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Application of oligoguluronates in preparation of drugs for prevention and treatment of liver damage and various hepatitis, liver fibrosis or cirrhosis

A technology of guluronic acid salt and polyguluronic acid, applied in the field of marine medicine, can solve the problems that have not yet been seen, and achieve the effects of broad development and application prospects, abundant resources, and easy industrialization

Active Publication Date: 2014-08-13
MARINE BIOMEDICAL RES INST OF QINGDAO CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, domestic and foreign literatures have reported that oligo-guluronic acid has various biological activities such as anti-oxidation, immune regulation, and regulation of mucosal protein function, but there is no report on its application in alcoholic liver injury, but it has not yet been reported. See reports on its application in chemical and immune liver injury and hepatitis

Method used

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  • Application of oligoguluronates in preparation of drugs for prevention and treatment of liver damage and various hepatitis, liver fibrosis or cirrhosis
  • Application of oligoguluronates in preparation of drugs for prevention and treatment of liver damage and various hepatitis, liver fibrosis or cirrhosis
  • Application of oligoguluronates in preparation of drugs for prevention and treatment of liver damage and various hepatitis, liver fibrosis or cirrhosis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Embodiment 1: Preparation of oligomeric guluronic acid salt (LPG)

[0024] Prepare alginate (sodium alginate in this example) into a 10wt% aqueous solution, heat it to 80-90°C with 1wt% dilute hydrochloric acid, stir and degrade it for 4-5 hours, neutralize it with 10wt% sodium carbonate aqueous solution after cooling, and then Adjust the pH to about 3.65 with 5wt% dilute hydrochloric acid, centrifuge and collect the precipitate, dissolve it with 2mol / L NaOH, add 3 times the volume of 95wt% ethanol and collect the precipitate, dry after dehydration with absolute ethanol to obtain polyguluronic acid sodium salt ( Mw = 11.2kD). The polyguluronic acid sodium salt was formulated with pure water into 10 wt% aqueous solutions of different concentrations, and degraded by the Fenton method to obtain oligomeric guluronic acids with different molecular weights. After the oligomeric guluronic acid is neutralized by lithium hydroxide, sodium hydroxide, potassium hydroxide, calcium...

Embodiment 2

[0029] Example 2: Oligomeric Guluronate (LPG) vs. CCl 4 Inhibitory effect of induced increase in mouse liver body mass index

[0030] The present embodiment adopts the oligomeric guluronic acid sodium salt obtained in Example 1. Sixty Kunming mice of 18-22 g were randomly divided into normal (control) group, model group, positive drug (bifendate) group and LPG administration group, 15 in each group. Adaptive feeding for 3 to 5 days. During the experiment period, the mice were free to eat common feed and drinking water. One dose of 100 mg / kg was given once, and 0.35 wt% CCl was given once 1 hour later. 4 10ml / kg, fasting without water. After 16 hours, the mice were sacrificed, the liver was separated, rinsed twice with pre-cooled PBS (0.1M, pH=7) solution, and then the water on the surface of the organ was blotted dry with filter paper, weighed, and the organ index was calculated. The calculation formula is as follows: organ index (%)=organ weight (g) / body weight (g)*100%, a...

Embodiment 3

[0035] Example 3: Oligomeric Guluronate vs. CCl 4 Inhibition of induced increase in serum ALT and AST levels in mice

[0036] The present embodiment adopts the oligomeric guluronic acid sodium salt obtained in Example 1. Sixty Kunming mice of 18-22 g were randomly divided into normal (control) group, model group, positive drug (bifendate) group and LPG administration group, 15 in each group. Adaptive feeding was carried out for 3 to 5 days. During the experiment period, the mice were free to eat common feed and water, 100 mg / kg was given once, and 0.35 wt% CCl4 10 ml / kg was given once 1 hour later, and water was not allowed. After 16 hours, the mice were killed, blood was collected from the eyeballs, serum was prepared at 3000 rpm×10 min, and ALT and AST indexes were measured. The experimental results are shown in Table 2.

[0037] Table 2 Oligomeric Guluronate LPG vs. CCl 4 Inhibitory effect of ALT, AST level increase

[0038] group Dose (mg / kg) ALT(U / L) AS...

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Abstract

The invention belongs to the field of marine drugs, and in particular relates to an application of oligoguluronates in preparation of drugs for prevention and treatment of liver damage and various hepatitis, liver fibrosis or cirrhosis. The oligoguluronates are used in preparation of the drugs for protection of livers and treatment of various hepatitis, liver fibrosis or cirrhosis; the oligoguluronates adopt algin as a raw material, and oligoguluronic acids with different molecular weights are obtained through a chemical degradation method or a physical degradation or a combination of the two degradation methods; the oligoguluronic acids are neutralized to prepare lithium salts, sodium salts, potassium salts, calcium salts or magnesium salts of the oligoguluronic acids with different molecular weights, wherein a molecular skeleton is a linear oligosaccharide compound formed by connecting L-guluronic acid (G) through alpha-(1,4)-glycosidic bonds. The products are derived from the marine natural product, have many advantages of abundant resources, easy industrialization, safety, effectivity and the like, and have broad development and application prospects in prevention and treatment of liver damage and various hepatitis, liver fibrosis or cirrhosis.

Description

technical field [0001] The invention belongs to the field of marine medicines, and in particular relates to the application of an oligomeric guluronic acid salt in the preparation of medicines for preventing and treating liver damage and various hepatitis, liver fibrosis or liver cirrhosis. Background technique [0002] As one of the largest and most functional substantive glandular organs in the human body, the liver is known as "the largest chemical factory in the human body". The liver participates in digestion, metabolism, excretion, detoxification and immunity in the body. The high incidence of development, environmental pollution, and food and drug safety incidents has led to an increasing trend in the incidence of diseases that cause liver function damage year by year. Studies have shown that liver lesions are diverse and refractory. At present, the treatment methods for liver diseases mainly include etiological treatment, diet therapy and drug therapy, and there is ...

Claims

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Application Information

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IPC IPC(8): A61K31/734A61K31/702A23L1/09A61P1/16A61P31/12
Inventor 管华诗郝杰杰于广利胡婷敦云楼周晓琳夏萱
Owner MARINE BIOMEDICAL RES INST OF QINGDAO CO LTD
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