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Dammarane type triterpene compound and application in preparation of medicine for treating cardiovascular diseases

A compound and solvate technology, which is applied in the field of drug preparation, can solve the problem of unknown pharmacodynamic material basis, achieve good application prospects, and improve the effects of heart failure indicators and thrombus indicators.

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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  • Dammarane type triterpene compound and application in preparation of medicine for treating cardiovascular diseases
  • Dammarane type triterpene compound and application in preparation of medicine for treating cardiovascular diseases
  • Dammarane type triterpene compound and application in preparation of medicine for treating cardiovascular diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0105] Embodiment 1, the preparation of compound 1-5 of the present invention

[0106] Take the roots of Salicoria chinensis (43.03kg), dry and 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 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), and use dichloromethane / methanol (70:1-0:1) for gradient elute. 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 with 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.

[0107] (1) Preparation...

experiment example 1

[0152] Experimental example 1, the preventive effect of the compound of the present invention on zebrafish heart failure

[0153] First, the maximum tolerated concentration (MTC) of the compounds of the present invention in two models of zebrafish heart failure and thrombus was tested, compound 1 was 0.05 μg / mL, and compounds 2, 3 and 5 were 0.5 μg / mL. Since the purity of compound 4 was less than 98%, its activity could not be evaluated. Subsequently, the preventive effect of each compound on heart failure and thrombosis in zebrafish at the concentration of its MTC was evaluated.

[0154] From Table 5 and Figure 4 , Figure 5 It can be seen that compounds 1–3 and 5 exhibited a significant preventive effect on heart failure in zebrafish at their MTC (P Figure 4 ), cardiac output (CO, Figure 5 A), zebrafish dorsal aortic blood flow velocity (BFV, Figure 5 B) and heart rate (HR, Figure 5 C) has an increasing effect. In particular, compared with the model group, compound...

experiment example 2

[0160] Experimental example 2, the preventive effect of the compound of the present invention on zebrafish thrombus formation

[0161] According to the patent of Hangzhou Huante Biotechnology Co., Ltd. (patent number: 201110126427), the intensity of red blood cell staining (RBC) in the heart is negatively correlated with the severity of thrombus formation, so RBC can be used to quantitatively evaluate the effect of the test product on ponatinib-induced thrombus preventive effect. According to the method described above in "Experimental Methods", the staining intensity of cardiac erythrocytes after treatment with each compound was counted.

[0162] The results are shown in Table 5 and Figure 6 As shown, when the concentration of compounds 1, 2, and 3 of the present invention is MTC, RBC is significantly increased, and zebrafish thrombus formation is reduced. Among them, compounds 2 and 3 (0.5 μg / mL) had the strongest effect on preventing thrombosis, which were 76% and 65% re...

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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 disclosed by the invention is novel in structure, can obviously improve the heart failure index and thrombus index of heart failure zebra fish, and has an improvement effect obviously superior to that of a positivecontrol drug. The compound 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 treating heart failure and thrombus.

Description

technical field [0001] The invention belongs to the field of medicine preparation, in particular to a dammarane-type triterpenoid compound and its application in the preparation of medicines for treating cardiovascular diseases. 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, h...

Claims

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Application Information

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IPC IPC(8): C07J71/00A61P9/04A61P9/10A61P7/02
CPCC07J71/0005A61P9/04A61P9/10A61P7/02Y02P20/55
Inventor 徐伟叶淼许文林羽
Owner FUJIAN UNIV OF TRADITIONAL CHINESE MEDICINE
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