CN103462950B - Application of scopariusins in preparation of medicine treating acute gout - Google Patents
Application of scopariusins in preparation of medicine treating acute gout Download PDFInfo
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- CN103462950B CN103462950B CN201310470419.9A CN201310470419A CN103462950B CN 103462950 B CN103462950 B CN 103462950B CN 201310470419 A CN201310470419 A CN 201310470419A CN 103462950 B CN103462950 B CN 103462950B
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Abstract
The invention provides the application of scopariusins in preparation of the medicine treating the acute gout. The experiment research result shows that the scopariusins has the protection effect on an acute gout model of human vascular endothelial cell damage caused by urate and inhibits ICAM-1 expression. The application of scopariusins in preparation of the medicine treating the acute gout is disclosed for the first time. The scopariusins has the advantages of being high in activity of prevention and treatment of the acute gout and prominent in substantive features, and makes remarkable progress in prevention and treatment of the acute gout.
Description
Technical field
The present invention relates to the novelty teabag of compound S copariusins, particularly relate to the application of Scopariusins in preparation treatment acute gout medicine.
Background technology
Gout (gouty), also known as gouty arthritis (gouty arthritis), is the disease in body caused by purine metabolic disturbance, shows as uric acid in blood too much, is easy to make urate (MSU) organize crystallization in joint etc.The acute attack of gout is that the MSU owing to being deposited on joint causes neutrophilic granulocyte local infiltration and inflammatory reaction.
The compound S copariusins that the present invention relates to is one and delivers (Min Zhou in 2013, et al., Scopariusins, A New Class of ent-Halimane Diterpenoids Isolated from Isodonscoparius, and Biomimetic Synthesis of Scopariusin A and Isoscoparin N.OrganicLetters, 2013, noval chemical compound 15(2): 314 – 317.), this compound has brand-new framework types, research finds not have significant inhibitory action (Min Zhou to melanoma cell etc., et al., Scopariusins, A NewClass of ent-Halimane Diterpenoids Isolated from Isodon scoparius, and BiomimeticSynthesis of Scopariusin A and Isoscoparin N.Organic Letters, 2013, 15(2): 314 – 317.), the purposes of the Scopariusins that the present invention relates in preparation treatment acute gout medicine belongs to first public.
Summary of the invention
The present invention MSU causes the acute gout model evaluation display that human vascular endothelial (HUVEC) damages, and causes HUVEC damage and has protective effect, and suppress ICAM-1 to express to MSU, can be used for preparation treatment acute gout anti-inflammatory drugs.The object of the present invention is to provide the novelty teabag of Scopariusins in medical science, specifically relate to the application of Scopariusins in preparation treatment acute gout medicine.
The object of the invention is to be realized by following technical scheme:
The present invention proposes the application of Scopariusins in preparation treatment acute gout medicine.Find out from pharmacological evaluation, Scopariusins has treatment acute pain wind action preferably.Due to the pharmacological action of the first public Scopariusins of the present invention in treatment acute gout.
Described compound S copariusins structure is as shown in formula I:
Result of study shows; the acute gout model evaluation display of HUVEC damage is caused with MSU; Scopariusins can protect MSU to cause HUVEC damage; reduce apoptosis; improve cytoactive; suppress ICAM-1 to express, have the activity of anti-acute gout inflammation, Scopariusins can be used for preparation treatment acute gout anti-inflammatory drugs.
The purposes of the Scopariusins that the present invention relates in preparation treatment acute gout medicine belongs to first public, because framework types belongs to brand-new framework types, and its control for acute gout is active strong, possess outstanding substantive distinguishing features, the control simultaneously for acute gout obviously has significant progress.
Detailed description of the invention
The preparation method of compound S copariusins involved in the present invention is see document (Min Zhou, et al., Scopariusins, A New Class of ent-Halimane Diterpenoids Isolated from Isodonscoparius, and Biomimetic Synthesis of Scopariusin A and Isoscoparin N.OrganicLetters, 2013,15(2): 314 – 317.)
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 S copariusins tablet involved in the present invention:
Get 5 g of compound Scopariusins, add 195 grams, dextrin, mixing, Conventional compression makes 1000.
Embodiment 2: the preparation of compound S copariusins capsule involved in the present invention:
Get 5 g of compound Scopariusins, add starch 195 grams, mixing, encapsulatedly makes 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
The anti-acute gout inflammation test of experimental example 1:Scopariusins:
1: method
1. solution preparation
5g uric acid adds 1000ml distilled water and boils, and add 5%NaOH solution and adjust PH7.4, stir, cooling crystallization makes Monosodium urate crystallization (MSU).By the MSU10mg autoclaving made, add not containing the DMEM culture fluid 10ml of serum, grinding is made into the DMEM solution of 1mg/ml.During experiment, this solution adds the MSU solution that DMEM culture fluid is made into variable concentrations DMEM again.
Scopariusins2.5mg, dissolve with dimethyl sulfoxide (DMSO), DMSO final concentration <0.02%, then the DMEM culture fluid adding serum-free, be mixed with concentration 2.5ug/ml, 25ug/ml, 250ug/ml.
Positive drug indomethacin 2.0mg, the same Scopariusins of method, compound concentration 20ug/ml.
2. the In vitro culture of vascular endothelial cell
Human umbilical vein endothelial cell HUVEC strain, thered is provided by preclinical medicine institute of Nanjing University of Traditional Chinese Medicine, cell is through detection of mycoplasma, and without mycoplasma contamination, cell is through 0.25% trypsinization, DMEM culture fluid containing 10% calf serum neutralizes, centrifugal (1000r/min × 6min), removes supernatant, adds the DMEM culture fluid containing 10% calf serum, move in Tissue Culture Flask, put 37 DEG C, 5%CO
2secondary Culture in incubator.
3. MSU is stimulated to the impact of HUVEC vigor
HUVEC cultivates in culture bottle, and in time growing to 70% ~ 80% and merge, with 0.25% trypsinization, centrifugal, 10% calf serum DMEM culture fluid washs 3 times, with 10% calf serum DMEM culture fluid furnishing 4 × 10
4/ ml cell suspension, implant 96 orifice plates (every hole 200ul), cultivate light sucking-off original fluid after 24 hours, carry out following experiment, often organize each 8 holes, concrete grouping and liquid feeding as follows: matched group (200ulDMEM culture fluid), model group (100ug/ml MSU solution), intervene A group (100ug/ml MSU solution+2.5ug/ml Scopariusins), intervene B group (100ug/ml MSU solution+25ug/mlScopariusins), intervene C group (100ug/ml MSU solution+250ug/ml Scopariusins), continue after liquid feeding to put 37 DEG C, 5%CO
2cultivate 24 hours in incubator, collect supernatant, remaining HUVEC is for measuring cytoactive, and every hole adds 5mg/ml MTT liquid 20ul again, continues to put 37 DEG C, 5%CO
2cultivate after 4 hours in incubator, abandon MTT liquid, add dimethyl sulfoxide 200ul and dissolve, concussion, read absorbance in microplate reader, wavelength 490nm.
Positive drug group liquid feeding (100ug/ml MSU solution+20ug/ml indomethacin), additive method is the same.
Data statistics processes, and cell viability (%)=experimental group absorbance/matched group absorbance × 100%, the results are shown in Table 1.
Compared with matched group, model group cell viability significantly reduces (P<0.01, P<0.05), after positive drug indomethacin and Scopariusins intervene, cell viability significantly improves (P<0.01, P<0.05), and be better than matched group, wherein, the cell viability of each concentration group of Scopariusins is better than positive drug indomethacin.
Table 1Scopariusins is on the impact (X ± s) of the vascular endothelial cell vigor that MSU stimulates
Compare with model group, * * P<0.01*P<0.05, compares with matched group,
##p<0.01
#p<0.05
4. impact is expressed on ICAM-1
To be in the HUVEC trypsinization of 0.25% of exponential phase, and blow and beat gently, make cell suspension, adjustment cell density is 5 × 10
9/ L, is inoculated in Tissue Culture Flask.After cell covers with (about 24h), abandoning supernatant, is divided into following group: matched group, model group (100ug/ml MSU solution), Scopariusins group (100ug/ml MSU solution+25ug/mlScopariusins), continue cultivation 24 hours, PBS collecting cell, centrifugally removes supernatant, adds CD54 monoclonal antibody, after 30min, PBS washs, re-suspended cell, application its positive percentage of flow cytomery (n=10000), repeat 3 times, the results are shown in Table 2.
Table 2Scopariusins is on the impact (X ± s) of the ICAM-1 Expression in Vascular Endothelial Cells that MSU stimulates
Compare with model group, * * P<0.01*P<0.05, compares with matched group,
##p<0.01
#p<0.05
2, result result display, blank group HUVEC almost expresses without ICAM-1, and the expression of model group ICAM-1 is the highest, and compared with model group, the expression of Scopariusins to ICAM-1 has stronger inhibitory action.
Conclusion: the acute gout model evaluation display causing HUVEC damage with MSU; Scopariusins can protect MSU to cause HUVEC damage; reduce apoptosis; improve cytoactive; ICAM-1 is suppressed to express; have the activity of anti-acute gout inflammation, Scopariusins can be used for preparation treatment acute gout anti-inflammatory drugs.
Claims (1)
1.Scopariusins the application in preparation treatment acute gout medicine, described compound S copariusins structure is as shown in formula I:
Formula I.
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| CN105287505A (en) * | 2015-11-05 | 2016-02-03 | 淄博齐鼎立专利信息咨询有限公司 | Application of Microphyllandiolide in preparation of acute gout treating medicine |
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Non-Patent Citations (2)
| Title |
|---|
| Scopariusins, A New Class of ent-Halimane Diterpenoids Isolated from Isodon scoparius, and Biomimetic Synthesis of Scopariusin A and Isoscoparin N;Min Zhou et al.;《Organic Letters》;20121224;第15卷(第2期);314-317 * |
| 唇形科香茶菜属植物化学成分研究;吴桂凡 等;《中医药学刊》;20030630;第21 卷(第6 期);1012-1013 * |
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