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Application of schisandrin b in preparing NADPH oxidase inhibitor

An oxidase inhibitor, schisandrin B technology, applied in the directions of active ingredients of heterocyclic compounds, drug combinations, cardiovascular system diseases, etc., can solve the problem of no schisandrin B inhibiting NADPH oxidase tumor metastasis and other problems

Inactive Publication Date: 2014-11-19
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] So far, there is no report on the inhibition of NADPH oxidase by Schizandrin B and its use in the treatment of tumor metastasis

Method used

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  • Application of schisandrin b in preparing NADPH oxidase inhibitor
  • Application of schisandrin b in preparing NADPH oxidase inhibitor
  • Application of schisandrin b in preparing NADPH oxidase inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Example 1: Schizandrin B has a concentration-dependent inhibitory effect on NADPH oxidase 4

[0020] Experimental materials: Siha cell line was purchased from American Type Culture Collection (ATCC); Siha cell lysate was used as the source of NAPDH oxidase 4; β-NADPH was purchased from Roche Company; Jing (Lucigenin), dimethyl sulfoxide (DMSO) were purchased from Sigma.

[0021] Experimental method: Different concentrations of schisandrin B were mixed with 100 μM NADPH and 5 μM lucigeinin in the reaction buffer, and the reaction activity of NADPH oxidase 4 was detected. The relative enzyme activity is relative to the enzyme reaction activity of the control group without adding Schisandrin B.

[0022] Experimental results: see the experimental results figure 1 , it can be seen that the inhibitory effect of schisandrin on NADPH oxidase 4 increases with the increase of drug concentration.

Embodiment 2

[0023] Example 2: Inhibition of Schizandrin B to NADPH Oxidase 4

[0024] Experimental materials: 4T1 mouse breast cancer cell line was purchased from American Type Culture Collection (ATCC); 4T1 cells were homogenized by a Dunes homogenizer, and 9000 g fraction was separated by differential centrifugation, and used as NADPH oxidase 4 Sources: β-NADPH was purchased from Roche; Schizandrin B was purchased from China Institute for the Control of Pharmaceutical and Biological Products; Lucigenin and DMSO were purchased from Sigma.

[0025] Experimental method: Different concentrations of schisandrin B were mixed with 100 μM NADPH and 5 μM lucigeinin in the reaction buffer, and the reaction activity of NADPH oxidase 4 was detected. The relative enzyme activity is relative to the enzyme reaction activity of the control group without adding Schisandrin B.

[0026] Experimental results: see the experimental results figure 2 , the experimental results proved again that the inhibito...

Embodiment 3

[0027] Example 3: Inhibitory relationship of Schizandrin B to the increase of reactive oxygen species mediated by NADPH oxidase 4 caused by TGF β factor

[0028] Experimental materials: 4T1 mouse breast cancer cell line was purchased from American Type Culture Collection (ATCC); TGF β factor was purchased from Peprotech; Schizandrin B was purchased from China Institute for the Control of Pharmaceutical and Biological Products; DA) was purchased from Sigma Company.

[0029] Experimental method: 10 μM Schizandrin B pretreated empty vector cells and NADPH oxidase 4 interference cells for 2 hours, and then added 5 ng / ml TGF β factor for 8 hours. DCFH-DA was used to detect the signal value of cellular reactive oxygen species. Relative signal is the ratio relative to the signal of untreated empty vector cells.

[0030] Experimental results: see the experimental results image 3 , the experimental results proved that the increase of ROS signal value caused by TGF β was mediated by...

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PUM

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Abstract

The invention provides an application of schisandrin b in preparing an NADPH oxidase inhibitor. The NADPH oxidase comprises various sub-types of oxidase. In in-vitro enzymatic experiments, the schisandrin b is capable of inhibiting super-oxygen ion generation reaction catalyzed by NADPH oxidase and reactive oxygen generation related to NADPH oxidase in cells, and does not have the function of scavenging free radicals, thus being an inhibitor of the NADPH oxidase. Furthermore, the NADPH oxidase is capable of changing the level of a plurality of signal transduction pathways and inhibiting generation of tumor metastasis, and can be applied to preparation of medicaments for treating tumor metastasis.

Description

technical field [0001] The invention belongs to the field of pharmacy, and mainly relates to the medical application of schisandra B in the preparation of NADPH oxidase (nicotinamide adenine dinucleotide phosphate oxidase) inhibitor. Background technique [0002] Schisandrin B is the biphenylcyclooctene lignan with the highest content in the traditional Chinese medicine Schisandra chinensis. Many studies have found that schisandra B can protect many tissues and organs, including the heart, liver, kidney, brain and skin, from free radical damage. [0003] NADPH oxidase is a class of proteins that can transfer electrons in biological membranes. Roughly speaking, oxygen molecules (O 2 ) is the electron acceptor, and the product of the electron transfer reaction is superoxide ion (?O 2- - ). Superoxide ion (?O 2- - ) will be further converted into hydroxyl radicals (HO?), peroxyl radicals (ROO?), alkoxylated radicals (RO?), hydroxyl peroxyl radicals (HOO?) in cells, and s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/36A61P35/04A61P35/00A61P11/00A61P25/00A61P9/00
Inventor 胡汛张彪刘振高锦明
Owner ZHEJIANG UNIV
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