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Application of 20(S)-ginsenoside Rg3 as SIRT1 protein agonist

A ginsenoside and agonist technology, applied in the field of 20-ginsenoside Rg3 as a SIRT1 protein agonist, can solve the problems of no research reports and achieve the effect of treating ischemic heart disease

Inactive Publication Date: 2015-12-23
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are no research reports on improving energy metabolism to prevent and treat cardiovascular diseases and diabetes

Method used

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  • Application of 20(S)-ginsenoside Rg3 as SIRT1 protein agonist
  • Application of 20(S)-ginsenoside Rg3 as SIRT1 protein agonist
  • Application of 20(S)-ginsenoside Rg3 as SIRT1 protein agonist

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1 Ginsenoside Rg 3 Agonistic effect on SIRT1 protein

[0028] In SIRT1, lysyl endopeptidase, NAD + And different concentrations of ginsenoside Rg 3 Add the fluorescent probe TPE-GK(Ac)YDD to the sample mixture, and make up to the same volume with the reaction buffer. After incubation for 2 hours, after the reaction, the fluorescence intensity of each well was measured with a TECAN microplate reader, the fluorescence excitation wavelength was 320nm, and the emission wavelength was 465nm. Calculation of ginsenoside Rg based on fluorescence intensity 3 Regulatory effects on SIRT1.

[0029] The result is as figure 1 Shown, ginsenoside Rg 3 It can activate SIRT1 in a concentration-dependent manner, thereby regulating energy metabolism.

Embodiment 2

[0030] Example 2 Cardiomyocyte Oxidative Damage Model

[0031] According to the literature method (KimDH, ParkCH, ParkD, et al. GinsenosideRcmodulatesAkt / FoxO1 pathways and suppresses oxidative stress [J]. Archives ofpharmacalresearch, 2014, 37(6): 813-820.), tert-butyl hydrogen peroxide was used to injure cardiomyocytes. H9c2 cells were seeded in 96-well plates, and ginsenoside Rg was added after 24 hours 3 (20mM), after pre-protection for 24 hours, add tert-butyl hydrogen peroxide to damage.

[0032] Experimental results such as figure 2 Shown, ginsenoside Rg 3 Increase the ATP content and mtDNA content of oxidatively damaged cardiomyocytes, improve the basal respiration of cardiomyocytes, reduce the reactive oxygen species in the cells, and have a protective effect on cardiomyocyte hypoxic damage.

Embodiment 3

[0033] Embodiment 3 ischemic cardiac insufficiency model

[0034]SD rats were induced to produce chronic cardiac insufficiency model by coronary artery ligation. First, the left anterior descending coronary artery (LAD) of rats was ligated to establish an acute myocardial infarction (AMI) model: SD rats were anesthetized with 5% chloral hydrate (0.6ml / 100g dose) solution, and then fixed on a mouse board. The surgical site was depilated, disinfected with iodine and alcohol, tracheal intubation was performed, and an oblique incision was made along the left side of the sternum. Fascia, and use hemostat to bluntly separate the junction of pectoralis major and serratus anterior, use hemostat to bluntly separate the 3rd and 4th intercostal space at the sternal border, open the chest cavity, cut the pericardium, and expose the heart. Under a stereomicroscope, find the coronary artery between the left atrial appendage and the conus pulmonary artery, and ligate it 2-3mm below the star...

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Abstract

The invention discloses an application of 20(S)-ginsenoside Rg3 as SIRT1 protein agonist and particularly relates to an application of 20(S)-ginsenoside Rg3 in preparing drugs for increasing myocardial energy metabolism, an application of 20(S)-ginsenoside Rg3 in preparing drugs for treating ischemic heart diseases, an application of 20(S)-ginsenoside Rg3 in preparing drugs for adjusting glycometabolism and an application of 20(S)-ginsenoside Rg3 in preparing drugs for treating 2-type diabetes. The invention further provides a drug composition with ginsenoside Rg3 as an effective ingredient. The application of 20(S)-ginsenoside Rg3 as the SIRT1 protein agonist in adjusting myocardial energy metabolism blocks and blood glucose metabolic disorders is disclosed for the first time, and therefore the aim of treating ischemic heart diseases and 2-type diabetes is achieved.

Description

technical field [0001] The present invention relates to the field of traditional Chinese medicine pharmacology, in particular to a kind of 20(S)-ginsenoside Rg 3 Use as a SIRT1 protein agonist. Background technique [0002] The disorder of energy metabolism in the body is an important cause of the occurrence and development of many diseases. Mitochondria are important organelles for energy metabolism in the body. Studies have shown that when the environment changes, the body will make metabolic responses suitable for the body. These metabolic adaptations are a kind of fine-tuning of mitochondrial function at the cellular level, and this fine-tuning is generally controlled by the regulation of PGC-1α, which will be in the body Assists mitochondrial activity when energy is needed, and also reduces mitochondrial numbers when energy requirements are low. PGC-1α mainly acts on cells, enabling cells to produce corresponding energy with changes in the environment, including enha...

Claims

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Application Information

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IPC IPC(8): A61K31/704A61P3/00A61P3/10A61P9/10
Inventor 程翼宇王毅赵筱萍樊官伟
Owner ZHEJIANG UNIV