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Immune regulation and biological therapeutic function of benzo-isoselenazole derivatives

A technology of benzisoselenazole and derivatives is applied in the field of benzisoselenazole derivatives, which can solve the problems such as immunomodulation research and biological treatment applications that have not yet been reported, and achieve the effect of enhancing immune function.

Inactive Publication Date: 2004-07-14
北京大学药学院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0015] There are several patents disclosing Ebselen derivatives as medicinal research, they are respectively Chinese patent 98124487.4 (application number) the effect of benzisoselenazolone sulfonamide derivatives in inhibiting inflammation and allergic diseases; Chinese patent 01118666.6 ( Application No.) Anti-inflammatory and anti-tumor effects of R-bis or sugar benzisoselenazole substituted compounds and PCT / CN02 / 00412 (Application No.) Benzisoselenazole derivatives with anti-inflammatory, anti-tumor and antithrombotic effects In terms of immunoregulation research, although there are numerous researches utilizing the Ebselen mother nucleus to transform it into immunoenhancing compounds, successful immunoenhancing drugs, especially the immunomodulatory research on the compounds involved in the application of the present invention and biotherapeutic applications have not been reported

Method used

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  • Immune regulation and biological therapeutic function of benzo-isoselenazole derivatives
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  • Immune regulation and biological therapeutic function of benzo-isoselenazole derivatives

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Example 1: Study on the Immunomodulatory Effect of Drugs on BALB / C Normal Mice

[0052] Animal grouping and dosing:

[0053] BALB / C mice were randomly divided into 4 groups, 20 animals in the experimental drug group, intraperitoneally injected with freshly prepared drugs, 10 mice at a dose of 25.0 mg / kg, and the other 10 mice at a dose of 12.5 mg / kg, once a day, continuously administered 7 days; 10 animals in the positive control group were intraperitoneally injected with the positive control drug ddp at a dose of 2.0 mg / kg, once a day for 7 consecutive days. In the control group, 10 rats were intraperitoneally injected with solvent, and the volume was adjusted according to body weight, which was the same as that of the drug group. Inject once a day for 7 consecutive days.

[0054] The mice in each of the above groups were given continuous administration, and were killed by necking on the 3rd day after drug withdrawal. The spleen was aseptically taken out, weighed wet...

Embodiment 2

[0060] Example 2: Immunomodulatory Effects of Drugs on IC2 of Common Grade 1 Albino Mice

[0061] Thirty-two IC2 mice with a weight of about 25 grams were randomly divided into 4 groups, 8 mice in each group. The first group was injected intraperitoneally with a dose of 25 mg / kg for 4 consecutive days; the second group was injected intraperitoneally with a dose of 12.5 mg / kg. mg / kg, for 4 consecutive days; the third group was injected intraperitoneally with DDP at a dose of 2 mg / kg; the fourth group was injected with the same volume of solvent intraperitoneally, for 4 consecutive days. On the fifth day, they were killed by necking, the spleen was taken, and the mononuclear cells were separated with lymphocyte separation medium to adjust the cell concentration to 2×10 6 / ml, as effector cells of NK cells. Take 3.6ml of mononuclear cell suspension, add 10 4 U / ml of IL 2 0.4ml, into a plastic culture bottle, after 48 hours of culture, absorb the culture medium and suspended c...

Embodiment 3

[0068] Example 3: Research on the bioregulatory effect of drugs on C57 tumor mice

[0069] (1) C57 tumor mice were injected intraperitoneally with EB (25 mg / kg), DDP and solvent respectively, and administered continuously for 7 days, and were killed by necking on the 10th day, and the spleen was taken out to weigh the spleen, and the mononuclear cells were isolated, and the proliferation of spleen cells was measured by MTT method Activity and NK / LAK cell activity, MTT method to measure NK cell activity, the method is the same as above. The results of spleen weight and spleen cell proliferation are shown in Table 3.

[0070] drug group

Positive Drug Panel (DDP)

blank control

Dose (mg / kg)

25

2

Splenocyte Proliferation (OD)

0.395

0.025

0.058

Spleen weight (g)

0.428

0.135

0.305

NK activity (%)

20.06

10.21

10.32

[0071] It can be seen from the table that the splenocy...

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Abstract

The present invention relates to benzo-isoselenazole derivative and its pharmaceutically acceptable salt. The derivative may be used in immunological regulation and biological therapy and as health composition with immunological regulation function.

Description

field of invention [0001] The invention relates to the application of a class of benzisoselenazole derivatives capable of enhancing the activity of NK cells and LAK cells of the cellular immune system in the human body. The present invention also relates to a pharmaceutical composition comprising the benzisoselazole derivative and its composition as a drug for immune regulation and biotherapy, a technical solution for drug application, an implementation field, and related treatments; The technical scheme and application method formed by the health care composition with immune regulation or bioregulation function. Background technique [0002] Biotherapeutic technology or bioregulatory therapy is the background technology that has an important relationship with the compounds involved in the application of the present invention. Biotherapy technology is a biomedical technology that has developed rapidly in recent years and corresponds to chemotherapy and radiotherapy. The ma...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/41A61K31/555A61K31/7052A61P31/04A61P31/12A61P37/02C07D293/12C07F15/00C07H19/02
Inventor 曾慧慧
Owner 北京大学药学院
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