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Use of 5,6,7,4'-tetra-acetoxyl flavone for preparing medicine for preventing and curing cardiovascular and cerebrovascular diseases

A technology for tetraacetoxyflavonoids and cardiovascular and cerebrovascular diseases, which is applied in the field of medicine and can solve the problems of poor stability and easy oxidation and deterioration of phenolic hydroxyl groups.

Inactive Publication Date: 2012-07-04
KPC PHARM INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The present invention aims at the disadvantages of 5,6,7,4'-tetrahydroxyflavone, which is an existing drug for treating and preventing cardiovascular and cerebrovascular diseases, that the phenolic hydroxyl group is easily oxidized and deteriorated, and has poor stability, and provides a structurally stable 5,6,7, Use of 4'-tetrahydroxyflavone derivative 5,6,7,4'-tetraacetoxyflavone in the preparation of primers for the prevention and treatment of cardiovascular and cerebrovascular diseases, 5,6,7,4'-tetraacetoxyflavone The structure is as follows:

Method used

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  • Use of 5,6,7,4'-tetra-acetoxyl flavone for preparing medicine for preventing and curing cardiovascular and cerebrovascular diseases
  • Use of 5,6,7,4'-tetra-acetoxyl flavone for preparing medicine for preventing and curing cardiovascular and cerebrovascular diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Example 1: Synthesis of 5,6,7,4'-tetraacetoxyflavone

[0016] Put 10.0g of 5,6,7,4'-tetrahydroxyflavone and 75ml of acetic anhydride in a 300ml Erlenmeyer flask, add 1 drop of concentrated hydrochloric acid (about 0.1ml), stir magnetically at room temperature for 1 hour, and detect the raw material point by TLC Disappeared, filtered and washed to neutral, and the filtrate was dried to obtain 5,6,7,4'-tetraacetoxyflavone. The yield is 92%, and the purity is 98% as detected by HPLC.

[0017] UV max (MeOH)(Abs.): 252(0.395), 278(0.585), 388(0.156)nm.IR KBr max : 3441, 1778, 11651, 1456, 1372, 1216, 1199, 1080, 1016, 840cm -1 .FAB-MS: m / z 455[M+H] + , 413 [M+H-COCH 2 ] + , 370[M+H-COCH 2 -COCH 2 ] + , 328 [M+H-COCH 2 -COCH 2 -COCH 2 ] + , calcd for C 23 h 19 o 10 , 455.0978. Molecular formula is C 23 h 18 o 10 , with a molecular weight of 454. 1 H (500MHz, DMSO-d 6 ) and 13 C NMR (125MHz, DMSO-d 6 ): See Table 1

[0018] Table 1.5,6,7,4′-Tetrahydro...

Embodiment 2

[0020] Example 2: Acute toxicity test of 5,6,7,4'-tetraacetoxyflavone on mice

[0021] Tested drug: 5,6,7,4'-tetraacetoxyflavone, provided by Kunming Pharmaceutical Group Co., Ltd. Drug Research Institute, batch number 20070312, grinded evenly with 0.5% sodium carboxymethylcellulose before use , dubbed into a suspension with a concentration of 0.1g / ml.

[0022] Experimental animals: ICR mice 18-22g, 20, male and female, provided by the Animal Laboratory of Kunming Pharmaceutical Group Co., Ltd., production license number SCXK (Dian) 2005-0006, use license number SYXK (Dian) 2005 -0006.

[0023] Test method and results: Select healthy ICR mice, weighing 20±2g, 20, half male and half male, orally gavage the mice with 5,6,7,4′-tetraacetoxyflavone with a concentration of 0.1g / ml Suspension 0.8ml / 20g body weight, continuous observation for 7 days, the mice were normal and agile, and did not cause death or abnormal reaction.

Embodiment 3

[0024] Embodiment 3: Chronic toxicity test experiment of 5,6,7,4'-tetraacetoxyflavone to rats

[0025] Tested drug: 5,6,7,4'-tetraacetoxyflavone, provided by Kunming Pharmaceutical Group Co., Ltd. Drug Research Institute, batch number 20070312, grinded evenly with 0.5% sodium carboxymethylcellulose before use , dubbed into a suspension with a concentration of 0.1g / ml.

[0026] Experimental animals: SD male rats, weighing 200-250 g, provided by the Experimental Animal Center of Kunming Medical College, production license number SCXK (Dian) 2005-0008, use license number SYXK (Dian) 2005-0008.

[0027] Test method and results: 30 SD male rats, weighing 200-250g, were divided into 3 groups, 10 in each group. 5,6,7,4′-Tetraacetoxyflavone was infused with doses of 1g / kg, 0.5g / kg, and 0.1g / kg for 3 months, and it was detected that it had significant effects on liver and kidney function, peripheral blood, behavior, There was no obvious effect on routine urine and stool, and no abnor...

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Abstract

The invention discloses use of 5,6,7,4'-tetra-acetoxyl flavone for preparing a medicine for preventing and curing cardiovascular and cerebrovascular diseases, relating to the medical field. The pharmacological tests show that the 5,6,7,4'-tetra-acetoxyl flavone can obviously improve behavior disorders of cerebral ischemic rat, reduce the area of cerebral infarction, improve the cerebral ischemia symptoms, and obviously protect the cerebral ischemia damages. The rat platelet aggregation can be obviously inhibited so as to inhibit the forming of thrombus in vivo. The 5,6,7,4'-tetra-acetoxyl flavone with different dosages can reduce the viscosity of whole blood of the rat, viscosity of plasma and hematokrit. The 5,6,7,4'-tetra-acetoxyl flavone can prolong the mouse blood coagulation time, has the dose-dependence, and can reducethe positive rate of rat myocardial ischemia caused by the pituitrin. The 5,6,7,4'-tetra-acetoxyl flavone is further featured with low toxicity and high safety, and has good application foreground for treating and preventing the cardiovascular disease.

Description

technical field [0001] The invention relates to the field of medicine, in particular to the use of 5,6,7,4'-tetraacetoxyflavone in the preparation of drugs for preventing and treating cardiovascular and cerebrovascular diseases. Background technique [0002] With the development of the economy, the improvement of people's living standards, and the aggravation of population aging, cardiovascular and cerebrovascular diseases are increasing day by day. Cardiovascular and cerebrovascular diseases are serious and are the first cause of human death, so their pathogenesis and treatment have received special attention from the medical community and society. [0003] Flavonoid derivatives mostly have the effect of treating and preventing cardiovascular and cerebrovascular diseases. At present, scutellarin has been widely used in the treatment of cardiovascular and cerebrovascular diseases. Clinical application shows that it can increase the blood flow of brain and coronary vessels, ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/352A61P9/10A61P9/00A61P7/02
Inventor 周荣光
Owner KPC PHARM INC
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