CN102335187A - Application of baicalin in preparing medicament for preventing and treating chronic obstructive pulmonary disease - Google Patents
Application of baicalin in preparing medicament for preventing and treating chronic obstructive pulmonary disease Download PDFInfo
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- CN102335187A CN102335187A CN2010102391302A CN201010239130A CN102335187A CN 102335187 A CN102335187 A CN 102335187A CN 2010102391302 A CN2010102391302 A CN 2010102391302A CN 201010239130 A CN201010239130 A CN 201010239130A CN 102335187 A CN102335187 A CN 102335187A
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Abstract
The invention belongs to the field of biomedicine, relates to a novel medical application of an effective component baicalin in a Chinese medicament and in particular relates to an application of baicalin in preparing a medicament for preventing and treating a chronic obstructive pulmonary disease. In the application, Chinese medicinal monomer baicalin is adopted to carry out an animal model experiment, and experimental results prove that the baicalin can protect the lung function of an experiment model of the chronic obstructive pulmonary disease caused by cigarette smoking exposure; and the baicalin can inhibit infiltration of inflammation cells and expression of proinflammatory cytokine of the experimental model in a body, and the effects of the baicalin are related to activation of inhibiting NF (nuclear factor)-kappa B. The baicalin provided by the invention can be used as a medicinal active component and a pharmaceutically acceptable carrier to prepare a medicinal composition for preventing and treating the chronic obstructive pulmonary disease.
Description
Technical field
The invention belongs to biomedical sector, the new pharmaceutical usage of pharmaceutically active ingredient baicalin in relating to is specifically related to the application of baicalin in preparation control chronic obstructive pulmonary disease medicine.
Background technology
Chronic obstructive pulmonary disease (COPD) be a kind of flow limitation not exclusively reversible, be carry out sexual development, with pneumonia reaction diseases associated.COPD mainly involves lungs, but also can the cause whole body ill effect of (or claim lung outer).Clinically mainly show as chronic cough, expectoration, breathe hard or dyspnea, pant and uncomfortable in chest,, have a strong impact on patient's work capacity and quality of life along with the progress of disease also systemic inflammatory reaction etc. can take place.It is reported that at present, the COPD number of patients is many, mortality rate is high, and social economy's burden is heavy, has become a global important public health problem.Research shows that smoking is the topmost risk factor of COPD, and whole world smoking population is about 1,300,000,000, and China has more than 300,000,000 approximately.China is one of COPD major country occurred frequently.According to the prediction of recent research report, China estimates to have nearly 6,500 ten thousand people to die from COPD in from now on 20 years.The intervention and the Mechanism Study of therefore, carrying out the COPD inflammation have important theory directive significance and practical value.
Chinese crude drug Radix Scutellariae bitter in the mouth, cold in nature, return lung, liver, gallbladder, large intestine, small intestine meridian.Has antipyretic and antidote functions.Baicalin baicalin) is the flavone compound that is extracted from the dry root of labiate Radix Scutellariae Scutellaria baicalensis Georgi; It is the main effects monomer of Radix Scutellariae; Up to now, do not see the correlational study report that has baicalin to be applied to prevent and treat chronic obstructive pulmonary disease both at home and abroad as yet.
Summary of the invention
The new pharmaceutical usage of pharmaceutically active ingredient baicalin in the purpose of this invention is to provide is specifically related to the application of baicalin in preparation control chronic obstructive pulmonary disease medicine.
Chinese medicine monomer baicalin of the present invention has the structure of formula (I), and its water solublity is minimum, has certain fat-solublely, under alkali condition, is easy to dissolving.
The present invention combines correlational study basis in the past; Adopt above-mentioned Chinese medicine monomer baicalin to carry out zoopery; COPD rat model due to the employing smoke from cigarette exposes; And intervene animal with Radix Scutellariae, experimental result shows, 1, baicalin smoke from cigarette is exposed due to the pulmonary function of COPD rat protective effect is arranged; 2, the infiltration of the inflammatory cell of COPD rat model, the expression of proinflammatory cytokine had inhibitory action due to baicalin exposed smoke from cigarette in vivo; 3, the above-mentioned effect of baicalin is relevant with the activation that suppresses NF-κ B.
Baicalin of the present invention can be used as active constituents of medicine, and acceptable carrier prepares the pharmaceutical composition of preventing and treating chronic obstructive pulmonary disease on the materia medica.
For the ease of understanding, below will describe in detail the new pharmaceutical usage of middle pharmaceutically active ingredient baicalin of the present invention with embodiment through concrete accompanying drawing.What need particularly point out is; Instantiation and accompanying drawing only are in order to explain; Obviously those of ordinary skill in the art can explain according to this paper, within the scope of the invention the present invention is made various corrections and change, and these corrections and change are also included in the scope of the present invention.
Description of drawings
Fig. 1. lung function result,
Wherein, (A) normal group, (B) COPD model group, (C) Dexamethasone group, (D) baicalin low dose group, (E) dose groups in the baicalin, (F) baicalin high dose group;
Statistical data is represented with means ± SEM, n=6; * be P＜0.05 of comparing with the A group; # is P＜0.05 of comparing with the B group.
Fig. 2. the microphotograph of lung tissue pathology (HE dyeing),
Wherein, (A) lung tissue of normal group, (B) lung tissue of COPD model group, (C) lung tissue of Dexamethasone group, (D) lung tissue of baicalin low dose group, (E) lung tissue of dose groups in the baicalin, (F) lung tissue of baicalin high dose group.
Fig. 3. cytokine concentrations,
Wherein, the result representes with means ± SEM;
(a) cytokine concentrations in the serum (n=6), * be with compared with normal than P＜0.05, # is for comparing P＜0.05 with the COPD model group;
(b) cytokine concentrations among the BALF (n=6), * be with compared with normal than P＜0.05, # is for comparing P＜0.05 with the COPD model group.
Fig. 4. NF-κ B p65 SABC microphotograph in the lung tissue,
The lung tissue of (A) normal group wherein, (B) lung tissue of COPD model group, (C) lung tissue of Dexamethasone group, the D) lung tissue of baicalin low dose group, (E) lung tissue of dose groups in the baicalin, (F) lung tissue of baicalin high dose group.
The specific embodiment
Embodiment 1
1. laboratory animal
36 healthy cleaning level male Sprague-Dauley (SD) rats (Chengdu reaches large bio tech ltd laboratory animal technology company to be provided), the monthly age is 21 ± January, body weight is at 500～600g.
2. divide into groups and modeling
The SD rat is divided into 6 groups at random: A group, B group, C group, D group, E group, F group, 6 every group.
The A group: normal group: rat is placed in the smoking apparatus, exposes with fresh air to replace smoke from cigarette to expose.Began to adopt sterile saline 1ml to irritate stomach on the 8th day from modeling, once a day, 5 days weekly, continuous 3 weeks.
B group: COPD model group: the method that reference literature provides, rat is placed fumigation in the airtight wooden case, medicated cigarette is filter-tipped peony brand fire-cured tobacco type medicated cigarette (Shanghai tobacco company provides), every medicated cigarette contains 1.0mg nicotine and 13mg tar; Each 20, each 1 hour, one day 2 times; 5 days weekly, in totally 5 weeks, began to adopt sterile saline 1ml to irritate stomach on the 8th day from modeling; Once a day, 5 days weekly, continuous 3 weeks.
C group: Dexamethasone group: rat is placed in fumigation in the smoking apparatus of describing like the B group.(Shanghai General Pharmaceutical Co., ltd. provides to give dexamethasone on the 8th day behind the fumigation; Lot number: 060110; 0.2mg/kg) irritate stomach, once a day, each 1 milliliter, 5 days weekly, continuous 3 weeks.
D group: baicalin low dose group (20mg/kg): rat is placed the smoking apparatus fumigation.Reinstate the 20mg/kg baicalin on the 8th day behind the fumigation and irritate stomach, once a day, each 1 milliliter, 5 days weekly, continuous 3 weeks.
E group: dose groups in the baicalin (40mg/kg): reinstated the 40mg/kg baicalin on the 8th day behind the fumigation and irritate stomach, all the other methods are organized with D.
F group: baicalin high dose group (80mg/kg): reinstated the 80mg/kg baicalin on the 8th day behind the fumigation and irritate stomach, all the other methods are organized with D.
3. index detects and the result
3.1 detect the pulmonary function of rat
The result shows that COPD model group pulmonary function is lower than normal group (P＜0.05) significantly, and normal group is compared no significant difference (P＞0.05) with the baicalin high dose group, and the baicalin that shows high dose can be protected the pulmonary function (as shown in Figure 1) of rat; The result also shows, COPD model group and the Dexamethasone group difference not statistically significant of comparing.
3.2. the lung tissue pathology morphological change of rat
The result is presented at that the baicalin high dose group approaches normal group most in 6 groups; In the lung tissue of dose groups a large amount of inflammatory cell infiltrations is arranged all in COPD model group, Dexamethasone group, baicalin low dose group, the baicalin; Comprise pulmonary alveolar macrophage, neutrophilic granulocyte and lymphocyte, the inflammation of COPD model group and Dexamethasone group performance the most serious (as shown in Figure 2) in four groups.
3.3 the ELISA result of cytokine
IL-8, IL-6 and TNF-α result that the ELISA method detects among serum (shown in Fig. 3 a) and the BALF (shown in Fig. 3 b) show: the proinflammatory factor ratio that the COPD among COPD model group serum and the BALF is crucial; Normal group increases (P＜0.05) significantly, and middle and high dose groups of baicalin and compared with normal difference not statistically significant (P＞0.05).
3.4 NF-κ B p65 SABC result (Fig. 4) in the lung tissue
Cell immunohistochemical staining method detects NF-κ B p65 and shows (shown in Fig. 4 A-F) in the result of the expression in the lung tissue; Nucleus is colored and is the positive cell that brown xanchromatic cell is NF-κ Bp65 expression; In normal group, baicalin in dose groups and the baicalin high dose group; The NF-κ B p65 of the few part in the cytoplasm is just dyeed, seldom just dyeed in the nucleus, yet; In COPD model group and Dexamethasone group, the nearly all bronchial epithelial cell and the nucleus of alveolar epithelial cells are all just dyeed by NF-κ B p65.
Experimental result shows that the pulmonary function of COPD rat had protective effect due to baicalin exposed smoke from cigarette; The infiltration of the inflammatory cell of COPD rat model, the expression of proinflammatory cytokine have inhibitory action due in vivo smoke from cigarette being exposed; The above-mentioned effect of baicalin is relevant with the activation that suppresses NF-κ B.
Claims (6)
1. the baicalin of formula (I) structure is prevented and treated the purposes in the chronic obstructive pulmonary disease medicine in preparation,
2. by the described purposes of claim 1, it is characterized in that the pulmonary function of the chronic obstructive pulmonary disease experimental model due to described baicalin protection smoke from cigarette exposes.
3. by the described purposes of claim 1, it is characterized in that the infiltration of the inflammatory cell of the chronic obstructive pulmonary disease experimental model due to described baicalin inhibition smoke from cigarette exposes or the expression of proinflammatory cytokine.
4. by claim 2 or 3 described purposes, it is characterized in that described baicalin suppresses the activation of NF-κ B.
5. by claim 2 or 3 described purposes, it is characterized in that described chronic obstructive pulmonary disease experimental model is due to smoke from cigarette exposes.
6. pharmaceutical composition of preventing and treating chronic obstructive pulmonary disease is characterized in that: comprise baicalin as active component, and acceptable carrier on the materia medica.
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113082015A (en) * | 2020-01-08 | 2021-07-09 | 深圳市罗湖区人民医院 | Application of genistein in preventing chronic obstructive pulmonary disease and verification method |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1907292A (en) * | 2006-08-14 | 2007-02-07 | 曾列丹 | Emulsion of baicalin for injection and its preparation process |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1907292A (en) * | 2006-08-14 | 2007-02-07 | 曾列丹 | Emulsion of baicalin for injection and its preparation process |
Non-Patent Citations (1)
| Title |
|---|
| 晁晖等: "黄芩苷对慢性阻塞性肺疾病大鼠模型防治作用的研究", 《国际呼吸杂志》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113082015A (en) * | 2020-01-08 | 2021-07-09 | 深圳市罗湖区人民医院 | Application of genistein in preventing chronic obstructive pulmonary disease and verification method |
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Application publication date: 20120201 |