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Application of tegaserod in preparation of antitumor drugs

An anti-tumor drug, the technology of tegaserod, applied in the field of medical applications, can solve problems such as difficult to meet the needs of patients, and achieve the effect of improving curative effect and prognosis

Pending Publication Date: 2020-10-27
QINGDAO HIGENE BIOPHARMACEUTICAL CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Tumor is currently the number one killer of human health and life, and current clinical medication is far from meeting the needs of patients. Anti-tumor drug development is an extremely important research direction in the field of current drug research and development

Method used

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  • Application of tegaserod in preparation of antitumor drugs
  • Application of tegaserod in preparation of antitumor drugs
  • Application of tegaserod in preparation of antitumor drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0085] Example 1 Tegaserod exhibits inhibitory activity in a constitutive STAT3 activated luciferase cell model.

[0086] Using a luciferase expressing cell model based on constitutive STAT3 activation (see Chinese Patent 1407357), it was found that tegaserod romanate has a significant inhibitory effect on STAT3, IC 50 5.06μM( figure 1 ).

Embodiment 2

[0087] Example 2 Tegaserod inhibits the activation of STAT3

[0088] Different concentrations of tegaserod were added to the normally cultured cells, and after 2 hours of action, the cell protein lysate was collected for protein immunoblotting detection, and the activation status of STAT3 was observed by the phosphorylation status of STAT3 Tyr705.

[0089] The results showed that Tegaserod in DU145( figure 2 A) and A549( figure 2 B) In the two constitutively activated cells of STAT3, both can inhibit the activation of STAT3 in a dose-dependent manner after 2 hours of drug treatment.

[0090] IL-6 is the main cytokine that activates STAT3 signaling. Hela cells were first treated with different concentrations of tegaserod for 2 hours, and then stimulated with 5ng / ml IL-6 for 10 minutes. The cells were harvested and the total protein was extracted. Western detection of STAT3 phosphorylation (Y705). Such as figure 2 As shown in C, in HeLa cells, tegaserod also inhibited the activatio...

Embodiment 3

[0091] Example 3 Tegaserod inhibits JAK kinase family activity.

[0092] STAT3 is usually activated by the phosphorylation of JAK kinase upstream of JAK kinase. Different concentrations of tegaserod were added to DU145 cells. After incubating for 2 hours, it was found that tegaserod at a concentration of 7.5μM could inhibit the phosphoric acid at JAK1 Tyr1022 / 1023 and JAK2 Tyr1007 / 1008 in DU145 cells. At a higher concentration (15μM), it also inhibits the phosphorylation of Tyr1054 / 1055 of TYK2 ( image 3 ). This indicates that tegaserod is an inhibitor of the JAK kinase family, which shows a higher affinity for JAK1 and JAK2 than TYK2. Tegaserod specifically inhibits the activation of JAK kinase, thereby down-regulating STAT3 phosphorylation in tumor cells.

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Abstract

The invention discloses an application of tegaserod or pharmaceutically acceptable salt thereof as a JAK-STAT3 signal channel inhibitor and an immunomodulator and an application of the tegaserod or the pharmaceutically acceptable salt thereof in preparation of antitumor drugs. The tegaserod and the pharmaceutically acceptable salt thereof have a very good inhibition effect on the growth of varioustumor cells in vivo and in vitro, and are expected to be used for treatment of various cancers.

Description

Technical field [0001] The invention belongs to the field of medical applications, and relates to a new medical use of tegaserod. Specifically, it is used as a JAK-STAT3 signal pathway inhibitor and immunomodulator, and can be used to prepare antitumor drugs. Background technique [0002] Tumors are currently the number one killer of human health and life, and current clinical drugs are far from meeting the needs of patients. The development of anti-tumor drugs is an extremely important research direction in the current drug development field. [0003] JAK-STATs signals in cells are crucial to the conduction of cell signals and various physiological activities. Abnormalities in this family of signals can lead to many diseases, including cancer and immune-related diseases. The JAKs family includes four members: JAK1, JAK2, JAK3 and Tyk2. The downstream STATs family of JAKs contains 7 members, of which STAT3 is an important family member, which is constitutively activated by abnorma...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/404A61P35/00A61P35/02
CPCA61K31/404A61P35/00A61P35/02A61K31/4045A61K9/0019A61K9/0053
Inventor 杨金波宋巧玲赵晨阳吴丽娟赵俊唐宇徐锡明
Owner QINGDAO HIGENE BIOPHARMACEUTICAL CO LTD
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