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Application of 3'-methoxy benzyl-4-hydroxy-3,5-dimethoxy-benzoate in preparation of drugs for treating acute inflammation

A technology of methoxybenzyl and dimethoxy, applied in the field of inhibiting proteasome compounds, to reduce inflammation, increase survival rate, and aggravate inflammation

Inactive Publication Date: 2014-04-30
NANTONG REPAIR AIR CHEM BIOENG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Despite this, no well-developed proteasome compound inhibitors are available for the treatment of sepsis

Method used

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  • Application of 3'-methoxy benzyl-4-hydroxy-3,5-dimethoxy-benzoate in preparation of drugs for treating acute inflammation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] In vitro target enzyme of polypeptide inhibitor: IC50 value of tumor necrosis factor releasing enzyme (both purchased from sigma company).

[0016] The activity of TNF-releasing enzyme was detected by cleaving the fluorescent substrate Mca-Pro-Leu-Ala-Gln-Ala-Val-Dpa-Arg-Ser-Ser-Ser-Arg-NH (excitation wavelength = 320 nm, Emission wavelength = 405 nm). Reactions were performed in 100 μl reactions at 37°C. Add 4 μl of 3'-methoxybenzyl-4-hydroxy-3,5-dimethoxy-benzoate stock solution (1 ng / μl) to the reaction system at the beginning of the reaction for the final concentration of the substrate to 10 μM. The measured IC50 value was 6.09 μmol.

Embodiment 2

[0018] In Vivo Viability of Compound (3'-Methoxybenzyl-4-Hydroxy-3,5-Dimethoxy-benzoate) Examination Using Endotoxic Shock Model

[0019] Before establishing the endotoxic shock model, we first determined that the LD50 of LPS (E. coli 0111: B4, purchased from sigma company) mice was 50 μg per mouse, and we used 100 μg per mouse in the experiment , In this way, the mice in the control group can all die. A positive control experiment was done with Regasepin2. The mice in the control group were injected with 100 μg of LPS, while the mice in the Regasepin2 experimental group were injected with 0.7 mg of the compound 5 minutes after LPS injection. By making a Kaplan-Meier survival curve, it was found that Regasepin2 can effectively protect mice injected with 100 μg and improve the survival rate. After the endotoxin shock model was successfully established in mice, the in vivo activity of the compound was tested using the model. The mice in the control group (12) were injected wi...

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Abstract

The invention relates to the field of drugs, and particularly relates to a compound capable of inhibiting proteasomes and relieving damage of an acute inflammatory reaction to bodies. The compound has the molecular structure of 3'-methoxy benzyl-4-hydroxy-3,5-dimethoxy-benzoate, can increase the survival rate of endotoxic shock mice in in-vivo tests, and has potential new drug development value.

Description

technical field [0001] The invention relates to proteasome-inhibiting compounds and applications thereof, in particular to compounds capable of inhibiting proteasomes and alleviating damage to the body caused by acute inflammatory reactions. Background technique [0002] Sepsis has always been a serious medical problem. Early sepsis without timely and effective treatment can progress to severe sepsis and septic shock, with mortality rates of 20% to 30% and 40% to 70%, respectively. The medical community has been studying effective treatments, such as early symptomatic treatment, activated protein C, and corticosteroid treatment. In recent years, with the deepening of medical research, great progress has been made in the understanding and treatment of sepsis. Among them, the proteasome plays an important role in endotoxic shock. [0003] Proteasomes are ubiquitous in eukaryotes and archaea. In eukaryotes, proteasomes are located in the nucleus and cytoplasm. The main func...

Claims

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Application Information

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IPC IPC(8): A61K31/235A61P29/00A61P31/00
Inventor 姚炎华朱鹏葛亮刘晓磊奚年英
Owner NANTONG REPAIR AIR CHEM BIOENG
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