CN102250087A - Use of several tetrahydro-proto-berberine compounds in relief of pain - Google Patents
Use of several tetrahydro-proto-berberine compounds in relief of pain Download PDFInfo
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- CN102250087A CN102250087A CN 201110125330 CN201110125330A CN102250087A CN 102250087 A CN102250087 A CN 102250087A CN 201110125330 CN201110125330 CN 201110125330 CN 201110125330 A CN201110125330 A CN 201110125330A CN 102250087 A CN102250087 A CN 102250087A
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Abstract
The invention discloses the use of several tetrahydro-proto-berberine compounds in relief of pain. Analgesics commonly used at present mainly include peripheral antipyretic analgesics and central opioid antipyretics. The peripheral antipyretic analgesics are effective for light and medium pain but not ineffective traumatic pain and viscera angina, and has side effects such as stomach pain, sickness, platelet agglutination inhibition and the like; and central opioid antipyretics are mainly used for treating medium and serious pain, is not ideal in treatment effect on some chronic pain, and produces tolerance, addiction, sickness, astriction, muscle stiffness, low immunity and other side effects in long-term use. The development of new analgesics has an active significance for the treatment of pain. The several tetrahydro-proto-berberine compounds disclosed by the invention have obvious analgesic effect.
Description
Technical field
The present invention relates to the chemotherapy field, be specifically related to the application in treatment pain medication field of several compound of Tetrahydro-proto-berberines class.
Background technology
Pain is a kind of complex physical psychological activity, is one of modal symptom clinically.Some secular having an intense pain has become a kind of insufferable torment.L-THP (rotundin) is the independently developed anodyne of Chinese scholar, belong to compound of Tetrahydro-proto-berberines class, can be used for multiple treatment of pain, as Encelialgia, headache, tonus pain etc., its mechanism with to relevant (the Hu Jiangyuan Jin nation chapter of the antagonistic action of dopamine 2 receptor, the analgesic activity mechanism and the Dopamine Receptors of rotundine (Rotundine). progress in pharmacology, 1999:64-73), present known compound of Tetrahydro-proto-berberines class has the avidity (Yu Leiping of Dopamine Receptors, Xu Shouxi, Korea Spro is even to eat old Yan, Jin nation's chapter.The Tetrahydro-proto-berberines congener is to the effect of D1 and D2 dopamine receptor subtype. Acta Pharmacologica Sinica, 1989.10 (2): 104-110).Based on this research, the structure with compound of Tetrahydro-proto-berberines class parent nucleus all might become the potent anodyne in analgesic and have DEVELOPMENT PROSPECT.
The invention provides the analgesia pharmacological action of 4 kinds of compound of Tetrahydro-proto-berberines class and the application in the preparation treatment analgesic.
Summary of the invention
The present invention studies the analgesic activities of four kinds of compound of Tetrahydro-proto-berberines class, experimental results show that these four compound of Tetrahydro-proto-berberines class have tangible analgesic activities, can with the anodyne that is prepared into various formulations.
Embodiment
The present invention has investigated the drug effect as periphery anodyne and central analgesia medicine of 4 compound of Tetrahydro-proto-berberines class by acetic acid twisting and two models of hot plate.Compound structure is seen structural formula I
The structure of the several compound of Tetrahydro-proto-berberines class of structural formula I
Embodiment 1:
4 kinds of compound of Tetrahydro-proto-berberines class are to the restraining effect of periphery inflammatory pain.
Blank: 5% glucose solution
Positive control: morphine hydrochloride injection (1mg/kg)
Sample: acetylated Tetrahydropalmatrubine vitriol, acetylated nandinine vitriol, THB-DM-A vitriol, bi-acetylated l-stepholidine vitriol, dissolve with 5% glucose solution respectively, be mixed with 10mg/kg, 20mg/kg, the solution of 40mg/kg.
Experimental technique: 140 of ICR mouse, the male and female dual-purpose, body weight 20 ± 2g, be divided into 14 groups at random, each is organized medicine and all adopts subcutaneous injection, 15min abdominal injection 0.6% acetic acid after the administration, with the mouse web portion indent, hind leg stretches, and buttocks lifts and is index, and mouse turning round the body number of times and calculating analgesia inhibition percentage in 15min respectively organized in record.Analgesia percentage (%)=(control group is turned round body mean one administration group and turned round the body mean)/control group is turned round body mean * 100%.
Experimental result: see Table 1
Table 1 compound of Tetrahydro-proto-berberines class Dichlorodiphenyl Acetate cause mouse writhing influence (M ± SEM, n=10)
By table 1 as seen, 4 kinds of compound of Tetrahydro-proto-berberines class all have the obvious suppression effect for the restraining effect of acetic acid twisting, and are dose-dependent trend.
Embodiment 2:
4 kinds of compound of Tetrahydro-proto-berberines class are as the effect of central analgesia medicine.
Blank: 5% glucose solution
Positive control: morphine hydrochloride injection (10mg/kg)
Sample: acetylated Tetrahydropalmatrubine vitriol, acetylated nandinine vitriol, THB-DM-A vitriol, bi-acetylated l-stepholidine vitriol, dissolve with 5% glucose solution respectively, be mixed with 10mg/kg, 20mg/kg, the solution of 40mg/kg.
Experimental technique:
The screening of laboratory animal: the temperature of hot plate is (55 ± 0.2) ℃, puts female mice on hot plate, measures the normal threshold of pain of each mouse.Licking metapedes with mouse is observation index, surveys altogether 2 times, each at interval greater than 5min, is qualified with average 5-30s.
Qualified mouse is divided into 14 groups, all adopt subcutaneous injection, 15min, 30min, 45min, 60min survey mouse lick sufficient latent period after administration, each mouse licks the percentage of sufficient prolongation of latency after calculating administration, prolongs percentage (%)=(the one basic threshold of pain, the threshold of pain after the administration)/basic threshold of pain * 100%.
Experimental result: see Table 2
Table 2 compound of Tetrahydro-proto-berberines class Dichlorodiphenyl Acetate cause mouse writhing influence (M ± SEM, n=10)
By table 2 as seen, compound of Tetrahydro-proto-berberines class has certain prolongation effect to the hot plate threshold of pain, and especially obvious with bi-acetylated l-stepholidine, THB-DM-A, onset is very fast, and 15min promptly reaches peak value.
Claims (6)
1.4 the structure of individual compound of Tetrahydro-proto-berberines class: structural formula I
The structure of 4 Tetrahydro-proto-berberines compounds of structural formula I
2. the configuration according to 14 carbon atoms of compound of Tetrahydro-proto-berberines class of claim 1 is R type or S type, or the mixtures of two configuration combinations.
3. according to acceptable inorganic or organic salt on the compound of Tetrahydro-proto-berberines class of claim 1 and the pharmacology thereof.Crystalline hydrate, solvate.
4. pharmaceutical composition comprises as acceptable inorganic or organic salt, crystalline hydrate, solvate on the compound of Tetrahydro-proto-berberines class of the claim 1 of activeconstituents and the pharmacology thereof, and acceptable accessories.
5. the compound of Tetrahydro-proto-berberines class of claim 1 is as the application of prodrug.
6. acceptable inorganic or organic salt, crystalline hydrate, the application of solvate in the preparation analgesic on the compound of Tetrahydro-proto-berberines class of claim 1 and the pharmacology thereof.
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| Application Number | Priority Date | Filing Date | Title |
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| CN 201110125330 CN102250087A (en) | 2011-05-16 | 2011-05-16 | Use of several tetrahydro-proto-berberine compounds in relief of pain |
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| CN 201110125330 CN102250087A (en) | 2011-05-16 | 2011-05-16 | Use of several tetrahydro-proto-berberine compounds in relief of pain |
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| CN 201110125330 Pending CN102250087A (en) | 2011-05-16 | 2011-05-16 | Use of several tetrahydro-proto-berberine compounds in relief of pain |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014075309A1 (en) * | 2012-11-19 | 2014-05-22 | 中国科学院大连化学物理研究所 | Use and preparation method of berberine compounds |
| CN112851662A (en) * | 2021-01-21 | 2021-05-28 | 中国药科大学 | Isoquinoline alkaloid and derivatives thereof, preparation method, pharmaceutical composition and application |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101584692A (en) * | 2008-05-19 | 2009-11-25 | 中国科学院上海药物研究所 | Application of L-stopholidine (L-spd) derivative |
-
2011
- 2011-05-16 CN CN 201110125330 patent/CN102250087A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101584692A (en) * | 2008-05-19 | 2009-11-25 | 中国科学院上海药物研究所 | Application of L-stopholidine (L-spd) derivative |
Non-Patent Citations (2)
| Title |
|---|
| 《药学学报》 19620831 金国章等 延胡索药理研究-VIII. 延胡索乙素同型物的化学结构和疗效关系 487-498 1-6 第9卷, 第8期 * |
| 《药学学报》 19650531 孙存济等 延胡索乙素（四氢巴马亭）有关化合物的合成-IV. 酰氧基和烷氧基小蘖因的合成 314-318 1-6 第12卷, 第5期 * |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014075309A1 (en) * | 2012-11-19 | 2014-05-22 | 中国科学院大连化学物理研究所 | Use and preparation method of berberine compounds |
| US9610281B2 (en) | 2012-11-19 | 2017-04-04 | Dalian Institute Of Chemical Physics, Chinese Academy Of Sciences | Use and preparation method of berberine compounds |
| CN112851662A (en) * | 2021-01-21 | 2021-05-28 | 中国药科大学 | Isoquinoline alkaloid and derivatives thereof, preparation method, pharmaceutical composition and application |
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Application publication date: 20111123 |