Application of rhinanthin as ACE2 activator

A technology of scrophroside and activator, which is applied in the application field of scrophroside as an ACE2 activator, can solve the problems such as the rare research on the function of harpagoside, and achieve the effects of rapid promotion, improvement of metabolic diseases, and high safety

Pending Publication Date: 2021-11-30
THE FIRST AFFILIATED HOSPITAL OF SUN YAT SEN UNIV +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The function of harpagoside in metabolic diseases is rarely studied

Method used

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  • Application of rhinanthin as ACE2 activator
  • Application of rhinanthin as ACE2 activator
  • Application of rhinanthin as ACE2 activator

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] The use of glucosinolate as a drug for activating ACE2 activator.

[0021] 1) Surface plasmon resonance (SPR) method: the purified ACE2 protein was coupled to the CM7 sensor chip, and then the Harpagoside solution was delivered to the surface of the sensor chip through a microinjection flow chuck, and Biacore T100 tracked and recorded the binding and reconciliation of Harpagoside and ACE2 process of leaving.

[0022] Experimental results such as figure 1 As shown, the experimental results prove that Harpagoside can directly combine with ACE2.

Embodiment 2

[0024] 1) After the well-growing HUVEC cells were lysed with ACE2 Lysis, the protein concentration was measured with BCA, and 20 ug of protein was incubated with Harpagoside for 30 minutes, and the substrate was added for reaction, and the fluorescence intensity was detected in kinetic mode within 5 minutes. Experimental results such as figure 2 As shown, the experimental results prove that Harpagoside can activate ACE2 enzyme activity.

Embodiment 3

[0026] The application of glucosinoside as a drug for activating ACE2 activator, the application of a drug for preventing and treating metabolic diseases, and the application of a drug for preventing and treating obesity, diabetes, cardiovascular disease, pulmonary and renal fibrosis, and atherosclerosis.

[0027] 1) HUVEC cells were treated with Harpagoside for 16 hours, collected cells were lysed with Trizol, RNA was extracted, and RT-PCR was used to detect genes of inflammation and glucose and lipid metabolism.

[0028] Experimental results such as image 3 As shown, the experimental results confirmed that Harpagoside can significantly activate the downstream glucose and lipid metabolism and inflammatory genes of the ACE2 pathway.

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Abstract

The invention relates to the technical field of medicinal chemistry, in particular to application of rhinanthin as an ACE2 activator, and the rhinanthin can effectively improve various metabolic diseases regulated by ACE2 in an RAS system, and is high in safety, small in side effect, wide in applicability and beneficial to rapid popularization.

Description

technical field [0001] The invention relates to the technical field of medicinal chemistry, in particular to the application of glucoside as an ACE2 activator. Background technique [0002] Angiotensin-converting enzyme ACE2 (Angiotensin-converting enzyme 2) is a metalloprotease encoding 805 amino acids and a type I transmembrane glycoprotein with a single extracellular catalytic domain. Widely expressed in lung, cardiovascular system, gut, kidney, central nervous system and adipose tissue. The renin-angiotensin system (RAS) plays a key role in maintaining blood pressure homeostasis and fluid and salt balance in mammals. Abnormal activation of RAS has been implicated in the pathogenesis of cardiovascular and renal diseases such as hypertension, myocardial infarction and heart failure. Studies have shown that ACE2 plays an important regulatory function in the RAS system. It can cleave AngII into Ang1-7 polypeptides, negatively regulate the activated RAS system, and has the ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7048A61P3/04A61P3/10A61P9/00A61P11/00A61P13/12A61P9/10A61P3/00
CPCA61K31/7048A61P3/04A61P3/10A61P9/00A61P11/00A61P13/12A61P9/10A61P3/00
Inventor 李梓伦陈思凡彭江云刘陈枢彭梅秀陈品黄侃
Owner THE FIRST AFFILIATED HOSPITAL OF SUN YAT SEN UNIV
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