Application of demethylzeylasteral to preparation of medicine for treating pancreatic cancer

A technology of norzeratin and pancreatic cancer, which is applied in the field of medicine, can solve the problems that the therapeutic effect of human pancreatic cancer has not been reported in the literature, and achieve the effect of enhancing anti-tumor effect, good inhibitory effect, and significant killing effect

Inactive Publication Date: 2017-05-31
ZHONGSHAN HOSPITAL FUDAN UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, the therapeutic effect of norzeratin on human pancreatic cancer has not been reported in the literature.

Method used

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  • Application of demethylzeylasteral to preparation of medicine for treating pancreatic cancer
  • Application of demethylzeylasteral to preparation of medicine for treating pancreatic cancer
  • Application of demethylzeylasteral to preparation of medicine for treating pancreatic cancer

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Experimental program
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Effect test

Embodiment 1

[0025] The preparation of embodiment 1 norzera wood aldehyde

[0026] 1. Preparation method

[0027] Pulverize the root bark of Tripterygium wilfordii, put it in the reflux pot, add 1.5 times of ethyl acetate, heat and reflux for 3 hours, repeat twice to get the ethyl acetate extract, recover the solvent, and get the dry extract with a yield of 8.25%. 7.5 times the amount of silica gel was subjected to column chromatography, and the gradient elution of n-hexane / acetone was used to obtain the crude product of norzeramydal (abbreviated as ZST93). Recrystallize with acetone, and dry the crystals in a vacuum oven at 60° C. for 4 hours to obtain ZST93 yellow crystals with a purity greater than 99%.

[0028] 2. Physical and chemical characteristics

[0029] The prepared ZST93 is yellow powder or crystal, odorless, with a melting point of 248°C. Molecular formula: C 29 h 36 o 6 , the molecular weight is: 480.59, and the structural formula is as figure 1 As shown in A.

[0030...

Embodiment 2

[0031] The use research of embodiment 2 norzera wood aldehyde

[0032] 1. Materials and methods

[0033] 1.1 Materials

[0034] Example 1 prepared ZST93 with a purity greater than 99%.

[0035] Human pancreatic cancer cell lines T3M4, Colo-357, Capan-1, ASPC-1, MIA PaCa-2 and PANC-1 were purchased from ATCC.

[0036] Cell Counting kit-8 was purchased from Dojindo Molecular Technologies Inc. (Kumamoto, Japan); ReverTra qPCR RT kit was purchased from TOYOBO (Tokyo, Japan); SYBR Green PCR MasterMix was purchased from TOYOBO (Tokyo, Japan); Apoptosis Detection Kit was purchased from BD Biosciences (San Jose, CA, USA); Tunel in situ apoptosis detection The kit was purchased from KeyGENBioTECH (Nanjing, China).

[0037] DMEM medium, RPMI-1640 medium, fetal bovine serum were purchased from Gibco (Grand Island, NY, USA); 3-MA, Z-VAD-FMK were purchased from Selleckchem (Houston, TX, USA); Anti-β-actin Antibody was purchased from MBLtechnologies (Woburn, MA, USA); Anti-cleaved cas...

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Abstract

The invention relates to application of demethylzeylasteral to preparation of a medicine for treating pancreatic cancer. The application proves that the compound demethylzeylasteral has a significant killing effect on human pancreatic cancer cells, can induce tumor cell cycle arrest in a G0/G1 phase and achieves a pancreatic cancer resisting effect through induction of autophagic death and Caspase-3-dependent apoptosis of the cells; in combination with gemcitabine, the demethylzeylasteral can significantly reduce the IC50 of the gemcitabine, and through combined drug administration, a better inhibitory effect on the human pancreatic cancer cells is achieved; at low concentration, the demethylzeylasteral can induce the autophagic death of the cells so as to improve the antitumor effect of the gemcitabine, while at high concentration, the demethylzeylasteral improves the chemotherapeutic effect of the gemcitabine mainly through promotion of the apoptosis. On the basis of the application, the demethylzeylasteral can be applied to preparation of the medicine for treating the pancreatic cancer, and the prepared medicine is combined with the gemcitabine for use, or the demethylzeylasteral can be used for researching a cell autophagy or apoptosis mechanism.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to the application of norzeramydal in the preparation of drugs for treating pancreatic cancer. Background technique [0002] The incidence of pancreatic cancer is increasing year by year, and its death rate ranks fourth among all tumors in the United States. The overall 5-year survival rate of patients is about 8%, and there has been no significant improvement for decades. Although chemotherapy based on gemcitabine can improve the prognosis of pancreatic cancer patients to a certain extent, the effective rate is still not satisfactory, and the quality of life of patients is significantly reduced. Although many attempts have been made to combine chemotherapy and targeted therapy, the overall therapeutic effect is not good, and it is highly effective and highly toxic. Compared with gemcitabine alone, the advantages of combination therapy are limited. At present, multidisciplinary co...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/56A61K31/7068A61P35/00A61P1/18
Inventor 杨春欣梁健王峰田孝东杨尹默
Owner ZHONGSHAN HOSPITAL FUDAN UNIV
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