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Application of a nitrophenyl ester sesquiterpene compound in the preparation of anti-inflammatory drugs

A technology of sesquiterpenoids and nitrophenyl esters, which can be used in anti-inflammatory agents, drug combinations, antipyretics, etc., and can solve the problems that biological activities have not been reported.

Active Publication Date: 2020-07-28
SOUTHERN MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Apart from this, other biological activities of FY11 have not been reported

Method used

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  • Application of a nitrophenyl ester sesquiterpene compound in the preparation of anti-inflammatory drugs
  • Application of a nitrophenyl ester sesquiterpene compound in the preparation of anti-inflammatory drugs
  • Application of a nitrophenyl ester sesquiterpene compound in the preparation of anti-inflammatory drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] An external transdermal absorption preparation of nitrophenyl sesquiterpenoid FY11, which contains 5 mg of nitrophenyl sesquiterpene FY11, an appropriate amount of petrolatum, an appropriate amount of liquid paraffin, and the structural formula of nitrophenyl sesquiterpene FY11 as follows:

[0024]

[0025] The preparation method is as follows: take the nitrophenyl sesquiterpene compound FY11 and put it in a mortar, add a small amount of liquid paraffin, grind it to a uniform and fine paste, then add vaseline step by step to the full amount, and grind until uniform.

Embodiment 2

[0027] Effects of nitrophenyl ester sesquiterpenoid FY11 transdermal preparation on carrageenan-induced acute arthritis

[0028] Take female C57BL / 6 mice about 8-10 weeks old, place them in a clean animal room in advance and adapt to the environment for a week, then divide the mice into blank group, model group, nitrophenyl ester sesquiterpenoid FY11 group and positive In the drug group, solvent ointment, 1% nitrophenyl ester sesquiterpene drug varnish, and positive control Voltaren emulsion were applied to the left and right hind limbs of the mice at the same time, once every 5 minutes, for 6 consecutive times. At 30 minutes after administration, 30 μl of 1% carrageenan was applied to the right hind paw s.c of each mouse to induce inflammation. After 5 hours, the mice were sacrificed, the thickness of the left and right toes of the mice was measured, and the mice's feet were cut symmetrically from the ankle joint, weighed, and the swelling degree of the mouse's feet was deter...

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Abstract

The invention discloses a nitrophenyl ester sesquiterpenoid compound FY11, a pharmaceutically acceptable derivative thereof or a prodrug thereof for preparing an anti-inflammatory drug. Nitrophenyl ester sesquiterpenoids FY11 has been proved to have a direct and significant inhibitory effect on inflammation, especially arthritis, so it can be used to prepare anti-inflammatory drugs and treat arthritis and other diseases.

Description

technical field [0001] The invention relates to the field of medicines, in particular to the application of nitrophenyl ester sesquiterpene compound FY11 in the preparation of anti-inflammatory drugs. Background technique [0002] Anti-inflammatory drugs are the second largest class of drugs in clinical practice after anti-infective drugs. Anti-inflammatory drugs currently used clinically can be roughly divided into: non-steroidal anti-inflammatory drugs, steroidal anti-inflammatory drugs. Non-steroidal anti-inflammatory drugs (NSAIDs) have antipyretic, analgesic, anti-inflammatory, and anti-rheumatic effects. Its pharmacological effects are mainly exerted by affecting the metabolites of arachidonic acid. With the increasing demand of NSAIDs, the side effects of digestive tract caused by them are becoming more and more prominent, especially in the gastrointestinal tract. Long-term use of traditional NSAIDs will inhibit the activity of COX-1 and reduce the synthesis of PGs...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/365A61P29/00A61P19/02C07D307/92
CPCA61K31/365A61P19/02A61P29/00C07B2200/07C07D307/92
Inventor 李晓娟谭艳辉邹斌华周雪峰
Owner SOUTHERN MEDICAL UNIVERSITY