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Resveratrol hydrophilic conjugate, its preparation method and application

A technology of hydrophilic polymers and resveratrol, applied in chemical instruments and methods, carrier binding/immobilizing peptides, active ingredients of hydroxyl compounds, etc., can solve the problems of insufficient oral bioavailability of resveratrol

Inactive Publication Date: 2012-11-07
YANTAI TARGET DRUG RES +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Pharmacokinetic studies suggest that the oral bioavailability of resveratrol is less than 1%.
For small-molecule drugs, PEG can impart many of its excellent properties to the formed complex when modified, such as improving the water solubility of the modified drug, increasing biocompatibility, improving tissue distribution, reducing toxic effects, extending circulation half-life and Enhanced curative effect, etc., which makes many small molecule drugs with significant curative effect but limited clinical application due to their hydrophobicity and toxicity have new development prospects

Method used

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  • Resveratrol hydrophilic conjugate, its preparation method and application
  • Resveratrol hydrophilic conjugate, its preparation method and application
  • Resveratrol hydrophilic conjugate, its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0079] mPEG-CH 2 Dissolve 30g of COOH (5000) in dichloromethane, add 13.695g of resveratrol, 0.4106g of 1-hydroxybenzotriazole (HOBT), 0.466g of 4-dimethylaminopyridine (DMAP), add 30mL of DMF and N,N'-dicyclohexylcarbodiimide (DCC) 1.476g. React at room temperature overnight. Filter, concentrate, add 300 mL of isopropanol (IPA), and filter to obtain 27.5 g of a white product. The yield is 91.67%.

Embodiment 2

[0081] 4arm-PEG-CH 2 Dissolve 25g of COOH (10000) in dichloromethane, add 11.42g of resveratrol, 0.851g of 1-hydroxybenzotriazole (HOBT), 1.4434g of 4-dimethylaminopyridine (DMAP), add 80mL of DMF and N, N'-dicyclohexylcarbodiimide (DCC) 2.1266g. React at room temperature overnight. Filter, concentrate, add 200 mL of isopropanol (IPA), and filter to obtain 19.3 g of a white product. Yield 77.2%.

Embodiment 3

[0083] mPEG-OCH 2 CH 2 Dissolve 1 g of COOH (10000) in dichloromethane, add 228 mg of resveratrol, 6.5 mg of 1-hydroxybenzotriazole (HOBT), 14.5 mg of 4-dimethylaminopyridine (DMAP), add 2 mL of DMF and N , N'-dicyclohexylcarbodiimide (DCC) 212mg. React at room temperature overnight. Filter, concentrate, add 10 mL of isopropanol (IPA), and filter to obtain 0.74 g of a white product. Yield 74%.

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Abstract

The invention discloses a novel conjugate composed of a hydrophilic polymer and resveratrol, a pharmaceutical composition including the conjugate, their preparation methods and applications in the preparation of drugs for treating tumor, diabetes and cardio cerebrovascular disease, wherein the hydrophilic polymer is selected from the group consisting of polyethylene glycol, polyglutamic acid, polyaspartic acid, polypropylene glycol, polyvinyl alcohol, polypropylene morpholine, polyethylene glycol-amino acid oligopeptide and their copolymer. Through modification of the hydrophilic polymer, a bound drug can be protected, stability and water solubility of the conjugate are raised, and active period of the conjugate in organisms is prolonged.

Description

technical field [0001] The present invention relates to a novel conjugate of hydrophilic polymer and resveratrol, a pharmaceutical composition containing the conjugate, their preparation method and their role in the preparation of drugs for treating tumors, diabetes and cardiovascular and cerebrovascular diseases. use. Background technique [0002] Resveratrol (Resveratrol, RES) is a natural non-flavonoid polyphenol compound containing stilbene structure, chemical name is 3,4',5-trihydroxy-trans-stilbene (3,5,4' -trihydroxystilbene), was first isolated from the root of Veratrum grandiflorum O.Loes in 1940, and has since been found in more than 70 other plants, including the genus Vitis in the family Vitis and the genus Arachis in the family Fabaceae , Cassia, Veratrum of Liliaceae, and knotweed, bilberry, etc. [0003] [0004] Show 1 the chemical structural formula of resveratrol (RES) [0005] Resveratrol is known as a phytoalexin (antibacterial agent) and has a wide...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G65/48C08G69/48C07K17/08A61K47/48A61K31/05A61P3/10A61P9/00A61P35/00
Inventor 刘珂赵宣许卉马永婷邹晓丽黄文哲
Owner YANTAI TARGET DRUG RES
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