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Preparation method and application of triptolide-carboxylation chitosan coupling drug

A technology of carboxylated chitosan and triptolide, which is applied in the field of medicine, can solve the problems of short biological half-life, large toxic and side effects of triptolide, and poor water solubility, and achieve long biological half-life and significant economic and social benefits , the effect of simple method

Active Publication Date: 2019-03-15
HENAN UNIV OF CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] For above-mentioned situation, in order to overcome the defective of prior art, the purpose of the present invention is to provide a kind of preparation method and the application of triptolide-carboxylated chitosan coupling drug, can effectively solve triptolide toxic and side effect big, Problems of poor water solubility and short biological half-life

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  • Preparation method and application of triptolide-carboxylation chitosan coupling drug

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Embodiment 1

[0017] Embodiment 1: the preparation method of a kind of triptolide-carboxylated chitosan coupling drug of the present invention comprises the following steps: (1), the synthesis of intermediate carboxylated triptolide (TP-L3): 1800mg (5mmol) of triptolide was dissolved in 10ml of pyridine, then 1720mg (20mmol) of malonic anhydride and 122mg (1mmol) of 4-dimethylaminopyridine (DMAP) were added, under the protection of nitrogen, the reaction was carried out at room temperature for 24h, and 100mL of dichloromethane, then washed with saturated copper sulfate solution and water for 1-3 times, take the organic phase, dry the organic phase with anhydrous sodium sulfate, and then use a volume ratio of CH 2 Cl 2 :CH 3 The mixture of OH=20-15:1 was used as the mobile phase for silica gel chromatography column purification, and then recrystallized from dichloromethane-acetone-ether to obtain the hydroxyl-functional intermediate carboxylated triptolide (TP-L3) ;

[0018] (2), triptoli...

Embodiment 2

[0019] Embodiment 2: the preparation method of a kind of triptolide-carboxylated chitosan coupling drug of the present invention comprises the following steps: (1), the synthesis of intermediate carboxylated triptolide (TP-L4): 360mg (1mmol) of triptolide was dissolved in 5ml of pyridine, then 400mg (4mmol) of succinic anhydride and 24mg (0.2mmol) of 4-dimethylaminopyridine (DMAP) were added, under the protection of nitrogen, the reaction was carried out at room temperature for 24h, and 60mL of dichloromethane, and then washed with saturated copper sulfate solution and water for 1-3 times, take the organic phase, dry the organic phase with anhydrous sodium sulfate, and then use a volume ratio of CH 2 Cl 2 :CH 3 The mixture of OH=20-15:1 was used as the mobile phase for silica gel chromatography column purification, and then recrystallized from dichloromethane-acetone-ether to obtain the hydroxyl-functional intermediate carboxylated triptolide (TP-L4) ;

[0020] (2), triptol...

Embodiment 3

[0021] Embodiment 3: the preparation method of a kind of triptolide-carboxylated chitosan coupling drug of the present invention comprises the following steps: (1), the synthesis of intermediate carboxylated triptolide (TP-L5): Dissolve 900mg (2.5mmol) of triptolide in 10ml of pyridine, then add 912mg (8mmol) of glutaric anhydride and 62mg (0.5mmol) of 4-dimethylaminopyridine (DMAP), and react for 24h under nitrogen protection and stirring at room temperature , add 100mL of dichloromethane, and wash with saturated copper sulfate solution and water for 1-3 times respectively, take the organic phase, dry the organic phase with anhydrous sodium sulfate, and then use a volume ratio of CH 2 Cl 2 :CH 3 The mixture of OH=20-15:1 was used as the mobile phase for silica gel chromatography column purification, and then recrystallized from dichloromethane-acetone-ether to obtain the hydroxyl-functional intermediate carboxylated triptolide (TP-L5) ;

[0022](2), triptolide-carboxylated...

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Abstract

The invention discloses a preparation method and application of a triptolide-carboxylation chitosan coupling drug. The preparation method comprises the following steps: (1) synthesis of intermediate carboxylation triptolide (TP-L); and (2) synthesis of the triptolide-carboxylation chitosan coupling drug (TP-L-CChit). The triptolide-carboxylation chitosan coupling drug (TP-L-CChit) prepared by themethod, as a pro-drug, has application for preparing drugs for treating rheumatoid arthritis, tumors and Alzheimer's disease; the drug is simple in method, easy for production preparation, high in yield and rich and easily obtained in raw materials, the product is high in water solubility, long in biological half life period, high in availability, free of toxic or side effect and good in curativeeffect and is innovation for preparing drugs for treating rheumatoid arthritis, tumors and Alzheimer's disease, and the economic and social benefits are obvious.

Description

technical field [0001] The invention relates to medicine, in particular to a preparation method and application of triptolide-carboxylated chitosan coupling medicine. Background technique [0002] Triptolide (TPL), also known as triptolide and triptolide, is an epoxy diterpene lactone compound extracted from the roots, leaves, flowers and fruits of Tripterygium wilfordii, which has broad-spectrum anti-inflammatory properties. , Anti-tumor effect. Studies have shown that the 12,13-epoxy group in the molecular structure of triptolide is its main anti-inflammatory active structure, and the 9,11-epoxy-14β-hydroxyl structure is its effective anti-tumor molecular structure. Modern medical research has revealed that TPL can inhibit angiogenesis, slow down the formation of synovial pannus and synovial proliferation, reduce its erosion and damage to articular cartilage and bone, and play a therapeutic role in rheumatoid arthritis. In addition, TPL can also specifically regulate cer...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/61A61K31/585A61P29/00A61P35/00A61P19/02A61P25/28
CPCA61K31/585A61K47/61A61P19/02A61P25/28A61P29/00A61P35/00
Inventor 曾华辉张振强闫敏张岚宋军营袁永谢治深武香香
Owner HENAN UNIV OF CHINESE MEDICINE
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