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Anti-cancer medicine containing low anticoagulant property heparin and taxol

A technology of hemagglutinating heparin and anti-cancer drugs, which can be applied in the directions of anti-tumor drugs, drug combinations, organic active ingredients, etc., and can solve the problems of limited application scope and poor solubility.

Inactive Publication Date: 2009-05-06
HUNAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0002] Paclitaxel is a drug with unique anticancer activity extracted from Taxus chinensis by American chemists in the 1960s. It is very effective in treating breast cancer and ovarian cancer. It has been widely used in clinical research in recent years, but due to its extremely poor solubility and other reasons limit its scope of application

Method used

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  • Anti-cancer medicine containing low anticoagulant property heparin and taxol
  • Anti-cancer medicine containing low anticoagulant property heparin and taxol
  • Anti-cancer medicine containing low anticoagulant property heparin and taxol

Examples

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preparation example Construction

[0023] (1) Preparation of oxyacetylated heparin

[0024] Weigh heparin sodium (250mg, 0.1mmol-OH), dissolve in 20mL deionized water, pass through 732 (H + ) cation exchange resin, and rinse with deionized water until the pH value is constant, the leachate is adjusted to a pH value of 6.0 with tributylamine, and the liquid is concentrated and freeze-dried to obtain tributylammonium heparin derivatives (500mg, 0.1mmol-OH ). in N 2 Dissolve it in 10ml DMF under protection, add DMAP (36mg, 0.3mmol) and acetic anhydride (1330mg, 13mmol) under stirring, then add triethylamine (1300mg, 13mmol), and react in ice bath for 30h, then transfer to React at room temperature for 24 hours. After the reaction is complete, add 200 mL of ice ethanol to the reaction solution, and magnetically stir for 1 hour to make it fully precipitate. After the solution is centrifuged, the supernatant is discarded, the precipitate is dissolved with a small amount of distilled water, and the liquid passes th...

Embodiment 1

[0043]Oxyacetylated heparin n=5, wherein oxyacetylated carboxyl groups account for 53% of all carboxyl groups, the drug is Drugl, the drug loading is 25.4%, and the anticoagulant performance, that is, the potency is 25 U / mg. As a comparison, the anticoagulant performance of oxyacetylated heparin alone was 127 U / mg; the IC50 value of the half inhibitory concentration on MCF-7 cells was 0.65 μg / mL, and as a comparison, the half inhibitory concentration of single paclitaxel on MCF-7 cells The concentration IC50 value is 4.2μg / mL.

Embodiment 2

[0045] Oxyacetylated heparin n=5, wherein oxyacetylated carboxyl groups account for 53% of all carboxyl groups, the drug is Drug2, the drug loading is 16.3%, and the anticoagulant performance, that is, the potency is 17 U / mg. As a comparison, the anticoagulant performance of oxyacetylated heparin alone was 127 U / mg; the IC50 value of the half inhibitory concentration on MCF-7 cells was 0.42 μg / mL, while as a comparison, the half inhibition of single paclitaxel on MCF-7 cells The concentration IC50 value is 4.2μg / mL.

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Abstract

The invention discloses an anticancer medicament of heparin-taxol with low hemagglutinating resistance, which relates to a chemical bonding type anticancer medicament. The heparin-taxol medicament is prepared by heparin derivatives and taxol or taxol derivatives by the chemical bonding method, and the anticancer medicament not only has the blood-clot resistance lower than the heparin, but also has the anticancer property stronger than pure taxol medicaments.

Description

technical field [0001] The present invention relates to a chemically bonded anticancer drug with low anticoagulation performance and strong anticancer performance. Background technique [0002] Paclitaxel is a drug with unique anticancer activity extracted from Taxus chinensis by American chemists in the 1960s. It is very effective in treating breast cancer and ovarian cancer. It has been widely used in clinical research in recent years, but due to its extremely poor solubility And other reasons limit its scope of application. my country's Yunnan, Shaanxi, Heilongjiang and other places have cultivated large areas of yew forests, which are rich in natural resources. The study of nano-anticancer targeted drugs with paclitaxel as the active ingredient is conducive to the utilization of my country's natural resources and provides a source for my country's in-depth development of paclitaxel. a new way. The chemically bonded nano-targeted anticancer drug system is to wrap the dru...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K31/337A61K31/727A61K47/36A61P35/00A61K47/61
Inventor 向建南刘承斌王莺
Owner HUNAN UNIV
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