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Anti-tumor pharmaceutical composition

A technology of composition and medicine, applied in the field of pharmacy, capable of solving problems such as allergic reactions

Active Publication Date: 2009-07-15
XIANGBEI WELMAN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But at the same time, cell mitosis inhibitors also have serious side effects, such as allergic reactions, neurotoxicity, bone marrow suppression, hematopoietic suppression, gastrointestinal mucositis, etc.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0099] Extraction of apophyllic alkaloids from Corydalis

[0100] (1) Soaking and filtering

[0101] The rhizome of Corydalis yanhusuo was 5.6Kg. After being completely crushed by a pulverizer, it was refluxed with a volume of 30L ethanol (concentration 95%) for 3 hours, and then filtered to remove the medicinal powder residue.

[0102] (2) Ethanol recovery

[0103] Distill and recover 30L ethanol, the temperature does not exceed 60 ℃, reflux for 2 hours, remove the extract in the reactor to the collection bucket (the extract is brownish-red, slightly viscous).

[0104] (3) The second heat reflow

[0105] Use the recovered 30L ethanol for the second heat reflux, and the filtration and distillation requirements are the same as before.

[0106] (4) The third heat reflow

[0107] Use the recovered 30L ethanol for the third heat reflux, and the filtration and distillation requirements are the same as before. 355 g of total extract was obtained.

[0108] (5) Extraction of total alkaloi...

Embodiment 2

[0123] Effects of apophyllic alkaloids on the cell cycle of human gastric cancer HGC

[0124] Experimental drugs:

[0125] Sea papaverine (a compound represented by formula II) was prepared in Example 1, paclitaxel was purchased from Sichuan Jiufeng Natural Pharmaceutical Co., Ltd., and vincristine was purchased from Shanghai Santikangsheng Phytochemical Co., Ltd.

[0126] Culture HGC cells in vitro. When the growth status is good, digest and inoculate 1×10 5 Cells adhered to the wall overnight in a 6cm petri dish. After the cells are in good condition, aspirate the medium and divide them into 7 groups randomly:

[0127] For group A alone, add sea papaverine diluted in culture medium to a final concentration of 2μM;

[0128] In group b alone, add sea papaverine diluted with culture medium to a final concentration of 50 nM;

[0129] Group c was treated with medicine alone, and vincristine diluted in culture medium was added to the final concentration of 10 nM;

[0130] In group d w...

Embodiment 3

[0138] Inhibitory effect of apophyl alkaloids and mitotic inhibitors on tumor growth in S180 tumor-bearing mice

[0139] Experimental animals:

[0140] Male SPF grade KM mice, purchased from Shanghai Slack Laboratory Animal Co., Ltd., weighing 18-22 g, raised in an SPF grade animal room, 12 hours of light / 12 hours of darkness, and free intake of feed and water.

[0141] Experimental drugs:

[0142] Sea papaverine, prepared in Example 1, paclitaxel was purchased from Sichuan Jiufeng Natural Pharmaceutical Co., Ltd., apomorphine (shown in structural formula V) was purchased from Qinghai Pharmaceutical Factory Co., Ltd., corydine (shown in structural formula IV) ) Was purchased from Hunan Neuer Biopharmaceutical Co., Ltd., and kaempferine (shown in structural formula III) was purchased from NADUCS, Inc., USA.

[0143] experimental method:

[0144] Except for the normal group, take 7-day-inoculated mice with S180 ascites, extract the ascites under aseptic conditions, and adjust the ce...

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Abstract

The invention discloses a composition which contains aporphine alkaloid shown in a formula I, mitotic inhibitors of cells and receivable carriers on pharmaco; in the formula I, R1 represents hydrogen, a hydroxyl group, a methyl group, an aldehyde group or an acetyl group, R2 represents hydrogen (having two different spatial configurations of R or S), R3 represents hydrogen, a hydroxyl group or a methyl group, R11 represents hydrogen, a hydroxyl group or a methyl group, R12 represents hydrogen or an aldehyde group, R4, R5, R6, R7, R8, R9 and R10 are respectively selected from hydrogen, a hydroxyl group or a methoxyl group, or R8 and R9 form an alcoxyl ring. The invention also discloses an application of the composition for treating tumors.

Description

Technical field [0001] The present invention relates to the field of pharmacology, and more specifically to a pharmaceutical composition containing apophylloid alkaloids and cell mitosis inhibitors. Background technique [0002] With the development of industry, malignant tumors are a serious threat to human health. Traditional chemotherapy and radiotherapy lack specificity. While achieving curative effects, they also often bring greater toxic and side effects to patients. Inhibitors of cell mitosis can affect the polymerization of cell microtubules, thereby preventing the division of cancer cells. At the same time, cells are also prone to death at this stage, and play a role in inhibiting the mitosis of cancer cells. But at the same time, cell mitosis inhibitors also have serious side effects, such as allergic reactions, neurotoxicity, bone marrow suppression, hematopoietic suppression, gastrointestinal mucositis and so on. The occurrence of these side effects is closely related...

Claims

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Application Information

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IPC IPC(8): A61K31/473A61K31/4355A61K31/475A61K31/4375A61K31/337A61K31/165A61P35/00
Inventor 俞强
Owner XIANGBEI WELMAN PHARMA CO LTD
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