CN109620833A - Application of the acetyl elemolic acid in preparation prevention and treatment Acute or chronic pain drug - Google Patents
Application of the acetyl elemolic acid in preparation prevention and treatment Acute or chronic pain drug Download PDFInfo
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- CN109620833A CN109620833A CN201910096088.4A CN201910096088A CN109620833A CN 109620833 A CN109620833 A CN 109620833A CN 201910096088 A CN201910096088 A CN 201910096088A CN 109620833 A CN109620833 A CN 109620833A
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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Abstract
The invention discloses acetyl elemolic acids to prepare the application in analgesic.The present invention is on the basis of the existing pharmacological activity of acetyl elemolic acid, the analgesic activity of acetyl elemolic acid is evaluated by the comprehensive combination of many experiments various Acute or chronic pain mouse models, the present invention passes through chronic pain mouse model caused by acute pain model caused by nocuity heat and mechanical stimulus, sciatic nerve ligation and complete Freund's adjuvant, acetyl elemolic acid is studied to the inhibiting effect of pain, the experimental results showed that oral acetyl elemolic acid significantly inhibits the various pain reactions of mouse in dose dependent.Acetyl elemolic acid provided by the invention can be prepared into the analgesic of efficient, the less toxic various acute and chronic pains of prevention and treatment, has important economic value, is worthy of promotion and application.
Description
Technical field
The present invention relates to a kind of active ingredient of Chinese herbs, and in particular to acetyl elemolic acid is preparing anti-treating acute and chronic pain drug
In application, belong to technical field of pharmaceuticals.
Background technique
Pain is a kind of offending feeling and emotional experience, with potential or substantial tissue damage, pain
Continue or intermittently continue 3 months or more persons to be defined as chronic ache.International Society of Pain is big in world's pain in 2002
Reach common understanding in meeting: chronic ache is a kind of disease.The substantial amounts of chronic pain patient in global range, various countries' illness rate
12%~50% etc..The illness rate of China's chronic ache constantly increases, particularly evident in elderly population, epidemiological survey
It has been shown that, the illness rate of 18~25 years old crowd are 29.72%, and the illness rate of the elderly's chronic ache is up to 42.23%.Chronic ache
Illness rate is high, durante dolors are long, easily causes the imbalance of patient's body function, immunity degradation, induces various complication；In addition,
Chronic pain patient is relatively susceptible to suffer from the inferior health problems such as insomnia, anxiety, depression, and serious shadow quality of life, increases family and society is negative
Load.
In recent years, pain is due to its high incidence and low cure rate gradually by multi-disciplinary attention.With pain Animals
It the foundation of model and constantly improve, Theory of Pain Mechanism research is also more deep.For many years research shows that its pathogenesis and periphery
Sensitization, central sensitization, the sympathetic pain of duration and downlink disinthibite etc. related.The cause of disease, pathogenesis and the symptom of pain
Between relationship it is complicated, although control method is numerous, current most of patients cannot still be cured；Overall cure rate is low, most of patients
Long-term administration is needed, financial burden is heavy.Neuropathic pain caused by different pathogeny to the reactions of various drugs, prevention and treatment dosage and
The course for the treatment of is inconsistent, and clinic need to fully consider the individual instances and the prevention and treatment sensibility rational use of medicines of patient.Although pain is especially
There are many means of prevention of chronic pain, but medical treatment remains its main control method.Clinically commonly using protective agents at present has
Antiepileptic, tricyclic antidepressant, local control's drug, opioid etc..Although the prevention and treatment of pain has achieved centainly
Progress, but its high incidence and low cure rate are still the present and following urgent problem to be solved.Wish multidisciplinary to combine to mind
Pathogenesis through pathologic pain and clinical prevention are carried out deeper into research, for it is following select more preferably means of prevention provide according to
According to.
Chinese medicine analgesia has long history, distinct characteristic and good effect.The present invention is comprehensive by many experiments
Multinomial Pain behaviour index discovery acetyl elemolic acid is closed to acute pain, sciatic nerve knot caused by nocuity heat and mechanical stimulus
It pricks and all has good inhibiting effect with chronic pain caused by complete Freund's adjuvant.
Summary of the invention
Goal of the invention: the purpose of the present invention is to solve the deficiencies of existing acute and chronic pain protective agents, by largely grinding
Study carefully screening, the results showed that acetyl elemolic acid has good therapeutic effect for a variety of acute and chronic pains, reachable by acetyl elemolic acid
To inhibiting slow caused by acute pain, sciatic nerve ligation and complete Freund's adjuvant (CFA) caused by nocuity heat and mechanical stimulus
Property pain, the present invention, which provides, on this basis a kind of effectively prevents drug for a variety of acute and chronic pains.
Technical solution: in order to achieve the above object, the technical scheme adopted by the invention is as follows:
Application of the acetyl elemolic acid in preparation prevention and treatment Acute or chronic pain drug.
Preferably, above-described prevention and treatment Acute or chronic pain drug is made of acetyl elemolic acid.
Preferably, various Acute or chronic pains described above include acute caused by nocuity heat and mechanical stimulus
Bitterly, chronic pain caused by sciatic nerve ligation and complete Freund's adjuvant.
Preferably, above-described acetyl elemolic acid mouse effective dose is 10~30mg/kg.
Preferably, above-described acetyl elemolic acid prevents and treats answering in various Acute or chronic pain drugs in preparation
With by paste made of acetyl elemolic acid and auxiliary agent, aqua etc. and the compound preparation formed containing acetyl elemolic acid.
Acetyl elemolic acid structural formula is as shown in Figure 1.Report the document of its structure are as follows:
Chen Ting, Su Shulan, section gold storehouse for grain, etc., Shang Erxin, Qian great Wei, Tang Yuping olibanum-myrrh compatibility front and back chemical component dissolution
Variation and its influence CHINA JOURNAL OF CHINESE MATERIA MEDICA that NO is generated to the macrophage of LPS- induction, 2013,38 (2): 179-185.
The utility model has the advantages that
Compared to the prior art, the present invention has the following advantages, base of the present invention in the existing pharmacological activity of acetyl elemolic acid
On plinth, furtherd investigate by many experiments and screen its new clinical efficacy, the present invention by various acute and chronic pain animal models,
Acetyl elemolic acid is studied to the inhibiting effect of the mouse pain sensation, the experimental results showed that oral acetyl elemolic acid can significantly inhibit
Chronic pain caused by acute pain caused by mouse nocuity heat and mechanical stimulus, sciatic nerve ligation and complete Freund's adjuvant.This
The acetyl elemolic acid that invention provides can be prepared into the protective agents of efficient, less toxic various acute and chronic pains, have important warp
Ji value, is worthy of promotion and application.
Detailed description of the invention
Fig. 1 is acetyl elemolic acid structural schematic diagram.
Specific embodiment
Combined with specific embodiments below, the present invention is furture elucidated, it should be understood that these embodiments are merely to illustrate the present invention
Rather than limit the scope of the invention, after the present invention has been read, those skilled in the art are to various equivalences of the invention
The modification of form falls within the application range as defined in the appended claims.
1 acetyl elemolic acid of embodiment inhibits pain caused by nocuity thermostimulation
(1) modeling method
Mouse is fixed in a mold, and tail half immerses 50 DEG C of hot water, and influence of the observation administration to the mouse whipping time is commented
The analgesic activity of valence acetyl elemolic acid, totally 30 mouse, every group 10.
(2) nocuity thermostimulation causes the control prece of pain
Administration group: acetyl elemolic acid.Dosage: low dosage (10mg/kg/day), high dose (30m g/kg/day).
Dosage form: 0.5% sodium carboxymethyl cellulose suspension liquid.Control group: 0.5% sodium carboxymethyl cellulose suspension liquid.
(3) medication
Gastric infusion.
(4) Pain behaviour measuring method
It is observed continuously after administration 4 hours.
(5) experimental result
As shown in table 1.The acetyl elemolic acid of 10mg/kg/day and 30m g/kg/day is shown well to injury
Property thermostimulation causes the inhibiting effect of pain.And inhibiting effect can continue 4 hours or more.The wherein second of 30m g/kg/day
Acyl elemolic acid shows better analgesic activity, so subsequent experimental dosage is the acetyl elemol of 30m g/kg/day
Acid.
The 1 mouse whipping time of table
* p < 0.05 (and control group compares)
2 acetyl elemolic acid of embodiment inhibits pain (1) modeling method caused by mechanical stimulus
Mouse is fixed in particular manufacturing craft, response frequency of the 0.4gVonfrey detection administration front and back mouse to mechanical stimulus
Change, totally 24 mouse.Every group 12.
(2) mechanical stimulus causes the control prece of pain
Administration group: acetyl elemolic acid.Dosage: acetyl elemolic acid (30m g/kg/day).Dosage form: 0.5% carboxymethyl
Sodium cellulosate suspension.Control group: physiological saline.
(3) medication
Gastric infusion.
(4) Pain behaviour measuring method
It is observed continuously after administration 2 hours.
(5) experimental result
Such as table 2, the experimental results showed that, the acetyl elemolic acid of 30m g/kg/day shows well to draw mechanical stimulus
Play the inhibiting effect of pain.And inhibiting effect can continue 2 hours or more.
2 mouse foot-up percentage of time of table
| Administration time (hour) | Control group (%) | Administration group (%) |
| 0 | 36±3 | 33±4 |
| 1 | 37±3 | 23±3* |
| 2 | 34±5 | 17±4* |
* p < 0.05 (and control group compares)
3 acetyl elemolic acid of embodiment inhibits the inhibiting effect of inflammatory pain caused by CFA model
(1) modeling method
Mouse sole injects the 5 inflammation inducing pain models of μ LCFA, the influence that observation administration is sensitized mouse thermalgesia, evaluation
The analgesic activity of acetyl elemolic acid, totally 20 mouse, every group 10.
(2) nocuity thermostimulation causes the control prece of pain
Protective agents: acetyl elemolic acid.Dosage: acetyl elemolic acid high dose (30m g/kg/day).Dosage form:
0.5% sodium carboxymethyl cellulose suspension liquid.Control group: 0.5% sodium carboxymethyl cellulose suspension liquid.
(3) medication
Gastric infusion.
(4) Pain behaviour measuring method
Observed behavior after administration 1 hour.
(5) experimental result
As table 3 the experimental results showed that, the chronic inflammatory pain mould that the acetyl elemolic acid of 30m g/kg/day induces CFA
Type shows good inhibiting effect.
The 3 mouse foot-up time of table
| Before modeling (second) | After modeling (second) | After administration (second) | |
| Control group | 10.6±0.69 | 4.7±0.32* | 5.3±0.48 |
| Administration group | 9.8±0.51 | 4.6±0.42* | 8.6±0.47# |
(compare before * and modeling, compare after # and modeling) p < 0.05
4 acetyl elemolic acid of embodiment inhibits the inhibiting effect of pain caused by neurogenic pain model
(1) modeling method
Neurogenic pain is by nervous system injury or a kind of abnormal caused pain status for being difficult to prevent and treat.Ischium
Nerve ligation model is most common Animal models of neuropathic pain.The present invention 1% amobarbital (10mg/kg, abdominal cavity
Injection) it anesthetized mice and is fixed on operating table, skin in the middle part of mouse right lower extremity stock, blunt separation muscle are cut after cropping disinfection
Exposure sciatic nerve is ligaturing 2 close to its crotch 4-0 silk thread, is being spaced about 1mm, ligatures intensity to cause Calf muscle
Slight trembling, slows down, but does not block and be advisable by the circulation of superficial blood vessel.The normal saline flushing surface of a wound, layer-by-layer suture notch, art
Finish and divides cage, conventinal breeding.The influence that observation administration is sensitized mouse thermalgesia evaluates the analgesic activity of acetyl elemolic acid, altogether
24 mouse.Every group 8.
(2) nocuity thermostimulation causes the control prece of pain
Administration group: acetyl elemolic acid.Dosage: acetyl elemolic acid high dose (30m g/kg/day).Dosage form: 0.5%
Sodium carboxymethyl cellulose suspension liquid.Control group: 0.5% sodium carboxymethyl cellulose suspension liquid.
Positive drug: Gabapentin 0.2g/kg/day
(3) medication
Gastric infusion.
(4) Pain behaviour measuring method
Observed behavior after administration 1 hour.
(5) experimental result
Such as table 4, the result shows that, the acetyl elemolic acid of 30m g/kg/day shows preferably neuropathic pain model
Inhibiting effect.
The 4 mouse foot-up time of table
| Before modeling (second) | After modeling (second) | Administration group (second) | |
| Control group | 9.7±0.68 | 3.2±0.21* | 3.5±0.37 |
| Administration group | 10.8±0.51 | 3.6±0.42* | 8.6±0.47# |
| Positive drug group | 10.6±0.82 | 3.5±0.17* | 10.3±0.82# |
(compare before * and modeling, compare after # and modeling) p < 0.05
Above the experimental results showed that, the function by acetyl elemolic acid with good anti-treating acute and chronic pain provided by the invention
Effect, and protective agents are non-hormone compounds, and safety is good and side effect is low.
The above is only a preferred embodiment of the present invention, it is noted that for the ordinary skill people of the art
For member, various improvements and modifications may be made without departing from the principle of the present invention, these improvements and modifications are also answered
It is considered as protection scope of the present invention.
Claims (6)
1. application of the acetyl elemolic acid in preparation prevention and treatment Acute or chronic pain drug.
2. application of the acetyl elemolic acid according to claim 1 in preparation prevention and treatment Acute or chronic pain drug, feature
It is, the application in acute pain drug caused by acetyl elemonic acid prevents and treats nocuity thermostimulation in preparation.
3. application of the acetyl elemolic acid according to claim 1 in preparation prevention and treatment Acute or chronic pain drug, feature
It is, the application in acute pain drug caused by acetyl elemonic acid prevents and treats noxious mechanical stimulation in preparation.
4. application of the acetyl elemolic acid according to claim 1 in preparation prevention and treatment Acute or chronic pain drug, feature
It is, application of the acetyl elemonic acid in preparation prevention and treatment neurogenic chronic pain drug.
5. acetyl elemolic acid according to claim 1 prevents and treats the application in various Acute or chronic pain drugs in preparation,
It is characterized in that, application of the acetyl elemonic acid in preparation prevention and treatment inflammatory chronic pain drug.
6. acetyl elemolic acid according to any one of claims 1 to 5 answering in preparation prevention and treatment Acute or chronic pain drug
With, which is characterized in that by paste made of acetyl elemolic acid and auxiliary agent, aqua and answering containing acetyl elemolic acid component
Square preparation.
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| Application Number | Priority Date | Filing Date | Title |
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| CN201910096088.4A CN109620833A (en) | 2019-01-31 | 2019-01-31 | Application of the acetyl elemolic acid in preparation prevention and treatment Acute or chronic pain drug |
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| Application Number | Priority Date | Filing Date | Title |
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| CN201910096088.4A CN109620833A (en) | 2019-01-31 | 2019-01-31 | Application of the acetyl elemolic acid in preparation prevention and treatment Acute or chronic pain drug |
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Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1615888A (en) * | 2004-08-31 | 2005-05-18 | 凌沛学 | Medicine composition and its use |
| WO2008058514A1 (en) * | 2006-11-14 | 2008-05-22 | Eberhard Karls Universität Tübingen | Preparations comprising boswellic acids for inhibiting the synthesis of prostaglandin e2 |
| DE102009004436A1 (en) * | 2008-10-15 | 2010-04-29 | Aureliasan Gmbh | Use of a tirucallic acid, a lupanic acid or a roburic acid and its salt, derivative or salt of the derivative as a medicament to treat pains, inflammations, fever, cancer, allergies, Crohn's disease, psoriasis and rheumatoid arthritis |
| CN106074660A (en) * | 2016-08-11 | 2016-11-09 | 南京中医药大学 | Olibanum and Myrrha application in preparation preventing and treating neuropathic pain disease medicament |
| CN108785357A (en) * | 2018-09-18 | 2018-11-13 | 南京中医药大学 | A kind of masticinic acid and myrrh terpene compatible composition and its preparation method and application |
-
2019
- 2019-01-31 CN CN201910096088.4A patent/CN109620833A/en active Pending
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1615888A (en) * | 2004-08-31 | 2005-05-18 | 凌沛学 | Medicine composition and its use |
| WO2008058514A1 (en) * | 2006-11-14 | 2008-05-22 | Eberhard Karls Universität Tübingen | Preparations comprising boswellic acids for inhibiting the synthesis of prostaglandin e2 |
| DE102009004436A1 (en) * | 2008-10-15 | 2010-04-29 | Aureliasan Gmbh | Use of a tirucallic acid, a lupanic acid or a roburic acid and its salt, derivative or salt of the derivative as a medicament to treat pains, inflammations, fever, cancer, allergies, Crohn's disease, psoriasis and rheumatoid arthritis |
| CN106074660A (en) * | 2016-08-11 | 2016-11-09 | 南京中医药大学 | Olibanum and Myrrha application in preparation preventing and treating neuropathic pain disease medicament |
| CN108785357A (en) * | 2018-09-18 | 2018-11-13 | 南京中医药大学 | A kind of masticinic acid and myrrh terpene compatible composition and its preparation method and application |
Non-Patent Citations (1)
| Title |
|---|
| 常允平等: "乳香的化学成分和药理活性研究进展", 《现代药物与临床》 * |
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