Application of Loureirin B in preparation of Kv1.3 channel blocker

A channel blocker, kv1.3 technology, applied in the field of medicine, can solve the problems that no reports of dragon's blood B treating autoimmune diseases have been seen, and the lack of dragon's blood B can achieve the effect of clear ingredients and controllable quality

Inactive Publication Date: 2015-04-22
SOUTH CENTRAL UNIVERSITY FOR NATIONALITIES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, there are few pharmacodynamic studies on dragon's blood B at home and abroad, and there is no report on the treatment of autoimmune diseases by dragon's blood B.

Method used

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  • Application of Loureirin B in preparation of Kv1.3 channel blocker
  • Application of Loureirin B in preparation of Kv1.3 channel blocker
  • Application of Loureirin B in preparation of Kv1.3 channel blocker

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Example 1 The patch clamp experiment technique was used to detect the inhibitory effect of dragon blood B on mammalian Kv1.3 channel function.

[0023] Jurkat E6-1T cells (ATCC TIB152) and HEK293T cells (ATCC ACS4500) were cultured in RPMI 1640 (Invitrogen, Carlsbad, CA, USA) supplemented with 10% fetal bovine serum, 100 units / mL penicillin, and 100 μg / mL streptomycin, respectively. ) and DMEM medium (Life Technologies, Grand Island, NY, USA), the cells were placed at 37°C and 5% CO 2 cultured in an incubator. The cDNA encoding the mKv1.3 channel protein in the vector pSP64 (gifted by Professor Stephan Grissmer, University of Ulm, Ulm, Germany) was subcloned into pIRES2-EGFP (Clontech, Inc., Mountain View, CA, USA) vector. The constructed clones were analyzed by DNA sequencing to confirm the correctness of their nucleotide sequences. The constructed vector was transfected into HEK293T cells with Lipofectamine 2000 (Invitrogen), and used for electrophysiological exper...

Embodiment 2

[0025] Example 2 Using calcium imaging technology to detect the effect of dragon blood B on free Ca in Jurkat T cells 2+ Inhibitory effect of concentration

[0026] The efflux of intracellular potassium ions caused by the opening of Kv1.3 channel can lead to the repolarization of T cell membrane potential, and the repolarization of T cell membrane potential is to promote the extracellular Ca of Jurkat T cells. 2+ The main electrical potential energy of the influx, thereby increasing the free Ca in Jurkat T cells 2+ concentration.

[0027] sarcoplasmic reticulum Ca 2+ - The ATPase inhibitor Cyclopiazonic acid (CPA) empties the calcium ions in the cellular calcium pool, and then uses Ca 2+ The indicator dye Fura-2 determines the effect of ascarin B on intracellular Ca in Jurkat T cells 2+ The effect of concentration changes.

[0028] When there is no Ca in the extracellular fluid 2+ 10 μM CPA induced Ca in Jurkat T cells 2+ The increase in concentration is small. When 2m...

Embodiment 3

[0030] Example 3 ELISA was used to detect the inhibition of the release of the inflammatory factor IL-2 in Jurktat cells by dragon blood B.

[0031] The opening of the Kv1.3 channel on the Jurkat T cell membrane causes the repolarization of the cell membrane potential, which is the main potential energy to maintain the continuous influx of extracellular calcium ions. Blocking the Kv1.3 channel current on the Jurkat T cell membrane will correspondingly prevent the influx of extracellular calcium ions, thereby reducing the concentration of intracellular free calcium ions. The cytokine IL-2 secreted by Jurkat T cells is affected by the intracellular free calcium concentration, and a decrease in the intracellular free calcium concentration will attenuate the release of the inflammatory cytokine IL-2.

[0032] 10 μg / mL phytohemagglutinin (PHA) was added to the cell culture medium to activate Jurkat T cells for 24 hours, and the concentration of inflammatory cytokine IL-2 released b...

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PUM

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Abstract

The invention discloses an application of Loureirin B in the preparation of a Kv1.3 channel blocker and provides a new drug approach for treating autoimmune diseases. The Loureirin B contains clear components and quality of the Loureirin B is controllable. The Loureirin B can effectively inhibit a Kv1.3 potassium channel, thus effectively treating various autoimmune diseases. Through various verification means of patch clamp experiment, calcium imaging techniques, ELISA assay and manufacturing of animal models of autoimmune encephalitis, rheumatoid arthritis and the like, it is found that the Loureirin B has a good therapeutical effect on autoimmune diseases at the overall level, can effectively overcome side effects of traditional therapeutics such as adrenocortical hormone and the like and can maintain normal protective immune responses of patients.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to 1. The application of dragon blood B in the preparation of Kv1.3 channel blockers. Background technique [0002] 5-8% of the world's population is seriously threatened by about 40 autoimmune diseases such as rheumatoid arthritis, systemic lupus erythematosus, and type 1 diabetes. The immunosuppressants (adrenal cortex hormones, etc.) Impairs the patient's normal immune defense response. How to find new drug therapeutic targets, so that the target drugs can maintain the normal immune response of the body while treating autoimmune diseases, has become a new research and development hotspot in the international pharmaceutical industry. In the traditional treatment of autoimmune diseases, the immunosuppressants (adrenal cortex hormones, etc.) used also weaken the patient's normal immune defense response. [0003] Dracaena is a resin extracted from the lipid-containing w...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/12A61P37/02A61P31/14A61P3/14A61P29/00
CPCA61K31/12
Inventor 尹世金胡青兰陆春兰陈璇
Owner SOUTH CENTRAL UNIVERSITY FOR NATIONALITIES
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