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Dipeptide derivative for improving liver function, and its application

A liver function and application technology, applied in the field of medicine, can solve the problems of lack of effective means to improve liver function, lack of improvement of survival rate, etc.

Active Publication Date: 2012-07-25
BEIJING CONTINENT PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] In addition, for patients with liver failure, there is still a lack of effective means to improve liver function and to improve survival rates

Method used

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  • Dipeptide derivative for improving liver function, and its application
  • Dipeptide derivative for improving liver function, and its application
  • Dipeptide derivative for improving liver function, and its application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0096] Give F573 after modeling

[0097] 1. Method

[0098] Wistar rats were randomly divided into 6 groups: normal control group, model group, positive drug N-acetylcysteine ​​(NAC 155mg / kg) group and F573 high dose (H 5.0mg / kg), middle dose (M 2.5 mg / kg), low-dose (L1.25mg / kg) groups, 10 rats in each group, except the blank group, each group was intraperitoneally injected (ip) with D-Gal 500mg / kg and LPS 20μg / kg for modeling. After 2 hours, each group ip corresponding NAC, F573, and the blank group was given the corresponding volume of solvent, namely:

[0099] ①Blank group: ip solvent (0.5% CMC physiological saline), ip 2ml / 200g according to body weight

[0100] ②Model group: ip D-Gal 500mg / kg and LPS 20μg / kg and ip solvent 1ml / 200g

[0101] ③NAC group: ip D-Gal 500mg / kg and LPS 20μg / kg+NAC 155mg / kg

[0102] ④F573H group: ip D-Gal 500mg / kg and LPS 20μg / kg+F573 5.0mg / kg

[0103] ⑤F573M group: ip D-Gal 500mg / kg and LPS 20μg / kg+F573 2.5mg / kg

[0104] ⑥F573L group: ip D-G...

Embodiment 2

[0162] Modeling while giving F573

[0163] 1. Method

[0164] Repeat Example 1, the difference is: 70 Wistar rats are randomly divided into 7 groups: normal control group, model group, positive drug N-acetylcysteine ​​(NAC 155mg / kg) group and F573 high dose (H : 5mg / kg), medium dose (M: 2.5mg / kg), low dose (L: 1.25mg / kg) and very low dose (LL: 0.625mg / kg) groups, 10 rats in each group, except the blank group In addition, the modeling drugs D-Gal 500 mg / kg and LPS 20 μg / kg were injected intraperitoneally (ip) in each group, and the corresponding NAC and F573 were administered in each group ip at the same time as the modeling (0 hour), and the corresponding volume of solvent was given to the blank group, namely:

[0165] ①Blank group: ip solvent (0.5% CMC physiological saline), ip 2ml / 200g according to body weight

[0166] ②Model group: ip D-Gal 500mg / kg and LPS 20μg / kg+ip solvent 1ml / 200g

[0167] ③NAC group: ip D-Gal 500mg / kg and LPS 20μg / kg+NAC 155mg / kg

[0168] ④F573H gr...

Embodiment 3

[0221] Give F573 before modeling

[0222] 1. Method

[0223] Repeat Example 1, the difference is: 4 hours before modeling, each group ip corresponding NAC, F573, and the blank group was given a corresponding volume of solvent, namely:

[0224] ①Blank group: ip solvent (0.5% CMC physiological saline), ip 2ml / 200g according to body weight

[0225] ②Model group: ip D-Gal 500mg / kg and LPS 20μg / kg+ip solvent 1ml / 200g

[0226] ③NAC group: ip D-Gal 500mg / kg and LPS 20μg / kg+NAC 155mg / kg

[0227] ④F573H group ip D-Gal 500mg / kg and LPS 20μg / kg+F573 5.0mg / kg

[0228] ⑤F573M group ip D-Gal 500mg / kg and LPS 20μg / kg+F573 2.5mg / kg

[0229] ⑥F573L group ip D-Gal 500mg / kg and LPS 20μg / kg+F573 1.25mg / kg

[0230] The experimental results showed that after the rats were treated with D-GalN / LPS, typical fulminant hepatic failure appeared, the levels of serum ALT, AST and T Bil increased sharply and significantly, and the cell apoptosis was significant, and the model was established.

[0231]...

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Abstract

The invention provides a dipeptide derivative for improving liver function, and its application, specifically an N-substituted 2(1H) dipeptide derivative and its pharmaceutically acceptable salt, and pharmaceutical composition containing the compound. The compound can effectively improve liver function, to lower alanine aminotransferase (ALT), aspartate aminotransferase (AST) and / or total bilirubin (Tbil). The compound can greatly improve survival rate of liver failure patient.

Description

technical field [0001] The present invention relates to the field of medicine, and more specifically relates to an N-substituted dipeptide derivative or a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing the compound, and an application thereof. The compound of the present invention can effectively improve liver function. The compounds of the present invention also significantly increase the survival rate of patients with liver failure. Background technique [0002] Liver failure refers to severe liver damage caused by various factors, leading to serious impairment or decompensation of the synthesis, detoxification, excretion and biotransformation of the liver itself. A group of symptoms manifested by dehydration, etc. Liver failure has a high mortality rate. [0003] In 2006, China's "Guidelines for the Diagnosis and Treatment of Liver Failure" divided liver failure into the following four categories: [0004] (a) Acute liver failure ref...

Claims

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Application Information

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IPC IPC(8): A61K38/06A61P1/16
Inventor 罗楹
Owner BEIJING CONTINENT PHARM CO LTD
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