CN105412098A - Application of Melodinine E in preparing drugs for anti-aseptic inflammation - Google Patents
Application of Melodinine E in preparing drugs for anti-aseptic inflammation Download PDFInfo
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- CN105412098A CN105412098A CN201510966734.XA CN201510966734A CN105412098A CN 105412098 A CN105412098 A CN 105412098A CN 201510966734 A CN201510966734 A CN 201510966734A CN 105412098 A CN105412098 A CN 105412098A
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- Prior art keywords
- melodininee
- inflammation
- melodinine
- aseptic inflammation
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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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines Containing Plant Substances (AREA)
Abstract
The invention relates to application of Melodinine E in preparing drugs for anti-aseptic inflammation, the inflammation is aseptic inflammation and the Melodinine E has good anti-inflammatory and antiphlogistic effects. The application of the Melodinine E related in the invention in preparing the drugs for anti-aseptic inflammation is disclosed for the first time, due to the fact that a matrix type belongs to a new matrix type, and the inhibitory activity to inflammation is unexpectedly high, the possibility that other components provide any revelations does not exist, the Melodinine E has outstanding substantive features, and obviously has remarkable improvement for anti-inflammation at the same time.
Description
Technical field
The present invention relates to the novelty teabag of compound MelodinineE, particularly relate to the application of MelodinineE in the anti-aseptic inflammation medicine of preparation.
Background technology
Inflammation occurs in local, also can affect whole body simultaneously.Local clinical feature be red, hot, swollen, pain and dysfunction.Red, heat is caused by inflammation local vascular dilation, blood flow are accelerated.Swollen is because local inflammation is congested, flow components oozes out and causes.The medicine that research and development have an antiinflammatory action for alleviation checking, palliate the agonizing sufferings significant.
The compound MelodinineE that the present invention relates to is one and delivers (AtsushiUmehara in 2014, etal., TotalSynthesesofLeuconoxine, LeuconodineB, andMelodinineEbyOxidativeCyclicAminalFormationandDiaster eoselectiveRing-ClosingMetathesis.Org.Lett.2014, 16, noval chemical compound 2526-2529.), this compound has brand-new framework types (AtsushiUmehara, etal., TotalSynthesesofLeuconoxine, LeuconodineB, andMelodinineEbyOxidativeCyclicAminalFormationandDiaster eoselectiveRing-ClosingMetathesis.Org.Lett.2014, 16, 2526-2529.), the purposes of the MelodinineE that the present invention relates in the anti-aseptic inflammation medicine of preparation belongs to first public.
Summary of the invention
The object of this invention is to provide MelodinineE and prepare the application in anti-inflammatory drug.
Described inflammation is aseptic inflammation.
Described compound MelodinineE structure is as shown in formula I:
The application of described MelodinineE in the anti-aseptic inflammation medicine of preparation, the mice ear caused by MelodinineE xylol and have inhibitory action to the foot swelling of rat agar.
A kind of anti-aseptic inflammation medicine, be that active component interpolation adjuvant is prepared from by MelodinineE, preparation method, for getting 5 g of compound MelodinineE, adds 195 grams, dextrin, and mixing, Conventional compression makes 1000.
A kind of anti-aseptic inflammation medicine, be that active component adds adjuvant and is prepared from by MelodinineE, preparation method, for getting 5 g of compound MelodinineE, adds starch 195 grams, mixing, encapsulatedly makes 1000.
MelodinineE is to prepare the beneficial effect applied in anti-inflammatory drug as follows:
Have employed mice ear model and rat agar foot swelling model, observe the MelodinineE of various dose within a certain period of time to the antiinflammatory action of laboratory animal, find that MelodinineE has effective antiinflammatory effect.
1, the mice ear caused by MelodinineE xylol has obvious inhibitory action, and the suppression ratio of MelodinineE to swelling is obvious dose-dependence, and inhibitory action increases with the increase of dosage.
2, MelodinineE has obvious inhibitory action to the foot swelling of rat agar.
The MelodinineE that the present invention relates to belongs to first public preparing the purposes in anti-inflammatory drug, because framework types belongs to brand-new framework types, and its inhibit activities for inflammation is unexpectedly strong, there is not the possibility being provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, for antiinflammatory, obviously there is significant progress simultaneously.
Detailed description of the invention
The preparation method of compound MelodinineE involved in the present invention is see document (AtsushiUmehara, etal., TotalSynthesesofLeuconoxine, LeuconodineB, andMelodinineEbyOxidativeCyclicAminalFormationandDiaster eoselectiveRing-ClosingMetathesis.Org.Lett.2014,16,2526-2529.)
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not by any restriction of specific embodiment, but be limited by claim.
Embodiment 1: the preparation of compound MelodinineE tablet involved in the present invention:
Get 5 g of compound MelodinineE, add 195 grams, dextrin, mixing, Conventional compression makes 1000.
Embodiment 2: the preparation of compound MelodinineE capsule involved in the present invention:
Get 5 g of compound MelodinineE, add starch 195 grams, mixing, encapsulatedly makes 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
Test example 1:MelodinineE antiinflammatory pharmacodynamic study
Test material
1. Kunming (KM) plants mice: male, 6 weeks, and 18.5-22.5g is provided by Jiangsu Province's Experimental Animal Center.
2. rat (Wistar): male, weight 140 ~ 160g, is provided by Jiangsu Province's Experimental Animal Center.
Test method
1. gavage MelodinineE is to the effect of mouse ear inflammation: getting quality is 18.5 ~ 22.5g healthy male mice 50, is divided into 5 groups at random, often organizes 10.MelodinineE is little, in, heavy dose of group (1.0,2.5,6.25mgkg-1), aspirin group (200mgkg-1), blank group (normal saline).Gastric infusion respectively, continuous 7d, 1h after the 7th day gavage, 5 groups of mices are all evenly coated with dimethylbenzene 0.02mL forward and backward of mouse right ear, prepare auricle inflammatory model.After 1h, mice is put to death in collare dislocation, cuts two ears, lay round auricle respectively, weigh and be accurate to 0.0001g with diameter 8mm card punch at the same position of two ears along auricle baseline.Another name quality is divided immediately with electronic balance, of poor quality as swelling using left and right two ear, and calculate its swelling and suppression ratio.
Swelling=auris dextra sheet weight-left auricle weight
Suppression ratio=(the average swelling of matched group-average swelling of administration group) average swelling * 100% of/matched group
Experimental result:
1. gavage MelodinineE is to the effect of rat agar foot swelling: get the healthy male Wistar rat 40 of weight 140 ~ 160g, be divided into 5 groups at random.MelodinineE is little, in, heavy dose of group (1.0,2.5,6.25mgkg-1), aspirin group (200mgkg-1), blank group (normal saline).Respectively gastric infusion, continuous 7d, 1h after the 7th day gavage, the right back foot of the rat subcutaneous injection 10g/L agar 0.1mL that wastes time prepares the swollen acute inflammation model of foot, surveys its right back sufficient normal volume with rat foot cubic content measurement instrument.Cause scorching after 1,3,5,8,24h measures the right back sufficient volume of each Mus respectively, and calculates swelling.
2, MelodinineE topical is on the impact of mouse ear inflammation
After causing inflammation, there is highly red and swollen phenomenon in each group mouse right ear at once.Aspirin group and the mice ear caused by MelodinineE group xylol all have obvious inhibitory action, and the suppression ratio of MelodinineE to swelling is obvious dose-dependence, and inhibitory action increases with the increase of dosage, the results are shown in Table 1.
The impact (x ± s) of table 1MelodinineE xylol induced mice auricle edema
Compare with model group, * * P<0.01*P<0.05
3, MelodinineE topical is on the impact of rat agar to foot swelling
After injection agar, each group rat foot claw all has tissue phenomenon to a certain degree.Under perusal, model group swelling is rubescent the most obvious, and slightly swelling is without obvious redness phenomenon for aspirin group, and MelodinineE group situation is between therebetween.Rat foot claw thickness all peaks when 3h, all slowly declines after 3h.Prolongation in time, each group of rat group turns swelling and is all diminishing, the swelling inhibitory action of aspirin group is the strongest, MelodinineE all has inhibitory action (p<0.05) to swollen 1,3, the 5 hour inflammation of rat foot, within 8 hours and 24 hours, compare zero difference with model group, in table 2.
Table 2MelodinineE is on the impact (x ± s) of rat agar toes swelling
Compare with model group, * * P<0.01*P<0.05
Conclusion: the mice ear caused by MelodinineE xylol has obvious inhibitory action; MelodinineE has obvious inhibitory action to the foot swelling of rat agar.MelodinineE may be used for preparing anti-aseptic inflammation medicine.
Claims (4)
- The application of 1.MelodinineE in anti-aseptic inflammation medicine, described compound MelodinineE structure is as shown in formula I:Formula I.
- 2. the application of MelodinineE in anti-aseptic inflammation medicine as claimed in claim 1, is characterized in that mice ear caused by MelodinineE xylol and has inhibitory action to the foot swelling of rat agar.
- 3. an anti-aseptic inflammation medicine, it is characterized in that by MelodinineE described in claim 1 being that active component interpolation adjuvant is prepared from, preparation method, for getting 5 g of compound MelodinineE, adds 195 grams, dextrin, and mixing, Conventional compression makes 1000.
- 4. an anti-aseptic inflammation medicine, it is characterized in that by MelodinineE described in claim 1 being that active component adds adjuvant and is prepared from, preparation method, for getting 5 g of compound MelodinineE, adds starch 195 grams, and mixing, encapsulatedly makes 1000.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510966734.XA CN105412098A (en) | 2015-12-20 | 2015-12-20 | Application of Melodinine E in preparing drugs for anti-aseptic inflammation |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510966734.XA CN105412098A (en) | 2015-12-20 | 2015-12-20 | Application of Melodinine E in preparing drugs for anti-aseptic inflammation |
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| Publication Number | Publication Date |
|---|---|
| CN105412098A true CN105412098A (en) | 2016-03-23 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN201510966734.XA Pending CN105412098A (en) | 2015-12-20 | 2015-12-20 | Application of Melodinine E in preparing drugs for anti-aseptic inflammation |
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Application publication date: 20160323 |