaccharide sample in 5 mL of anhydrous dimethylformamide (DMF), place it in an oil bath at 60 °C, and add 5 mL of 200 mg sulfur trioxide-pyridine complex (SO 3 -Py) (article number: 26412-87-3, supplier: Shanghai Wokai Chemical Reagent Co., Ltd.) solution dissolved in dimethylformamide, the round bottom flask with a stopper was sealed and reacted in an oil bath at 60°C After 4 hours, adjust the pH to neutral with dilute sodium hydroxide, dialyze with deionized water for 72 hours, and freeze-dry to obtain the sulfated derivative of Dendrobium nobile polysaccharide.

[0038] Product analysis and structure identification

[0039] The Dendrobium n...

experiment Embodiment 1

[0058] Experimental example 1 Dendrobium nobile polysaccharide and sulfated polysaccharide inhibit the formation of human microvascular endothelial cell lumen in vitro

[0059] The cell model-human microvascular endothelial cells (HMEC-1) tube formation assay was used to evaluate the anti-angiogenic activity of sulfated polysaccharides in vitro.

[0060] With 0 μM as a control group, observe that HMEC-1 cells are respectively subjected to 0.1 μM, 0.2 μM, and 0.4 μM of the Dendrobium nobile polysaccharide of Preparation Example 1 ( Figure 3A ) and the sulfated polysaccharide of Preparation Example 2 ( Figure 3B ) changes in the cell lumen after culture, the specific experimental operations are as follows:

[0061] Put the 96-well plate in the -20°C refrigerator in advance, and then thaw the Matrigel at 4°C. After the Matrigel is completely thawed, add 50 μL per well to the pre-cooled 96-well plate, and culture at 37°C. 30min in the oven to completely solidify the Matrigel. ...

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Abstract

The invention relates to a sulfation derivative of dendrobium stem polysaccharide and a preparation method and application of the sulfation derivative. Dendrobium stem polysaccharide is shown as the following structural formula. In-vitro and in-vivo experimental studies indicate that the sulfation derivative of dendrobium stem polysaccharide has the anti-angiogenic drug activity.

Description

technical field [0001] The invention relates to a sulfated derivative of dendrobium nobile polysaccharide, a preparation method and application thereof. Background technique [0002] Tumor is one of the main diseases that cause human death, and there is still a lack of therapeutic drugs with strong specificity, good curative effect and little side effects. Anti-tumor by inhibiting angiogenesis is a new idea for the treatment of tumors. Therefore, it is imminent to find anti-angiogenic polysaccharide products with high activity and low side effects. Contents of the invention [0003] One object of the present invention is to find a polysaccharide drug with anti-angiogenic effect and low toxic and side effects. [0004] One aspect of the present invention provides a sulfated derivative of Dendrobium nobile polysaccharide, wherein the polysaccharide of Dendrobium nobile has the following structure: [0005] [0006] The weight average molecular weight (Mw) scope of desc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08B37/02A61K31/737A61P35/00
CPCA61K31/737C08B37/006
Inventor 丁侃靳灿王铮
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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