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Pectin-5-efudix colon cancer double-target prodrug and preparation method

A technology of fluorouracil and colon cancer, which is applied in the field of colon cancer targeted therapy drugs and its preparation, can solve the problems of low concentration in the colon, high toxicity and side effects, and difficult tolerance of patients, and achieves the reduction of immunosuppression, the stability of drug loading, and the improvement of selective effect

Inactive Publication Date: 2011-11-09
FOURTH MILITARY MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

5-FU is the basic drug for the clinical treatment of colon cancer, but the effective rate of conventional treatment is only 15-21%.
The reason is that the concentration of 5-FU reaching the colon is low after intravenous administration, and the toxic and side effects are large, which is difficult for patients to tolerate.

Method used

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  • Pectin-5-efudix colon cancer double-target prodrug and preparation method
  • Pectin-5-efudix colon cancer double-target prodrug and preparation method
  • Pectin-5-efudix colon cancer double-target prodrug and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043]Add 15g of pectin and 3N NaOH aqueous solution, stir overnight at 37°C, cool to room temperature, ethanol precipitate, add concentrated hydrochloric acid to adjust the pH value to 3, stir overnight at 37°C, adjust the pH value to neutral, evaporate the solvent under reduced pressure, and concentrate Dissolve the suspension in an appropriate amount of distilled water, move it to a dialysis bag (molecular weight cut-off 8000), use distilled water as the external fluid for dialysis, and freeze-dry for 24 hours after concentration until the color of the internal dialysis fluid no longer changes to obtain 13.6 g of light brown powder; HPLC Detect that the degree of esterification is less than 30%; weigh 0.5g of modified pectin and dissolve it in 20mL DMSO, add 0.25g of DCC and 15mg of DAMP, then add 0.5g of 5-FU, stir at 40°C for 24h, after the reaction is over, pour the reactants into In ethanol, the jelly was precipitated, filtered, rinsed with methanol, and dried in vacuum ...

Embodiment 2

[0046] Take 15g of pectin, add pectinase to citrate buffer (pH=4-5), stir at 50°C for 4-6h, cool to room temperature, distill off the solvent under reduced pressure, add appropriate amount of distilled water to the concentrated suspension until fully dissolved , moved to a dialysis bag (molecular weight cut-off 8000), and distilled water was used as the external fluid for dialysis. The dialysis was stopped until the color of the dialysis internal fluid no longer changed. After concentration, freeze-dry for 24 hours to obtain 13.6 g of light brown powder. The degree of esterification detected by HPLC is less than 30%. Weigh 0.5g of modified pectin and dissolve it in 20mL of DMSO, add 0.25g of DCC and 15mg of DAMP, then add 0.5g of 5-FU, and stir at 40°C for 24h. Filter, rinse with methanol, and dry in vacuo to obtain the product.

[0047]

Embodiment 3

[0049] Add 15g of pectin to methanol solution of 2mol / L NaOH, stir vigorously, heat and reflux at 60-80°C for 4-6h, cool to room temperature, add concentrated hydrochloric acid to adjust the pH value to 3, stir vigorously, heat and reflux at 50-70°C for 7- After 10 hours, evaporate the solvent under reduced pressure, add an appropriate amount of distilled water to the concentrated suspension until it is fully dissolved, transfer it to a dialysis bag (molecular weight cut-off 8000), use distilled water as the external fluid for dialysis, and stop dialysis until the color of the internal fluid no longer changes. Freeze-dried for 24 hours to obtain 13.6g of light brown powder. The degree of esterification detected by HPLC is less than 30%. Weigh 0.5g of modified pectin and dissolve it in 20mL of DMSO, add 0.25g of DCC and 15mg of DAMP, then add 0.5g of 5-FU, and stir at 40°C for 24h. Filter, rinse with methanol, and dry in vacuo to obtain the product.

[0050]

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Abstract

The invention relates to a pectin-5-fluorouracil colon cancer two-targeting prodrug and the preparation method thereof, and mainly synthesizes a two-targeting prodrug for colon cancer by utilizing an anti-cancer drug, 5-fluorouracil (5-FU), and pectin. The two-targeting prodrug for colon cancer is used for treating colon cancer and is characterized in that the 6-digit carboxyl is utilized to be combined with 5-FU directly or through different bridging groups to synthesize a series of two-targeting prodrugs for colon cancer. The prodrug first targets 5-FU to the colon by utilizing pectin to realize colon positioned release, and then 5-FU-galactose is identified through high expression of colon cancer galactin-3, and then 5-Fu is targeted to the colon cancer cells to realize two-targeting of colon cancer to treat colon cancer. The prodrug improves the selectivity of 5-FU greatly, enhances the curative effect and reduces adverse reactions. In addition, the hydrolysis fragments of pectin play a role in resisting tumor metastasis and can have a synergic action with 5-FU. The pectin-5-fluorouracil two-targeting prodrug for colon cancer focuses on the drug design ideas of drug delivery, targeting and coordination; therefore, the prodrug achieves the goal of high selectivity, high efficiency and low toxicity.

Description

technical field [0001] The invention relates to a colon cancer targeted therapy drug and a preparation method thereof, and mainly relates to a colon cancer targeted prodrug synthesized by the 6-carboxyl group of an anticancer drug 5-fluorouracil (5-FU) and pectin and a preparation method thereof. Background technique [0002] Due to changes in lifestyle and aggravation of environmental pollution, the incidence of colon cancer in my country has risen sharply, with an annual incidence of more than 20 / 100,000, and the mortality rate of colon cancer has jumped to the second place among malignant tumors. However, there is no specificity. treatment method. With surgical treatment, the postoperative recurrence rate reaches 50%, and the 5-year survival rate is less than 5%. 5-FU is the basic drug for clinical treatment of colon cancer, but the effective rate of conventional treatment is only 15-21%. The reason is that the intravenous administration of 5-FU reaches a low concentrati...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/732A61K31/7072A61K47/48A61P35/00C08B37/06A61K47/61
Inventor 刘莉梅其炳白卉孙阳郭振军李宇华
Owner FOURTH MILITARY MEDICAL UNIVERSITY
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