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Application of adenanthin in pharmacy

A glandularin and drug technology, applied in the field of biotechnology and medicine, can solve the problems of difficult standardization of drug dosage, difficult control of toxic and side effects, and difficult mechanism of action, etc., and achieve good medicinal prospects, strong pharmacological effects, and easy absorption. Effect

Inactive Publication Date: 2012-05-23
SHANGHAI JIAOTONG UNIV SCHOOL OF MEDICINE +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the complex ingredients of traditional Chinese medicine prescriptions, it is difficult to clarify the mechanism of action, control the toxic and side effects, and standardize the dosage of drugs, which greatly limits its clinical application.

Method used

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  • Application of adenanthin in pharmacy
  • Application of adenanthin in pharmacy
  • Application of adenanthin in pharmacy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Example 1: Adenine inhibits the activation of NF-kB induced by TNFa in THP-1 cells.

[0038] An in vitro screening platform for NF-kB inhibitors was established, that is, in the human monocytic leukemia cell line THP-1, electroporated into pGL4.32[luc2P / NF-kB-RE / Hygro] Vector (Promega) plasmid , The cell line stably transfecting the NF-kB reporter gene was obtained by Hygro screening. By adding TNFa to activate the cytokine of NF-kB, it is confirmed that this system can well reflect the activity of NF-kB ( figure 1 B). Different concentrations of adenosine were treated with pGL4.32-NF-kB-RE-THP-1 cells for 1 hour and then 10ng / ml TNFa was added to stimulate for 5 hours, and the luciferase activity was detected. The results suggest that adenosine can inhibit TNFa-induced NF-kB activation in a dose-dependent manner ( figure 1 B).

[0039] Furthermore, the THP-1 cells were pretreated with different concentrations of adenoidin for 1 hour, and then 10ng / ml TNFa was added for...

Embodiment 2

[0040] Example 2: Adenochrome inhibits NF-kB activity and downstream target gene expression through multiple steps.

[0041] In order to study the mechanism of adenin inhibiting NF-kB, observe which link of adenin's effect on TNFa-induced NF-kB activation. THP-1 cells were pretreated with 4mM, 10mM adenosine for 1 hour and then stimulated with 10ng / ml TNFa for 15 minutes, WESTERN detected pi-IKKa / b, IKKa, pi-IkBa, IkBa, pi-p65, p65, p50 and b-actin ( figure 2 A). We found that the low concentration (4mM) does not affect the phosphorylation and degradation of IkBa, and the high concentration (10mM) completely inhibits the phosphorylation and degradation of IkBa. Consistent with this, the results of NF-kB immunofluorescence showed that low concentrations only partially inhibited nuclear translocation of NF-kB, while high concentrations almost completely inhibited nuclear translocation of NF-kB. THP-1 cells were treated with 4mM, 10mM adenosine for 1 hour, and 10ng / ml TNFa was ...

Embodiment 3

[0042] Example 3: Adenoflavin inhibits LPS-induced NF-kB activation in RAW264.7 cells.

[0043] In the mouse macrophage cell line RAW264.7, electroporated into pGL4.32[luc2P / NF-kB-RE / Hygro] Vector (Promega) plasmid, and selected by Hygro to obtain a cell line stably transfected with NF-kB reporter gene . The cytokine that activates NF-kB by adding LPS confirms that this system can well reflect the activity of NF-kB ( image 3 A). Different concentrations of adenosine were treated with pGL4.32-NF-kB-RE-RAW264.7 cells for 1 hour, then 100ng / ml LPS was added to stimulate for 5 hours, and the luciferase activity was detected. The results suggest that adenosine can inhibit the activation of NF-kB induced by LPS in a dose-dependent manner ( figure 1 B).

[0044] Furthermore, through immunofluorescence experiments, we found that RAW264.7 cells were pretreated with adenosine at different concentrations (4mM, 10mM) for 1 hour and then stimulated with 100ng / ml LPS for 30 minutes, the LP...

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Abstract

The invention discloses an application of adenanthin in preparing medicines for preventing or treating multiple sclerosis, and an NF-kB inhibitor which is adenanthin. The adenanthin disclosed herein is safe, has low toxicity, and has strong pharmacological action and good medicinal foreground. The adenanthin active substance has the advantages of easy absorption, good stability, and the like, and is suitable for being as an additive of novel medicament, food, health products and / or meals for development.

Description

technical field [0001] The invention relates to the fields of biotechnology and medicine, in particular to the application of active substance adenanthin in the preparation of drugs for preventing or treating multiple sclerosis. Background technique [0002] Multiple sclerosis (MS) is one of the most common neuroimmune diseases, manifested as demyelination of the central nervous system, and about 50% of patients cannot walk independently 15 years after onset. MS is the most common non-traumatic neurological disability in Western Europe and South America. In my country, according to incomplete statistics, the prevalence of the disease has reached about 5 / 100,000, and it is increasing year by year. Because it occurs frequently in young and middle-aged people, and has a high disability rate, it has extremely adverse effects on society and families. The lesion site of the disease is in the brain or spinal cord, and the clinical feature is that the lesion is widely spread, and ...

Claims

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Application Information

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IPC IPC(8): A61K31/22A61P25/28
Inventor 陈国强孙汉董吴英理刘传绪阴倩倩普建新肖伟烈
Owner SHANGHAI JIAOTONG UNIV SCHOOL OF MEDICINE
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