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Annonaceous acetogenins compound with anti-tumor activity and application of annonaceous acetogenins compound

A technology of annona lactone and anti-tumor activity, applied in the field of medicine, can solve the problems of high toxicity and side effects, poor patient tolerance, high price, etc., and achieve the effect of strong anti-tumor activity

Inactive Publication Date: 2018-02-09
JIANGSU JIANKANG VOCATIONAL COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But as we all know, the existing chemotherapeutic drugs have limited anti-tumor activity, high toxicity and side effects, poor patient tolerance, and high prices.

Method used

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  • Annonaceous acetogenins compound with anti-tumor activity and application of annonaceous acetogenins compound
  • Annonaceous acetogenins compound with anti-tumor activity and application of annonaceous acetogenins compound
  • Annonaceous acetogenins compound with anti-tumor activity and application of annonaceous acetogenins compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] The preparation of embodiment 1 single tetrahydropyran type annonaceous lactone compound

[0027] Take 5 kilograms of dried custard apple seeds, percolate with chloroform after crushing, reclaim and combine the percolation liquid, filter, the filtrate is recovered under reduced pressure to obtain a concentrated solution, and the concentrated solution is separated by column chromatography with normal phase silica gel, and purified with petroleum ether-ethyl acetate Gradient elution, a total of 20 fractions were collected, according to thin-layer chromatography, kedde reagent (3,5-dinitrobenzoic acid) was used for color development, the 6th to 13th fractions were combined, separated by column chromatography on silica gel, and petroleum Ether-ethyl acetate (20:1~1:5) gradient elution, according to thin layer chromatography, kedde reagent (3,5-dinitrobenzoic acid) for color development, divided into 10 parts, take the 10th part The eluate was recrystallized from petroleum e...

Embodiment 2

[0034] Example 2 The Inhibitory Effect of Monotetrahydropyran-type Annonaceae Compounds on Human Tumor Cells in Vitro

[0035] Human gastric cancer (SGC-7901), human colorectal cancer (SW480), human lung cancer (MCF-7), breast cancer (A-5408), human liver cancer (SMMC-7451), human cervical cancer (Hela) and 5 types Tumor strain, adopt thiazolyl blue reduction method (MTT) to carry out in vitro anti-tumor experiment, the monotetrahydropyran type annonaceous lactone compound that embodiment 1 prepares is set 5 concentrations, take paclitaxel (Taxol) as 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 2, it can be seen that the single tetrahydropyran-type custard apple compound has different inhibitory effects on 6 strains of human tumor cells. Lactone compounds show strong antitumor activity.

[0036] Table 2 Inhibitory ...

Embodiment 3

[0038] The preparation of embodiment 3 tablet

[0039]Take the monotetrahydropyran-type annona lactone compound of the above-mentioned Example 1, add an appropriate amount of pharmaceutical excipients such as starch and magnesium stearate, mix thoroughly, and press into tablets to make each tablet containing 1 mg of the above-mentioned Anoxetine The tablet of C is used orally.

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Abstract

The invention discloses a novel monotetrahydropyrane annonaceous acetogenins compound with anti-tumor activity. Chemical compounds of an annonaceous seed are systematically and deeply researched; analysis of spectral data mass spectrometric data shows that one novel monotetrahydropyrane annonaceous acetogenins compound is separated from the annonaceous seed; an in-vitro anti-tumor activity research shows that the monotetrahydropyrane annonaceous acetogenins provided by the invention has extremely high anti-tumor activity for cells of various tumors including gastric cancer, intestinal cancer,lung cancer, breast cancer, liver cancer and cervical cancer, and is expected to be developed into an anti-tumor medicine.

Description

technical field [0001] The invention relates to compounds with anti-tumor activity, in particular to an annona lactone compound with anti-tumor activity and its application in preventing and treating tumor diseases, belonging to the technical field of medicine. Background technique [0002] Malignant tumors are frequently-occurring and common diseases that seriously endanger human health and life. In many countries including China, especially moderately developed countries, the death caused by malignant tumors ranks first or second among all causes of death. The incidence of cancer is on the rise. Among the four major therapies of tumor surgery, radiotherapy, chemotherapy, and biological therapy, chemotherapy is still the main treatment method. But as we all know, the existing chemotherapeutic drugs have limited anti-tumor activity, relatively high toxicity and side effects, poor patient tolerance, and are expensive. [0003] Annonaceae lactones are a class of natural comp...

Claims

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Application Information

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IPC IPC(8): C07D407/06A61K31/365A61P35/00
CPCC07D407/06
Inventor 杨海军张宁刘美辉曾庆琪张威
Owner JIANGSU JIANKANG VOCATIONAL COLLEGE
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