Application of calycosin as TGFBR1 inhibitor and in preparation of medicine for treating ventricular remodeling and myocardial fibrosis

A technology of TGFBR1 and calycosin, applied in the field of medicine

Inactive Publication Date: 2021-10-26
THE SECOND AFFILIATED HOSPITAL OF GUANGZHOU MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The pharmacological mechanism of calycosin is widely involved, but there are no relevant reports on its regulation of transforming growth factor beta receptor 1 (TGFBR1) and its effect on ventricular remodeling after myocardial infarction

Method used

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  • Application of calycosin as TGFBR1 inhibitor and in preparation of medicine for treating ventricular remodeling and myocardial fibrosis
  • Application of calycosin as TGFBR1 inhibitor and in preparation of medicine for treating ventricular remodeling and myocardial fibrosis
  • Application of calycosin as TGFBR1 inhibitor and in preparation of medicine for treating ventricular remodeling and myocardial fibrosis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Example 1 Molecular Simulation Virtual Screening

[0030] Using Autodock Vina software to simulate the interaction between Calycosin and TGFBR1 to generate the optimal conformation, the simulation suggests that Calycosin and TGFBR1 have a strong binding ability.

[0031] Molecular docking diagram of the inhibitory effect of calycosin on TGFBR1 figure 1 As shown, the molecular docking results show that the binding energy of the Calycosin-TGFBR1 complex is -9.267kcal / mol, indicating a good binding force. Depend on figure 1 It can be seen that calycosin can hydrogen bond with amino acid residues GLU-45, ASP-151 and SER-80 of TGFBR1. figure 2 It can be seen from the surface visualization model that calycosin can be stably bound in the binding pocket of TGFBR1 from 0ns to 80ns; image 3 is the root mean square deviation (RMSD) of the heavy atoms of the calycosin-TGFBR1 complex during the evolution process between 0ns and 80ns, and the RMSD of the calycosin-TGFBR1 binding...

Embodiment 2

[0032] In vitro binding ability between embodiment 2 Calycosin and TGFBR1

[0033] The surface plasmon resonance imaging (SPRi) molecular interaction experiment was used for analysis, and the 3D Dextran chip was selected for spotting and immobilization. The specific operation process is as follows:

[0034] (1) Put 0.765g EDC (1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride) and 0.115g NHS (N-N-hydroxysuccinimide) in two tubes respectively 50ml special centrifuge tube, then add 10ml double distilled water to the centrifuge tube to fully dissolve and mix well, pour the two solutions into a square box when using, make the solution cover the surface of the chip to be activated, and then place it in a shaker The bed reacted for 15 minutes.

[0035] (2) For TGFBR1 protein spotting, place the chip on the spotting instrument according to the operating procedure of the biological spotting instrument and set up the program, then start the spotting operation, paste the chip ...

Embodiment 3

[0041] Example 3 Calycosin improves the heart structure and function of mice after myocardial infarction, and improves ventricular remodeling

[0042] Establishment of myocardial infarction model in mice: 8-week-old mice were selected and divided into sham operation group (Sham), model group (ligation of left anterior descending coronary artery), low-dose calycocetin group (ligation of left anterior descending coronary 25mg / kg calycosin), high dose group of calycosin (ligation of the left anterior descending coronary artery+50mg / kg calycosin), 5 rats in each group. Ligation of the left anterior descending coronary artery: fasting before the operation, and using 2% pentobarbital sodium to anesthetize the mice at a dose of 50 mg / kg intraperitoneally, and after the mice were anesthetized (the pinch reflex disappeared), the mice were The limbs and tail were fixed on the dissection table with medical adhesive tape in the supine position, the skin was prepared, and the tracheal intu...

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Abstract

The invention discloses an application of calycosin as a TGFBR1 inhibitor and in preparation of medicine for treating ventricular remodeling and myocardial fibrosis, and relates to the technical field of medicines. Based on the natural and safe characteristics of the calycosin, the calycosin provides possibility for treating diseases caused by TGF-beta pathway disorder, and particularly provides an application of the calycosin in the medicine responding to TGFBR1 related diseases.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to the application of calycocetin as a TGFBR1 inhibitor and in the preparation of drugs for treating ventricular remodeling and myocardial fibrosis. Background technique [0002] Acute myocardial infarction (AMI) refers to acute necrosis of local myocardium on the basis of coronary artery disease. Ventricular remodeling (Ventricular Remodeling) refers to the dynamic pathophysiological process of myocardial structure and function changes caused by the increase of preload and postload or myocardial injury, including the repair of the lesion and the overall compensation of the ventricle. Myocardial fibrosis after myocardial infarction refers to complex molecular signal changes and reexpression of embryonic genes and proteins in the heart after myocardial infarction, resulting in proliferation of myocardial fibroblasts and deposition of extracellular collagen. Myocardial fibrosis afte...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A23L33/105A61P9/00
CPCA61K31/352A23L33/105A61P9/00A23V2002/00A23V2200/30A23V2250/2116
Inventor 刘彬周迎春许红琳张竞之
Owner THE SECOND AFFILIATED HOSPITAL OF GUANGZHOU MEDICAL UNIV
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