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Application of physalis a in the preparation of jak2-stat3 signaling pathway inhibitors and antitumor drugs

An anti-tumor drug, Physalis, which is applied in the field of anti-tumor drugs, can solve the problems of less research on anti-tumor mechanisms and achieve good anti-tumor activity

Active Publication Date: 2015-10-28
浙江美新控股有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Physalis A is an active compound extracted from Jindeng. At present, there are few studies on the anti-tumor mechanism of Physalis A, and there are only a few reports in the literature. For example, Physalis A activates the death receptor pathway and further activates the downstream Apoptotic proteins caspase-3 and caspase-8, and then induce the apoptosis of fibrosarcoma cell HT1080 (J Nat Prod.2013May24;76(5):880-8.); Physalis A activates the tumor suppressor gene p53- NOXA pathway, produces ROS and induces apoptosis of melanoma cell A375-S2 (J Ethnopharmacol.2013Jul9;148(2):544-55.)

Method used

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  • Application of physalis a in the preparation of jak2-stat3 signaling pathway inhibitors and antitumor drugs
  • Application of physalis a in the preparation of jak2-stat3 signaling pathway inhibitors and antitumor drugs
  • Application of physalis a in the preparation of jak2-stat3 signaling pathway inhibitors and antitumor drugs

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0074] Dry the persistent calyx (10.0kg) of the Physalis plant hanging golden lamp, and use 8 times the amount of 95% ethanol aqueous solution (80kg) to reflux extract 3 times, each time for 2 hours, and recover the obtained ethanol extract The extract can be obtained after there is no alcohol smell. The medicinal extract was dissolved in 3L of hot water, extracted 4 times with 1L of petroleum ether, 1L of dichloromethane and 1L of ethyl acetate successively to obtain the total sample of each extraction layer (30.5g of petroleum ether layer, Dichloromethane layer 160.0g, ethyl acetate layer 46.7g).

[0075] The dichloromethane layer (160.0g) was separated by silica gel column chromatography, and eluted sequentially with the dichloromethane / methanol elution system, and the elution gradients were 5, respectively 100:1, 50:1, 30:1, 20 :1 and 10:1 (dichloromethane to methanol volume ratio), Fr.1-55 fractions were obtained.

[0076] The Fr.2 fraction was separated by preparative ...

Embodiment 2

[0077] Example 2: Physalis A inhibits the JAK2 kinase 1007 / 1008 tyrosine (Tyr1007 / 1008) of human non-small cell lung cancer cell NCI-H292, and the phosphorylation level of JAK2 and its inhibitory effect are concentration- and time-dependent decline.

[0078] Such as figure 1 Shown: 5-15 μM Physalis A can inhibit the phosphorylation level of JAK2 in NCI-H292 cells in 4 hours, and 15 μM Physalis A can obviously inhibit the phosphorylation level of JAK2 in NCI-H292 cells in 2-4 hours. Phosphorylation level, its inhibition degree was time- and concentration-dependent, but physalicin A had no change on the expression of JAK2 total protein.

[0079] The experimental method is as follows:

[0080] NCI-H292 cells were cultured according to standard methods, and the medium used was RPMI1640 containing 10% FBS (GIBCO). When the cells grow to 70%-80%, add different concentrations of Physalis A to the culture medium, 37℃5%CO 2 Incubate in an incubator (Thermo), and after 4 hours of dr...

Embodiment 3

[0081] Example 3: The effect of physidin A on the phosphorylation level of Src kinase and the expression level of phosphatase SHP1 in human non-small cell lung cancer cell NCI-H292.

[0082] Such as figure 2 Shown: 15 μM Physalis A acts on NCI-H292 cells, and it has no significant effect on the phosphorylation level of the kinase Src upstream of STAT3 and the expression level of the phosphatase SHP1.

[0083] Experimental method is the same as embodiment 2.

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Abstract

The invention discloses an application of physalin A in preparation of a JAK2-STAT3 signal channel inhibitor and an antitumor drug. The physalin A is a compound with a structure shown in a formula I. The JAK2-STAT3 signal channel inhibitor can inhibit various tumor cells. As the JAK2-STAT3 is abnormally activated to lead to uncontrollable growth of tumor and apoptosis resistance of tumor cells, tumor cell proliferation is further inhibited and tumor cell apoptosis is further induced. The physalin A can be applied to preparation of the antitumor drug. The physalin A is combined with the chemotherapeutic drug (cis-platinum) can remarkably inhibit tumor cell proliferation so as to realize the purpose of enhancing effect and reducing toxicity. Particularly, the physalin A and cis-platinum combined in use to prepare the antitumor drug troches can generate a very strong synergistic effect, and the antitumor drug troches prepared have very good antitumor activity.

Description

technical field [0001] The invention relates to the field of antitumor drugs, in particular to the application of Physicine A in the preparation of JAK2-STAT3 signaling pathway inhibitors and antitumor drugs. Background technique [0002] Malignant tumors are major diseases that seriously endanger human life and health. In recent years, the morbidity and mortality of most tumors have been on the rise. Surgical treatment, chemotherapy, and radiotherapy are the main means of treating tumors at present, but most tumor patients are already in the middle and advanced stages and lose the chance of surgery. Survival rate and survival time, and bring great misery to the patient, and its quality of life is obviously reduced. Therefore, the development of specific, efficient and safe tumor-targeted drugs is the current research direction. [0003] Signal transducers and transcription activators 3 (STAT3 for short) is an important nuclear transcription factor that regulates tumor cel...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/366A61P35/00A61K33/24
Inventor 陈喆朱凡凡余立雁马忠俊
Owner 浙江美新控股有限公司
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