阅读说明：本技术 远志甘油酯及长链烯酸类化合物作为抗抑郁和抗帕金森药物的新用途 (The new application of Radix Polygalae glyceride and long alkenoic acid class compound as antidepression and anti-Parkinson drug ) 是由 王鲁明 王磊 于 2018-05-22 设计创作，主要内容包括：本发明公开了远志甘油酯以及中长链烯酸类化合物作为抗抑郁和抗帕金森药物的新用途。本发明是用利血平递质耗竭抑郁模型,对33种植物药抗抑郁效果筛选、追踪有效中药的活性成分,并经过提取、分离、生物活性评价等得以实施。本发明涉及的远志甘油酯以及长链烯酸类化合物,经试验表明,可明显改善小鼠抑郁症模型的症状,升高利血平抑郁模型小鼠体温。缩短小鼠游泳不动时间和悬尾不动时间。对脑组织中5-HT的含量有明显的升高作用,但不超过正常组的水平,无5-HT综合征之忧；同时能升高DA水平,改善帕金森症状。表明远志脂类化合物是一种疗效明确、安全、理想的抗抑郁症的药物和抗帕金森症的药物。(The invention discloses Radix Polygalae glyceride and in new application of the long alkenoic acid class compound as antidepression and anti-Parkinson drug.The present invention is to exhaust depression model with reserpine mediator, to 33 kinds of botanical medicine antidepressant effect screenings, tracks the active constituent of effective Chinese medicine, and be carried out by extracting and developing, biological evaluation etc..Radix Polygalae glyceride of the present invention and long alkenoic acid class compound, the results showed, it can obviously improve the symptom of mouse depression model, increase reserpine depression model mouse temperature.Shorten mouse non-swimming time and outstanding tail dead time.There is apparent raising to act on the content of 5-HT in brain tissue, but is no more than the level normally organized, the sorrow of no 5-HT syndrome；DA level can be increased simultaneously, improve parkinson symptom.Show that Radix Polygalae lipoid substance is a kind of drug of clear, safe, the ideal depression of curative effect and the drug of anti-Parkinson disease.)

1. more than kinds of Radix Polygalae glyceride (Polygala Triglycerides) extract has preparation antidepression and anti-Parkinson's drug The new application of object.

2. new application of the Radix Polygalae glyceride in antidepressant according to claim 1, it is characterised in that:

There are mainly five types of glyceride, R in milkwort extract₁、R₂、R₃It is that (note: O is oil by OLL, OLO, OOO, POE, SOEd respectively Acid, L are linoleic acid, P is palmitic acid, S is stearic acid, E is eicosenoic acid, Ed is eicosadienoic acid).It wherein plays main Antidepressant effect be POE and SOEd, because of eicosenoic acid and eicosadienoic acid wherein containing protection nerve cell, The chemical property of itself is just very stable, makes it more containing palmitic acid and stearic acid respectively again in the triglycerides of its composition Stablize.Enteron aisle a part is hydrolyzed into glycerol, various fatty acid are absorbed after triglycerides is oral, partial hydrolysis is at single glycerol Ester, double glyceride and not hydrolyzed partial glyceride play a role at chylomicron.Triglycerides and wherein 20 carbon Olefin(e) acid and eicosadienoic acid play a role through blood-brain barrier.

3. the new application of eicosenoic acid and eicosadienoic acid in antidepressant according to claim 2, feature Be: pharmaceutically acceptable salt, ester or with the pharmaceutical compositions such as glucoside formed by sugar, including pharmaceutical carrier combination, for pre- Anti- and treatment depression and parkinsonism drug.

4. the tablet that the drug according to claim 3, formed using it as active constituent can be prepared into, capsule, dripping pill, The pharmaceutically acceptable dosage form such as solution, suspension.

Technical field

The present invention relates to pharmaceutical technology field, it is related to Radix Polygalae glyceride (Polygala Triglycerides) and hydrolysis produces Object eicosenoic acid (Paullinic acid) and eicosadienoic acid (eicosadienoic acid) long alkenoic acid class chemical combination New application of the object as antidepression and anti-Parkinson drug.

Background technique

We once disclosed the Chinese prescription (China Patent No. of a kind of antidepression and treatment hypothermia 2004100098171).Exhaust that depression model tracks active Chinese medicine and ingredient with reserpine mediator afterwards, the results showed that with difference The extraction and purification of solvent determines that its antidepressant active constituent is a series of long alkenoic acid after triglycerides and catabolism Analog derivative.Combined coefficient is extremely low in long alkenoic acid human body, or even cannot synthesize, so also known as essential fatty acid.This Class fatty acid has the function of powerful physiological activity and special.

Summary of the invention

The inventors discovered that from the long-chain diluted acid analog derivative after the glyceride and catabolism extracted in Chinese medicine polygala root, Has the function of highly significant to mouse reserpine depression model, Learned helplessness depression model etc..Prove it to this class model With the related disease of receptor, especially depressive illness, there is good effect.Prevention and treatment antidepression can be thus made into And its drug of related disease.

There are five types of glyceride, R for discovery in Radix Polygalae₁、R₂、R₃It is that (note: O is oil by OLL, OLO, OOO, POE, SOEd respectively Acid, L are linoleic acid, P is palmitic acid, S is stearic acid, E is eicosenoic acid, Ed is eicosadienoic acid).

The first aspect of the invention relates to the triglycerides extracted from Chinese medicine polygala root, it is characterised in that mouse tail suspension and The Learned helplessness such as forced swimming depression model shows the antidepressant effect of highly significant.

The second aspect of the invention is related to the preparation method of above-mentioned conjunction object, and this method includes extracting and developing and purifying.

The third aspect of the invention is related to containing its pharmaceutically acceptable salt of above compound as active constituent, with And one or more pharmaceutically acceptable carriers.

The above compound that the fourth aspect of the invention is related to is used for acquired with mouse reserpine depression model, mouse The drug of related disease and application thereof that helpless equal models confirm, the especially drug and its use to antidepression and anti-Parkinson On the way.

The fifth aspect of the invention is related to above compound and prepares a kind of curative for effect, significant effect, peace easy to use Full antidepressants, dosage form are tablet, capsule and the pill of above-mentioned each compound.

Detailed description of the invention:

Fig. 1 is ultrahigh pressure liquid phase chromatogram；Fig. 2 is the mass spectrogram at the peak retention time 15.92min；Fig. 3 is retention time 16.18min the mass spectrogram at peak；Fig. 4 is the mass spectrogram at the peak retention time 16.42min；16.68 He of Fig. 5 retention time 16.69min the mass spectrogram at peak.

Specific embodiment

Here is but to be not meant to any limitation of the invention to further description of the invention.Acute poison Property test do not measure toxicity, therefore it is unlisted.