Preparation technology and anti-tumor application of modified pectin with high bioavailability

A technique of modifying pectin and utilization, which is applied in the direction of antineoplastic drugs, medical preparations containing active ingredients, drug combinations, etc. It can solve the problems affecting the efficacy of MPHB, achieve control of molecular weight and distribution, and improve biological The effect of utilization

Active Publication Date: 2011-12-14
XINXIANG MEDICAL UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Many intestinal absorption enhancers are cytotoxic, thereby affecting the pharmacodynamic effect of MPHB

Method used

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  • Preparation technology and anti-tumor application of modified pectin with high bioavailability
  • Preparation technology and anti-tumor application of modified pectin with high bioavailability
  • Preparation technology and anti-tumor application of modified pectin with high bioavailability

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Weigh 5kg of citrus pectin with an esterification degree of 60%, add 5000L of water, mix, heat to 60°C, and keep for 12h to fully swell; cool to 45°C, and adjust the pH to 8.0 with sodium carbonate solution in the same container, Add commercially available pectin esterase and stir evenly. It was determined that when the degree of pectin esterification was reduced to 1%, the temperature was raised to 80° C. and kept for 1 hour to terminate the action of pectin esterase. Commercially available polygalacturonase was added to the same container, and after enzymatic degradation, the molecular weight and molecular weight distribution were detected by high performance gel chromatography, so that the peak average molecular weight of the main components of the product was in the range of 70000Da to 2000Da. Use the first set of membranes with a molecular weight cut-off (hereinafter referred to as MWCO) of 100,000Da to separate and remove high-molecular-weight pectin and enzymes; ...

Embodiment 2

[0028] Weigh 100kg of ponkan peel pectin with a degree of esterification of 40%, add 1000L of water, mix, heat to 95°C, keep for 3h, and swell; cool to 55°C, and adjust the pH to 4.5 with potassium carbonate solution in the same container , add pectin esterase and stir evenly. It was determined that when the degree of pectin esterification decreased to 0.4%, the temperature was raised to 90°C and kept for 30 minutes. Pectin lyase is added into the same container, and through enzymatic degradation, the peak average molecular weight of the main components of the product is in the range of 50000Da to 2000Da. A membrane with a MWCO of 70,000Da was used to separate and remove high-molecular-weight pectin and enzymes; a membrane with a MWCO of 45,000Da was used to concentrate the pectin solution, and the product was spray-dried to obtain 83.50kg of MPHB with antitumor activity and oral administration.

Embodiment 3

[0030] Weigh 1kg of pomelo (Citrus grandis) peel pectin with a degree of esterification of 70%, add 50L of water, mix, heat to 90°C, keep for 8h, and swell; cool to 50°C, and adjust the pH to 8.5, add pectin esterase and stir evenly. It was determined that when the degree of esterification of pectin decreased to 10%, the temperature was raised to 85°C and kept for 90 minutes. A mixture of pectin lyase and polygalacturonase is added to the same container, and the peak average molecular weight of the main components of the product is about 20,000 Da through enzymatic degradation. MWCO 80000Da membrane was used to separate and remove high molecular weight pectin and enzymes; MWCO 20000Da membrane was used to concentrate the pectin solution, and the product was freeze-dried to obtain 0.68kg MPHB with anti-tumor activity and oral administration.

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Abstract

The invention relates to a process for preparing polysaccharide and application of the polysaccharide, in particular to a process for preparing modified pectin (MPHB) with high bioavailability and low molecular weight and application of the modified pectin in the antitumor field. The process comprises the following steps of: mixing pectin and water, heating, and swelling; cooling, regulating the pH value by using carbonate solution, reducing the degree of esterification by using pectinesterase (EC 3.1.1.11), and raising the temperature to inactivate the pectinesterase; and cooling, degrading a main chain of the pectin by using polygalacturonase (EC 3.2.1.15) or pectate lyase (EC 4.2.2.10), and performing membrane filtration on a product, desalting, concentrating and drying to obtain the MPHB. The process is favorable for preparing the MPHB on a large scale and controlling the molecular weight and molecular weight distribution of the MPHB. The MPHB has the activities of resisting livercancer, cervical carcinoma and the like; and the adding of an intestinal absorption enhancer in an oral formula of the MPHB is favorable for further improving the bioavailability.

Description

technical field [0001] The invention relates to a preparation process and application of a polysaccharide, in particular to a preparation process of a highly bioavailable modified pectin and its application in the field of antitumor. Background technique [0002] Improving biological activity, reducing toxicity, and increasing bioavailability are important methods for developing new drugs and achieving success. Improving bioavailability is especially significant for polymer drugs. [0003] Pectin is a polysaccharide mainly derived from plants, which is produced in the primary cell wall and interstitium of higher plants. It is a heterogeneous branched heteropolysaccharide family. Pectin is found in almost all plants, especially in fruits such as citrus and apples. Pectin has been identified as a food raw material by the World Food and Agriculture Organization (FAO), the World Health Organization (WHO), and its safety has been confirmed. Using pectin as a raw material to pr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C12P19/14C12P19/04A61K31/732A61P35/00
Inventor 张文博徐萍高林闫清华
Owner XINXIANG MEDICAL UNIV
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