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Anticancer prior-medicine and method for preparing the same and use thereof

A technology of anticancer drugs and prodrugs, which is applied in the field of anticancer prodrugs and their preparation, and can solve the problems of unseen coupling of pectin and anticancer drugs

Active Publication Date: 2008-03-05
SICHUAN YINGRUI PHARMA TECH CO
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, there is no report that pectin is used to prepare lymphatic-targeted drugs, liver-targeted drugs or lung-targeted drugs, nor is pectin coupled with anticancer drugs for the preparation of drugs for the treatment of solid cancer or its draining lymph node metastasis , or reports on the use of drugs for the treatment of liver cancer or lung cancer

Method used

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  • Anticancer prior-medicine and method for preparing the same and use thereof
  • Anticancer prior-medicine and method for preparing the same and use thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0040] Embodiment 1, high-ester pectin alkali method lowering ester

[0041] Weigh 10g of high-ester pectin, dissolve it in 1000mL of secondary water, adjust the pH to 10-13 with sodium hydroxide solution, keep at 10-60°C, stir and react for 30, 60, 90, 120, 150 and 180 min respectively, After the reaction, adjust the pH to 2.8-3.5 with concentrated hydrochloric acid, add 300ml of ethanol, centrifuge at 4500r / min for 15min, wash the precipitate with 60% ethanol solution to remove chloride ions, and dry at 100°C to obtain low-ester pectin.

Embodiment 2

[0042] Embodiment two, molecular weight segmentation

[0043] Pour the processed Sephadex G 75 into the chromatographic column while stirring, let it settle naturally for 20 minutes, and finally put a circular filter paper slightly smaller than the inner diameter of the chromatographic column, and carefully add the prepared pectin solution to the On the gel column, use a constant flow pump to adjust the secondary water flow rate to 4ml / tube / 6 minutes, measure the molecular weight distribution of pectin by GPC, and then combine pectin with a certain molecular weight range to obtain low-ester fruit with a molecular weight range of 1000-70000 glue.

Embodiment 3

[0044] Embodiment three, preparation one of pectin-doxorubicin conjugate

[0045] Weigh 100mg of low-ester pectin, dissolve it in a 100ml round bottom flask with 10ml of secondary water, and dissolve 50mg of doxorubicin hydrochloride in a mixed solution of 10ml of dimethylformamide / water (V / V=1:1) , temperature controlled at 30°C, and stirred for 30 minutes. Then 300mg of EEDQ was added, the temperature was controlled at 30°C, and the reaction was stirred for 24 hours. When the desired time is reached, the reaction mixture is transferred to a dialysis bag with a molecular weight cut off of 5000 and dialyzed against secondary water for 24 hours. Add 150 ml of absolute ethanol to the inner liquid of the dialysis bag to generate a precipitate, centrifuge, wash the precipitate with absolute ethanol, and dry to obtain a water-soluble conjugate. The UV diagram of the water-soluble conjugate of pectin and doxorubicin is shown in Figure 1, and the ultraviolet absorption of pectin, d...

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Abstract

The present invention is one kind of anticancer prodrug and its preparation process and use, and belongs to the field of medicine and chemical technology. The anticancer prodrug is macromolecular conjugate formed with lower ester pectin and anticarcinogen containing amino group or hydroxyl group and through amido bond or ester bond coupling. The present invention provides one new way for designing and developing new anticarcinogen and is scientifically significant for applying anticancer prodrug in treating tumor. The macromolecular conjugate is hopeful in developing lymph targeting anticancer prodrug, liver targeting anticancer prodrug and lung targeting anticancer prodrug.

Description

technical field [0001] The invention relates to an anticancer prodrug and its preparation method and application, belonging to the field of anticancer pharmaceuticals. Background technique [0002] Traditional anticancer drugs are administered orally, intravenously, etc., and then reach a certain blood concentration and distribute throughout the body to produce therapeutic effects. The biggest defect of this treatment method is the lack of selectivity. Most commonly used anticancer drugs have low molecular weight and are easy to diffuse in the body, resulting in relatively even tissue distribution and large toxic and side effects, which seriously affect the anticancer therapeutic value of these drugs. By changing the structure of the drug, the drug can be accumulated in the target tissue, while the distribution in other parts of the body is reduced, which can improve the curative effect and reduce the side effects. Conjugate anticancer drugs with macromolecules to form macr...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K47/36A61K45/08A61K9/08A61K9/127A61K9/14A61K9/16A61K9/19A61P35/00A61K47/61
Inventor 唐小海邱宇谢永美宋鑫
Owner SICHUAN YINGRUI PHARMA TECH CO
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