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Target hydrophilic polymer-triptolide conjugate

The technology of a hydrophilic polymer and triptolide is applied in the direction of drug combinations, organic active ingredients, and medical preparations of non-active ingredients. Reduce toxicity and ensure the effect of drug concentration

Inactive Publication Date: 2014-05-28
BEIJING FORESTRY UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The pure product of triptolide is white columnar crystal, almost insoluble in water, and has great toxic and side effects
These shortcomings have greatly hindered its further promotion in clinical application.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Synthesis of folic acid-α-polyglutamic acid-triptolide conjugate (1): 50 mg triptolide, 5 mg folic acid, 0.2 g α-polyglutamic acid (Mw 30,000) dissolved in 10 ml anhydrous To N,N-dimethylformamide, add 30 mg of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide, 30 mg of N-hydroxysuccinimide, and 5 mg of 4- Dimethylaminopyridine was stirred at room temperature and reacted overnight. Add 30 ml of chloroform to the solution, filter to obtain a solid, and dissolve in NaHCO 3 The saturated solution is dialyzed and the product is freeze-dried. Obtain folic acid-α-polyglutamic acid-triptolide (1).

[0049]

[0050] (1).

Embodiment 2

[0052] Synthesis of folic acid-γ-polyglutamic acid-triptolide conjugate (2): 50 mg triptolide, 5 mg folic acid, 0.2 g γ-polyglutamic acid (Mw 30,000) dissolved in 10 ml anhydrous To N,N-dimethylformamide, add 30 mg of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide, 30 mg of N-hydroxysuccinimide, and 5 mg of 4- Dimethylaminopyridine was stirred at room temperature and reacted overnight. Add 30 ml of chloroform to the solution, filter to obtain a solid, and dissolve in NaHCO 3 The saturated solution is dialyzed and the product is freeze-dried. Get folic acid-γ-polyglutamic acid-triptolide (2)

[0053]

[0054] (2).

Embodiment 3

[0056] Synthesis of folic acid-γ-polyglutamic acid-glycine-triptolide conjugate (3): 50 mg triptolide, 50 mg Boc-glycine dissolved in 10 ml of anhydrous methylene chloride, at 0 °C Add 50 mg of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide and 10 mg of 4-dimethylaminopyridine, stir to dissolve for 2 hours, and wash the product with 10 ml of 0.5% sodium bicarbonate. Twice, wash with 10ml of water once, wash with 10ml of 0.1N hydrochloric acid solution twice, and wash with 10ml of saturated saline once, and finally dry with anhydrous magnesium sulfate, filter to remove insolubles, dry the solution in vacuo, and dissolve the obtained solid in 5ml 4M dioxane hydrochloric acid solution, stirred at room temperature for 1 hour, added 50 ml of ether, filtered the solid and dissolved in 10 ml of dichloromethane, adjusted the pH to 2.5 with saturated sodium bicarbonate, and used anhydrous carbonic acid for the organic phase After drying over magnesium, the product was dissolved in 5 ml o...

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Abstract

The invention provides a target hydrophilic polymer-triptolide conjugate (I), wherein P represents a water-soluble polymer; D represents triptolide; T represents a target molecule; and L and Z represent linking groups. The conjugate improves water solubility of triptolide, reduces toxicity of triptolide and prolongs circulating half-life period of triptolide in a living body.

Description

technical field [0001] The invention relates to a targeted water-soluble polymer-triptolide conjugate and a preparation method thereof, in particular to a folic acid compound-polyglutamic acid-triptolide prodrug and a preparation method thereof. Background technique [0002] Tripeterygium wilfordii (Tripeterygium wilfordii) is a plant belonging to the genus Maureaceae. This genus is mainly distributed in Zhejiang, Hunan, Anhui, Fujian, Guangdong, Guangxi, Yunnan and other provinces south of the Yangtze River Basin in China and the Changbai Mountain area in Northeast China. This product has been circulated among the people as a herbal medicine for a long time. The main medicinal part is the root, which has the functions of promoting blood circulation and eliminating addiction, clearing away heat and detoxification, reducing swelling and dissipating stagnation, killing insects and stopping bleeding, etc., but it is poisonous. In recent years, studies have shown that Tripteryg...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K31/585A61K47/22A61P35/00
Inventor 雷建都戴林何静邓丽红刘静王潞莹
Owner BEIJING FORESTRY UNIVERSITY
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