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Compound with effects of resisting inflammation and platelet activation and aggregation as well as preparation method and application thereof

An anti-platelet and compound technology, applied in the direction of steroids, medical preparations containing active ingredients, anti-inflammatory agents, etc., can solve the problems of limited research on the mechanism of pharmacological action, and achieve a significant anti-platelet-related inflammation effect

Inactive Publication Date: 2011-07-13
THE SECOND AFFILIATED HOSPITAL OF GUANGZHOU MEDICAL UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But so far, there are not many studies involving the above pharmacological mechanisms

Method used

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  • Compound with effects of resisting inflammation and platelet activation and aggregation as well as preparation method and application thereof
  • Compound with effects of resisting inflammation and platelet activation and aggregation as well as preparation method and application thereof
  • Compound with effects of resisting inflammation and platelet activation and aggregation as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Example 1: Extraction, separation and structural identification of compounds

[0024] 1. Instruments, reagents and fillers

[0025] Yanaco melting point analyzer (uncorrected); Shimadzu FTIR8900 infrared spectrophotometer, KBr pellets; ESI-MS was determined by Bruker Esquire 2000 mass spectrometer; NMR experiment was carried out by Bruker AVANCE-400 superconducting nuclear magnetic resonance Determination under the following method; optical rotation was determined by Jasco P-1020 polarimeter; high performance liquid chromatography: system controller: SCL-10AVP, detector: differential detector: RID-10A (SHIMADZU), diode array detector: SPD-M10A (SHIMADZU), pump: LC-10ATVP (analytical), LC-8A (preparative), column oven: CTO-10ASVP, column: analytical: Shim-pack VP-ODS (SHIMADZU), Preparation: Shim-pack PREP-ODS (SHIMADZU).

[0026] Methanol (chromatographically pure): Chinese Academy of Medical Sciences Tianjin Union Medical Technology Co., Ltd. Methanol (analytical ...

Embodiment 2

[0033] Example 2: Compounds inhibit platelet aggregation

[0034] 1. Materials and methods

[0035] Compound; ADP (Sigma);

[0036] AR-C67085MX (N6-(2-methylthioethyl)-2-(3,3,3-trifluoropropylthio)-β,γ-dichloromethyleneATP, positive control) (AstraZeneca UK), aspirin (Sigma); platelet aggregometer (Helena Packs- Type 4, USA).

[0037] 1.1. Preparation of platelet-rich plasma (PRP)

[0038] Healthy volunteers, 5 males and 5 males, with a median age of 31 years old. Antiplatelet drugs such as aspirin and dipyridamole have not been used within a week. Extract venous blood, anticoagulate with sodium citrate (1:6), centrifuge at 125g×10min to remove red blood cells, wash with platelet washing solution (138mmol / L NaCl, 2.7mmol / L KCl, 12mmol / L NaHCO 3 , 0.36mmol / LNaH2PO 4 , 5.5mmol / L glucose and 1mmol / LEDTA, pH 7.4) washed twice, and then with suspension (138mmol / L NaCl, 2.7mmol / L KCl, 12mmol / LNaHCO 3 , 0.36mmol / LNaH 2 PO 4 , 0.49mmol / L MgCl 2 , 5.5mmol / L glucose and 0.25g ...

Embodiment 3

[0048] Example 3: Anti-platelet Activation of Compounds

[0049] 1. Reagents and methods

[0050] 1.1. Reagents

[0051] Fluorescein-labeled platelet monoclonal antibodies: CD62P-FITC (fluorescein isothiocyanate) and CD61-PE (phycoerythrin) are both products of Immunotech, France, and the instrument is an EpicsXL flow cytometer produced by Beckman Coulter, USA.

[0052] 1.2. Method

[0053] Platelet-rich plasma (PRP) was prepared as described above. Operations were performed at room temperature to avoid activation of platelets.

[0054] Take 500μl platelet suspension (2.5×10 8 / ml) were inoculated in 24-well plates, and were added with different concentrations of compounds (5, 20, 80, 320 μmol / L), AR-67085MX (10 μmol / L), or PBS pre-incubated (1, 5, 10, 15, 30min ), then add ADP (20 μmol / L) to act for 5min and collect the platelets in each group of orifice plates, fix with 1% paraformaldehyde, wash and centrifuge, add 10 μl of FITC-labeled mouse anti-human CD62P antibody a...

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Abstract

The invention relates to a compound with effects of resisting inflammation and platelet activation and aggregation as well as a preparation method and application thereof. The compound has the structure of (25R)-26-oxy-beta-D-glucopyranose-5alpha-furostanol-3beta,12beta,22,26-tetraalcohol-3-oxy-beta-D-glucopyranose(1->2)[beta-D-glucopyranose(1->3)]-beta-D-glucopyranose(1->4)-beta-D-galapyranoside. The effects of the compound in the field of cardial vessels are comprehensively researched from platelet aggregation, platelet activation, platelet calcium ion variation, platelet activation signal transduction pathway and expression of platelet activation relevant inflammatory factors in the invention for the first time. Results show that the compound is a substance found to be with a strong effect on resisting platelet aggregation so far in the allium macrostemon saponin compounds, which has the stronger effect than that of aspirin with the same concentration; and the compound simultaneously has an obvious effect on resisting relevant platelet inflammations. The compound provided by the invention can be applied to medicines for treating thrombus and atherosclerosis.

Description

technical field [0001] The invention relates to a compound with anti-platelet activation, aggregation and inflammation and its preparation method and application, which is suitable for preparing medicines for treating thrombus and atherosclerosis. It belongs to the technical field of biological and chemical drugs. Background technique [0002] With the aging of society and the improvement of living standards, the incidence and mortality of cardiovascular and cerebrovascular diseases in my country are increasing day by day. The main cause of cardiovascular and cerebrovascular diseases is due to the formation of thrombus in blood vessels, and the clinical manifestations are acute myocardial infarction, cerebral thrombosis, stroke and vascular embolism. Thrombosis is not an independent clinical disease. It is the cause or complication of many diseases, such as atherosclerosis, coronary heart disease, cerebrovascular disease, deep vein thrombosis after surgery or trauma, and pu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J71/00A61K31/7048A61P7/02A61P29/00A61P9/10
Inventor 区文超刘世明陈海峰刘东萍姚新生张晓坤
Owner THE SECOND AFFILIATED HOSPITAL OF GUANGZHOU MEDICAL UNIV
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