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Application of long effective curcumin derivative in preparing anti-tumor disease drug

A curcumin derivative, anti-tumor technology, applied in anti-tumor drugs, drug combinations, medical preparations of non-active ingredients, etc., can solve the problem of low solubility of curcumin

Active Publication Date: 2010-03-17
北京鼎国昌盛生物技术有限责任公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Curcumin has low solubility in water

Method used

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  • Application of long effective curcumin derivative in preparing anti-tumor disease drug
  • Application of long effective curcumin derivative in preparing anti-tumor disease drug
  • Application of long effective curcumin derivative in preparing anti-tumor disease drug

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0037] Determination of Curcumin in Experimental Example 1 Mouse Plasma

[0038] Mice administration method: subcutaneous injection, administration dose: 100mg / kg body weight, sampling: 5min, 10min, 30min, 45min, 1h, 1.5h, 2h, 6h and 2nd, 3rd, 4th, 5th after administration , 6, 7 days mice were picked to take blood from eyeballs, 6 mice for each blood collection point, put the blood in blood collection tubes coated with heparin, after centrifuging the samples, take 0.2ml supernatant, extract twice with ethyl acetate, Freeze and vacuum dry, dissolve in methanol to 0.2ml, and use for HPLC determination.

[0039] Preparation of standard curve: take about 0.5 mg of curcumin, add a certain amount of peanut oil to make the concentration 0.5 mg / ml. Take blank plasma, and precisely add different concentrations of curcumin. Prepare the standard together according to the plasma sample preparation method.

[0040] Curcumin HPLC-MS / MS determination method: spectrum condition: chromat...

experiment example 2

[0042] Experimental example 2 S-180 anti-tumor experiment in tumor-bearing mice

[0043] ICR male mice were divided into 5 groups (n=15, each group), three doses of long-acting curcumin administration components were high, medium and low; the positive control group was given 5-FU; Inoculate S-180 sarcoma cells (×10 5 ). Dosing began the next day, and the long-acting curcumin group was given a dose of 7 days at a time, and 5-FU was given once a day. After 7 days, the mice were killed by decapitation, the tumors were taken, and the body weight and tumor weight were weighed.

[0044] see figure 2 As shown, there is a significant difference in tumor weight / body weight between the long-acting curcumin administration group and the control group; the tumor inhibition rate is 28.5% in the low-dose group, 57.8% in the middle-dose group, 50.1% in the high-dose group, and 50.1% in the 5-FU group. was 55.8%.

experiment example 3

[0045] Experimental example 3 Anti-tumor experiment of tumor-bearing mice HCT116

[0046] ICR male mice were divided into 5 groups (n=15, each group), three doses of long-acting curcumin administration components were high, medium and low; the positive control group was given 5-FU; Inoculate HCT116 cells (×10 5 ). Dosing began the next day, and the long-acting curcumin group was given a dose of 7 days at a time, and 5-FU was given once a day. After 7 days, the mice were killed by decapitation, the tumors were taken, and the body weight and tumor weight were weighed.

[0047] see image 3 As shown, there is a significant difference in tumor weight / body weight between the long-acting curcumin administration group and the control group; the tumor inhibition rate is 29.6% in the low-dose group, 58.4% in the middle-dose group, 49.3% in the high-dose group, and 49.3% in the 5-FU group. was 52.8%.

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Abstract

The invention relates to an application of a long effective curcumin derivative in preparing an anti-tumor disease drug. The long effective curcumin derivative is an ester which is formed in such a way that C1 to C50 saturated or unsaturated fatty acids or acyls thereof react with hydroxyl groups of curcumin substances by esterification respectively and independently. Through the research on the anti-tumor action of various animal models, the long effective curcumin derivative can reserve the inherent anti-tumor drug effect of the curcumin and also has the effects of the slow release and the prolongation of the drug effect and a favorable prospect of clinical application. The long effective curcumin derivative can be also used for preparing anti-tumor drinks, foods, food additives or health products.

Description

technical field [0001] The invention relates to a drug for treating tumors, in particular to the application of a long-acting curcumin derivative in the preparation of anti-tumor drugs. Background technique [0002] Curcuminoids (Cur) is a phenolic pigment extracted from the root and stem of the traditional Chinese medicine turmeric, usually a mixture of curcumin, demethoxycurcumin and demethoxycurcumin. Modern pharmacological studies have shown that it has anti-inflammatory, anti-oxidation, anti-coagulant, hypolipidemic, anti-atherosclerosis, anti-tumor effects, etc., especially as an anti-cancer drug with good development prospects, its anti-tumor effect has increasingly attracted attention. People's attention has become a research hotspot. Numerous cell experiments and animal experiments have proved that curcumin has definite anti-tumor activity, its anti-cancer spectrum is wide, and its toxic and side effects are small. It is a new anti-cancer drug with broad applicatio...

Claims

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Application Information

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IPC IPC(8): A61K31/222A61P35/00A61K47/48A61K31/12A61K47/54
Inventor 库宝善周卫东于凤华姚海燕姚广印
Owner 北京鼎国昌盛生物技术有限责任公司
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