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Phenyl isoquinoline alkaloid compound as well as preparation method and application thereof

A compound and solvate technology, applied in the field of phenylisoquinoline alkaloid compounds and their preparation, can solve the problems of unclear main pharmacological active components in the treatment of cardiovascular system diseases, and achieve the effect of good myocardial protection effect

Active Publication Date: 2022-04-01
CHENGDU UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Phytochemical studies have shown that aconite contains a large number of diterpenoid alkaloid components, and other components such as flavonoids and their glycosides, steroids, nucleosides, amides, aconite glycosides, polysaccharides, fatty acids and other types of components have also been reported, but among them The main pharmacologically active ingredients for the treatment of cardiovascular system diseases are not yet clear

Method used

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  • Phenyl isoquinoline alkaloid compound as well as preparation method and application thereof
  • Phenyl isoquinoline alkaloid compound as well as preparation method and application thereof
  • Phenyl isoquinoline alkaloid compound as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Embodiment 1, the preparation of compound of the present invention

[0053] (1) Experimental materials:

[0054] ① Medicinal materials

[0055] The decoction pieces of raw aconitum (58 kg in total) were purchased from Jiangyou Zhongba Fuzi Technology Development Co., Ltd. (batch number: 160701), and it was identified as a processed product of the root of Aconitum carmichaelii Debx. by Mr. Gao Jihai of Chengdu University of Traditional Chinese Medicine.

[0056] ②Reagents and fillers

[0057] Rudolph Autopol I high-precision polarimeter (Rudolph Corporation, USA)

[0058] Agilent cary 600FT-IR infrared spectrometer (Agilent Corporation, USA)

[0059] Applied photophysics circular dichroism spectrometer (UK Applied Photophysics Company)

[0060] Bruker AVIII HD 600 nuclear magnetic resonance instrument (Bruker, USA)

[0061] Waters Synapt G2 Tof-HDMS mass spectrometer (Waters, USA)

[0062] RE-2000A rotary evaporator (Shanghai Yarong Instrument Biochemical Factory) ...

experiment example 1

[0095] Experimental example 1, cardioprotective cell test

[0096] (1) Experimental materials:

[0097] ①Drugs

[0098] The test compound was prepared as a 50 μmol / mL stock solution in DMSO and stored at -10°C. The modeling drug (doxorubicin) was prepared with cell culture medium.

[0099] ② cells

[0100]The H9c2 cell line was purchased from Wuhan Purosai Life Technology Co., Ltd.

[0101] ③ Reagent

[0102] Doxorubicin (Chengdu Croma Biotechnology Co., Ltd., batch number 25316-40-9)

[0103] DMEM high glucose medium (Gibco, USA, batch number 1812193)

[0104] Fetal bovine serum (Sijiqing company, batch number 20150511)

[0105] Dimethyl sulfoxide (DMSO) (Chengdu Kelong Chemical Co., Ltd., batch number 2019101701) Phosphate buffer saline (PBS) (Beijing Zhongshan Jinqiao Biology, batch number 00005197-240232)

[0106] Thiazolium blue (MTT) (Germany BioFroxx company, batch number EZ6789A155)

[0107] Trypsin (YM) (Beijing Solarbio company, batch number 910O041)

[010...

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PUM

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Abstract

The invention provides a novel phenylisoquinoline alkaloid compound as shown in a formula I, or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, or a solvate thereof, or a prodrug thereof, or a metabolite thereof. The compound can be separated and extracted from radix aconiti carmichaeli or prepared according to a conventional synthesis method in the chemical field. The compound disclosed by the invention has a good myocardial protection effect and provides a new choice for clinically preparing myocardial protection medicines.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine, and in particular relates to a phenylisoquinoline alkaloid compound and a preparation method and application thereof. Background technique [0002] Myocardial injury can be induced by cardiogenic factors such as acute myocardial infarction, myocarditis, etc., or by some non-cardiac factors such as severe infection, severe renal insufficiency, etc. Myocardial injury often further causes heart failure (HF) and damages the ventricle The ability to fill or drain blood, causing insufficient perfusion of body organs and tissues. Heart failure has the characteristics of high morbidity, high mortality and inability to be completely cured, which has caused a huge medical burden and is a major public health problem. Although ACE inhibitors, beta-blockers, diuretics, and aldosterone antagonists are options for initial treatment, they still fall short of expectations and have significant side eff...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D217/24A61K31/472A61P9/00
Inventor 彭成熊亮蒙春旺刘杰林巧
Owner CHENGDU UNIV OF TRADITIONAL CHINESE MEDICINE
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