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Application of resorcin compound for preparing antitumor medicine

A technology of anti-tumor drugs and compounds, applied in the direction of anti-tumor drugs, active ingredients of hydroxyl compounds, drug combinations, etc., can solve the problems of no literature reports on anti-tumor effects, and achieve good anti-tumor effects

Inactive Publication Date: 2007-05-02
CENT SOUTH UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0024] There is no literature report that any of the above compounds have anti-tumor effect

Method used

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  • Application of resorcin compound for preparing antitumor medicine
  • Application of resorcin compound for preparing antitumor medicine
  • Application of resorcin compound for preparing antitumor medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Griffin inhibits the proliferation of a variety of tumor cell lines.

[0051] Grifolin was dissolved in DMSO, nasopharyngeal carcinoma cell line (CNE1) was treated with different concentrations of ghrifolin (0, 15, 20, 25, 33 and 43 μM), and detected by MTT (reference J.CancerRes . Clin Oncol.126 (2000) 448-454), 24 hours, 48 ​​hours and 72 hours after CNE1 inhibition, the results are shown in Figure 1.

[0052] Breast cancer cell lines (MCF7), cervical cancer cell lines (HeLa), colon cancer cell lines (SW480), Burkitt Lymphoma cell line (Raji), chronic myelogenous leukemia cell line (K562), and marmoset lymphoma cell line (B95-8) were detected by MTT, and the results are shown in FIG. 2 .

[0053] The IC50 of griffin was calculated by Bliss method, and the results are shown in Table 1.

[0054] Cell Lines

Embodiment 2

[0056] Griffin induces apoptosis in tumor cell lines.

[0057] Treat CNE1 cells with different concentrations of grifeline, use AO / EB double staining, and detect under a fluorescent microscope. It is found that different concentrations of grifeline can induce different degrees of apoptosis in CNE1 cells after 48 hours, as shown in Figure 5 . Among them, early apoptotic cells with nuclear pyknosis and marginalization were mainly seen at 30 μM induction, and late apoptotic bodies were rarely seen; while at 40 μM induction, not only early apoptotic cells with nuclear pyknosis and lateralization were seen, but also a large number of late apoptotic cells were seen. The production of corpuscles was induced by 50 μM. Since most of the cells had already detached, a large number of late apoptotic corpuscles and nuclear fragmentation could be seen mainly in the detached and suspended cells.

Embodiment 3

[0059] The apoptosis rate of tumor cell lines induced by griffin was detected by flow cytometry.

[0060] cell line

[0061] Tumor cell lines were treated with different concentrations of griffulin solutions, and the apoptosis rate was detected by flow cytometry and PI single staining. It was found that griffulin induced apoptosis in a variety of tumor lines in a dose-dependent manner. The results See Table 2. When the apoptosis rate of 0μM is below 4%, there is basically no apoptosis, and with the increase of the dose of griffin, the apoptosis rate gradually increases. At the dose of 50μM, the apoptosis rate of CNE1 induced apoptosis is as high as 81%. %, several other cell lines have also exceeded 50%, indicating that Griffin has a significant ability to induce apoptosis.

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Abstract

An application of the resorcin compounds in preparing antineoplastic medicines with high curative effect s disclosed.

Description

technical field [0001] The present invention relates to the medical use of diphenol compounds. technical background [0002] With the development of molecular biology and the in-depth study of the mechanism of tumorigenesis, people gradually realized that tumor is a kind of disease with abnormal signal transduction. During the development of tumors, due to the changes of various gene levels, the cells show many differences from normal cells in the signal transmission network, and some signal transduction pathways related to cell growth, division and proliferation are in an abnormally active state. , Some signal transduction pathways that should be activated in tumor cells, such as the apoptosis pathway, are often blocked in transmitting signals. Aiming at the key target molecules of the abnormal links in the signal transduction pathway, a large number of molecular targets available for drug intervention have been identified, and the anti-tumor drugs have been shifted from t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/05A61P35/00
Inventor 曹亚叶茂刘吉开
Owner CENT SOUTH UNIV
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