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Application of 2(ammonia alkyloxy) phenyl pentadiene ketone compound in preparation of drugs for treating chemical ache and/or immunologic injury

A technology of phenylpentadienone and aminoalkoxy, which is applied in the field of medicine and can solve problems such as easy dependence and reduced curative effect

Inactive Publication Date: 2011-11-02
WENZHOU MEDICAL UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The treatment of pain and immune damage usually uses drugs such as morphine and hormones, but it is prone to dependence and the curative effect will gradually decrease

Method used

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  • Application of 2(ammonia alkyloxy) phenyl pentadiene ketone compound in preparation of drugs for treating chemical ache and/or immunologic injury
  • Application of 2(ammonia alkyloxy) phenyl pentadiene ketone compound in preparation of drugs for treating chemical ache and/or immunologic injury
  • Application of 2(ammonia alkyloxy) phenyl pentadiene ketone compound in preparation of drugs for treating chemical ache and/or immunologic injury

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Example 1 Synthesis of two (aminoalkoxy) phenyl pentadienone compounds

[0044] Synthetic general method: Dissolve 10 mmol of substituted benzaldehyde in 10 mL of absolute ethanol, stir at room temperature for 5 min, then add the corresponding ketone, continue stirring for 10 min, the solution remains unchanged. Sodium metal was dissolved in methanol to prepare 18% (w / v) sodium methoxide / methanol solution. Slowly add 1.5 mL of the sodium methoxide solution (containing 5 mmol of sodium methoxide) into the reaction solution. After stirring for 2 hours, a large amount of insoluble yellow matter appears. The reaction solution is detected by TLC, and the purple color of substituted benzaldehyde no longer appears under a 320nm ultraviolet lamp. Spots, the product spots are clear and yellow. Stop the reaction, filter the reaction solution, wash the product with water first, then wash twice with ice ethanol and ice acetone, and dry in vacuum at 30°C overnight to obtain a yello...

Embodiment 2

[0047] Example 2 Compounds A12 and C12 inhibit the production of IL-12, IL-1β and COX-2 (cyclooxygenase-2) mRNA in primary macrophages induced by LPS (lipopolysaccharide)

[0048] 1.2×10 6 Primary mouse macrophages were cultured at 37°C with 1640 culture medium. After 24 hours, the culture medium was renewed and different concentrations of compounds were added for pretreatment for 2 hours, and then treated with 0.5 μg / ml LPS for 6 hours, and the cells were collected and extracted. For total RNA, after reverse transcription, fluorescent quantitative PCR was used to detect the contents of IL-12, IL-1β and COX-2 mRNA, and β-actin mRNA was used as an internal reference to quantify genes. The result is as figure 2 As shown, compounds A12 and C12 significantly inhibited the increase of IL-12, IL-1β and COX-2 mRNA induced by LPS (there were significant differences, *p<0.05, **p<0.01).

Embodiment 3

[0049] Example 3 Injection of compounds A12 and C12 inhibits the mRNA expression of IL-1β, iNOS (inducible nitric oxide synthase), COX-2 and mPGES (membrane-associated prostaglandin synthase) in LPS-induced mouse liver tissue

[0050] In order to further confirm that compounds A12 and C12 can inhibit the expression of various cytokines and enzymes induced by LPS in vivo, we measured IL-1β, iNOS, COX-2 and mPGES in mouse liver tissue at the mRNA level by RT-qPCR. mRNA levels. C57BL / 6 mice were first intravenously injected with A12 or C12 (15 mg / kg), and the control group was injected with the same dose of normal saline, and 15 minutes later, LPS (10 mg / kg) was injected intravenously. After different time, the mice were killed, the liver tissue was homogenized, and the total RNA was extracted, and the content of these related mRNAs, such as iNOS, COX-2, IL-1β and mPGES, were detected by RT-qPCR technology, and Actin was used as the control Gene. The result is as image 3 show...

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Abstract

The invention belongs to the technical field of medicine, and specifically relates to the application of a 2(ammonia alkyloxy) phenyl pentadiene ketone compound in the preparation of drugs for treating chemical ache and / or immunologic injury. The 2(ammonia alkyloxy) phenyl pentadiene ketone compound can inhibit cells induced by lipopolysaccharide from generating IL-12, IL-1beta and / or cyclooxygenase-2 in vitro.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to the application of the medicine for treating mammalian chemical pain and / or immune injury, especially the derived method and the medicine kit. Background technique [0002] Many chemical substances can cause human lesions, such as chemical pain due to the abuse of some chemicals, and other chemical substances can cause excessive immune responses in the body, resulting in immune damage to the body. The treatment of pain and immune damage usually adopts drugs such as morphine and hormones, but it is prone to dependence, and the curative effect will gradually decrease. [0003] For this reason, the inventor has found several specific compounds from hundreds of bis(aminoalkoxy)phenylpentadienone compounds through long-term and in-depth research, which have the properties of treating mammalian chemical pain and immunity simultaneously. The role of injury, and no toxic sid...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/138A61P29/00A61P11/00A61P37/00
Inventor 梁广赵承光王怡俞聪聪李校堃
Owner WENZHOU MEDICAL UNIV
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