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Application of ethyl acetate part of caper in preparation of antitumor drugs

An anti-tumor drug, the technology of ethyl acetate, applied in the field of medicine, can solve the problems of the material basis of anti-tumor efficacy and the unclear mechanism of anti-tumor action, etc.

Inactive Publication Date: 2018-06-08
SOUTH CENTRAL UNIVERSITY FOR NATIONALITIES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there are many reports on the anti-tumor activity of wild watermelon, but the material basis of its anti-tumor efficacy and the mechanism of anti-tumor action are still unclear.

Method used

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  • Application of ethyl acetate part of caper in preparation of antitumor drugs
  • Application of ethyl acetate part of caper in preparation of antitumor drugs
  • Application of ethyl acetate part of caper in preparation of antitumor drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] The preparation of embodiment 1 capers ethyl acetate part

[0029] 1.1 The preparation of capers ethyl acetate part comprises the following steps:

[0030] Take by weighing capers powder 7kg, soak overnight with 95% ethanol (V / V, the percentage concentration of ethanol described in this manual refers to the volume percentage concentration, hereinafter not described in detail) with 56L, then heat and continuously reflux with 95% ethanol Extract 4 times (extract directly with 95% ethanol soaked overnight for the first time), each time for 2 hours, filter with suction, combine the filtrates to obtain filtrate 1, then continue to reflux extraction with 56L of 75% ethanol for 3 times, each time for 2 hours. After suction filtration, the filtrates were combined to obtain filtrate 2, and filtrate 1 and filtrate 2 were combined and then concentrated under reduced pressure to obtain 368 g of extract. After adding a small amount of water to the extract, heat and ultrasonically mi...

Embodiment 2

[0041] Example 2 Inhibitory effect of capers ethyl acetate fraction on cell proliferation of human liver cancer cell HepG2

[0042] 1. Culture of HCC cells

[0043] The ethyl acetate fraction drug mentioned in this example is prepared from the ethyl acetate fraction powder prepared in Example 1 with PBS buffer solution, and the co-solvent is a mixed solution of DMSO and PEG400 with a volume ratio of 1:1.

[0044] The human liver cancer cell line HepG2 in the logarithmic growth phase was placed in DMEM medium containing 10% fetal bovine serum, at 37°C, 5% CO 2 , Cultured in a constant temperature incubator with a relative humidity of 100%, observe the growth of the cells every day, and change the liquid regularly. During the process, the cells whose growth density exceeds 80% of the bottom area of ​​the bottle are digested and passaged, and the ratio of each passage is 1:3 . After washing twice with PBS buffer, add 2 mL of 0.25% trypsin to it for digestion, place it at 37°C f...

Embodiment 3

[0049] Example 3 Capers ethyl acetate part to H 22 Inhibitory effect of liver cancer solid tumor model mice and its effect on lifespan of mice with ascites tumor

[0050] The ethyl acetate fraction drug mentioned in this example is prepared from the ethyl acetate fraction powder prepared in Example 1 with 0.5% CMC-Na (sodium carboxymethylcellulose) aqueous solution.

[0051] will grow well in H 22 Ascites tumor cells were prepared with normal saline to a concentration of 10 6 cells / mL of the cell suspension was injected into the peritoneal cavity of healthy mice, and the mice were killed by cervical dislocation after 3 passages. Suspension (cell concentration about 10 6 cells / mL), and then subcutaneously inoculate 0.2mL of the cell suspension under the armpit of each healthy mouse (quickly carried out under sterile conditions), to establish H 22 For the solid tumor model, the mice were randomly divided into groups 24 hours after inoculation, and 6 solid tumor experimental ...

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Abstract

The invention relates to the technical field of medicines and in particular relates to application of an ethyl acetate part of caper in preparation of antitumor drugs. The invention further provides apreparation method of the ethyl acetate part of caper. The preparation method comprises the following steps: (1) with caper powder, performing reflux extraction with an alcohol aqueous solution, filtering, and performing vacuum concentration to obtain extract; and (2) dispersing the extract with water, sequentially extracting with petroleum ether, chloroform and ethyl acetate, concentrating and drying, thereby obtaining the ethyl acetate part. Possible positions achieving an antitumor effect in the ethyl acetate part prepared in the invention are total alkaloids; the tumor control rate of theethyl acetate part on transplanted H22 tumor-bearing mice reaches 38.2%; the life of ascitic tumor mice can be obviously prolonged; HE staining results show that tumor tissue cells are sparsely arranged, large-area necrosis occurs and great cytoplasm vacuolization is caused; and meanwhile, the ethyl acetate part does not have any obvious influence on immune organs, hepatic and renal functions andblood routine examination and has potential of being developed into a novel antitumor drug.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to the application of the ethyl acetate fraction of capers in the preparation of antitumor drugs. Background technique [0002] The Uygur medicine caper is the fruit of the wild watermelon (Capparis spinosa L.), also known as mouse melon and wild watermelon. Capers have a long history of application in Uighur medicine, and are clinically used for the treatment of diseases such as gout and rheumatoid arthritis, with remarkable curative effects. Malignant tumor is a serious disease that threatens people's health and life. Finding low-toxicity and high-efficiency natural anti-tumor drugs has been a research hotspot in recent years. The anti-tumor mechanism of some alkaloids has been preliminarily clarified and applied clinically. Such as paclitaxel, hydroxycamptothecin and so on. The total alkaloids of capers contain stachydrine, betaine, dehydrobetaine, caperine, etc., among whic...

Claims

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Application Information

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IPC IPC(8): A61K36/185A61P35/00A61K131/00
CPCA61K36/185A61K2236/333A61K2236/39A61K2236/51
Inventor 邓旭坤余惠凡吕晓宇付千
Owner SOUTH CENTRAL UNIVERSITY FOR NATIONALITIES
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