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Application of Gamabufotalin and salt thereof in preparing medicament for treating gynaecologic tumor

A technology for bufatalin and gynecological tumors, which is applied to the application field of bufatalin and its salts in the preparation of medicines for treating gynecological tumors, can solve the problems such as the complex composition of toad preparations, and achieves strong anti-gynecological tumor effect. Convenient clinical application, clear effect of active ingredients

Inactive Publication Date: 2009-07-22
NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The technical problem to be solved by the present invention is to overcome the complex components of the current toad preparations, the high incidence of adverse reactions, provide clear components, controllable quality, and use bufabadine and its salts as active components to prepare the application of drugs for the treatment of gynecological tumor diseases

Method used

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  • Application of Gamabufotalin and salt thereof in preparing medicament for treating gynaecologic tumor
  • Application of Gamabufotalin and salt thereof in preparing medicament for treating gynaecologic tumor
  • Application of Gamabufotalin and salt thereof in preparing medicament for treating gynaecologic tumor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Example 1: Inhibitory effect of bufasterene extract, cinobufafelin, bufafalin, bufafalin or jenobufafalin on human ovarian cancer cell A2780.

[0029] According to the method of MTT experiment, the inhibitory effects of bufadene extract and four monomeric compounds cinobufagin, bufafelin, bufafetolin or jenobufafeline on human ovarian cancer cells (A2780) were investigated.

[0030] The experimental results showed that the bufasterene extract and the four monomeric compounds cinobufagin, bufafelin, bufafetalin or bufafetalin all had a strong inhibitory effect on human ovarian cancer cells (A2780). Each dose group showed a better dose-effect relationship, and bufafetobufalin showed better anti-human ovarian cancer cell (A2780) activity, and its IC50 value of 59.948nM was lower than that of other drug groups. The specific experimental results are shown in Table 1 and Table 2.

[0031] Table 1 The effect of bufasterene extract on human ovarian cancer cells (A2780)

[0032]...

Embodiment 2

[0035] Example 2: Inhibitory effect of bufasterene extract, cinobufagin, bufafelin, bufafetal or jenobufafeline on human ovarian cancer cells (SK-OV-3).

[0036] Inhibitory effects of bufadene extract and four monomeric compounds cinobufagin, bufafelin, bufafetolin or jenobufafeline on human ovarian cancer cells (SK-OV-3) were investigated according to the MTT assay method .

[0037] The experimental results showed that the bufasterene extract and the four monomeric compounds cinobufagin, bufafelin, bufafetolin or jenobufafeline all had a strong effect on human ovarian cancer cells (SK-OV-3). Inhibitory effect, each dose group showed a better dose-effect relationship, among which bufafetobufalin showed better activity against human ovarian cancer cells (SK-OV-3), and its IC50 value was 76.83nM less than that of other drugs Group. The specific experimental results are shown in Table 3 and Table 4.

[0038] Table 3 Effects of bufasterene extract on human ovarian cancer cells ...

Embodiment 3

[0042] Example 3: Inhibitory effect of bufadene extract, cinobufagin, bufafelin, bufafetal or jenobufafeline on human cervical cancer cells (SiHa).

[0043] Inhibitory effects of bufadene extract and four monomeric compounds cinobufagin, bufafelin, bufafetolin or jenobufafeline on human ovarian cancer cells (SK-OV-3) were investigated according to the MTT assay method .

[0044] The experimental results showed that the bufasterene extract and the four monomeric compounds cinobufagin, bufafalin, bufafalin or jenobufafeline all had strong inhibitory effects on human cervical cancer cells (SiHa). Dosage groups showed a better dose-effect relationship, among which bufafetoxin showed better activity against human cervical cancer cells (SiHa), and its IC50 value was 85.001nM which was lower than that of other drug groups. The specific experimental results are shown in Table 5 and Table 6.

[0045] Table 5 Effect of bufasterene extract on human cervical cancer cells (SiHa)

[0046...

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Abstract

The invention provides application of gamabufotalin and a salt compound thereof in preparation of a medicine for treating gynecological tumor. By comparing in vitro anti-cancer experiments of a bufadienolide extract and monomeric compounds, namely the gamabufotalin, cinobufagin, bufalin and bufotalin as well as hydrochlorides or sulfates of the four compounds to four gynecological tumors, namely human ovarian cancer cells A2780, human ovarian cancer cells SK-OV-3, human cervical carcinoma cells and human endometrial cancer cells, an experimental result shows that the gamabufotalin has stronger activity against gynecological tumor cells than the bufadienolide extract and the monomeric compounds, namely the cinobufagin, the bufalin and the bufotalin, and the hydrochloride or the sulfate of the gamabufotalin has stronger activity against gynecological tumor cells than the hydrochlorides or the sulfates of three compounds, namely the cinobufagin, the bufalin and the bufotalin. The gamabufotalin and the salt compound thereof provided by the invention have the advantages of clear components, controllable quality, strong anti-cancer activity, and small adverse reaction, and are expect to be developed into a novel anti-cancer drug.

Description

technical field [0001] The present invention relates to the new application of jenobufadyl and its salt, in particular to the application of jexafin and its salt in the preparation of medicines for treating gynecological tumors. Background technique [0002] Gynecological tumors are major diseases that endanger women's health. Common malignant tumors include endometrial cancer, cervical cancer, breast cancer, ovarian cancer, etc. The prevalence and mortality of cervical cancer in my country account for about one-third of the world. one. Treatment of gynecological tumors The treatment options routinely adopted by domestic and foreign medical circles are chemotherapy, radiation therapy and surgical resection. While achieving certain clinical curative effect, this program also brought patients serious medical problems due to the toxic and side effects of chemical drugs, radiation damage caused by radiotherapy, and iatrogenic problems and corresponding diseases caused by total o...

Claims

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Application Information

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IPC IPC(8): A61K31/585C07J19/00A61P35/00A61P15/00
Inventor 马宏跃段金廒周婧唐于平
Owner NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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