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Application of peimine in preparation of novel immunosuppressive agent

An immunosuppressant and fritillary technology, which is applied in the application field of fritillin A for preparing new immunosuppressants, can solve problems such as many side effects, and achieve the effects of weakening activation, reducing T cell activity, and reducing cellular immunity

Active Publication Date: 2015-09-30
OLIVE PHARMASOLUTINS LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Early studies have found that the broad-spectrum potassium ion channel blocker 4-aminopyridine (4-Aminopyridine, 4-AP) can improve the symptoms of MS (multiple sclerosis) patients, but due to its broad-spectrum blocking effect and many side effects, it is limited. It's applied thus to Kv1.3 and IK Cal Screening highly selective potassium ion channel blockers for the target has become a research hotspot

Method used

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  • Application of peimine in preparation of novel immunosuppressive agent
  • Application of peimine in preparation of novel immunosuppressive agent
  • Application of peimine in preparation of novel immunosuppressive agent

Examples

Experimental program
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Effect test

Embodiment 1

[0040] Example 1, Peiminin A selectively inhibits Kv1.3 ion channels and inhibits immunity. The molecular formula of the Peiminin A is C27H45NO3 and the molecular weight is 431.6511. Its structural formula is as follows:

[0041] 1 Study on the Inhibitory Effect of Peiminin A on Kv1.3 Ion Channel

[0042] 1.1 Solution and reagents: intracellular fluid is composed of potassium aspartate solution (mmol / L): 137mM potassium aspartate potassium aspartate, 10mM HEPES, 4mM MgATP, 4mM MgCl2, 10mM EGTA; adjust the pH value to 7.3 with NaOH ; Extracellular fluid (bath solution composition (de Vries et al.)): NaCl, 136mM; KCl, 8mM; CaCl 2 , 2mM; MgCl 2 , 2mM; glucose, 10mM; and HEPES, 20mM; all were purchased from San Diego, USA. Peimine (Peimine) was purchased from Sichuan Master Company, dissolved in DMSO solution, made 300 times mother solution and stored in -80 degree refrigerator for later use; diluted 300 times for use in extracellular fluid during experiments.

[0043] 1.2 Cell...

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Abstract

The invention relates to a novel application of peimine, and in particular relates to an application of peimine in preparation of a novel immunosuppressive agent. An experiment on the inhibiting effects of Kv1.2-Kv1.8 ion channels through peimine shows that the peimine can be combined with the Kv1.3 ion channel with relatively high selectivity, so that overexciting T lymphocyte is reduced; activation on the T lymphocyte is weakened, so that the activity of the T lymphocyte is lowered; the cellular immunity is finally lowered; and the effect on other potassium ion channels is weak. The peimine selectively penetrates through the inhibiting Kv1.3 ion channel, so that adverse effects caused by treatment of immune system function hyperfunction diseases such as scleroderma and lupus erythematosus can be reduced; and normal immunologic functions are not affected. Therefore, the peimine is of great significance on development of novel medicines.

Description

technical field [0001] The invention relates to a new application of peiminin, in particular to the application of peiminin in the preparation of novel immunosuppressants. Background technique [0002] T lymphocyte subtypes participate in all stages of immune response and play a key role in immune regulation. When the immune regulation is disordered and the immune balance regulation mechanism is destroyed, it will lead to the occurrence of autoimmune diseases. Autoimmune diseases mainly include scleroderma, systemic lupus erythematosus, serum sickness, rheumatoid arthritis, etc. The reason for their occurrence is that some self-reactive T Cells are able to escape clonal clearance, recognize their own peripheral tissue antigens and mount an autoimmune response. By regulating the function of T lymphocyte membrane ion channels to change the activity of T cells, the purpose of treating autoimmune diseases can be achieved. At present, the traditional methods of treating autoimm...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/58A61P37/06A61P5/14A61P5/16A61P3/10A61P21/04A61P1/04A61P1/00A61P11/00A61P13/12A61P29/00A61P1/16A61P25/00A61P17/00A61P19/02A61P9/00
Inventor 陈渊
Owner OLIVE PHARMASOLUTINS LTD
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