CN109568306A - 2 methyl -5- acetyl -4- furans Ji Ma -1(10)-alkene -6- ketone preparing the application in analgesic - Google Patents
2 methyl -5- acetyl -4- furans Ji Ma -1(10)-alkene -6- ketone preparing the application in analgesic Download PDFInfo
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- CN109568306A CN109568306A CN201910106798.0A CN201910106798A CN109568306A CN 109568306 A CN109568306 A CN 109568306A CN 201910106798 A CN201910106798 A CN 201910106798A CN 109568306 A CN109568306 A CN 109568306A
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
- A61K31/343—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
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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 2 methyl -5- acetyl -4- furans Ji Ma -1 (10)-alkene -6- ketone to prepare the application in analgesic.The present invention is on 2 methyl -5- acetyl -4- furans Ji Ma -1 (10)-alkene -6- ketone existing pharmacological activity basis, multinomial pain model in mice is combined to evaluate the analgesic activity of the compound by many experiments, the present invention passes through chronic pain mouse model caused by acute pain model, complete Freund's adjuvant caused by nocuity heat and mechanical stimulus, the compound is studied to the inhibiting effect of pain, the experimental results showed that the compound significantly inhibits the various pain reactions of mouse in dose dependent.2 methyl -5- acetyl -4- furans Ji Ma -1 (10) provided by the invention-alkene -6- ketone can be prepared into the protective agents 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 2 methyl -5- acetyl -4- furans Ji Ma -1 (10)-alkene -
6- ketone prevents and treats the application in various acute and chronic pain drugs in preparation, belongs 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 2 methyl -5- acetyl -4- furans Ji Ma -1 (10)-alkene -6- ketone is closed to nocuity heat and mechanical thorn
Chronic pain caused by acute pain, complete Freund's adjuvant caused by swashing all has good inhibiting effect.
Summary of the invention
Goal of the invention: the purpose of the present invention is to solve the deficiencies of existing acute and chronic protective agents, pass through a large amount of molecules
Mechanism Study screening, the results showed that 2 methyl -5- acetyl -4- furans Ji Ma -1 (10)-alkene -6- ketone has a variety of acute and chronic pains
There is good therapeutic effect, can reach by 2 methyl -5- acetyl -4- furans Ji Ma -1 (10)-alkene -6- ketone and inhibit nocuity heat and machinery
Chronic pain caused by acute pain, complete Freund's adjuvant (CFA) caused by stimulating, the present invention provides a kind of for more on this basis
Kind acute and chronic pain effectively prevents drug.
Technical solution: in order to achieve the above object, the technical scheme adopted by the invention is as follows:
2 methyl -5- acetyl -4- furans Ji Ma -1 (10)-alkene -6- ketone is preparing the application in analgesic.
Preferably, the above-described various Acute or chronic pain drugs of prevention and treatment are lucky by 2 methyl -5- acetyl -4- furans
Ma -1 (10)-alkene -6- ketone composition.
Preferably, 2 methyl -5- acetyl -4- furans Ji Ma -1 (10)-alkene -6- ketone is preparing anti-treating acute and chronic pain
Application in pain drug.
Above-described Acute or chronic pain includes acute pain caused by nocuity heat and mechanical stimulus and complete Freund's adjuvant
Caused chronic pain.
Preferably, above-described 2 methyl -5- acetyl -4- furans Ji Ma -1 (10)-alkene -6- ketone acid mouse has
Effect dosage is 30mg/kg.
Preferably, above-described 2 methyl -5- acetyl -4- furans Ji Ma -1 (10)-alkene -6- ketone is anti-in preparation
The application in various Acute or chronic pain drugs is controlled, by 2 methyl -5- acetyl -4- furans Ji Ma -1 (10)-alkene -6- ketone and auxiliary agent system
At paste, aqua etc. and contain 2 methyl -5- acetyl -4- furans Ji Ma -1 (10)-alkene -6- ketone composition compound preparation.
2 methyl -5- acetyl -4- furans Ji Ma -1 (10)-alkene -6- ketone structural formula is as shown in Figure 1, report the text of its structure
It offers 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, and the present invention is in 2 methyl -5- acetyl -4- furans Ji Ma -1
(10) it on-alkene -6- ketone existing pharmacological activity basis, is furtherd investigate by many experiments and screens its new clinical efficacy, this
Invention studies 2 methyl -5- acetyl -4- furans Ji Ma -1 (10)-alkene -6- ketone to mouse by various acute and chronic pain animal models
The inhibiting effect of the pain sensation, the experimental results showed that oral 2 methyl -5- acetyl -4- furans Ji Ma -1 (10)-alkene -6- ketone can be significant
Inhibit chronic pain caused by acute pain caused by mouse nocuity heat and mechanical stimulus and complete Freund's adjuvant.It is provided by the invention
2 methyl -5- acetyl -4- furans Ji Ma -1 (10)-alkene -6- ketone can be prepared into the prevention and treatment medicine of efficient, less toxic various acute and chronic pains
Object has important economic value, is worthy of promotion and application.
Detailed description of the invention
Fig. 1 is 2 methyl -5- acetyl -4- furans Ji Ma -1 (10)-alkene -6- ketone 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.
12 methyl -5- acetyl -4- furans Ji Ma -1 (10) of embodiment-alkene -6- ketone inhibits pain caused by nocuity thermostimulation
Bitterly
(1) modeling method
Mouse is fixed in a mold, and influence of the hot irradiation experiment observation administration of sole to mouse foot-up delay time is commented
2 methyl -5- acetyl -4- furans Ji Ma -1 (10) of valence-alkene -6- ketone analgesic activity, (control group 16, be administered totally 32 mouse
Group 16).
(2) nocuity thermostimulation causes the control prece of pain
Administration group: 2 methyl -5- acetyl -4- furans Ji Ma -1 (10)-alkene -6- ketone, dosage: 30mg/kg/day.Dosage form is
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 24 hours.
(5) experimental result
As table 1 the result shows that, 2 methyl -5- acetyl -4- furans Ji Ma -1 (10)-alkene -6- ketone table of 30m g/kg/day
Reveal the inhibiting effect for causing pain to heat irradiation stimulation well.And inhibiting effect can continue 4 hours or more.
The 1 mouse whipping time of table
* p < 0.05 (and control group compares)
22 methyl -5- acetyl -4- furans Ji Ma -1 (10) of embodiment-alkene -6- ketone inhibits pain caused by mechanical stimulus
(1) modeling method
Mouse is fixed in a mold, and 0.4gVonfrey detection administration front and back mouse changes the response frequency of mechanical stimulus,
Totally 24 mouse.(control group 12, administration group 12).
(2) mechanical stimulus causes the control prece of pain
Administration group: 2 methyl -5- acetyl -4- furans Ji Ma -1 (10)-alkene -6- ketone；Dosage: 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 2 hours.
(5) experimental result
Such as table 2 the experimental results showed that, 2 methyl -5- acetyl -4- furans Ji Ma -1 (10)-alkene -6- ketone of 30m g/kg/day
Show the inhibiting effect for causing pain to mechanical stimulus well.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 | 35±3.7 | 36±5.1 |
| 1 | 38±4.2 | 19±3.8* |
| 2 | 36±6.3 | 21±4.7* |
* p < 0.05 (and control group compares)
32 methyl -5- acetyl -4- furans Ji Ma -1 (10) of embodiment-alkene -6- ketone inhibits inflammatory caused by CFA model to ache
Bitterly
(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 2
Methyl -5- acetyl -4- furans Ji Ma -1 (10)-alkene -6- ketone analgesic activity, totally 28 mouse.(control group 14, administration group
14).
(2) nocuity thermostimulation causes the control prece of pain
Administration group: 2 methyl -5- acetyl -4- furans Ji Ma -1 (10)-alkene -6- ketone；Dosage: 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
Such as table 3 the experimental results showed that, 2 methyl -5- acetyl -4- furans Ji Ma -1 (10)-alkene -6- ketone of 30m g/kg/day
Good inhibiting effect is shown to the chronic inflammatory pain model of CFA induction.
The 3 mouse foot-up time of table
| Before modeling | After modeling | After stomach-filling | |
| Control group | 9.4±0.27 | 4.4±0.31* | 4.4±0.50 |
| Administration group | 9.8±0.51 | 4.6±0.42* | 7.6±0.63# |
(compare before * and modeling, compare after # and modeling) p < 0.05
Above the experimental results showed that, it is provided by the invention by 2 methyl -5- acetyl -4- furans Ji Ma -1 (10)-alkene -6- ketone
Has effects that good anti-treating acute and chronic pain, and protective agents are non-hormone compounds, 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 (5)
1.2 methyl -5- acetyl -4- furans Ji Ma -1 (10)-alkene -6- ketone is preparing the application in analgesic.
2. 2 methyl -5- acetyl -4- furans Ji Ma -1 (10)-alkene -6- ketone according to claim 1 is preparing analgesic
In application, which is characterized in that 2 methyl -5- acetyl -4- furans Ji Ma -1 (10)-alkene -6- ketone preparation prevent and treat nocuity Spurs
Application in Acute Pain drug caused by swashing.
3. 2 methyl -5- acetyl -4- furans Ji Ma -1 (10)-alkene -6- ketone according to claim 1 is preparing analgesic
In application, which is characterized in that 2 methyl -5- acetyl -4- furans Ji Ma -1 (10)-alkene -6- ketone is mechanical in preparation prevention and treatment nocuity
Application in acute pain drug caused by stimulating.
4. 2 methyl -5- acetyl -4- furans Ji Ma -1 (10)-alkene -6- ketone according to claim 1 is preparing analgesic
In application, which is characterized in that 2 methyl -5- acetyl -4- furans Ji Ma -1 (10)-alkene -6- ketone preparation prevent and treat inflammatory chronic pain
Application in drug.
5. prepared by 2 methyl -5- acetyl -4- furans Ji Ma -1 (10)-alkene -6- ketone according to any one of claims 1 to 4
Application in anti-treating acute and chronic pain disease medicament, which is characterized in that by 2 methyl -5- acetyl -4- furans Ji Ma -1 (10)-alkene -6-
Ketone and auxiliary agent are made paste, aqua and contain 2 methyl -5- acetyl -4- furans Ji Ma -1 (10)-alkene -6- ketone component compound
Preparation.
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| CN201910106798.0A CN109568306A (en) | 2019-02-02 | 2019-02-02 | 2 methyl -5- acetyl -4- furans Ji Ma -1(10)-alkene -6- ketone preparing the application in analgesic |
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|---|---|---|---|
| CN201910106798.0A CN109568306A (en) | 2019-02-02 | 2019-02-02 | 2 methyl -5- acetyl -4- furans Ji Ma -1(10)-alkene -6- ketone preparing the application in analgesic |
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Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
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- 2019-02-02 CN CN201910106798.0A patent/CN109568306A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
|---|
| 陈婷等: "乳香-没药配伍前后化学成分溶出变化及其对LPS-诱导的巨噬细胞产生NO的影响", 《中国中药杂志》 * |
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