Usage of oxidized aporphine derivative and composition thereof

A technology for oxidizing apophytate and compounds, which is applied in the field of pharmacy, can solve the problem that the antitumor activity of oxidized apophytate compounds enhances the antitumor effect of mitotic inhibitors and the like.

Active Publication Date: 2009-10-28
XIANGBEI WELMAN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] However, there is no report on whether the oxidized apomorphine compounds have anti-tumor activity and enhance the anti-tumor effect of mitosis inhibitors.

Method used

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  • Usage of oxidized aporphine derivative and composition thereof
  • Usage of oxidized aporphine derivative and composition thereof
  • Usage of oxidized aporphine derivative and composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0115] Example 1 Corydalis extracts oxygen sea papaverine

[0116] 1. Soaking and filtering

[0117] Corydalis rhizome 5.6Kg, pulverizer complete pulverization, with volume 30L ethanol (concentration 95%) heat reflux for 4 hours, then filter to remove medicinal material powder residue.

[0118] 2. Ethanol recovery

[0119] Recover 30L of ethanol by distillation, the temperature does not exceed 60°C, reflux for 2 hours each time, and remove the extract in the reaction kettle to the collection bucket (the extract is brownish red, slightly viscous).

[0120] 3. Secondary heat reflux distillation

[0121] Use the recovered 30L ethanol to reflux twice, and the requirements for filtration and distillation are the same as before.

[0122] 4. Three times of heat back distillation

[0123] Heat reflux three times with recovered 30L ethanol, filter and distillation requirements are the same as before. Obtain total extract 355g.

[0124] 5. Extraction of total alkaloids

[0125] D...

Embodiment 2

[0138] The inhibitory effect of oxysea papaverine on the growth of various tumor cells in the in vitro test of embodiment 2

[0139] In vitro culture of human embryonic kidney cancer 293 cells and human liver cancer HepG 2 Cells, human lung cancer A549 and CRL-5895 cells, human gastric cancer HGC cells. After the cells grow to the logarithmic growth phase, digest the cells with trypsin, centrifuge at 1000rpm for 5min, discard the supernatant, suspend with an appropriate amount of medium, and adjust the cell concentration to 3.5×10 4 / ml. Inoculate the cell suspension into a 96-well plate, 100 μl per well, and place in a cell culture incubator (37°C, 5% CO 2 ) after culturing for 24 hours, each well of the medication group was added with 100 μl of oxysea papaverine diluted in cell culture medium, with a final concentration of 0.5 μg / ml, and the same amount of cell culture medium was added to the blank control group, and 6 replicate wells were set in each group. After culturi...

Embodiment 3

[0145] Effects of Oxapaverine on Cell Cycle of Human Gastric Carcinoma HGC

[0146] Experimental Drugs:

[0147] Papaverine (compound represented by formula I) was prepared in Example 1, paclitaxel was purchased from Sichuan Jiufeng Natural Pharmaceutical Co., Ltd., and vincristine was purchased from Shanghai Anti Kangsheng Phytochemical Co., Ltd.

[0148] Culture HGC cells in vitro, when the growth state is good, digest and inoculate 1×10 5 Cells were placed in a 6cm culture dish and adhered to the wall overnight. After the cells were in good condition, the medium was sucked off, and they were randomly divided into 8 groups:

[0149] For group A of medication alone, add oxapaverine diluted with culture medium, with a final concentration of 0.25 μM;

[0150] For group B, which is administered alone, add oxapaverine diluted with culture medium, with a final concentration of 1 μM;

[0151] For group C, which is administered alone, add oxapaverine diluted with culture medium,...

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Abstract

The invention belongs to the technical field of pharmacy and in particular relates to a usage of an oxidized aporphine derivative and a composition thereof. The invention discovers that the oxidized aporphine derivative can effectively inhibit the tumor proliferation and that when the oxidized aporphine derivative is used together with antitumor drugs to cure tumor, the synergy can be achieved, the cure effect can be enhanced, and the amount of the antitumor drugs in use can be reduced, thereby obviously reducing the toxic and side effects of the antitumor drugs.

Description

technical field [0001] The invention belongs to the technical field of pharmacy, and specifically relates to the use and composition of an oxidized aporphi derivative. Background technique [0002] Tumor is a serious disease that threatens human health and life. According to the statistics of the World Health Organization (WHO), about 10 million people in the world have tumors every year, and 7 million people die. Tumors have become second only to cardiovascular diseases. Disease is the second killer of human beings. Therefore, tumor prevention and treatment has received widespread attention from all walks of life. Tumor chemotherapy (hereinafter referred to as chemotherapy) is one of the three basic methods of tumor treatment. After more than 50 years of development, the drugs used for tumor treatment have made great achievements, and a large number of clinical anti-tumor drugs with different mechanisms of action have been obtained. Unfortunately, these antineoplastic drug...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/473A61K31/4741A61P35/00
Inventor 俞强
Owner XIANGBEI WELMAN PHARMA CO LTD
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