Preparation method of targeting folic acid-hydrophobic anticancer drug hydrogel

An anti-cancer drug, folic acid technology, applied in the preparation method of peptides, pharmaceutical formulations, anti-tumor drugs, etc., to achieve the effect of slow release of paclitaxel and simple synthesis

Inactive Publication Date: 2012-02-15
NANKAI UNIV
View PDF0 Cites 8 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, there have been no reports of using polypeptides to link hydrophobic anticancer drugs a...

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Preparation method of targeting folic acid-hydrophobic anticancer drug hydrogel
  • Preparation method of targeting folic acid-hydrophobic anticancer drug hydrogel
  • Preparation method of targeting folic acid-hydrophobic anticancer drug hydrogel

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] (1) For the synthesis of Fmoc-ss, see the attached instructions for the synthesis steps figure 1

[0022] The first step: the synthesis of ss

[0023] Take by weighing 10mmol (2.252g) Cystamine dihydrochloride and 30mmol (2.52g) sodium bicarbonate and dissolve it in the mixed solution of 90ml water and 35ml 1,4-dioxane to dissolve it, then weigh 10mmol (1.007g)1 , 4-succinic anhydride and dissolved in 3ml N,N-dimethylformamide, added to the above mixed solution, reacted overnight.

[0024] Step 2: Synthesis of Fmoc-ss

[0025] Weigh 10mmol (3.377g) fluorenyl methaneoxycarbonyl succinimide and dissolve it in 50ml acetone solution, slowly add the above reaction solution dropwise with a constant pressure funnel, react at room temperature for 4h, then filter to remove the white precipitate, and use a rotary evaporator Concentrate the filtrate by means of 1M hydrochloric acid to adjust the pH of the filtrate to acidity, separate out a white precipitate, let it stand for a...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

No PUM Login to view more

Abstract

The invention relates to a preparation method of small molecular hydrogel precursor molecules based on folic acid-anticancer drugs. The obtained compound is prepared into small molecular hydrogel by reducing disulfide bonds using reducing agents (glutathione and dithiothreitol). Specifically, the preparation method comprises the following steps of: firstly, synthesizing folic acid connected small peptides by a solid phase synthesis method, then derivatizing an anticancer drug (taxol, camptothecin, hydroxycamptothecine and the like) by butanedioic anhydride or glutaric anhydride to remove one carboxyl group, and connecting the folic acid connected small peptides with the derivatized anticancer drug. The precursor molecules not only have a targeting effect, but also have good solubility and are capable of self assembling into small molecular hydrogel by reduction of the disulfide bonds. The novel transmission system of the hydrophobic anticancer drug established by the invention not only greatly improves the solubility of the hydrophobic anticancer drug in water, but also is capable of targeting tumor tissues, thus reducing toxic side effects.

Description

technical field [0001] The technical solution of the present invention relates to a class of small molecule hydrogel precursor molecules based on folic acid and anticancer drugs, and the precursor molecules form a stable injectable small molecule under reducing agent (glutathione or dithiothreitol) conditions. Molecular hydrogel approach Background technique [0002] In 1963, American chemists Varney and Wall discovered that the bold substance of the western yew trunk had anti-tumor activity, but it was not until 1971 that they cooperated with Professor McFarr of Duke University to determine the structure of its active ingredient and named it for paclitaxel. This drug entered clinical research in 1983 and entered the Chinese market in 1994. It is a new anticancer drug, but it is very hydrophobic, so its clinical application is limited, that is, some co-solvents are often needed to dissolve it for administration. However, these co-solvents, such as polyoxyethylene castor o...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
IPC IPC(8): A61K9/00A61K47/48A61K31/337A61K31/4745C07D305/14C07K7/02C07K1/06C07K1/04C07K1/113A61P35/00
CPCY02P20/55
Inventor 杨志谋王玲杨成彪王怀民
Owner NANKAI UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap