Application of bufanolide alkene compound in preparation of medicine or health care product for treating EGFR and/or STAT3 driven diseases

A technology of bufastenes and compounds, which is applied in the field of new applications of bufastenes, can solve the problems of unclear efficacy of tumors and limiting the value of anti-tumor medicines, so as to promote cytotoxicity, prevent cell cycle, and inhibit cell proliferation Effect

Active Publication Date: 2022-02-08
SHANGHAI JIAO TONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although bufastenoids have certain antitumor activity against a variety of tumors, it is not clear which type of tumors bufastenoids are effective for, which limits the antitumor medicinal value of these compounds

Method used

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  • Application of bufanolide alkene compound in preparation of medicine or health care product for treating EGFR and/or STAT3 driven diseases
  • Application of bufanolide alkene compound in preparation of medicine or health care product for treating EGFR and/or STAT3 driven diseases
  • Application of bufanolide alkene compound in preparation of medicine or health care product for treating EGFR and/or STAT3 driven diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0066] Bufadene compounds inhibit the proliferation of EGFR-overexpressing PTEN-deficient glioma cells.

[0067] figure 1 It reflects the inhibitory effect of eight bufadenoids on the proliferation of EGFR overexpressing glioma cells (U87MG-EGFR and U87MG-EGFRvIII) and control cells (U87MG and U87MG-PTEN). The modification of different sites on the nucleus affects the selectivity and activity of this type of compound. Comprehensive analysis shows that cinobufagin and cinobufotalin are more effective in inhibiting the proliferation of U87MG-EGFR and U87MG-EGFRvIII cells, while Less impact on other cells, better selectivity. The control DMSO had no inhibitory effect on the cells. **P<0.01.

Embodiment 2

[0069] Bufadene compounds induce apoptosis, cytotoxicity, arrest cell cycle and inhibit cell proliferation by inhibiting EGFR / STAT3 signaling pathway.

[0070] figure 2 It embodies the molecular mechanism of the bufasteine ​​compound cinobufagin to specifically inhibit the EGFR / STAT3 signaling pathway: the inhibitory effect of cinobufagin on the EGFR / STAT3 signaling pathway is dose-dependent and time-dependent, and DMSO without drugs The control has no effect on the EGFR / STAT3 signaling pathway;

[0071] image 3 It reflects the effects of bufasteine ​​compounds cinobufagin and esterbufagenin on specifically inducing the apoptosis and cytotoxicity of EGFR overexpressing glioma cells: cinobufagin induces apoptosis of U87MG-EGFR cells (caspase3 / 7 activity) and cytotoxicity (LDH release) were significantly stronger than those of the control cells U87MG-PTEN and MEF, and the cytotoxicity induced by cinobufagin in U87MG-EGFR was stronger than that of bufagenin;

[0072] Figur...

Embodiment 3

[0074] The bufasteine ​​compound cinobufagin inhibits the proliferation of EGFR-positive tumor cells by inhibiting the EGFR / STAT3 signaling pathway

[0075] Figure 5 It reflects the effect and mechanism of the bufasteine ​​compound cinobufagin on specifically inhibiting the proliferation of EGFR-positive and mutant lung cancer cells by inhibiting the EGFR / STAT3 signaling pathway. sex;

[0076] Image 6 It reflects the effect and mechanism of the bufasteine ​​compound cinobufacien to specifically inhibit the proliferation of EGFR-positive colorectal cancer cells by inhibiting the EGFR / STAT3 signaling pathway: the inhibitory effect of cinobufacien on the EGFR-positive cell HCT116 is significantly higher than that of the control cell SW620 ;

[0077] Figure 7 It reflects the effect and mechanism of the bufasteine ​​compound cinobufaginin specifically inhibiting the proliferation of EGFR-positive liver cancer cells by inhibiting the EGFR / STAT3 signaling pathway.

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Abstract

The invention discloses an application of a bufanolide alkene compound in preparation of a medicine or a health care product for treating EGFR (epidermal growth factor receptor) and/or STAT3 (signal transducer and activator of transcription 3) driven diseases. According to the present invention, the bufanolide alkene compound can significantly inhibit the phosphorylation of EGFR and STAT3 in vitro and in vivo, and can reduce the activity, such that the downstream signal molecules regulated by EGFR and STAT3 can be inhibited, the tumor cell apoptosis and cytotoxicity can be promoted, the cell cycle can be prevented, and the cell proliferation can be inhibited, and the obvious inhibition effect can be provided for the EGFR and/or STAT3 positive tumor; the bufanolide alkene compound has important research significance and application significance in developing medicines or health care products for treating or synergistically treating EGFR and/or STAT3 driven diseases by using the bufanolide alkene compound.

Description

technical field [0001] The invention belongs to the technical field of new applications of bufastenoids, and specifically relates to the application of bufastenes in the preparation of medicines or health care products for treating EGFR and / or STAT3-driven diseases. Background technique [0002] There are 3.929 million new cases of malignant tumors in the country every year, the incidence rate is as high as 285.83 / 100,000, and the number of deaths is about 2.338 million. The top five malignant tumors were lung cancer (572,600), breast cancer (452,900), gastric cancer (293,100), colorectal cancer (282,000), and liver cancer (269,200). The top five mortality rates are lung cancer (458,700), liver cancer (237,200), stomach cancer (211,600), esophageal cancer (136,800), and colorectal cancer (136,100). Brain tumors rank among the top ten in the incidence and mortality of malignant tumors in China. Gliomas account for more than two-thirds of brain cancers, and their overall surv...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/00A61K31/585A61P35/00A61P29/00A61P11/00A61P1/16
CPCA61K45/00A61K31/585A61P35/00A61P29/00A61P11/00A61P1/16
Inventor 周元飞何昆燕
Owner SHANGHAI JIAO TONG UNIV
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