Application of deacetylase inhibitors in preparation of medicaments for promoting insulin secretion

An acetylase inhibitor and deacetylase technology, applied in the field of medicine, can solve the problem of no literature report on the secretion relationship, and achieve the effect of obvious promoting effect and good therapeutic effect.

Inactive Publication Date: 2013-10-23
RUIJIN HOSPITAL AFFILIATED TO SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Nicotinamide (NAM) is an inhibitor of the sirtuin family, and trichostatin A (TSA) is an inhibitor of HDAC Ⅰ and Ⅱ. There is no research on the relationship between sirtuin inhibitors and insulin secretion. literature report

Method used

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  • Application of deacetylase inhibitors in preparation of medicaments for promoting insulin secretion
  • Application of deacetylase inhibitors in preparation of medicaments for promoting insulin secretion
  • Application of deacetylase inhibitors in preparation of medicaments for promoting insulin secretion

Examples

Experimental program
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Effect test

Embodiment 1

[0023] 1. Primary isolation and culture of rat islets

[0024] 1) Take SD rats and fix them under intraperitoneal anesthesia with 10% chloral hydrate;

[0025] 2) Open the abdominal cavity, find the large papilla of the duodenum, and clamp the large papilla of the duodenum with curved blood vessel forceps;

[0026] 3) Find the common bile duct, cut a small opening with ophthalmic scissors, and insert the thin hose connected with the syringe into the common bile duct towards the pancreas;

[0027] 4) Slowly push the type XI collagenase (dissolved in Hank's solution containing 1% BSA) with a concentration of 0.5mg / ml in the syringe into the pancreas until the entire pancreas is completely filled, along the cecum to the duodenal wall Separate the pancreas and place it in a 50ml centrifuge tube;

[0028] 5) After warming in a water bath at 37°C for 17 minutes, shake off the whole pancreas;

[0029] 6) Stop digestion with ice Hank's solution containing 0.25% BSA;

[0030] 7) Ce...

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Abstract

The invention relates to the technical field of medicines, especially relates to an application of deacetylase inhibitors in preparation of medicaments for promoting insulin secretion, and wherein the deacetylase inhibitor is nicotinamide (NAM) or trichostatin A (TSA). The rat islet cells are co-incubated with the deacetylase inhibitor NAM for 1 h, and insulin secretion stimulated by glucose is improved by about 50%; by using the deacetylase inhibitor TSA to treat islet cells for 12 h while the glucose concentration is 3.3 mmol/L, insulin secretion can be improved, and insulin secretion is improved obviously after 16 h; and insulin secretion is mildly up-regulated after islet cells are treated by NAM for 16 h. Therefore, the inhibitors NAM and TSA are applicable to preparation of the medicaments for promoting insulin secretion, and the medicaments will have good treatment effect in diabetes treatment. Also, more scientific bases are provided for more reasonable clinic use of the deacetylase inhibitors NAM and TSA.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to the application of sirtuin inhibitors in the preparation of drugs for promoting insulin secretion. Background technique [0002] Protein acetylation is an important means of post-translational modification. Acetyltransferases (HATs) and deacetylases (HDACs) catalyze the binding and dissolving of acetyl groups derived from acetyl-CoA and lysine residues in protein peptide chains, respectively. away from the process. It was initially found that the acetylation modification of histones and some nuclear transcription factors is involved in the regulation of gene transcription and expression. With the emergence of new proteomics methods, more and more proteins with acetylation modification have been found, involving almost all cellular functions. Regulation of biological processes. Studies have found that in addition to regulating gene transcription through histones and transcripti...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/455A61K31/165A61P5/50A61P3/10
Inventor 宁光建方方王晓周丽斌
Owner RUIJIN HOSPITAL AFFILIATED TO SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE
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