CN103127154A - Application of Gypensapogenin A in medicines resisting aseptic inflammation - Google Patents
Application of Gypensapogenin A in medicines resisting aseptic inflammation Download PDFInfo
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- CN103127154A CN103127154A CN 201210415363 CN201210415363A CN103127154A CN 103127154 A CN103127154 A CN 103127154A CN 201210415363 CN201210415363 CN 201210415363 CN 201210415363 A CN201210415363 A CN 201210415363A CN 103127154 A CN103127154 A CN 103127154A
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- gypensapogenin
- inflammatory
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- inflammation
- swelling
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Abstract
The invention relates to application of Gypensapogenin A in preparing anti-inflammatory medicines. The inflammatory is aseptic inflammation, and the Gypensapogenin A has an excellent anti-inflammatory and inflammatory-eliminating effect. The application of the Gypensapogenin A in preparing anti-inflammatory medicines is made public for the first time, due to the fact that matrix type is brand novel, besides, the Gypensapogenin A has an unexpectedly high acute renal failure inhibitory activity, the probability that inspiration is obtained from other compounds does not exist, and the Gypensapogenin A possesses outstanding substantial characteristics, meanwhile, significant progress is obviously achieved by the application of the Gypensapogenin A in anti-inflammatory.
Description
Technical field
The present invention relates to the application of Gypensapogenin A in the preparation anti-inflammatory drug.
Background technology
Inflammation occurs in the 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 verify, palliate the agonizing sufferings significant for alleviating.
the compound Gypensapogenin A that the present invention relates to is one and delivered (Li in 2012, N. et al., 2012. Triterpenes possessing an unprecedented skeleton isolated from hydrolyzate of total saponins from Gynostemma pentaphyllum. European Journal of Medicinal Chemistry 50, 173 – 178.) New skeleton compound, this compound has brand-new framework types, present purposes only relates to the cytotoxic activity (Li of human tumor cell line, N. et al., 2012. Triterpenes possessing an unprecedented skeleton isolated from hydrolyzate of total saponins from Gynostemma pentaphyllum. European Journal of Medicinal Chemistry 50, 173 – 178.), belong to open first for the purposes of the Gypensapogenin A that the present invention relates in the preparation anti-inflammatory drug, because framework types belongs to brand-new framework types, and its inhibition for inflammation is active unexpectedly strong, there is not the possibility that is provided any enlightenment by other compounds, possesses outstanding substantive distinguishing features, be used for simultaneously antiinflammatory and obviously have significant progress.
Summary of the invention
The purpose of this invention is to provide the application of Gypensapogenin A in the preparation anti-inflammatory drug.
Described inflammation is aseptic inflammation.
Described compound Gypensapogenin A structure is as shown in formula I:
Formula I
The beneficial effect that Gypensapogenin A uses in the preparation anti-inflammatory drug is as follows:
First proved Gypensapogenin A have the effective antiinflammatory effect.Adopted mice ear model and rat agar foot swelling model due to classical dimethylbenzene, the Gypensapogenin A that observes various dose is within a certain period of time to the antiinflammatory action of laboratory animal.Studies show that:
1, the mice ear due to Gypensapogenin A xylol has obvious inhibitory action, and Gypensapogenin 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 Gypensapogenin A to rat agar.
The purposes of the Gypensapogenin A that the present invention relates in the preparation anti-inflammatory drug belongs to open first, because framework types belongs to brand-new framework types, and its inhibition for inflammation is active unexpectedly strong, there is not the possibility that is provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, be used for simultaneously antiinflammatory and obviously have significant progress.
The specific embodiment
the preparation method of compound Gypensapogenin A involved in the present invention is referring to document (Li, N. et al., 2012. Triterpenes possessing an unprecedented skeleton isolated from hydrolyzate of total saponins from Gynostemma pentaphyllum. European Journal of Medicinal Chemistry 50, 173 – 178. and Wei, J.X. et al., 1982. Two new dammaran sapogenins from leaves of Panax notoginseng. Planta Medica, 45 (3): 167-171.).
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 limited by claim.
Embodiment 1: the preparation of compound Gypensapogenin A tablet involved in the present invention:
Get 20 and digest compound Gypensapogenin A, add conventional adjuvant 180 grams that prepare tablet, mixing, conventional tablet machine are made 1000.
Embodiment 2: the preparation of compound Gypensapogenin A capsule involved in the present invention:
Get 20 and digest compound Gypensapogenin A, add the conventional adjuvant such as starch 180 grams that prepare capsule, mixing is encapsulatedly made 1000.
Further illustrate its pharmaceutically active below by pharmacodynamic experiment.
Test example 1:Gypensapogenin A antiinflammatory pharmacodynamic study
Test material
1. Kunming (KM) plants mice: male, in 6 weeks, 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. the effect of gavage Gypensapogenin A to mice ear inflammation: get 50 of weight 18.5 ~ 22.5g healthy male mices, be divided at random 5 groups, 10 every group.Gypensapogenin A is little, in, heavy dose of group (1.0,2.5,6.25mgkg
-1), aspirin group (200 mgkg
-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, preparation auricle inflammatory model.After 1h, mice is put to death in the collare dislocation, cuts two ears along the auricle baseline, lays round auricle at the same position of two ears respectively with diameter 8mm card punch, and weighing is accurate to 0.0001g.Divide the another name quality with electronic balance immediately, of poor quality as swelling with left and right two ears, and calculate its swelling and suppression ratio.
Swelling=auris dextra sheet weight-left auricle is heavy
Suppression ratio=(the average swelling of matched group-average swelling of administration group)/average swelling * 100% of matched group
1. the effect of gavage Gypensapogenin 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.Gypensapogenin A is little, in, heavy dose of group (1.0,2.5,6.25mgkg
-1), aspirin group (200 mgkg
-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 is surveyed 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.
Result of the test
1, the impact of Gypensapogenin 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 Gypensapogenin A group xylol all has obvious inhibitory action, Gypensapogenin A is obvious dose-dependence to the suppression ratio of swelling, inhibitory action increases with the increase of dosage, the results are shown in Table 1.
The impact of table 1 Gypensapogenin A xylol induced mice auricle edema (x ± s)
Compare * P＜0.001, * * P＜0.001 with model group
2, Gypensapogenin A topical is on the impact of rat agar to foot swelling
After injection agar, each organizes rat foot claw all to a certain degree the phenomenon of organizing.Under perusal, model group swelling is rubescent the most obvious, and the aspirin group slightly has swelling without obvious rubescent phenomenon, and Gypensapogenin A group situation is between both.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 Gypensapogenin A all has inhibitory action (p＜0.05) to swollen 1,3, the 5 hour inflammation of rat foot, compared zero difference with model group, and saw Table 2 in 8 hours and 24 hours.
Table 2 Gypensapogenin A is on the impact of rat agar toes swelling (x ± s)
Compare * P＜0.001, * * P＜0.001 with model group
Conclusion: the mice ear due to Gypensapogenin A xylol has obvious inhibitory action; Foot swelling has obvious inhibitory action to Gypensapogenin A to rat agar.Gypensapogenin A can be for the preparation of anti-inflammatory drug.
Claims (2)
1.Gypensapogenin the application of A in anti-inflammatory drug is characterized in that described inflammation is aseptic inflammation.
According to claim 1 Gypensapogenin A in the application of preparation in anti-inflammatory drug, described compound Gypensapogenin A structure as
Formula IShown in:
Formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 201210415363 CN103127154A (en) | 2012-10-26 | 2012-10-26 | Application of Gypensapogenin A in medicines resisting aseptic inflammation |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 201210415363 CN103127154A (en) | 2012-10-26 | 2012-10-26 | Application of Gypensapogenin A in medicines resisting aseptic inflammation |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN103127154A true CN103127154A (en) | 2013-06-05 |
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Family Applications (1)
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|---|---|---|---|
| CN 201210415363 Withdrawn CN103127154A (en) | 2012-10-26 | 2012-10-26 | Application of Gypensapogenin A in medicines resisting aseptic inflammation |
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| Country | Link |
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| CN (1) | CN103127154A (en) |
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2012
- 2012-10-26 CN CN 201210415363 patent/CN103127154A/en not_active Withdrawn
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| PB01 | Publication | ||
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| C04 | Withdrawal of patent application after publication (patent law 2001) | ||
| WW01 | Invention patent application withdrawn after publication |
Application publication date: 20130605 |