A class of Crotane-type diterpene compounds and their application in pharmacy

A technology of crotane-type diterpenes and compounds, which is applied in the fields of drug combination, organic chemistry, pharmaceutical formulation, etc.

Active Publication Date: 2021-09-21
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Compounds 1-6 are Crotane-type diterpene compounds, and Compounds 1-4 are new compounds. So far, there have been no reports of any Crotane-type diterpene compounds having cardiomyocyte protective activity

Method used

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  • A class of Crotane-type diterpene compounds and their application in pharmacy
  • A class of Crotane-type diterpene compounds and their application in pharmacy
  • A class of Crotane-type diterpene compounds and their application in pharmacy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] The preparation method and structural identification of Crone-type diterpene compound 1-6:

[0028] Preparation method: Take the aboveground part of Salvia hispanica, dry it and crush it, soak it in acetone for three times and extract it three times, combine the three extracts, concentrate under reduced pressure to obtain the total extract, which is subjected to silica gel column chromatography , the elution system is petroleum ether / acetone, detected by TLC, combined according to the main spots, and 5 components Fr.1-Fr.5 are obtained, and then Fr.3 is mixed with polyamide, dried and packed into a column. Select MCI reverse-phase chromatography column, connect to medium-pressure liquid chromatograph, select ethanol / water gradient elution, after vacuum distillation and concentration, each fraction is detected by TLC and merged according to the main spots to obtain 8 groups of Fr .3.1-Fr.3.8, Fr.3.1 was subjected to silica gel column chromatography, and the elution syste...

Embodiment 2

[0048] Evaluation of the protective effect of compounds 1-6 on hydrogen peroxide-induced injury in primary neonatal rat cardiomyocytes:

[0049] 1. Experimental method

[0050] 1.1 Culture of primary cardiomyocytes in suckling mice

[0051] Select newborn SD suckling mice 1-3 days old, disinfect the skin with 75% alcohol, decapitate, open the chest and take out the heart. Drain the blood from the heart and cut off excess tissue, cut it into 1-2mm 3 sized tissue pieces and transferred to a 15 mL centrifuge tube. Discard the DMEM high-glucose medium, add digestion solution, and repeatedly blow and digest with a dropper until the tissue pieces are completely digested. The culture solution in each centrifuge tube was filtered through a 200-mesh filter, repackaged, and centrifuged at 1000r / min for 5min. Discard the supernatant, add new cell culture medium, pipette repeatedly with a dropper to disperse into single cells, and dilute with 1×10 5 cells / mL were inoculated into a 96...

Embodiment 3

[0068] Preparation of tablets:

[0069] According to Example 1, various compounds of the present invention were firstly prepared, and the excipients were added in a weight ratio of 1:5-1:10, granulated and pressed into tablets according to their own independence or arbitrary mixing.

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Abstract

The invention discloses a Crotane-type diterpene compound 1-6 represented by a structural formula, a pharmaceutical composition using it as an active ingredient, a preparation method thereof, and an application thereof in preparing a cardioprotective drug. Pharmacological activity test shows: compound 1-6 of the present invention can significantly increase cardiomyocyte survival rate, finds compound 1-6 simultaneously to H 2 o 2 Inducing primary cardiomyocyte injury in suckling rats has a better protective effect in a concentration-dependent manner. The results of this study indicate that the compounds can be developed into cardiomyocyte-protecting drugs for the prevention and treatment of cardiovascular diseases such as coronary heart disease, angina pectoris, myocardial infarction, myocarditis, and arrhythmia caused by myocardial ischemia and hypoxia.

Description

Technical field: [0001] The invention belongs to the technical field of medicines, and in particular relates to a class of clodanone-type diterpene compounds 1-6 which have the effect of protecting cardiomyocytes, a pharmaceutical composition using it as an active ingredient, a preparation method thereof, and a method for preparing cardioprotective medicines. in the application. Background technique: [0002] Myocardial ischemia is the most common clinical cause of myocardial injury, mostly due to coronary insufficiency or increased myocardial oxygen consumption. In developed or developing countries, heart disease (ischemic heart disease, IHD) caused by myocardial cell ischemia and hypoxia is an important fatal and disabling disease. It is widespread and harmful, and seriously threatens human beings. Health affects human life expectancy and quality of life. [0003] In recent years, the role of apoptosis in the pathogenesis of cardiovascular system diseases (such as heart ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D493/10C07D493/20C07D307/94A61K31/366A61K31/365A61P9/10A61P9/06A61P9/00
CPCA61P9/00A61P9/06A61P9/10C07D307/94C07D493/10C07D493/20
Inventor 赵勤实范敏吴兴德彭丽艳
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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