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Application of ring icariine in the preparation of medicine for preventing and treating organ transplantation rejection

A cyclic icariin and rejection technology is applied in the directions of drug combination, drug delivery, active ingredients of heterocyclic compounds, etc., to achieve good anti-rejection effect, inhibit rejection, and improve the function of transplanted organs.

Inactive Publication Date: 2007-02-28
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Tests have found that these newly developed drugs also have similar problems to CsA

Method used

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  • Application of ring icariine in the preparation of medicine for preventing and treating organ transplantation rejection
  • Application of ring icariine in the preparation of medicine for preventing and treating organ transplantation rejection
  • Application of ring icariine in the preparation of medicine for preventing and treating organ transplantation rejection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Example 1: Preparation of cyclic icariin

[0018] (1) Preparation of icariin: method reported in literature [Yang Xiaoping, Chinese Pharmaceutical Journal, 1992, 28(1), 37; Li Wenkui et al., Northwest Pharmaceutical Journal, 1995, 10(3), 138], from Yin Icariin with a content of 90% is obtained by separating and purifying from the whole sheep herb.

[0019] (2) Preparation of cyclic icariin (as shown in formula I): Dissolve 1 g of icariin in 50-500 mL of methanol, then add concentrated sulfuric acid with a volume of 5-30% of the solution, and heat to reflux 2-10 hours. After the reaction is completed, cool down and add 2-10 times of water, and a large amount of precipitation will be produced at this time. The precipitate was collected by filtration and washed with water until neutral. After the precipitate was dried, it was purified by silica gel column chromatography to obtain a light yellow solid product. The yield is 30-60%. The structure of the product has been ...

Embodiment 2

[0020] Example 2: In vitro immunosuppressive test of cyclic icarigenin

[0021] Experiment 1: Inhibitory effect of cyclic icario aglycone on normal human peripheral blood mononuclear cells (PBMCs) γ-interferon (interferon-gamma, IFN-γ)

[0022] (1) Isolation of normal human peripheral blood mononuclear cells (PBMCs)

[0023] The peripheral blood of normal people was taken for anticoagulation with heparin, diluted with an equal amount of Hank's buffer, mixed evenly, and layered on top of dextran-Ficoll-Hypaque. Centrifuge at 24°C for 25 minutes (2500 rpm). After centrifugation, draw the PBMCs layer, wash it twice with buffer, and then add RPMI1640 complete medium to suspend the cells.

[0024] (2) Cell culture

[0025] Adjust PBMCs to 2 × 10 6 Cells / ml, cultured in 96-well plate, 200uL per well, 3 replicate wells for each group. PBMCs added anti-CD3 monoclonal antibody (0.2 μg / mL) and anti-CD3 monoclonal antibody + different concentrations of cyclopicaridin, 5% CO 2 , 37 ...

Embodiment 3

[0030] Example 3: Cyclic icariin prevents and treats rejection in a rat heart transplant model

[0031] Test drug: cyclic icariin. Control drug: tacrolimus (FK506).

[0032] Test animals: Donor Brown Norway (BN, RT1 n ) rat; recipient Lewis (LEW, RT1 1 ) rats.

[0033] Experimental method: Allogeneic heart transplantation was performed among rats of different strains, and the allogeneic heart transplantation model was constructed. On the first day after operation, cyclic icariin and FK506 were administered orally to recipient rats respectively. The dose of cyclic icariin is 6-24 mg / kg per day, and the dose of FK506 is 0.5-1.5 mg / kg per day. The survival time of recipient rats after transplantation was observed.

[0034] test results:

[0035] Compared with the control group, the recipients of the rat heart transplantation model in the 6mg / kg day, 12mg / kg day, 24mg / kg day cyclic icariin and 1.0mg / kg day, 1.5mg / kg day FK506 groups The survival time of rats was significan...

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Abstract

The invention discloses an immune inhibiting drug and application based on ring-icariin in the formula I, which is characterized by the following: inhibiting immuse exclusive reaction in the organ transplanting course, modifying transplanted organ function.

Description

technical field [0001] The invention relates to the application of cyclic icariin as an immunosuppressive drug for preventing and treating organ transplantation rejection. technical background [0002] In the past 30 years, with the research progress of immunobiology of transplanted organ rejection, especially the clinical use of anti-immune rejection drugs, the number, type and success rate of organ transplantation have been significantly increased. [0003] At present, the most commonly used anti-immune rejection drug is cyclosporine (CsA). CsA is actually an immunosuppressant, which improves the function of transplanted organs and prolongs the survival time by inhibiting immune rejection in the body. However, the dose-dependent hepatotoxicity and nephrotoxicity caused by CsA, as well as the high price limit the use of CsA. At present, nearly 30 immunosuppressants have been discovered, some of which have been clinically used to treat immune rejection in organ transplant p...

Claims

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Application Information

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IPC IPC(8): A61K31/35A61K9/20A61K9/08A61K9/10A61P37/06
Inventor 王长希古练权黄民吴长有
Owner SUN YAT SEN UNIV
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