Hydrophobic polysaccharide and its preparation method and application

A hydrophobization and polysaccharide technology, applied in the field of biomedicine, can solve the problems of high toxicity and side effects and limit clinical application, and achieve the effect of high pharmacological activity

Active Publication Date: 2022-06-24
BENGBU MEDICAL COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

They are chemically synthesized small molecule drugs, which limit their clinical application due to their high toxicity and side effects.
Cholesterol modifiers of polysaccharides are widely used as functional emulsifiers for vaccine loading, drug delivery, and delivery systems of amino acids and peptides due to their low toxicity and cell-targeting properties. However, studies on immunomodulators have rarely been reported.

Method used

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  • Hydrophobic polysaccharide and its preparation method and application
  • Hydrophobic polysaccharide and its preparation method and application
  • Hydrophobic polysaccharide and its preparation method and application

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preparation example Construction

[0065] The present invention provides a novel hydrophobized polysaccharide, a preparation method thereof, and an application in pharmaceutical preparations as an immunomodulatory substance. Such hydrophobized polysaccharides (also known as hydrophobized polysaccharide modifications) have various physiological activities, such as anti-immunity and immune-enhancing activities. It can be used as a carrier of anti-inflammatory, antibacterial, antiviral, antitumor drugs, amino acids, peptides, and various anti-inflammatory drugs, various antibacterial drugs, various antiviral drugs, various antitumor drugs, various amino acids, various It is used together with various peptides for the treatment of various immune diseases. For example, various types of inflammation, various types of fungal infections, various types of viroid infections, various types of tumor treatment, treatment of diabetes, treatment of multiple sclerosis, including the treatment of immune diseases such as myasthe...

Embodiment 1

[0104] Example 1 Hydrophobized glucan modification and preparation method thereof

[0105] For the hydrophobized polysaccharide prepared in this example, the linking arm of diacetoxysuccinamide was first synthesized, and then the hydroxyl group of cholesterol reacted with the carboxyl group at one end of the linking arm to prepare cholesterol-esterified diacetoxysuccinamide, which was then reacted with dextran to obtain Hydrophobized dextran modifications. The specific preparation method is as follows:

[0106] 1. Dissolve 100g (0.01mol) succinic acid in 2L toluene, add 0.02mol carboxyl-protected glycine, add catalyst DMAP 1g and dehydrating agent DCC 10g, react at room temperature for 48h, filter to remove by-product dicyclohexylurea, add water to the filtrate A small amount of the reaction was terminated, and 2 L of absolute ethanol was added to obtain a white precipitate, which was diacetoxysuccinamide.

[0107] 2. Remove the protection of the carboxyl group of diacetoxys...

Embodiment 2

[0110] Example 2 Hydrophobized glucan modification and preparation method thereof

[0111] The specific preparation method is as follows:

[0112] 1. Dissolve 100g (0.02mol) succinic acid in 4L toluene, add 0.04mol carboxyl-protected glycine, add catalyst DMAP 2g and dehydrating agent DCC 20g, react at 40°C for 24h, filter to remove by-product dicyclohexylurea, the filtrate A small amount of water was added to terminate the reaction, and 4 L of absolute ethanol was added to obtain a white precipitate, which was diacetoxysuccinamide.

[0113] 2. Remove the protection of the carboxyl group of diacetoxysuccinamide. The specific method is as follows: add 100 g of diacetoxysuccinamide to 1 L of 1N NaOH aqueous solution for 2 hours at room temperature, and then add 50 mL of 1N HCl aqueous solution to neutralize the remaining hydrogen Sodium oxide to free the carboxyl group of diacetoxysuccinamide. After the reaction system was distilled under reduced pressure to remove water, it wa...

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Abstract

The invention provides a hydrophobized polysaccharide and its preparation method and application. The general structural formula of the hydrophobized polysaccharide is G-P-O; wherein, G is a polysaccharide or a disaccharide, P is a connecting molecule with carboxyl groups at both ends formed by condensation of an amino acid and a diacid, and O is cholesterol; G and The P is connected to the hydroxyl group on the polysaccharide or disaccharide through an ester bond, and the P and O are connected through an ester bond. The hydrophobized polysaccharide of the present invention has the property of immunoregulation, and can play the role of immunoregulation together with the extract of Bupleurum chinensis. The raw materials used in the synthesis of the hydrophobized polysaccharide of the present invention are all safe and non-toxic, and can be used in the fields of food and medicine. Hydrophobic polysaccharides are non-toxic and can be completely decomposed in nature without toxicity. The hydrophobized polysaccharide modification of the present invention belongs to a new type of high-efficiency drug delivery carrier. The prepared medicinal liquid has high pharmacological activity and is stronger than the existing drug delivery system. A small amount of medicinal liquid plays a significant pharmacological effect. Drugs have the property of once cured without relapse.

Description

technical field [0001] The invention relates to the field of biomedicine, in particular to a hydrophobized polysaccharide and a preparation method and application thereof. Background technique [0002] At present, the representative drugs of immunomodulators are levamisole and tylorone, which mainly exert antiviral effects by inducing the body to produce interferon. They belong to chemically synthesized small-molecule drugs, and their clinical application is limited due to their large toxic and side effects. Cholesterol modifications of polysaccharides, due to their low toxicity and cell targeting, are widely used as functional emulsifiers for vaccine loading, drug delivery, and delivery systems for amino acids and peptides. However, studies as immunomodulators are rarely reported. SUMMARY OF THE INVENTION [0003] The purpose of the present invention is to provide a novel hydrophobized polysaccharide and its preparation method and application. [0004] In order to achie...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08B37/08C08B37/10C08B31/00C08B37/18C08B37/02C08B15/06C07J9/00A61K31/716A61P29/00A61P35/00A61P31/04A61P31/10A61P31/16A61P31/18A61P31/22A61P31/20A61P31/02A61K47/36A61K45/06A61K36/233A61P17/04A61P17/00A61P31/12A61P3/10A61P25/00A61P21/04A61P37/02A61K8/73A61Q19/00A61Q19/08A61Q5/12
CPCC08B37/0072C08B37/0069C08B37/0081C08B31/00C08B37/00C08B37/003C08B37/0006C08B37/0018C08B37/0051C08B15/06C07J9/00A61K31/716A61P29/00A61P35/00A61P31/04A61P31/10A61P31/16A61P31/18A61P31/22A61P31/20A61P31/02A61K47/36A61K45/06A61K36/233A61P17/04A61P17/00A61P31/12A61P3/10A61P25/00A61P21/04A61P37/02A61K8/73A61Q19/00A61Q19/08A61Q5/12A61K2300/00
Inventor 不公告发明人
Owner BENGBU MEDICAL COLLEGE
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