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Method for preparing Fissistigma oldhamii lactam alkali compound and application thereof to preparing anti-tumour medicine

A technology of xyllactam base and compound, which is applied in the preparation of quinolactam base compound and its application in the preparation of anti-tumor drugs, which can solve the problems of unsatisfactory drug curative effect, large toxic and side effects, etc.

Inactive Publication Date: 2012-05-30
GUIZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The technical problem to be solved by the present invention is to provide a method for extracting lactam base compounds from pure natural plants and its application in the preparation of antitumor drugs, so as to solve the problem that the curative effect of current drugs is not ideal, and the toxicity and side effects are extremely high. question

Method used

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  • Method for preparing Fissistigma oldhamii lactam alkali compound and application thereof to preparing anti-tumour medicine
  • Method for preparing Fissistigma oldhamii lactam alkali compound and application thereof to preparing anti-tumour medicine
  • Method for preparing Fissistigma oldhamii lactam alkali compound and application thereof to preparing anti-tumour medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] Example 1: Get Dushangua Fumu powder, pass through a 20-mesh sieve to obtain 5 kg, and repeatedly extract with 80% ethanol solution until the color of the extract becomes lighter, recycle the ethanol with a rotary evaporator, evaporate the extract to dryness, and obtain 500 grams dry extract. The extract is dissolved in water, ultrasonically assisted, extracted and decolorized with petroleum ether until the color of the petroleum ether extract is clear. Then extract with dichloromethane until the color is clear, combine the dichloromethane extracts, and recover the dichloromethane by a rotary evaporator to obtain 200 g of the extract. The extract was applied to a silica gel column with a particle size of 200-300 mesh, and was eluted with dichloromethane-methanol (volume ratio 8:2). The eluate was collected in sections, and 5 components were obtained according to TLC detection. The third component was further separated on the column to obtain 20 g of the compound.

Embodiment 2

[0015] Example 2: Preparation of Dushan Guafu Cryllactam Base Capsules

[0016] 1. Preparation of prescription

[0017] 5g of Dushanguafu xylactam base, 4.5g of microcrystalline cellulose (MCC), 5g of ethyl cellulose (EC), 7g of hypromellose (K4M), and an appropriate amount of 50% ethanol solution.

[0018] 2. Preparation process

[0019] Firstly, crush the Dushangua formosan base and auxiliary materials and pass through a 100-mesh sieve. Weigh the prescription amount of raw materials and auxiliary materials, mix them evenly, add an appropriate amount of 50% ethanol to make soft materials, extrude them into thin strips with an extrusion sieve plate (aperture 0.8mm), and then put the strip materials into a spheronizer to make them fully spheroidized , take out the pellets, and dry them at 60°C for about 2 hours to control the moisture content at 3% - 4%. Take 24-mesh pellets with a loading capacity of 250 mg per capsule, and fill the capsules with a filling machine.

Embodiment 3

[0020] Example 3: Chick Embryo Vascular Inhibition Test of Dushangua Fugui lactam base compound

[0021] 1. Experimental materials

[0022] The fertilized breeding eggs of Laihang Chicken (provided by the Breeding Livestock and Poultry Farm of Guizhou Province), and the chemical reagents are all of analytical grade.

[0023] 2. Experimental method

[0024] Put fertilized eggs at a temperature of 37.8 0 C. In an incubator with a humidity of 60%, after 8 days, drill a small hole of about 1.0 – 2.0 mm at the end of the air chamber of the egg and penetrate the shell membrane of the air chamber; use a small grinding wheel to cut the window at the lower right of the embryo head (0.5 cm×1.5cm), cut the shell membrane to expose the chorioallantoic membrane; carefully add the drug-containing paper on the surface of the membrane (the diameter of the paper is 5 mm, and use the paper without drug as a control); use sterile transparent After sealing the window with tape, put it into the...

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Abstract

The invention discloses a method for preparing a Fissistigma oldhamii lactam alkali compound and application thereof to preparing an anti-tumour medicine. The method comprises the following steps of: taking Fissistigma oldhamii powder, repetitively extracting the Fissistigma oldhamii powder by using 80% ethanol till the colour of extract becomes thin, recovering the ethanol, and evaporating and drying the extract; dissolving the extract by using water, ultrasonically fluxing the extract, and extracting and decolouring the extract by using petroleum ether till the colour of the extract of the petroleum ether becomes clear; extracting the extract by using dichloromethane till the colour becomes clear, mixing dichloromethane extract, and recovering the dichloromethane to obtain extract; and applying the extract on a silicagel column, eluting the extract by using dichloromethane-methanol, and collecting eluent in a sectional manner to obtain the compound. A characteristic plant in Guizhou, namely kopje Fissistigma oldhamii, has obvious inhibitory activity on neovascularisation; a plurality of active compounds are separated from the Fissistigma oldhamii; experiments prove that the compound not only can inhibit formation of neovascularisation but also has an inhibitory action on tumour cell strains; furthermore, found from animal internal anti-cancer experiments, the compound has obvious anti-tumour activity on a plurality of solid tumours and lung cancers.

Description

technical field [0001] The invention relates to a preparation method of a lactam base compound and its application in the preparation of antitumor drugs. Background technique [0002] Cancer is one of the major diseases that seriously endanger human health. According to the survey of the World Health Organization, cancer patients are increasing year by year, and the annual incidence of cancer in my country is about 1.3 million. my country is an area with a high incidence of lung cancer, and the cancer mortality rate remains high. [0003] For most cancer patients, there is currently no ideal drug. In the existing chemotherapeutic drugs, no matter they are synthetic drugs or natural drugs, the curative effect is not satisfactory, and the toxic and side effects are extremely large. Organometallic complexes such as cisplatin have strong anticancer properties, but they have disadvantages such as large toxic and side effects, narrow anticancer spectrum, and high cost; alkylati...

Claims

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Application Information

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IPC IPC(8): C07D491/048A61K31/4741A61P35/00A61P35/02
Inventor 杨再昌马小彦牛玉乐乔冲
Owner GUIZHOU UNIV
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