CN106727602A - Application of the ursolic acid in treatment gout medicine is prepared - Google Patents
Application of the ursolic acid in treatment gout medicine is prepared Download PDFInfo
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- CN106727602A CN106727602A CN201611247667.7A CN201611247667A CN106727602A CN 106727602 A CN106727602 A CN 106727602A CN 201611247667 A CN201611247667 A CN 201611247667A CN 106727602 A CN106727602 A CN 106727602A
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
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Abstract
The present invention relates to application of the ursolic acid in treatment gout medicine is prepared, the characteristics of with instant effect, short treating period, effect stability.
Description
Technical field
The present invention relates to pharmaceutical technology field, application of the ursolic acid in treatment gout medicine is prepared is specifically related to.
Background technology
Hyperuricemia and gout have turned into one of ciril disease of the modern life, be one kind due to internal purine anabolism
Increase, uric acid produce excess or because uric acid excretion is bad cause blood in uric acid raise, hyperuricemia is gout
One biochemical marker.The clinical manifestation of gout is often divided into acute stage, intermittent phase, chronic phase and renal lesions etc., is mainly shown as
Urarthritis and gouty nephropathy.Renal lesions is the result of long-term hyperuricemia development, hyperuricemia
Kidneys of patients pathologic finding almost has different degrees of infringement, and renal symptom occurs in the course of disease in about 1/3 patient.On height
The treatment of uricacidemia, secondary hyperuricemia is treated mainly for its underlying diseases, and primary hyperuricemia
Treatment, drug therapy is typically subject to using diet, motion control.Suppress uric acid generation medicine main mechanism to suppress xanthine
Oxidizing ferment（XO）Activity.Allopurinol is the representative of this kind of medicine, is all the time the clinical first-line drug of antigout, although drop
Uric acid effect is significant, but it is very weak to the defencive function of kidney.
Compound ursolic acid of the present invention, its No. CAS:77-52-1, can carry from the leaf of rosaceous plant loquat
Obtain, be a kind of triterpene compound being present in natural plants, with calmness, anti-inflammatory, antibacterial, anti-diabetic, anti-burst
The various biological effects such as ulcer, reduction blood sugar.It is first public that the present invention is used as preparing anti-ventilation medicine.
The content of the invention
It is of the invention in order to realize it is an object of the invention to provide application of the ursolic acid in treatment gout medicine is prepared
Purpose, intends adopting the following technical scheme that：
One aspect of the present invention is related to application of the ursolic acid in treatment gout medicine is prepared, and the structural formula of described compound is：
In a preferred embodiment of the present invention, described medicine includes or does not include other active components.
In a preferred embodiment of the present invention, described medicine does not contain other active components, also contains pharmacy
Upper acceptable auxiliary material.
The present invention provides new medicine for gout patients, the characteristics of with instant effect, short treating period, effect stability.
Specific embodiment
If not specified, the conventional meanses that technological means used is well known to those skilled in the art in embodiment.
Embodiment 1
Its pharmaceutical activity is further illustrated below by pharmacodynamic experiment.
Experimental example 1：The anti-acute gout inflammation test of ursolic acid：
1:Method
1. solution is prepared
5g uric acid adds 1000ml distilled water to boil, plus 5% NaOH solution adjusts pH7.4, stirring, cooling crystallization to be made urine
Sour sodium crystallizes (MSU).The MSU10mg autoclavings that will be made, plus the DMEM nutrient solution 10ml without serum, grinding are matched somebody with somebody
Into the DMEM solution of 1mg/ml.During experiment, this solution adds DMEM nutrient solutions to be made into the MSU of various concentrations DMEM again
Solution.
Ursolic acid 2.5mg, is dissolved, final concentration with ethanol<0.02%, then add the DMEM nutrient solutions of serum-free, prepare
Into concentration 2.5ug/ml, 25ug/ml, 250ug/ml.
Positive drug Indomethacin 2.0mg, the same ursolic acid of method, compound concentration 20ug/ml.
2. the in vitro culture of vascular endothelial cell
Human umbilical vein endothelial cell HUVEC plants, provided by Guangxi medical college, cell is former without branch through detection of mycoplasma
Body pollution, cell is neutralized through 0.25% Trypsin Induced, the DMEM nutrient solutions containing 10% calf serum, and (1000r/ is centrifuged
Min × 6min), remove supernatant, plus the DMEM nutrient solutions containing 10% calf serum, in moving into Tissue Culture Flask, put 37 DEG C, 5%
Secondary Culture in CO2 incubators.
3. the influence of HUVEC vigor is stimulated MSU
HUVEC is cultivated in blake bottle, to be grown when 70%~80% fusion, with 0.25% Trypsin Induced, centrifugation,
10% calf serum DMEM nutrient solutions are washed 3 times, and 4 × 104/ml is tuned into 10% calf serum DMEM nutrient solutions
Cell suspension, 96 orifice plates of implantation (per hole 200ul), culture gently suctions out original fluid, carries out following experiment after 24 hours,
Every group of each 8 hole, specific packet and liquid feeding are as follows：Control group (200ulDMEM nutrient solutions), (100ug/ml MSU are molten for model group
Liquid), intervene A groups (100ug/ml MSU solution+2.5ug/ml ursolic acid), (100ug/ml MSU are molten to intervene B groups
Liquid+25ug/ ml ursolic acid), intervene C groups (100ug/ml MSU solution+250ug/ml ursolic acid), liquid feeding is follow-up
It is continuous to put 37 DEG C, cultivate 24 hours in 5% CO2 incubators, supernatant is collected, remaining HUVEC is used to determine cell work
Property, per Kong Zaijia 5mg/ml MTT liquid 20ul, continue to put 37 DEG C, in 5% CO2 incubators after culture 4 hours, abandon
MTT liquid, adds dimethyl sulfoxide (DMSO) 200ul dissolvings, concussion to read absorbance, wavelength 490nm in ELIASA.
Positive drug group liquid feeding (100ug/ml MSU solution+20ug/ml Indomethacins), other method is ibid.
Statistical data treatment, cell viability (%)=experimental group absorbance/control group absorbance ×
100%, the results are shown in Table 1.
Compared with control group, model group cell viability is substantially reduced (P<0.01, P<0.05), positive drug Indomethacin and
Cell viability significantly improves (P after ursolic acid intervention<0.01, P<0.05), and control group is better than, wherein, each concentration of ursolic acid
The cell viability of group is better than positive drug Indomethacin.
The influence (X ± s) of the vascular endothelial cell vigor that the ursolic acid of table 1 stimulates MSU
| Group | Drug concentration（Mcg/ml） | N/ holes | Cell viability（%） |
| Control group | 0 | 8 | 100 |
| Model group | 0 | 8 | 84 |
| Positive drug | 20 | 8 | 103 |
| Intervene A groups | 2.5 | 8 | 169 |
| Intervene B groups | 25 | 8 | 200 |
| Intervene C groups | 250 | 8 | 195 |
4. ICAM-1 is expressed influences
By the HUVEC in exponential phase with 0.25% Trypsin Induced, gently blow and beat, be made cell suspension, adjust
Whole cell density is 5 × 109/L, is inoculated in Tissue Culture Flask.After cell is covered with (about 24h), abandoning supernatant is divided into
Following group：Control group, model group (100ug/ml MSU solution), ursolic acid group (100ug/ml MSU solution+25ug/ml
Ursolic acid), continue to cultivate 24 hours, PBS collects cell, and supernatant is removed in centrifugation, adds CD54 monoclonal antibodies, 30min
Afterwards, PBS washings, re-suspended cell, using its positive percentage (n=10000) of flow cytomery, repeats 3
It is secondary, the results are shown in Table 2.
The influence (X ± s) of the vascular endothelial cell ICAM-1 expression that the ursolic acid of table 2 stimulates MSU
| Group | Drug concentration | ICAM is expressed |
| Control group | 0 | 12±67 |
| Model group | 0 | 231±55 |
| Ursolic acid group | 25 | 155±37 |
Compare with model group, * * P<0.01*P<0.05, compare with control group, ##P<0.01#P<0.05 2, result result shows,
Blank group HUVEC is expressed almost without ICAM-1, the expression highest of model group ICAM-1, compared with model group, ursolic acid
There is stronger inhibitory action to the expression of ICAM-1.
Conclusion：The acute gout model evaluation that HUVEC is damaged is caused to show that ursolic acid can protect MSU to cause with MSU
HUVEC is damaged, and reduces Apoptosis, improves cytoactive, suppresses ICAM-1 expression, and with antigout activity, ursolic acid can
For preparing treatment acute gout anti-inflammatory drugs.
The above is the preferred embodiments of the present invention, it is noted that come for those skilled in the art
Say, on the premise of principle of the present invention is not departed from, some improvements and modifications can also be made, these improvements and modifications also should
It is considered as protection scope of the present invention.
Claims (3)
1. application of the ursolic acid in treatment gout medicine is prepared, the structural formula of described compound is：
。
2. the application according to claim 1, it is characterised in that described medicine includes or do not include other activity
Composition.
3. medicine according to claim 2, described medicine does not contain other active components, also containing can pharmaceutically connect
The auxiliary material received.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201611247667.7A CN106727602A (en) | 2016-12-29 | 2016-12-29 | Application of the ursolic acid in treatment gout medicine is prepared |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201611247667.7A CN106727602A (en) | 2016-12-29 | 2016-12-29 | Application of the ursolic acid in treatment gout medicine is prepared |
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| CN106727602A true CN106727602A (en) | 2017-05-31 |
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| CN201611247667.7A Pending CN106727602A (en) | 2016-12-29 | 2016-12-29 | Application of the ursolic acid in treatment gout medicine is prepared |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112587573A (en) * | 2021-01-15 | 2021-04-02 | 广西壮族自治区中医药研究院 | Application of Zhuang medicine-Wuye alcohol extract in preparation of anti-hyperuricemia medicine |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101049360A (en) * | 2007-05-10 | 2007-10-10 | 周兰兰 | Preparation of Chinese traditional medicine for treating gout disease, and application of extractive of Chinese feveruine |
-
2016
- 2016-12-29 CN CN201611247667.7A patent/CN106727602A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101049360A (en) * | 2007-05-10 | 2007-10-10 | 周兰兰 | Preparation of Chinese traditional medicine for treating gout disease, and application of extractive of Chinese feveruine |
Non-Patent Citations (2)
| Title |
|---|
| 于泓 等: "抗痛风胶囊对急性痛风性关节炎大鼠的抗炎作用及机制探讨", 《中国实验方剂学杂志》 * |
| 董帅 等: "熊果酸对2型糖尿病大鼠肾功能的影响", 《中国煤炭工业医学杂志》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112587573A (en) * | 2021-01-15 | 2021-04-02 | 广西壮族自治区中医药研究院 | Application of Zhuang medicine-Wuye alcohol extract in preparation of anti-hyperuricemia medicine |
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Application publication date: 20170531 |