CN103340874B - The application of Myriberine A in the anti-aseptic inflammation medicine of preparation - Google Patents

The application of Myriberine A in the anti-aseptic inflammation medicine of preparation Download PDF

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CN103340874B
CN103340874B CN201310331712.7A CN201310331712A CN103340874B CN 103340874 B CN103340874 B CN 103340874B CN 201310331712 A CN201310331712 A CN 201310331712A CN 103340874 B CN103340874 B CN 103340874B
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myriberine
inflammation
swelling
group
preparation
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CN103340874A (en
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赵巧英
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Shanghai Tianlong Pharmaceutical Co., Ltd.
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Shangyu City Zhong Tai Medical Science And Technology Co Ltd
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Abstract

The present invention relates to Myriberine A and preparing the application in anti-inflammatory drug, described inflammation is aseptic inflammation, and described Myriberine A has good antiinflammatory, antiinflammation.The Myriberine 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.

Description

The application of Myriberine A in the anti-aseptic inflammation medicine of preparation
Technical field
The present invention relates to the novelty teabag of compound Myriberine A, particularly relate to the application of Myriberine 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 Myriberine A that the present invention relates to is one and delivers (Sheng-Dian Huang in 2012, et al., Myriberine A, a New Alkaloid with an Unprecedented Heteropentacyclic Skeleton from Myrioneuron faberi.Organic Letters, 2012, 3 (15), 590 – 593.) noval chemical compound, this compound has brand-new framework types, current purposes only relates to and suppresses hepatitis C virus (Sheng-Dian Huang, et al., Myriberine A, a New Alkaloid with an Unprecedented Heteropentacyclic Skeleton from Myrioneuron faberi.Organic Letters, 2012, 3 (15), 590 – 593.), the purposes of the Myriberine 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 Myriberine A and prepare the application in anti-inflammatory drug.
Described inflammation is aseptic inflammation.
Described compound Myriberine A structure is as shown in formula I:
Myriberine A is to prepare the beneficial effect applied in anti-inflammatory drug as follows:
First demonstrate Myriberine A and there is effective antiinflammatory effect.Have employed the classical mice ear model caused by dimethylbenzene and rat agar foot swelling model, observe the Myriberine A of various dose within a certain period of time to the antiinflammatory action of laboratory animal.Research shows:
1, the mice ear caused by Myriberine A xylol has obvious inhibitory action, and the suppression ratio of Myriberine A to swelling is obvious dose-dependence, and inhibitory action increases with the increase of dosage.
2, Myriberine A has obvious inhibitory action to the foot swelling of rat agar.
The Myriberine 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 Myriberine A involved in the present invention is see document (Sheng-Dian Huang, et al., Myriberine A, a New Alkaloid with an Unprecedented Heteropentacyclic Skeleton from Myrioneuron faberi.Organic Letters, 2012,3 (15), 590 – 593.)
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 Myriberine A tablet involved in the present invention:
Get 5 g of compound Myriberine A, add 195 grams, dextrin, mixing, Conventional compression makes 1000.
Embodiment 2: the preparation of compound Myriberine A capsule involved in the present invention:
Get 5 g of compound Myriberine A, add starch 195 grams, mixing, encapsulatedly makes 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
Test example 1:Myriberine 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 Myriberine 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.Myriberine 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 Myriberine 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.Myriberine 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, Myriberine 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 Myriberine A group xylol all have obvious inhibitory action, and the suppression ratio of Myriberine 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 1Myriberine A xylol induced mice auricle edema
Compare with model group, * * P<0.01 * P<0.05
3, Myriberine 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 Myriberine 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, Myriberine 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 2Myriberine 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 Myriberine A xylol has obvious inhibitory action; Myriberine A has obvious inhibitory action to the foot swelling of rat agar.Myriberine A may be used for preparing anti-inflammatory drug.

Claims (1)

  1. The application of 1.Myriberine A in the anti-aseptic inflammation medicine of preparation, described compound Myriberine A structure is as shown in formula I:
CN201310331712.7A 2013-08-01 2013-08-01 The application of Myriberine A in the anti-aseptic inflammation medicine of preparation Active CN103340874B (en)

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Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
Myriberine A, a New Alkaloid with an Unprecedented Heteropentacyclic Skeleton from Myrioneuron faberi;Sheng-Dian Huang等;《ORGANIC LETTERS》;20130115;第15卷(第3期);第590-593页 *
生物碱类化合物药理作用研究进展;蒙其淼等;《时针国医国药》;20031231;第14卷(第11期);第700-702页 *
马爱瑛.生物碱的提取与分离.《固原师专学报(自然科学)》.2006,第27卷(第3期), *

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