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Clerodane diterpenoid compounds and application thereof in pharmacy

A technology of crotane-type diterpenes and compounds, which is applied in the directions of organic chemistry, drug combination, and pharmaceutical formulations

Active Publication Date: 2019-08-06
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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  • Clerodane diterpenoid compounds and application thereof in pharmacy
  • Clerodane diterpenoid compounds and application thereof in pharmacy
  • Clerodane diterpenoid compounds and application thereof in pharmacy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] The preparation method and structural identification of Crone-type diterpene compound 1-6:

[0033] 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

[0053] Evaluation of the protective effect of compounds 1-6 on hydrogen peroxide-induced injury in primary neonatal rat cardiomyocytes:

[0054] 1. Experimental method

[0055] 1.1 Culture of primary cardiomyocytes in suckling mice

[0056] 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

[0073] Preparation of tablets:

[0074] 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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PUM

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Abstract

The invention discloses Clerodane diterpenoid compounds shown in 1-6 structural formulas, a pharmaceutical composition taking the Clerodane diterpenoid compounds 1-6 as effective components, a preparation method thereof and application thereof in preparing myocardial protection drugs. Pharmacological activity tests show the the compounds 1-6 can obviously increase the survival rate of myocardial cells, and at the same time, the compounds 1-6 are found to have better protective effect on H2O2-induced primary myocardial cell injury in neonatal rats, and the protective effect shows concentrationdependence. The research results show the the compounds can be developed into drugs for myocardial cell protection, and can be used for preventing and treating cardiovascular diseases such as coronaryheart disease, angina pectoris, myocardial infarction, myocarditis, arrhythmia and the like caused by myocardial ischemia and hypoxia.

Description

[0001] Technical field: [0002] 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. [0003] Background technique: [0004] 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. [0005] In recent years, the role of apoptosis in the pathogenesis of cardiovascular system diseases ...

Claims

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Application Information

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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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