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Triterpene compound, preparation method and application thereof

A compound and solvate technology, applied in the field of drug preparation, can solve problems such as unknown pharmacodynamic material basis, and achieve the effects of improving heart failure indicators and good application prospects

Active Publication Date: 2021-01-08
FUJIAN UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] However, the pharmacodynamic material basis of the root of Saltwort root in the treatment of coronary heart disease is still unclear.

Method used

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  • Triterpene compound, preparation method and application thereof
  • Triterpene compound, preparation method and application thereof
  • Triterpene compound, preparation method and application thereof

Examples

Experimental program
Comparison scheme
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Embodiment 1

[0060] Embodiment 1, the preparation of compound of the present invention

[0061] Take the roots of Salakia (43.03kg), dry, pulverize, extract with 95% methanol at 70°C for 4 times under reflux, each time for 6 hours, and concentrate under reduced pressure to obtain the total methanol extract (6.61kg). Suspend the methanol extract in water, extract with petroleum ether, select the extract from petroleum ether, use a silica gel column (100-200 mesh, 120cm*15cm), use dichloromethane / methanol (volume ratio 70:1-0:1) Perform gradient elution. According to the results of the TLC development system, comprehensive analysis and judgment were carried out, and the collected fluids were combined to finally obtain 13 subcomponents (Fr.1–13). Based on our TLC combined HPLC-DAD / ELSD / MS compound detection method and LC-MS chemical profile analysis of each subcomponent, the target components to be separated were determined according to the measurement results.

[0062] Fr.7 (137.52g, elute...

experiment example 1

[0087] Experimental example 1, the preventive effect of the compound of the present invention on zebrafish heart failure

[0088] First, the maximum tolerated concentration (MTC) of compound 6 of the present invention in the zebrafish heart failure model was tested, which was 0.5 μg / mL. Subsequently, the preventive effect of the compound on the development of heart failure in zebrafish at the concentration of its MTC was evaluated.

[0089] According to Table 4, it can be seen that the compounds exhibited significant preventive effects on zebrafish heart failure at their MTC (P image 3 with Figure 4 It can be seen that the compound of the present invention has an improvement effect on heart enlargement and venous sinus blood stasis area, and has an effect on cardiac output (CO, Figure 4 A), zebrafish dorsal aortic blood flow velocity (BFV, Figure 4 B) and heart rate (HR, Figure 4 C) There is an increasing effect; moreover, compared with the model group, the compound of ...

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Abstract

The present invention provides a compound represented by a formula I, or a pharmaceutically acceptable salt, or an optical isomer, or a stereoisomer, or a solvate thereof. The compound is novel in structure, and can significantly improve the heart failure index of heart failure zebra fish, wherein the improvement effect of the compound is obviously superior to that of a positive control drug. Thecompound provided by the invention can be used as a lead compound for improving structural heart disease and preload and postload of heart, and has a very good application prospect in preparation of drugs for preventing and / or treating heart failure.

Description

technical field [0001] The invention belongs to the field of medicine preparation, and in particular relates to a triterpenoid compound and its preparation method and application. Background technique [0002] In the past 17 years, coronary heart disease is one of the most common cardiovascular diseases, which seriously threatens human health. There are various limitations in the current therapeutic drugs for coronary heart disease, and the research and development of coronary heart disease drugs is in the ascendant. Natural products have attracted much attention in the search for new drugs. According to "Kaibao Materia Medica", the traditional Chinese medicine Rhus chinensis Mill., the white bark of the tree can break blood and stop bleeding, and the rhizome can promote blood circulation and remove blood stasis. Shuguantong Syrup (Z35020635), a Fujian-produced single-taste preparation with the original medicinal material, has proven clinical efficacy in the treatment of c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J21/00A61P9/04A61P9/10
CPCC07J21/00A61P9/04A61P9/10Y02A50/30
Inventor 徐伟叶淼许文林羽
Owner FUJIAN UNIV OF TRADITIONAL CHINESE MEDICINE