Application of indole-3-carbinol, diindolyl methane and derivatives thereof in preparation of medicaments for treating osteoporosis

A technology of diindolylmethane and osteoporosis, which is applied in the field of biomedicine, can solve the problems of lack of pertinence in osteoporosis, and achieve the effect of low price, stable properties and easy access

Active Publication Date: 2012-02-01
宁国市吴越医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

At present, there is still a lack of targeted

Method used

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  • Application of indole-3-carbinol, diindolyl methane and derivatives thereof in preparation of medicaments for treating osteoporosis
  • Application of indole-3-carbinol, diindolyl methane and derivatives thereof in preparation of medicaments for treating osteoporosis
  • Application of indole-3-carbinol, diindolyl methane and derivatives thereof in preparation of medicaments for treating osteoporosis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] (Preparation of 5-chloroindole-3-methanol and 5,5'-dichlorodiindole methane)

[0030] 0.86ml phosphoryl chloride was slowly added to 2.9ml dimethylformamide which had been cooled to 0°C. Dissolve 8.6mmol 5-chloroindole (purchased from Nanjing Ruima Fine Chemical Co., Ltd.) in 1.0ml of dimethylformamide, and then slowly add it to the pre-cooled phosphoryl chloride solution. The resulting suspension is in 37 Heat at ℃ for 60 minutes, until the clear yellow solution becomes a pale yellow paste. Then 1ml of ice water was added to this paste-like substance, and then 10ml of aqueous solution containing 3.75g of KOH was slowly added. The mixture is heated to boiling and then cooled, filtered, washed with water, and dried in the air to obtain 5-chloroindole-3-acetaldehyde.

[0031] 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 add 50ml of water to the reactant, cool to 0°C, filter...

Embodiment 2

[0034] (Preparation of 5-nitroindole-3-methanol and 5,5'-dinitrodiindole methane)

[0035] 5-Nitroindole can be purchased commercially (Nanjing Ruima Fine Chemical Co., Ltd.). 0.92ml phosphoryl chloride was slowly added to 2.9ml dimethylformamide which had been cooled to 0°C. Dissolve 8.2mmol 5-nitroindole in 1.0ml of dimethylformamide, and then slowly add it to the pre-cooled phosphoryl chloride solution. The resulting suspension is heated at 42°C for 90 minutes until a clear yellow solution It becomes a pale yellow paste-like substance. Then 1ml of ice water was added to this paste-like substance, and then 10ml of aqueous solution containing 3.75g of KOH was slowly added. The mixture is heated to boiling and then cooled, filtered, washed with water, and dried in the air to obtain 5-nitroindole-3-acetaldehyde.

[0036] 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 ...

Embodiment 3

[0039] (Preparation of 5-pentylindole-3-methanol and 5,5'-dipentyl-diindolemethane)

[0040] 5-pentylindole can be purchased commercially (Nanjing Ruima Fine Chemical Co., Ltd.). 0.82ml phosphoryl chloride was slowly added to 2.9ml dimethylformamide which had been cooled to 0°C. Dissolve 9.2mmol 5-pentylindole in 1.0ml of dimethylformamide, and then slowly add it to the pre-cooled phosphoryl chloride solution. The resulting suspension is heated at 37°C for 40-60 minutes until it is clear The yellow solution becomes a pale yellow paste-like substance. Then 1ml of ice water was added to this paste-like substance, and then 10ml of aqueous solution containing 3.75g of KOH was slowly added. The mixture is heated to boiling and then cooled, filtered, washed with water, and dried in the air to obtain 5-pentylindole-3-acetaldehyde.

[0041] 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 ...

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Abstract

The invention provides new application of indole-3-carbinol, diindolyl methane and derivatives thereof in preparation of medicaments for treating osteoporosis. The indole-3-carbinol (I3C), the diindolyl methane (DIM) and the derivative compounds thereof can inhibit growth and functions of osteoclasts through medicaments, and can be used for preventing and treating the osteoporosis in principle. The DIM, the I3C and the derivative compounds can effectively reduce the pathogenetic symptoms of osteoporosis animal models, and can be used as candidate medicament molecules for treating the osteoporosis. Meanwhile, the adopted small molecular substances are easily obtained, are low in price, stable in properties and convenient for storage and transportation, and have broad application prospect.

Description

Technical field [0001] The invention belongs to the technical field of biomedicine, and specifically relates to the application of indole-3-methanol, diindolylmethane and their derivatives in the preparation of medicines for treating osteoporosis. Background technique [0002] Osteoporosis is a group of bone diseases caused by various reasons. The bone tissue has normal calcification, the calcium salt and the matrix are in a normal ratio, and the metabolic bone disease is characterized by a decrease in the amount of bone tissue per unit volume. In most osteoporosis, the reduction of bone tissue is mainly due to increased bone resorption. The incidence of osteoporosis is high. Among women over 45 years old, one third of them suffer from osteoporosis to varying degrees; and among women over 75 years old, 90% suffer from osteoporosis. Complications after fractures caused by osteoporosis are one of the important fatal factors in elderly patients. At present, there is still a lack o...

Claims

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Application Information

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IPC IPC(8): A61K31/404A61P19/10
Inventor 董磊
Owner 宁国市吴越医药科技有限公司
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