Pharmaceutical uses of oxidized apofil derivatives

A technique for oxidizing aporphi and its uses, applied in the field of pharmacy, can solve the problems that the anti-tumor activity of oxidized aporphi compounds can be enhanced, and the anti-tumor effect of mitosis inhibitors has not been reported.

Active Publication Date: 2014-10-08
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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  • Pharmaceutical uses of oxidized apofil derivatives
  • Pharmaceutical uses of oxidized apofil derivatives
  • Pharmaceutical uses of oxidized apofil derivatives

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0115] Example 1 Extraction of Oxypapaverine from Corydalis

[0116] 1. Soaking and filtering

[0117] The rhizome of Corydalis yanhusuo was 5.6Kg, pulverized completely and refluxed with a volume of 30L ethanol (concentration 95%) for 4 hours, and then filtered to remove the medicinal powder residue.

[0118] 2. Ethanol recovery

[0119] Distill and recover 30L of ethanol at a temperature not exceeding 60°C and reflux for 2 hours each time. Remove the extract in the reactor 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 for a second time, and the filtration and distillation requirements are the same as before.

[0122] 4. Three hot back distillation

[0123] Use the recovered 30L of ethanol to reflux for three times, and the requirements for filtration and distillation are the same as before. 355 g of total extract was obtained.

[0124] 5. Extraction of total alkaloi...

Embodiment 2

[0138] Example 2 The inhibitory effect of oxypapaverine on the growth of various tumor cells in the in vitro test

[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 1000 rpm for 5 minutes, discard the supernatant, suspend an appropriate amount of medium, and adjust the cell concentration to 3.5×10 4 / ml. The cell suspension was inoculated into a 96-well plate, 100μl per well, and placed in a cell incubator (37℃, 5% CO 2 After 24 hours of culture in ), the medication group was added with 100μl of oxypapaverine diluted in cell culture medium to each well, the final concentration was 0.5μg / ml, the blank control group was added with the same amount of cell culture medium, and each group had 6 multiple wells. After culturing in an incubator for 66 hours, add 2...

Embodiment 3

[0145] Effect of Papaverine on Human Gastric Cancer HGC Cell Cycle

[0146] Experimental drugs:

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

[0148] Culture HGC cells in vitro. When the growth status is good, digest and inoculate 1×10 5 The cells adhered to the wall overnight in a 6cm petri dish. After the cells are in good condition, remove the medium and divide them into 8 groups randomly:

[0149] Single medication group a, add oxypapaverine diluted in culture medium to a final concentration of 0.25μM;

[0150] For group b, the drug alone was added with oxypapaverine diluted in culture medium to a final concentration of 1μM;

[0151] For group c, the drug alone was added with oxypapaverine diluted in culture medium to a final concentration of 30μM;

[0152] In group d with the drug alone, vinc...

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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 of an oxidized apophene derivative and its composition. Background technique [0002] Tumors are a serious disease threatening human health and life. According to statistics from the World Health Organization (WHO), there are currently about 10 million tumors and 7 million deaths worldwide each year. Tumors have become second only to cardiovascular disease. Diseases are the second killer of human beings. Therefore, tumor prevention and treatment have 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, drugs used for tumor treatment have made great achievements and obtained a large number of clinical anti-tumor with different mechanisms of action Drugs, unfortunately, these anti-tumor drugs have varying degree...

Claims

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Application Information

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