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Traditional Chinese medicine active component curcumenol derivative

A technology of active ingredient, curcumol, which is applied in the field of curcumitol derivatives, an active ingredient of traditional Chinese medicine, can solve problems such as gastrointestinal side effects, water and salt metabolism disorders, liver and kidney damage, etc., and achieve mild reaction conditions, enhanced pharmacological activity, and clinical application. wide range of effects

Pending Publication Date: 2021-08-06
TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Among them, non-steroidal anti-inflammatory drugs are the most commonly used adjuvant antirheumatic drugs to help relieve symptoms, but these drugs have limited therapeutic effects on RA and are likely to cause side effects such as gastrointestinal tract; common biological agents include TNF- α antagonists, but these drugs have the disadvantages of large side effects and high prices; glucocorticoids cannot cure RA, and many adverse reactions such as water and salt metabolism disorders will occur after long-term use; Chinese medicine and Chinese medicine preparations have their unique advantages in the treatment of RA. It has the characteristics of overall regulation, multi-level, and multi-target points, such as Qingfengmenine, total glucosides of paeony, triptolide, etc., which have certain curative effects but have toxic side effects such as liver and kidney damage

Method used

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  • Traditional Chinese medicine active component curcumenol derivative
  • Traditional Chinese medicine active component curcumenol derivative
  • Traditional Chinese medicine active component curcumenol derivative

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] A traditional Chinese medicine active ingreditial alcohol derivative, characterized in that the double bond of the ziglogloo alcohol is structurally modified, and a non-steroidal anti-inflammatory drug having a benzoic acid structure is combined to form a composite active molecule V;

[0019] The structural formula of the composite active molecule is as follows:

[0020]

[0021] The composite active molecular synthesis route is as follows:

[0022]

[0023] Preferably, R 2 From epoxy group, ibuprofen, diclofenac, aspirin, indomethacin, Boc-L-leucine, BOC-L-proline, benzoyl, and pagrated.

[0024] Preferably, preferred, compound III is prepared: rather rather ratio I (0.5116 g, 2.35 mmol), methacol (0.5186 g, 2.35 mmol), mixed with 1: 1, dissolved with dichloromethane, The mixture was stirred at room temperature for 4 h, TLC monitors, 10% NaOH was extracted three times, and the lower layer, CH2Cl2 layer was removed, and then a moderate amount of anhydrous sodium sulfate...

Embodiment 2

[0026] A traditional Chinese medicine active ingreditial alcohol derivative, characterized in that the double bond of the ziglogloo alcohol is structurally modified, and a non-steroidal anti-inflammatory drug having a benzoic acid structure is combined to form a composite active molecule V;

[0027] The structural formula of the composite active molecule is as follows:

[0028]

[0029] The composite active molecular synthesis route is as follows:

[0030]

[0031] Preferably, R 2 From epoxy group, ibuprofen, diclofenac, aspirin, indomethacin, Boc-L-leucine, BOC-L-proline, benzoyl, and pagrated.

[0032] Preparation method of Compound III: It is weighing extracondays I (0.5116 g, 2.35 mmol), alcohol peroxybenzoic acid (0.5186 g, 2.35 mmol), 1: 1 mixed, dissolved with dichloromethane, stirred at room temperature for 4 h The TLC was monitored, 10% NaOH was extracted three times, and the lower layer, CH2Cl2 layer was removed, and then a moderate amount of anhydrous sodium sulfate...

Embodiment 3

[0034] A traditional Chinese medicine active ingreditial alcohol derivative, characterized in that the outer double bond of the 术 类 类 外 改 改, 改 非 分 分 分 分 分 分 分 分 分 分 分 分 分 分V;

[0035] The structural formula of the composite active molecule is as follows:

[0036]

[0037] The composite active molecular synthesis route is as follows:

[0038]

[0039] Preparation method of Compound III: It is weighing extracondays I (0.5116 g, 2.35 mmol), alcohol peroxybenzoic acid (0.5186 g, 2.35 mmol), 1: 1 mixed, dissolved with dichloromethane, stirred at room temperature for 4 h , TLC monitoring, 10% NaOH extract three times, remove the layer, CH 2 CL 2 The layer is added to the dichloromethane layer to add an appropriate amount of anhydrous sodium sodium sulfate dry and place.

[0040] Preferably, the preparation method of Compound V: It is mixed with compound IV (50.9 mg, 0.20 mmol) and 2 times ibuprofen (88.3 mg, 0.43 mmol) for mixing, dissolved with dichloromethane (5 mL), stirred at ro...

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Abstract

The invention discloses a traditional Chinese medicine active component curcumenol derivative, curcumenol exocyclic double bonds are subjected to structural modification, and non-steroidal anti-inflammatory drugs with benzoic acid structures are combined with curcumenol to form two types of compounds. Curcumenol, which is very wide in clinical application, safe and low in toxicity is selected, an exocyclic double bond of curcumenol is structurally modified, the non-steroidal anti-inflammatory drug with a benzoic acid structure is combined with the curcumenol through an ester bond, the synthesis method is green and environment-friendly, the reaction condition is mild, heating is not needed, the reaction can be completed by stirring at room temperature for 3 hours, and high efficiency and high yield are achieved. The compound active molecules formed after modification can relieve the side effects of the non-steroidal anti-inflammatory drugs, and also can enhance the pharmacological activity of curcumenol.

Description

Technical field [0001] The present invention relates to the field of clause alcohol, and is specifically a Chinese medicine active ingredient ingurol derivative. Background technique [0002] The zero alcohol and its derivatives can significantly inhibit the expression of the fat polysaccharide induced with the expression of TNF-α, and the expression of TH cell IL-17A has an inhibitory effect, and is induced by collagen-induced mice The sexy (CIA) model verifies the efficacy of the 术 lycol on RA, further proves that the 醇 醇 is a potential health molecule for treating RA. However, due to the chemical inertness of the structure itself, the chemically modified site in the zone alcohol structure is very limited, and there is a relatively small report to the structure of the zero alcohol. [0003] The drug currently used to treat RA can be divided into four major categories, namely non-steroidal anti-inflammatory drugs, biological agents, glucocorticoids, and traditional Chinese medic...

Claims

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Application Information

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IPC IPC(8): C07D493/10A61P29/00A61P19/02
CPCA61P19/02A61P29/00C07B2200/07C07D493/10
Inventor 邱峰陈曦李凤云李阳李根张坚曹世杰彭绪玲郭雅静巩少轩
Owner TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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