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Application of DIM and derivative thereof in preparing drug for preventing and controlling injuries caused by chemotherapy

A technology of chemotherapeutic drugs and derivatives, which is applied in the field of biomedicine, can solve the problems such as no auxiliary drugs for treatment and chemotherapy, and achieve the effect of inhibiting inflammation, stable properties, and easy access

Inactive Publication Date: 2018-07-06
NANJING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In recent years, many studies about the effect of DIM on inflammatory diseases have shown that DIM and its derivatives can reduce the level of free radicals in damaged tissues and relieve tissue inflammatory damage. This research has been verified in the inventor's laboratory, and it has not yet been tested Research reports on adjuvant drugs used in the treatment of chemotherapy

Method used

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  • Application of DIM and derivative thereof in preparing drug for preventing and controlling injuries caused by chemotherapy
  • Application of DIM and derivative thereof in preparing drug for preventing and controlling injuries caused by chemotherapy
  • Application of DIM and derivative thereof in preparing drug for preventing and controlling injuries caused by chemotherapy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] 3, the preparation of 3'-diindolylmethane and indole-3-carbinol and derivatives thereof, the specific preparation steps are as follows:

[0050] 1) Indole derivatives (eg, 5-methoxy, 5-chloro, 5-bromo, 5-fluoro, 5'-methyl, 5-nitro, N-methyl and 2-methylindole ) can be purchased commercially (Nanjing Ruima Fine Chemical Co., Ltd.), and the substituted indole-3-acetaldehyde product is derived by reducing the aldehyde group with a suitable alcohol such as methanol and sodium borohydride to give I3C. 2.9ml of dimethylformamide was cooled to 0°C in an ice-salt bath, then slowly added 0.86ml of phosphorus oxychloride (more than 30min), and 8.6mmol of indole derivatives were dissolved in 1.0ml of dimethylformamide , and then slowly add it to the previously cooled phosphorus oxychloride solution (time greater than 10min), the formed suspension is heated at 37°C for 60min-90min until the clear yellow solution becomes a slightly yellowish paste, and then to Add 1ml of ice water ...

Embodiment 2

[0054] Application of oral 3,3'-diindolylmethane, indole-3-carbinol and derivatives thereof in the preparation of prevention and treatment of liver, kidney and digestive tract tissue damage caused by chemotherapy drugs.

[0055] I3C, DIM, and its derivative compounds 5-chloroindole-3-methanol (5-Cl-I3C), 5,5'-chlorodiindolylmethane (5,5'-Cl-DIM), 2-pentane Indole-3-carbinol (2-C5-I3C), 2,2'-pentyl-diindolylmethane (2,2'-C5-DIM), 5-nitroindole-3-carbinol (5 -NO-I3C), 5,5'-nitrodiindolylmethane (5,5'-NO-DIM), N-methoxyindole-3-methanol (N-MOE-I3C) and N,N '-Methoxy-diindolylmethane (N,N'-MOE-DIM), respectively dissolved in corn oil, prepared as a 2.0 mg / ml stock solution for future use.

[0056] 1. Experimental animals

[0057] Clean-grade male ICR mice, weighing 16-18 g, were purchased from Beijing Weitong Lihua Company and raised in the Experimental Animal Center of Nanjing University.

[0058] 2. Experimental grouping and processing

[0059]Mice were randomly divided into...

Embodiment 3

[0097] Application of intraperitoneal injection of aqueous solution preparations of 3,3'-diindolylmethane, indole-3-carbinol and their derivatives in the preparation of prevention and treatment of liver, kidney and digestive tract tissue damage caused by chemotherapy drugs.

[0098] I3C, DIM, and its derivative compounds 5-chloroindole-3-methanol (5-Cl-I3C), 5,5'-chlorodiindolylmethane (5,5'-Cl-DIM), 2-pentane Indole-3-carbinol (2-C5-I3C), 2,2'-pentyl-diindolylmethane (2,2'-C5-DIM), 5-nitroindole-3-carbinol (5 -NO-I3C), 5,5'-nitrodiindolylmethane (5,5'-NO-DIM), N-methoxyindole-3-methanol (N-MOE-I3C) and N,N '-Methoxy-diindolylmethane (N,N'-MOE-DIM), prepared with cyclodextrin and physiological saline to prepare a stock solution of 1.0 mg / kg for future use.

[0099] 1. Experimental animals

[0100] Clean-grade male ICR mice, weighing 16-18 g, were purchased from Beijing Weitong Lihua Company and raised in the Experimental Animal Center of Nanjing University.

[0101] 2. Expe...

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Abstract

The invention discloses application of a DIM and a derivative thereof in preparing drug for preventing and controlling injuries caused by chemotherapy. The DIM and the derivative thereof can effectively protect an organism from being injured by free radicals and prevent activation, induced by the free radicals, of hepatic stellate cells, related collagen expression, inflammations and a renal fibrosis state caused by renal tubular epithelial cell injuries in kidney and injuries such as gland and mucosal lining patch-like rupture caused by gastrointestinal epidermal cell injuries and the like, thus alleviating pains of patients receiving chemotherapy and increasing the tolerated dose of the patients to a chemotherapeutic drug. For the application, the organism is protected from being injuredby the free radicals by giving the drugs containing 3,3,- diindolylmethane, indole-3-methanol as a precursor compound of the 3,3,-diindolylmethane and derivative compounds of the 3,3,-diindolylmethane and the indole-3-methanol, so that the inflammation caused by tissue injuries are inhibited, and the used small molecular drug is available, is low in cost, stable in property and convenient to store and transport and has important clinic application value in preventing and controlling the tissue injuries caused by chemotherapy.

Description

technical field [0001] The present invention relates to the application of DIM and its derivatives in the preparation of drugs for the prevention and treatment of chemotherapy-induced damage, in particular to the application of 3,3'-diindolylmethane (DIM) and its derivatives in the preparation of drugs for the prevention and treatment of liver, kidney and digestive tract damage caused by chemotherapy drugs. The application in injury medicine belongs to the technical field of biomedicine. Background technique [0002] Malignant tumors are one of the common diseases that seriously threaten human health. In recent years, tumor treatment research has achieved rapid development. Tumor treatment emphasizes comprehensive treatment, and chemotherapy is one of the important means. With the continuous introduction of anti-tumor drugs and the application of various combination chemotherapy, the survival cycle of patients with malignant tumors has been prolonged. However, there are li...

Claims

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Application Information

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IPC IPC(8): A61K31/404A61P29/00A61P13/12A61P1/16A61P1/00
CPCA61K31/404
Inventor 董磊
Owner NANJING UNIV
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