CN103393673B - Application of compound in anti-aseptic inflammation drug preparation - Google Patents
Application of compound in anti-aseptic inflammation drug preparation Download PDFInfo
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- CN103393673B CN103393673B CN201310359421.9A CN201310359421A CN103393673B CN 103393673 B CN103393673 B CN 103393673B CN 201310359421 A CN201310359421 A CN 201310359421A CN 103393673 B CN103393673 B CN 103393673B
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- Prior art keywords
- neonectrolide
- inflammation
- compound
- swelling
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- 206010061218 Inflammation Diseases 0.000 title claims abstract description 22
- 230000004054 inflammatory process Effects 0.000 title claims abstract description 18
- 150000001875 compounds Chemical class 0.000 title claims abstract description 15
- 238000002360 preparation method Methods 0.000 title claims abstract description 10
- 239000003814 drug Substances 0.000 title claims abstract description 9
- 229940079593 drug Drugs 0.000 title abstract 3
- 230000000694 effects Effects 0.000 abstract description 5
- 230000008030 elimination Effects 0.000 abstract 1
- 238000003379 elimination reaction Methods 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 230000008961 swelling Effects 0.000 description 19
- 241000700159 Rattus Species 0.000 description 13
- 210000002683 foot Anatomy 0.000 description 10
- 241000699670 Mus sp. Species 0.000 description 9
- 230000002401 inhibitory effect Effects 0.000 description 9
- 229920001817 Agar Polymers 0.000 description 8
- 239000008272 agar Substances 0.000 description 8
- CTQNGGLPUBDAKN-UHFFFAOYSA-N O-Xylene Chemical compound CC1=CC=CC=C1C CTQNGGLPUBDAKN-UHFFFAOYSA-N 0.000 description 6
- BSYNRYMUTXBXSQ-UHFFFAOYSA-N Aspirin Chemical group CC(=O)OC1=CC=CC=C1C(O)=O BSYNRYMUTXBXSQ-UHFFFAOYSA-N 0.000 description 5
- 230000003110 anti-inflammatory effect Effects 0.000 description 5
- 238000003304 gavage Methods 0.000 description 4
- 230000001629 suppression Effects 0.000 description 4
- 241000699666 Mus <mouse, genus> Species 0.000 description 3
- 241001335047 Neonectria sp. Species 0.000 description 3
- 239000002260 anti-inflammatory agent Substances 0.000 description 3
- 229940124599 anti-inflammatory drug Drugs 0.000 description 3
- 210000005069 ears Anatomy 0.000 description 3
- 240000001307 Myosotis scorpioides Species 0.000 description 2
- 208000005141 Otitis Diseases 0.000 description 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
- 210000000078 claw Anatomy 0.000 description 2
- 230000002496 gastric effect Effects 0.000 description 2
- 238000001802 infusion Methods 0.000 description 2
- 230000003285 pharmacodynamic effect Effects 0.000 description 2
- 238000012360 testing method Methods 0.000 description 2
- 230000000699 topical effect Effects 0.000 description 2
- 240000006409 Acacia auriculiformis Species 0.000 description 1
- 229920001353 Dextrin Polymers 0.000 description 1
- 239000004375 Dextrin Substances 0.000 description 1
- 241000196324 Embryophyta Species 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 206010030113 Oedema Diseases 0.000 description 1
- 241000700157 Rattus norvegicus Species 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 208000038016 acute inflammation Diseases 0.000 description 1
- 230000006022 acute inflammation Effects 0.000 description 1
- 238000010171 animal model Methods 0.000 description 1
- 230000000259 anti-tumor effect Effects 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 230000017531 blood circulation Effects 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 230000006835 compression Effects 0.000 description 1
- 238000007906 compression Methods 0.000 description 1
- 235000019425 dextrin Nutrition 0.000 description 1
- 230000010339 dilation Effects 0.000 description 1
- 230000003467 diminishing effect Effects 0.000 description 1
- 230000004064 dysfunction Effects 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 108010084652 homeobox protein PITX1 Proteins 0.000 description 1
- 230000002757 inflammatory effect Effects 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 238000012827 research and development Methods 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 238000010254 subcutaneous injection Methods 0.000 description 1
- 239000007929 subcutaneous injection Substances 0.000 description 1
- 238000010998 test method Methods 0.000 description 1
- 210000003371 toe Anatomy 0.000 description 1
- 230000002792 vascular Effects 0.000 description 1
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The present invention relates to an application of Neonectrolide A in anti-inflammation drug preparation, wherein the inflammation is aseptic inflammation, and the Neonectrolide A has a good anti-inflammation and inflammation elimination effect. According to the present invention, the use of the Neonectrolide A in anti-inflammation drug preparation is firstly disclosed; and a skeleton type of the Neonectrolide A belongs to a completely new skeleton type, inflammation inhibition activity of the Neonectrolide A is strong, possibility that other compounds provide revelations for the Neonectrolide A can not exist, prominent substantive characteristics are provided, and significant progress for anti-inflammation is provided.
Description
Technical field
The present invention relates to the novelty teabag of compound N eonectrolide A, particularly relate to the application of Neonectrolide A 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 N eonectrolide A that the present invention relates to is one and delivers (Jinwei Ren in 2012, et al., Neonectrolide A, a New Oxaphenalenone Spiroketal from the Fungus Neonectria sp.Organic Letters, 2012, 14(24) 6226 – 6229.) noval chemical compound, this compound has brand-new framework types, current purposes has anti-tumor activity (Jinwei Ren, et al., Neonectrolide A, a NewOxaphenalenone Spiroketal from the Fungus Neonectria sp.Organic Letters, 2012, 14(24) 6226 – 6229.), the purposes of the Neonectrolide A 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 Neonectrolide A and prepare the application in anti-inflammatory drug.
Described inflammation is aseptic inflammation.
Described compound N eonectrolide A structure is as shown in formula I:
Neonectrolide A 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 Neonectrolide A of various dose within a certain period of time to the antiinflammatory action of laboratory animal, find that Neonectrolide A has effective antiinflammatory effect.
1, the mice ear caused by Neonectrolide A xylol has obvious inhibitory action, and the suppression ratio of Neonectrolide A to swelling is obvious dose-dependence, and inhibitory action increases with the increase of dosage.
2, Neonectrolide A has obvious inhibitory action to the foot swelling of rat agar.
The Neonectrolide A 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 N eonectrolide A involved in the present invention is see document (Jinwei Ren, et al., Neonectrolide A, a New Oxaphenalenone Spiroketal from the Fungus Neonectria sp.Organic Letters, 2012,14(24) 6226 – 6229.)
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 N eonectrolide A tablet involved in the present invention:
Get 5 g of compound Neonectrolide A, add 195 grams, dextrin, mixing, Conventional compression makes 1000.
Embodiment 2: the preparation of compound N eonectrolide A capsule involved in the present invention:
Get 5 g of compound Neonectrolide A, add starch 195 grams, mixing, encapsulatedly makes 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
Test example 1:Neonectrolide A 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 Neonectrolide A 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.Neonectrolide A 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 Neonectrolide A 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.Neonectrolide A 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, Neonectrolide A 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 Neonectrolide A group xylol all have obvious inhibitory action, and the suppression ratio of Neonectrolide A 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 1Neonectrolide A xylol induced mice auricle edema
Compare with model group, * * P<0.01*P<0.05
3, Neonectrolide A 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 Neonectrolide A 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, Neonectrolide A 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 2Neonectrolide A 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 Neonectrolide A xylol has obvious inhibitory action; Neonectrolide A has obvious inhibitory action to the foot swelling of rat agar.Neonectrolide A may be used for preparing anti-aseptic inflammation medicine.
Claims (1)
- The application of 1.Neonectrolide A in the anti-aseptic inflammation medicine of preparation, described compound N eonectrolideA structure is as shown in formula I:
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310359421.9A CN103393673B (en) | 2013-08-17 | 2013-08-17 | Application of compound in anti-aseptic inflammation drug preparation |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310359421.9A CN103393673B (en) | 2013-08-17 | 2013-08-17 | Application of compound in anti-aseptic inflammation drug preparation |
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| Publication Number | Publication Date |
|---|---|
| CN103393673A CN103393673A (en) | 2013-11-20 |
| CN103393673B true CN103393673B (en) | 2015-04-22 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN201310359421.9A Expired - Fee Related CN103393673B (en) | 2013-08-17 | 2013-08-17 | Application of compound in anti-aseptic inflammation drug preparation |
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| Country | Link |
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- 2013-08-17 CN CN201310359421.9A patent/CN103393673B/en not_active Expired - Fee Related
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