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Deacetylcedilan glucosyl modified compound liposome and its application

A deacetylcedilan, glucose-based technology, applied in the directions of steroids, drug combinations, organic chemistry, etc., can solve the problems of shortened maintenance time, reduced anticancer activity titer, high risk of anticancer application, etc. Enhanced inhibition rate, reduced arrhythmia, prolonged anti-cancer effect

Active Publication Date: 2021-05-14
GUILIN MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, deacetyl cedilan (cedilan) can lose glucose and acetic acid through hydrolysis in the body, and form digoxin with almost no anti-hepatic effect, which reduces the anticancer activity of deacetyl cedilan and maintains its effect. shortening of time
In addition, due to the prevalent cardiotoxicity of cardiac glycosides, their anticancer application is risky

Method used

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  • Deacetylcedilan glucosyl modified compound liposome and its application
  • Deacetylcedilan glucosyl modified compound liposome and its application
  • Deacetylcedilan glucosyl modified compound liposome and its application

Examples

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Embodiment Construction

[0036] The anti-cancer experiments of the above drugs in vivo and in vitro are carried out by establishing in vitro cell culture and in vivo animal models. The experimental method includes the following steps:

[0037] ① Carry out the culture of cancer cells and normal cells;

[0038] ②Comparison of deacetylated cedilan glucosyl-modified compound and cedilan in vitro anti-cancer and toxicity to normal cells;

[0039] ③Establish a nude mouse animal model of liver cancer, and carry out in vivo anti-cancer comparative experiments between deacetylated cedilan glucosyl-modified compound liposomes and cedilan liposomes;

[0040] ④Evaluation of acetylated cedilan glucosyl-modified compound liposome and cedilan cardiotoxicity.

[0041] 1. In vitro anticancer experiment

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Abstract

The invention discloses a deacetylcedilan glucosyl modified compound liposome and application thereof. It is mainly modified from the glucosyl group of cedilan, using glucose and 2-glucosamine as raw materials for partial modification of the molecule, and then connecting with the terminal 3-hydroxyl of digoxin to generate a glucosyl-modified product of deacetyl cedilan. Select the desired molecule under the activity guide. By synthesizing deacetylated cedilan glucosyl-modified compounds (2‑O‑benzyl‑β‑D‑glucopyranoside‑deacetyl cedilan, etc.), to strengthen the anticancer effects of these compounds and improve efficacy Increase the potency and prolong the half-life. At the same time, the modified compound is prepared into liposomes to improve its liver targeting effect and reduce cardiotoxicity.

Description

technical field [0001] The invention relates to a modified compound, in particular to a new compound obtained by chemically modifying the traditional drug deacetylcedilan for the treatment of heart failure, and its application in anti-cancer after modification of liposome dosage form, namely deacetylcedilan chemical Modified into deacetylcedilan glucosyl modified compound (2-O-benzyl-β-D-glucopyranoside-deacetylcedilan) and prepared into liver targeting liposomes in anti-liver cancer drugs Applications. Background technique [0002] Among the common cancers in the world, the incidence of liver cancer ranks seventh, and the incidence of cases in China exceeds 50% of the global total, despite the adoption of treatment methods including tumor resection, liver transplantation, sorafenib and local therapy (radiofrequency ablation) However, the mortality rate of liver cancer has not decreased yet. Therefore, the development of high-efficiency and low-toxicity anti-liver cancer dr...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J63/00A61K31/56A61P35/00A61P1/16A61K9/50A61K9/10A61K47/36
Inventor 谭宁徐庆潘光玉秦永俊陈果
Owner GUILIN MEDICAL UNIVERSITY
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