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LA-GFLG-DOX conjugate, preparation method and use thereof

A technology of LA-GFLG-DOX and conjugates, applied in the field of LA-GFLG-DOX conjugates and their preparation, to achieve the effect of reducing damage and reducing side effects

Active Publication Date: 2019-09-03
CAPITAL UNIVERSITY OF MEDICAL SCIENCES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no report on conjugates that modify LA at one end of GFLG to reduce the side effects of DOX.

Method used

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  • LA-GFLG-DOX conjugate, preparation method and use thereof
  • LA-GFLG-DOX conjugate, preparation method and use thereof
  • LA-GFLG-DOX conjugate, preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] 1. Preparation of LA-GFLG-DOX conjugates

[0036] Synthetic route such as figure 1 Shown:

[0037] 1. Synthesis of Boc-GF-OMe

[0038]At room temperature, Boc-Gly-OH (10.0mmol) was dissolved in tetrahydrofuran, under ice-cooling, 1-hydroxybenzotriazole (10.0mmol) and 1-ethyl-(3-dimethylaminopropyl) carbonyl Diimine hydrochloride (10.0 mmol), reacted for 30 minutes. Continue to add HCl·Phe-OMe (10.0 mmol), adjust the pH value at 8-9 with N,N-diisopropylethylamine, and stir overnight at room temperature. After the reaction was completed, the solvent was spin-dried by a rotary evaporator, and the obtained oil was dissolved in 30 mL of ethyl acetate and transferred to a 100 mL separatory funnel. The ethyl acetate layer was washed with 50 mL of 5% NaHCO 3 Extract and wash three times, 50mL 5% NaHSO 4 Solution extraction and washing three times, 50mL saturated NaCl solution extraction and washing three times, 50mL 5% NaHCO 3 Extract and wash three times, extract and wa...

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Abstract

The invention relates to an antitumor drug, a preparation method and use thereof, which belong to the field of a medicine, and particularly discloses a LA-GFLG-DOX conjugate, a preparation method thereof and use thereof, and the LA-GFLG-DOX conjugate is a compound formed by sequential connection of lipoic acid, glycine, phenylalanine, leucine, glycine, and doxorubicin molecules through an amide bond. The conjugate retains the toxicity of DOX to tumor cells, and utilizes the antioxidant capacity of LA to resist damage to normal cells caused by reactive oxygen produced by DOX. From the anti-tumor activity test and the toxic side effects on normal cells, the LA-GFLG-DOX conjugate has a significant inhibitory effect on tumor cells, can reduce damage to normal cells, and reduces the toxic sideeffects of DOX.

Description

technical field [0001] The present invention relates to antineoplastic drugs in the field of medicine and their preparation methods and applications, in particular to a LA-GFLG-DOX conjugate and their preparation methods and applications. Background technique [0002] Lipoic acid (LA) is a naturally occurring antioxidant that belongs to the B vitamins. It has good fat solubility and water solubility, and can exert its antioxidant effect under both water-soluble and non-water-soluble conditions. Lipoic acid can be distributed in various tissues in the body, and it is also an indispensable antioxidant substance in the human body. It is called "universal antioxidant". The antioxidant capacity of lipoic acid is 400 times that of vitamin C and vitamin E. It has been approved as a functional ingredient of food and health products in the United States, Japan and other countries. In cells, lipoic acid mainly exists in the mitochondria of cells, which removes active oxygen such as ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/64A61K31/704A61K31/385A61P35/00C07K5/103C07K1/08C07K1/06
CPCA61K47/64A61K31/704A61K31/385A61P35/00C07K5/1008C07K19/00A61K2300/00Y02P20/55
Inventor 房晨婕支晓敏钱迪
Owner CAPITAL UNIVERSITY OF MEDICAL SCIENCES
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