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A kind of sulfated derivative of dendrobium nobile polysaccharide and its preparation method and application

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: 2021-01-05
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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  • A kind of sulfated derivative of dendrobium nobile polysaccharide and its preparation method and application
  • A kind of sulfated derivative of dendrobium nobile polysaccharide and its preparation method and application
  • A kind of sulfated derivative of dendrobium nobile polysaccharide and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

preparation Embodiment 1

[0033] Preparation Example 1 Preparation of Dendrobium chinensis polysaccharide

[0034] The dried stems of Dendrobium candidum were taken, degreased with 95% ethanol for 1 week, and dried at room temperature after degreasing. After drying, 5 kg of dried stems of Dendrobium chinensis were extracted with boiling water, and 40 L of water was added each time for 4 hours each time, and the sugar content of the extract was detected by the sulfuric acid-phenol method until the sugar reaction was not obvious. The extracts from each were combined, concentrated to a small volume, and dialyzed against running water for 2 days. The inner dialysate was concentrated to a small volume, centrifuged to remove the precipitate, and the supernatant was precipitated by adding 4 times the volume of 95% ethanol under stirring, and allowed to stand at 4°C overnight. Using the principle of siphon, the supernatant after sedimentation was sucked out, and the remaining small amount of solution and sedi...

preparation Embodiment 2

[0036] Preparation Example 2 Preparation of sulfated derivatives of Dendrobium chinensis polysaccharides (hereinafter referred to as sulfated polysaccharides)

[0037] 100 mg of Dendrobium chinensis polysaccharide was weighed and placed in a stoppered round bottom flask (25 mL) and dried in a vacuum desiccator overnight. The dried polysaccharide sample was suspended in 5 mL of anhydrous dimethylformamide (DMF), placed in an oil bath at 60 °C, and 5 mL of 200 mg of sulfur trioxide-pyridine complex (SO 3 -Py) (Item No.: 26412-87-3, Supplier: Shanghai Wokai Chemical Reagent Co., Ltd.) dissolved in dimethylformamide, the round-bottomed flask with stopper was sealed and reacted in an oil bath at 60°C After 4 hours, the pH was adjusted to neutral with dilute sodium hydroxide, dialyzed with deionized water for 72 hours, and freeze-dried to obtain the sulfated derivative of Dendrobium chinensis polysaccharide.

[0038] Product Analysis and Structural Identification

[0039] The poly...

experiment Embodiment 1

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

[0059] A cell model-human microvascular endothelial cell (HMEC-1) lumen formation assay was used to evaluate the in vitro antiangiogenic activity of sulfated polysaccharides.

[0060] Taking 0 μM as the control group, it was observed that HMEC-1 cells were treated with 0.1 μM, 0.2 μM, and 0.4 μM of the Dendrobium officinale polysaccharide ( 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 put it into the 37°C culture. 30min in the box to completely solidify the Matrigel. Then, th...

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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 chinensis polysaccharide and 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 specific drugs, good curative effect and less toxic and side effects. Anti-tumor by inhibiting angiogenesis is a new idea for tumor treatment. Therefore, it is urgent to find anti-angiogenic polysaccharide products with high activity and low side effects. SUMMARY OF THE INVENTION [0003] One object of the present invention is to find a polysaccharide drug with anti-angiogenesis effect and low toxicity and side effects. [0004] One aspect of the present invention provides a sulfated derivative of Dendrobium chinensis polysaccharide, wherein the Dendrobium chinensis polysaccharide has the following structure: [0005] [0006] The weight-average molecular weight (Mw) of the Dendrobium chinensis p...

Claims

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Application Information

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Patent Type & Authority Patents(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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