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Application of indole-3-carbinol, diindolylmethane and derivatives thereof to preparation of medicine for preventing and controlling atherosclerosis

A technology of atherosclerosis and diindolylmethane, which is applied in the field of preparation of anti-atherosclerosis drugs, can solve the problems of no obvious advantages in long-term curative effect, achieve low price, promote free radical scavenging, and reduce inflammation The effect of response level

Inactive Publication Date: 2012-03-28
合肥博太医药生物技术发展有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the main treatment method is the use of angiogenesis inhibitors and lipid-lowering drugs. Although interventional therapy can recanalize blood vessels, restenosis is still a medical problem that cannot be solved at present, especially the long-term efficacy has no obvious advantages.

Method used

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  • Application of indole-3-carbinol, diindolylmethane and derivatives thereof to preparation of medicine for preventing and controlling atherosclerosis
  • Application of indole-3-carbinol, diindolylmethane and derivatives thereof to preparation of medicine for preventing and controlling atherosclerosis
  • Application of indole-3-carbinol, diindolylmethane and derivatives thereof to preparation of medicine for preventing and controlling atherosclerosis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] (Preparation of 5-chloroindole-3-methanol and 5,5'-dichlorodiindolylmethane)

[0028] Slowly add 0.86ml of phosphorus oxychloride to 2.9ml of dimethylformamide that has been cooled to 0°C in advance. 8.6mmol 5-chloroindole (purchased from Nanjing Ruima Fine Chemical Co., Ltd.) was dissolved in 1.0ml of dimethylformamide, and then slowly added to the aforementioned precooled phosphorus oxychloride solution, the formed suspension was at 37 °C for 60 minutes until the clear yellow solution turns into a pale yellow paste. Then 1 ml of ice water was added to the pasty mass, followed by slow addition of 10 ml of an aqueous solution containing 3.75 g of KOH. Heat this mixture to boil and then cool, filter, wash with water, and dry in air to obtain 5-chloroindole-3-acetaldehyde.

[0029] 1.0 g of 5-chloroindole-3-acetaldehyde was dissolved in 5.0 ml of methanol, and solid sodium borohydride was continuously added until excess. Then 50ml of water was added to the reactant, co...

Embodiment 2

[0032] (Preparation of 5-nitroindole-3-methanol and 5,5'-dinitrodiindolylmethane)

[0033] 5-Nitroindole can be purchased commercially (Nanjing Ruima Fine Chemical Co., Ltd.). Slowly add 0.92ml of phosphorus oxychloride to 2.9ml of dimethylformamide cooled to 0°C in advance. Dissolve 8.2mmol of 5-nitroindole in 1.0ml of dimethylformamide, then slowly add it to the aforementioned pre-cooled phosphorus oxychloride solution, and heat the formed suspension at 42°C for 90 minutes until a clear yellow solution Turned into a light yellow pasty substance. Then 1 ml of ice water was added to the pasty mass, followed by slow addition of 10 ml of an aqueous solution containing 3.75 g of KOH. Heat this mixture to boil and then cool, filter, wash with water, and dry in air to obtain 5-nitroindole-3-acetaldehyde.

[0034] 1.0 g of 5-nitroindole-3-acetaldehyde was dissolved in 5.0 ml of methanol, and solid sodium borohydride was continuously added until excess. Then 50ml of water was add...

Embodiment 3

[0037] (Preparation of 5-pentylindole-3-carbinol and 5,5'-dipentyl-diindolylmethane)

[0038] 5-Pentylindole can be purchased commercially (Nanjing Ruima Fine Chemical Co., Ltd.). Slowly add 0.82 ml of phosphorus oxychloride to 2.9 ml of dimethylformamide cooled to 0°C in advance. Dissolve 9.2mmol of 5-pentylindole in 1.0ml of dimethylformamide, then slowly add to the aforementioned pre-cooled phosphorus oxychloride solution, and heat the formed suspension at 37°C for 40-60 minutes until clear The yellow solution turned into a pale yellow paste. Then 1 ml of ice water was added to the pasty mass, followed by slow addition of 10 ml of an aqueous solution containing 3.75 g of KOH. Heat this mixture to boil and then cool, filter, wash with water, and dry in air to obtain 5-pentylindole-3-acetaldehyde.

[0039] 1.0 g of 5-pentylindole-3-acetaldehyde was dissolved in 5.0 ml of methanol, and solid sodium borohydride was continuously added until excess. Then 50ml of water was add...

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PUM

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Abstract

The invention provides new application of indole-3-carbinol, diindolylmethane and derivatives thereof to preparation of a medicine for preventing and controlling atherosclerosis (AS). The indole-3-carbinol, diindolylmethane and derivatives thereof have obvious effects of resisting oxidation and improving endothelial functions, can ensure that the expression and proportion of all vaso-active substances in a human body are normal and the endothelial functions can be recovered normally, and have the good effects of reducing blood fat, and resisting AS. Meanwhile, the active ingredients of the used small molecule medicines can be obtained easily, and the indole-3-carbinol, diindolylmethane and derivatives thereof are low in price, have stable performance and are convenient to store and transport, and have wide application prospect.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and specifically relates to the application of indole-3-carbinol, diindolylmethane and derivatives thereof in the preparation of drugs for preventing and treating atherosclerosis. Background technique [0002] Atherosclerosis (AS) is the most common and important one in a group of vascular diseases called arteriosclerosis, and is the most important pathogenic factor leading to coronary heart disease and other cardiovascular and cerebrovascular diseases. In recent years, the incidence of atherosclerosis (AS) has a tendency to increase significantly in our country. According to the results of autopsy, the detection rates of coronary artery and aortic atherosclerotic lesions were 58.36% and 88.31% respectively among people aged 40 to 49, and gradually increased with age. The occurrence of AS is closely related to endothelial dysfunction, and a variety of cytokines and apoptosis affect the proce...

Claims

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Application Information

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IPC IPC(8): A61K31/404A61P9/10A61P39/06A61P29/00A61P3/06
Inventor 董磊
Owner 合肥博太医药生物技术发展有限公司
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