Mono-tetrahydrofuran type sugar apple lactone compound with anti-tumor activity and application thereof

A tetrahydrofuran-type, annona lactone technology, applied in the direction of antineoplastic drugs, organic active ingredients, medical preparations containing active ingredients, etc., can solve the problems of large toxic and side effects, high price, poor tolerance of patients, etc., to achieve Strong antitumor activity and low toxicity

Inactive Publication Date: 2011-05-25
NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In many countries including China, especially moderately developed countries, the death caused by malignant tumors accounts for the first or second place among all causes of death, and the incidence rate is still on the rise worldwide. Among the four major therapies of chemotherapy, chemotherapy and biological therapy, chemotherapy is still the main treatment method, but as we all know, the existing chemotherapy drugs have limited anti-tumor activity, high toxicity and side effects, poor patient tolerance, and high prices

Method used

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  • Mono-tetrahydrofuran type sugar apple lactone compound with anti-tumor activity and application thereof
  • Mono-tetrahydrofuran type sugar apple lactone compound with anti-tumor activity and application thereof
  • Mono-tetrahydrofuran type sugar apple lactone compound with anti-tumor activity and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1 Preparation of Monotetrahydrofuran Anemone Lactone Compound (Amoxime Promethazine)

[0032] Take 10 kilograms of dried custard apple seeds, percolate with chloroform after crushing, reclaim and combine the percolation liquid, filter, and reclaim the filtrate under reduced pressure to obtain 1 kg of concentrated solution, and the concentrated solution is separated by column chromatography with normal phase silica gel, and separated by petroleum ether-acetic acid Gradient elution with ethyl ester-methanol, a total of 400 fractions were collected, combined into five fractions (F1-F5) according to thin-layer chromatography, and F2 (63 g) was separated by normal-phase silica gel column chromatography, and petroleum ether -Ethyl acetate (20:1~0:1) gradient elution, divided into 8 parts (F6~F13) according to thin-layer chromatography, and the precipitates of the combined liquid of F9 were recrystallized from petroleum ether-ethyl acetate to obtain The compound anoxam...

Embodiment 2

[0036] Example 2 Acute Toxicity Test of Anoxetizumab

[0037] Calculate the half lethal dose LD of mice according to Bliss method 50 value, and the measurement results are shown in Table 2:

[0038] Table 2 Acute Toxicity Test Data of Anoxetrim

[0039]

[0040] LD obtained from the experiments in Table 2 50 value, indicating that the acute toxicity of the compound Anoxetizumab provided by the present invention is relatively low, and the toxicity of the compound Anoxetizumab administered orally in the route of administration is minimal.

Embodiment 3

[0041] Example 3 Inhibitory Effect of Anoxetizumab on Human Tumor Cells in Vitro

[0042] Using 5 tumor lines of human lung cancer (MCF-7), breast cancer (A-5408), human liver cancer (SMMC-7451), human cervical cancer (Hela) and human gastric cancer (SGC-7901), the thiazolyl blue reduction method ( MTT) for in vitro anti-tumor experiments, the compound Anoxamethoxamine was set at 5 concentrations, taxol (Taxol) was used as the positive control group, and the solvent of the sample, namely dimethyl sulfoxide, was used as the negative control group. The mice used were clean-grade Kunming mice. From the experimental results in Table 3, it can be seen that the compound Anoxamethoxam has different inhibitory effects on 5 strains of human tumor cells, and the in vitro anti-tumor experimental data show that the compound Anoxamol provided by the present invention shows It has strong anti-tumor activity, among which it has stronger tumor cell selection inhibitory activity on lung cance...

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Abstract

The invention discloses a new mono-tetrahydrofuran type sugar apple lactone compound with anti-tumor activity, through systematic in-depth research of chemical ingredients of sugar apple seeds, the analysis of wave spectrum and mass spectrum data shows that the new mono-tetrahydrofuran type sugar apple lactone compound (Anno Shikemominbing) can be separated from the sugar apple seeds, in vivo and in vitro anti-tumor activity researches show that mono-tetrahydrofuran type sugar apple lactone provided by the invention has very strong anti-tumor activity for a variety of tumor cells, including lung cancer, breast cancer, liver cancer, cervical cancer and gastric cancer, and the toxicity test research shows that the mono-tetrahydrofuran type sugar apple lactone compound with the anti-tumor activity provided by the invention is expected to be developed into new anti-tumor medicaments.

Description

technical field [0001] The invention relates to a compound with antitumor activity, in particular to a novel monotetrahydrofuran type anemone lactone compound with antitumor activity and its application in preventing and treating tumor diseases, belonging to the technical field of medicine. Background technique [0002] Malignant tumors are frequent and common diseases that seriously endanger human health and life. As early as 2000-3000 years ago, there were records about tumors in Egypt and my country. In many countries including China, especially moderately developed countries, the death caused by malignant tumors accounts for the first or second place among all causes of death, and the incidence rate is still on the rise worldwide. Among the four major therapies of chemotherapy, chemotherapy, and biological therapy, chemotherapy is still the main treatment method, but as we all know, the existing chemotherapy drugs have limited anti-tumor activity, large toxic and side ef...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D307/58A61K31/365A61P35/00
Inventor 李祥陈勇陈建伟
Owner NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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