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RyR2 stabilizer as well as preparation method, corresponding medicinal composition and application thereof

A stabilizer and composition technology, applied in the field of RyR2 stabilizer and its preparation, to achieve the effects of reducing attack rate, restoring sinus rhythm, and inhibiting myocardial cell calcium leakage

Active Publication Date: 2022-03-01
SHENZHEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Zizhi is often used as Zizhi in the folk. Studies have found that Zizhi is rich in phenolic heteroterpenoid subtypes and has a variety of pharmacological activities, such as kidney protection, anti-tumor, anti-inflammation, etc., but in the treatment of rare diseases There is no relevant report in CPVT

Method used

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  • RyR2 stabilizer as well as preparation method, corresponding medicinal composition and application thereof
  • RyR2 stabilizer as well as preparation method, corresponding medicinal composition and application thereof
  • RyR2 stabilizer as well as preparation method, corresponding medicinal composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] (-) - Extraction separation and structural identification of Fornicin A

[0037] The anti-Handerma cochlear 200kg, pulverized, 80% ethanol reflux extraction (3 × 120L, 4H, 3H, 3H), the decompression recovered ethanol, gave a dipole cream (i.e., alcohol extract) 16.8 kg, 8 kg of immersion The paste was suspended in warm water, extracted 3 times with a volume of ethyl acetate, to give a portion of the ethyl acetate 4.0 kg.

[0038] Acetate moiety (4.0 kg) linear silica gel column chromatography, petroleum ether / acetone (91: 9, 120L; 88: 12, 120L; 85: 15, 150L; 80: 20, 150L; 70: 30, 150L; 60: 40, 150L; 50 : 50, 150L; 0: 100, 100, 100L) EtOAc EtOAc (EtOAc) EtOAc. Among them, Fr.b (860.0g) row MCI Gel CHP 20P column chromatography, methanol / water (60: 40, 5L; 65: 35, 10L; 70: 30, 8L; 75: 25, 10L; 80: 20, 28L; 85: 15, 18L; 90: 10, 18L; 95: 5, 10L; 100: 0, 10L) room temperature gradient elution, TLC detection, combined with the same flow, to obtain 6 components, respectively, ...

Embodiment 2

[0045] Example 1 Compound (-) - fornicin A can be injected after the injection of synthesis, fine filtration, and irrigation sterilization in accordance with regular method.

Embodiment 3

[0053] Example 1 Compound (-) - fornicin A can be made into a tablet in various pharmaceutical excipients according to conventional law.

[0054] The compound (-)-fornicin a as the drug active ingredient is used as the drug active ingredient, and several excipients are used as the excipient ingredient of the combined pharmaceutical tablet, and each piece contains 1-100 mg of the pharmaceutical ingredient 1-100 mg according to a certain ratio ratio. Samples.

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PUM

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Abstract

The invention provides an RyR2 stabilizer, a preparation method of the RyR2 stabilizer, a corresponding pharmaceutical composition and application of the RyR2 stabilizer, and relates to the technical field of chemical drugs, and the RyR2 stabilizer is FornicinA or a pharmaceutical salt thereof. The Fornicin A can be used as a RyR2 stabilizer, and can inhibit calcium leakage of myocardial cells by interacting with a raney base receptor 2 (RyR2), so that the Fornicin A can be used for treating a rare disease CPVT. Particularly, (-)-Fornicin A has an inhibition effect on calcium spark release of primary cardiac muscle cells of RyR2-R2474S transgenic mice, and has a dose-dependent relationship; the calcium release abnormal events after pace-making of the primary myocardial cells of the RyR2-R2474S transgenic mouse can be reduced; the electrocardiogram of the WT mouse is not influenced; the preventive administration can significantly reduce the attack rate of ventricular tachycardia; the sinus rhythm can be recovered within 30 minutes through therapeutic administration.

Description

Technical field [0001] The present invention relates to the field of chemical medicines, in particular, refer to an RYR2 stabilizer and a preparation method thereof, a corresponding pharmaceutical composition and application. Background technique [0002] Ryr2 is a receptor of Ryanodine, a calcium ion release passage present on the myocardial cell (CMS) Suspentry Network (SR), which plays an important role in control myocardial excitation - shrinkage coupling. The occurrence of catecholamine sensitive polymorphic ventricular vented (CPVT) is related to Ryr2 gene mutation, and the study that RYR2 gene mutation causes a diastolic CA through the RYR2 channel during catecholamine release. 2+ Release unusual enhancement, abnormal enhanced muscle net CA 2+ Leakage is in turn drives NA + / CA 2+ The activity of the exchanger is generated to generate a demetivation NA + Current (I Na ), Touch the power potential abnormality, early stage (EAD) or delarged delay (DAD) after depolarization,...

Claims

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Application Information

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IPC IPC(8): C07D307/58A61K31/341A61P9/00A23L33/105
CPCC07D307/58A61P9/00A23L33/105C07B2200/07A23V2002/00A23V2200/326Y02A50/30
Inventor 程永现刘杰秦付营万江帆
Owner SHENZHEN UNIV
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