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Application of long effective curcumin derivative in preparing anti-depression drug

A curcumin derivative, anti-depressant technology, applied in the direction of drug combination, non-active ingredient medical preparations, medical preparations containing active ingredients, etc., can solve the problem of poor water solubility, ester solubility, low bioavailability, fast metabolism, etc.

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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Problems solved by technology

[0011] Chinese patent application No. 200410013118.4 discloses the application of the above three curcumin and its derivatives for the preparation of drugs for the treatment of depression. The defect in this patent application is that the bioavailability is low and the metabolism rate is fast, and it needs to be administered every day.
[0012] However, the bioavailability of existing curcumin and its derivatives is very low, and its water solubility and ester solubility are relatively poor.

Method used

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

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preparation example Construction

[0028] The long-acting curcumin derivative of the present invention is to adopt the esters formed by the esterification reaction between curcuminoids and C1-C50 saturated fatty acids, and its preparation method comprises the following steps:

[0029] Weigh 1.49 grams of curcumin, dissolve in 50 milliliters of dioxane, add 0.73 grams of pyridine, and then add 1.64 grams of decanoyl chloride dropwise to the system. The reaction was carried out in an ice-water bath for 2 hours. The reaction process was monitored by TLC, developed with 3:1 chloroform and ethyl acetate.

[0030] Pour the above product into 40 ml of petroleum ether, filter and dissolve the precipitate in 30 ml of ethyl acetate, wash twice with 20 ml of 1N hydrochloric acid solution, wash once with saturated sodium carbonate solution, add 3 g of anhydrous Sodium sulfate was dried for 2 hours, then filtered, and the filtrate was spin-dried to obtain the crude product curcumin caprate.

[0031] The above-mentioned cr...

experiment example 1

[0038] Determination of Curcumin in Experimental Example 1 Mouse Plasma

[0039] 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.

[0040] 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.

[0041] Curcumin HPLC-MS / MS determination method: spectrum condition: chromat...

experiment example 2

[0043] Experimental example 2 acute antidepressant effect experiment

[0044] 2.1 Mouse tail suspension test

[0045] see figure 2 As shown, the experiment was divided into 3 groups (24 male ICR mice in each group): control group, curcumin group (10mg / kg), long-acting curcumin group (18.4mg / kg, given the amount of 20 days at a time) ). Tail suspension experiments were carried out on 3 days, 7 days and 14 days after the administration, respectively, and the curcumin group did not participate in the experiment on the 14th day.

[0046] The part about 1 cm away from the tip of the tail of the mouse was glued on a special iron stand with adhesive tape, and the height of the animal from the ground was 50 cm. Observe the behavior of the experimental animals within 6 minutes, and record the cumulative immobility time of the mice within the last 4 minutes.

[0047] The mouse tail suspension test showed that the curcumin dose of 10 mg / kg on the 3rd day and the 7th day after adm...

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Abstract

The invention relates to an application of a long effective curcumin derivative in preparing an anti-depression 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-depression action of various animal models, the long effective curcumin derivative can reserve the inherent anti-depression 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-depression drinks, foods, food addiitives or health products.

Description

technical field [0001] The invention relates to a medicine for treating depression, in particular to the application of a long-acting curcumin derivative in the preparation of antidepressant medicine. 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 various pharmacological activities such as anti-cancer, anti-inflammation, anti-oxidation, lowering blood fat, and anti-depression, and has little toxic and side effects. [0003] Depression is a complex psychological disorder, mainly manifested as low mood, decreased speech, mental and motor slowness, and its incidence rate is increasing year by year. Many diseases are often accompanied by depression, which seriously endangers people's health. Antidepressant drugs currently used clinically generally exert...

Claims

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Application Information

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IPC IPC(8): A61K31/222A61P25/24A61K47/48A61K31/12A61K47/54
Inventor 库宝善周卫东姚海燕
Owner 北京鼎国昌盛生物技术有限责任公司
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