CN103393673A - Application of compound in anti-aseptic inflammation drug preparation - Google Patents
Application of compound in anti-aseptic inflammation drug preparation Download PDFInfo
- Publication number
- CN103393673A CN103393673A CN2013103594219A CN201310359421A CN103393673A CN 103393673 A CN103393673 A CN 103393673A CN 2013103594219 A CN2013103594219 A CN 2013103594219A CN 201310359421 A CN201310359421 A CN 201310359421A CN 103393673 A CN103393673 A CN 103393673A
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- Prior art keywords
- neonectrolide
- inflammation
- compound
- swelling
- drug preparation
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 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 12
- 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 4
- 230000005764 inhibitory process Effects 0.000 abstract description 2
- 230000008030 elimination Effects 0.000 abstract 1
- 238000003379 elimination reaction Methods 0.000 abstract 1
- 230000008961 swelling Effects 0.000 description 17
- 241000700159 Rattus Species 0.000 description 13
- 241000699670 Mus sp. Species 0.000 description 11
- 210000002683 foot Anatomy 0.000 description 10
- 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
- 210000005069 ears Anatomy 0.000 description 4
- 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
- 239000000203 mixture Substances 0.000 description 3
- 208000005141 Otitis Diseases 0.000 description 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
- 230000017531 blood circulation Effects 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
- 230000002522 swelling 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
- 239000002775 capsule Substances 0.000 description 1
- 230000003247 decreasing effect Effects 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
- 208000024891 symptom Diseases 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
Landscapes
- 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 new purposes of compound N eonectrolide A, relate in particular to the application of Neonectrolide A in the anti-aseptic inflammation medicine of preparation.
Background technology
Inflammation occurs in part, also can affect whole body simultaneously.Local Clinical symptoms is red, hot, swollen, bitterly and dysfunction.Red, heat is due to due to inflammation local vascular dilation, blood flow accelerate.Swollen is because local inflammation is congested, the blood flow composition oozes out and causes.Research and development have the medicine of antiinflammatory action and for alleviating, verify, palliate the agonizing sufferings significant.
the compound N eonectrolide A that the present invention relates to is one and delivered (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, present 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 open first.
Summary of the invention
The purpose of this invention is to provide the application of Neonectrolide A in preparing anti-inflammatory drug.
Described inflammation is aseptic inflammation.
Described compound N eonectrolide A structure is as shown in formula I:
Neonectrolide A applies in preparing anti-inflammatory drug beneficial effect is as follows:
Adopted mice ear model and rat agar foot swelling model, observed the Neonectrolide A of various dose within a certain period of time to the antiinflammatory action of laboratory animal, found that Neonectrolide A has the effective antiinflammatory effect.
1, the mice ear due to Neonectrolide A xylol has obvious inhibitory action, and Neonectrolide A is obvious dose-dependence to the suppression ratio of swelling, and inhibitory action increases with the increase of dosage.
2, foot swelling has obvious inhibitory action to Neonectrolide A to rat agar.
It is open first that the purposes of Neonectrolide A in preparing anti-inflammatory drug that the present invention relates to belongs to, because framework types belongs to brand-new framework types, and its inhibition for inflammation is active unexpectedly strong, there do not is the possibility that is provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, for antiinflammatory, obviously have significant progress simultaneously.
The specific embodiment
The preparation method of compound N eonectrolide A involved in the present invention is referring to 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 subjected to 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 and digest compound Neonectrolide A, add dextrin 195 grams, mix, conventional tabletting is made 1000.
Embodiment 2: the preparation of compound N eonectrolide A capsule involved in the present invention:
Get 5 and digest compound Neonectrolide A, add starch 195 grams, mix, encapsulatedly make 1000.
Below by pharmacodynamic experiment, further illustrate its pharmaceutically active.
Test example 1:Neonectrolide A antiinflammatory pharmacodynamic study
Test material
1. Kunming (KM) plants mice: male, in 6 weeks, 18.5-22.5g, provided by Jiangsu Province's Experimental Animal Center.
2. rat (Wistar): male, weight 140～160g, provided by Jiangsu Province's Experimental Animal Center.
Test method
1. the effect of gavage Neonectrolide A to mice ear inflammation: getting quality is 50 of 18.5～22.5g healthy male mices, is divided at random 5 groups, 10 every group.Neonectrolide A is little, in, heavy dose of group (1.0,2.5,6.25mgkg-1), aspirin group (200mgkg-1), blank group (normal saline).The difference gastric infusion, continuous 7d, 1h after the 7th day gavage, 5 groups of mices all evenly are coated with dimethylbenzene 0.02mL forward and backward of mouse right ear, prepare the auricle inflammatory model.After 1h, mice is put to death in the collare dislocation, along the auricle baseline, cuts two ears, with diameter 8mm card punch, at the same position of two ears, lays round auricle respectively, weighs and is accurate to 0.0001g.With electronic balance, divide the another name quality immediately, left and right two ears of usining are of poor quality as swelling, 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. the effect of gavage Neonectrolide A to the foot swelling of rat agar: get 40 of the healthy male Wistar rats of weight 140～160g, be divided at random 5 groups.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, 7d continuously, 1h after the 7th day gavage, the right back foot of rat the swollen acute inflammation model of subcutaneous injection 10g/L agar 0.1mL preparation foot of wasting time, survey its right back sufficient normal volume with rat foot cubic content measurement instrument.Cause scorching after 1,3,5,8,24h measures respectively the right back sufficient volume of each Mus, and calculates swelling.
2, the impact of Neonectrolide A topical on mice ear inflammation
After causing inflammation, each is organized mouse right ear and highly red and swollen phenomenon occurs at once.Mice ear due to aspirin group and Neonectrolide A group xylol all has obvious inhibitory action, and Neonectrolide A is obvious dose-dependence to the suppression ratio of swelling, and inhibitory action increases with the increase of dosage, the results are shown in Table 1.
The impact of table 1Neonectrolide A xylol induced mice auricle edema (x ± s)
With model group, compare * * P<0.01*P<0.05
3, Neonectrolide A topical is on the impact of rat agar to foot swelling
After injection agar, each organizes rat foot claw all the phenomenon of organizing to a certain degree.Under perusal, model group swelling is rubescent the most obvious, and the aspirin group slightly has swelling without obvious rubescent phenomenon, and Neonectrolide A group situation is between between the two.Rat foot claw thickness all peaks when 3h, slow decreasing all after 3h.Prolongation in time, each is organized rat group and turns swelling and all diminishing, and the swelling inhibitory action of aspirin group is the strongest, and Neonectrolide A all has inhibitory action (p<0.05) to swollen 1,3, the 5 hour inflammation of rat foot, with model group, compared zero difference in 8 hours and 24 hours, in Table 2.
Table 2Neonectrolide A is on the impact of rat agar toes swelling (x ± s)
With model group, compare * * P<0.01*P<0.05
Conclusion: the mice ear due to Neonectrolide A xylol has obvious inhibitory action; Foot swelling has obvious inhibitory action to Neonectrolide A to rat agar.Neonectrolide A can be for the preparation of anti-aseptic inflammation medicine.
Claims (1)
1.Neonectrolide the application of 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 |
Applications Claiming Priority (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 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103393673A true CN103393673A (en) | 2013-11-20 |
| CN103393673B CN103393673B (en) | 2015-04-22 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201310359421.9A Expired - Fee Related CN103393673B (en) | 2013-08-17 | 2013-08-17 | Application of compound in anti-aseptic inflammation drug preparation |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN103393673B (en) |
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2013
- 2013-08-17 CN CN201310359421.9A patent/CN103393673B/en not_active Expired - Fee Related
Non-Patent Citations (1)
| Title |
|---|
| JINWEI REN,ET AL.: "Neonectrolide A, a New Oxaphenalenone Spiroketal from the Fungus Neonectria sp.", 《ORGANIC LETTERS》 * |
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| Publication number | Publication date |
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| CN103393673B (en) | 2015-04-22 |
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