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Application of picrolactone p in the preparation of antitumor drugs

An anti-tumor drug, the technology of ceramide lactone, which is applied in the field of anti-tumor drugs, can solve the problems of far-reaching differences in cancer treatment, achieve significant cell inhibition, broad application prospects, and the effect of inhibiting growth and proliferation

Active Publication Date: 2016-03-09
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

This technical scheme successfully extracts the compound with the structure of formula II that has cancer prevention effect, and it has been verified by preliminary tests that it has certain cancer prevention effect, but it is still far behind in cancer treatment

Method used

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  • Application of picrolactone p in the preparation of antitumor drugs
  • Application of picrolactone p in the preparation of antitumor drugs
  • Application of picrolactone p in the preparation of antitumor drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1: Preparation process of STAT3 inhibitor picrolactone P with anti-tumor activity.

[0032] 1) Put 1Kg of the persistent calyx of Phyllostachys chinensis into the extraction tank, add 95% ethanol aqueous solution (i.e. 5Kg of ethanol aqueous solution) containing 5 times of the weight of the persistent calyx of Phyllostachys dioica, each time, and extract under reflux at 90°C, The time of each extraction is 2h, a total of 4 extractions (ethanol aqueous solution totals 20Kg), and the combined extracts;

[0033]2) Concentrate the extract obtained in step 1) (recover ethanol) to nearly dryness to obtain 130 g of thick extract, which is diluted with 1 L of water and extracted with 1 L of ethyl acetate each time for a total of 3 extractions, and the extracts are combined;

[0034] 3) 20 g of the extract obtained by concentrating the extract obtained in step 2) is passed through a silica gel chromatographic column (wet column loading, dry loading), wherein the filler u...

Embodiment 2

[0037] Example 2: Kumarin P inhibits the phosphorylation level of Tyr705 (Tyr705) of STAT3 kinase in human gastric cancer cell HGC27, and its inhibitory effect decreases in a concentration-dependent manner.

[0038] experimental method:

[0039] Human gastric cancer cells HGC27 were grown in RPMI1640 medium containing 10% (wt) FBS (GIBCO) at 37°C in 5% CO 2 Incubator (Thermo) cultivation. When the cells grow to 70%-80%, intervene the cells with different concentrations of picrolactone P (0, 5 μM, 7.5 μM, 10 μM). After 4 hours of drug treatment, collect the cells, discard the supernatant, and add 1ml 4°C The cells were washed with pre-cooled 1×PBS (pH7.4±0.2), and centrifuged at 8000 rpm for 5 minutes. Discard the supernatant, add 0.1ml RIPA lysate, and lyse the cells on ice for 30 minutes, shaking every 10 minutes. After the cells are fully lysed, centrifuge the lysate at 8000rpm for 10 minutes, transfer the supernatant to another 1.5ml Eppendorf tube, measure the protein c...

Embodiment 3

[0041] Example 3: Effects of picrolactone P on the phosphorylation levels of Src and JAK2 kinases and the expression levels of phosphatases SHP1 and SHP2 in human gastric cancer cell HGC27.

[0042] Experimental method: with embodiment 2, its detection result is as figure 2 shown.

[0043] Such as figure 2 As shown, different concentrations of picrolactone P acted on HGC27, and it had no significant effect on the phosphorylation levels of kinases Src and JAK2 upstream of STAT3 and the expression levels of phosphatases SHP1 and SHP2.

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Abstract

The invention discloses an application of physagulin P in preparation of antitumor drug. The physagulin P is a compound, the structure of which is shown as formula I in the specification; the invention firstly finds that the physagulin P can lower the expression level of tumor apoptosis resistance genes XIAP and Mcl-1 so as to further inhibit tumor cell proliferation and induce tumor cell apoptosis through inhibiting phosphorylation of STAT3 kinase 705 tyrosine (Tyr705); the physagulin P can obviously inhibit the growths of a variety of malignant tumor cells, such as stomach cancer, lung cancer, liver cancer, myeloma, breast cancer, and the like. The physagulin P shows excellent anti-tumor activity when being used as an anti-tumor activity containing inhibitor of a new specific STAT3 signaling pathway, especially in conjunction with resveratrol and arsenic trioxide. The formula I is as shown in the specification.

Description

technical field [0001] The invention relates to the field of antitumor drugs, in particular to the application of picrolactone P as a STAT3 signaling pathway inhibitor and in the preparation of antitumor drugs. Background technique [0002] As a malignant disease, cancer seriously threatens human life and health. According to the survey report of the World Health Organization, it is estimated that the number of cancer deaths worldwide may increase to 13.2 million by 2030, and cancer will become the number one killer of human beings. Although surgery, chemotherapy, radiotherapy, and biological therapy are currently the main means of treating tumors, patients may have lost the opportunity for surgery when they are diagnosed. Chemotherapy has severe side effects, poor patient tolerance, and low targeting. expensive. Therefore, active development of new tumor-targeted drugs through the study of new anticancer substances in natural medicines is still the top priority of current...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K33/36A61P35/00A61K31/05A61K31/585
Inventor 陈喆朱凡凡马忠俊吕望王慧中
Owner 浙江美新控股有限公司
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