CN104027392A - Application of Radix Scutellariae extract in pharmacy - Google Patents
Application of Radix Scutellariae extract in pharmacy Download PDFInfo
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- CN104027392A CN104027392A CN201310072178.2A CN201310072178A CN104027392A CN 104027392 A CN104027392 A CN 104027392A CN 201310072178 A CN201310072178 A CN 201310072178A CN 104027392 A CN104027392 A CN 104027392A
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Abstract
The invention relates to an application of a Radix Scutellariae extract (with the scutelloside content of 50-95%) in the pharmacy. The Radix Scutellariae extract (with the scutelloside content of 50-95%) is exploited to form medicines for treating pulmonary hypertension. A result of in vitro artery strip experiments shows that the Radix Scutellariae extract can substantially relax potassium chloride contracted pulmonary artery strips; the Radix Scutellariae extract can reduce the rat high pulmonary artery pressure caused by monocrotaline in a concentration-dependent manner; and the Radix Scutellariae extract also can inhibit the smooth muscle cell proliferation of pulmonary artery tunica media and promote the cell apoptosis. A new medical use of the known compound baicalin is excavated in the invention, and a new application field is developed. Researches find that the Radix Scutellariae extract has a very good pulmonary artery pressure reduction effect, can reduce the hypertrophy index of the right heart of the pulmonary artery high pressure rat and reverse the pulmonary artery tunica media reconstruction, and can rise the vein smooth muscle cell apoptosis associated protein Bax and decrease Bcl-2. The Radix Scutellariae extract has the advantages of nontoxic raw material, low price, low cost, safety and high efficiency.
Description
Technical field
The present invention relates to the new purposes that Radix Scutellariae extract contains the Radix Scutellariae extract of Radix Scutellariae glycosides 50-95%, be specifically related to the application of preparation treatment pulmonary hypertension, reverse pulmonary artery reconstruct medicine.
Background technology
Radix Scutellariae glycosides plant origin is the root of labiate Radix Scutellariae (Scutellaria baicalensis Georgi), molecular formula and molecular weight: C21H18011; 446.36; Pharmacological action: baicalin has antiinflammatory, antiallergic action, diuresis, function of gallbladder promoting, cholesterol reducing, antithrombotic formation, relieving asthma, eliminating fire and detoxication, hemostasis, the effect such as antiabortive.Also be the specific inhibitor of mammalian liver sialidase, there is the effect that regulates some disease.Industrial allergy, the panting property pneumonia of being used for taking it as the former phosphate ester of waste baicalin, also makes astringent, hemorrhage.
Pulmonary hypertension (pulmonary arterial hypertension, PAH) mainly increases with pulmonary vascular resistance extremely as the disease of feature extremely taking pulmonary artery pressure.Wherein, the proliferative disorder of pulmonary artery abnormality of diastolic function and lung vascular wall has been brought into play important effect in PAH develops.Baicalin (Baicalin) is as the main component in Chinese medicine Radix Scutellariae; important therapeutical effect in performance in a lot of clinical diseases; application in cardiovascular disease more and more obtains numerous scholars' attention, but has no relevant report at preparation treatment pulmonary hypertension, chronic obstructive pneumonia and myocardial ischemia, ischemia protection medicine.The present invention, according to the basic pharmacological properties of Radix Scutellariae extract (containing baicalin 50%-95%), studies the application of its treatment pulmonary hypertension.
Summary of the invention
The object of the invention is Radix Scutellariae extract to be prepared as the medicine for the treatment of pulmonary hypertension.
In order to achieve the above object, technical scheme of the present invention be to provide Radix Scutellariae extract at preparation treatment pulmonary hypertension, reverse the application of pulmonary artery reconstruct medicine.Described Radix Scutellariae extract is containing baicalin 50%-95% (percentage by weight).
Below by experiment and experimental result, the new purposes of Radix Scutellariae extract at pharmaceutical field is described.
The impact of the P of Rats AH of Radix Scutellariae extract on MCT induction.
Observation index and method:
1. rat pulmonary artery bar expansion experiment:
Separate rat pulmonary artery trunk, in the K-H of 4 DEG C of saturated oxygens liquid, make the wide vascular ring of 4 ± 0.2mm.Gently hang blood vessel 4-5 time with blunt nosed tweezer, to remove endothelium.Vascular ring is hung in the middle of the bath containing K-H liquid (pH=7.4), temperature keeps 37 DEG C, continues to pass to 95%O2+5%CO2 mist.Give the rest tension of 2g, balance 2h; Within every 15 minutes, change K-H liquid once.Repeatedly shrink 20 minutes with 30mmolL-1KCL, reach plateau value to shrinking; Accumulation adds Radix Scutellariae extract 5,10,15mgL-1; The NaCl that matched group accumulation adds same concentrations, records diastolic rate, diastolic rate=(shrinking maximum tension-diastole minimum tension)/(shrinking maximum tension-rest tension).
2. pulmonary arterial pressure in rats mensuration, the loose index in right ventricle, pulmonary artery morphologic detection:
90 of rats, are divided into blank group at random, model group, 50%, 60%, 80% Radix Scutellariae extract treatment group (establish respectively basic, normal, high three groups, n=8).MCT subcutaneous injection induction Pulmonary Hypertension, each Radix Scutellariae extract treatment group in respectively with 20,40,80mg/kg/d gavage; Blank group injection equivalent normal saline.After 30 days, after 10% chloral hydrate (4mlkg-1) intraperitoneal anesthesia, tracheotomy connects miniature respirator.Through external jugular vein, the self-control microguide (head end is smooth) of heparinization is inserted to pulmonary artery, is connected to polygraph by pressure transducer and records pressure waveform and pulmonary artery pressure.Air tap inserting method is put to death animal, takes out cardiopulmonary tissue.Remove the left atrium of vein, separate right ventricle, residue is that left ventricle adds interventricular septum, after PPS rinses well, filter paper blots, and weighs, and right ventricle/(left ventricle+interventricular septum) is hypertrophy of right heart index (RV/ (LV+S)).Isolated lung tissue, draw materials along the horizontal crosscut of hilus pulumonis, 10% neutral formalin is fixed 48h, HE dyeing, choose the lung flesh small artery of external diameter at 100～200 μ m, use leica Qwin analysis software to measure lung small artery media thickness, calculate media thickness and account for the percentage ratio (WT%) of blood vessel external diameter and Pulmonary vascular cell area and account for the ratio (WA%) of the blood vessel gross area.
Result: the experiment of Arterial Rings In Vitro bar shows as shown in Figure 1, the Radix Scutellariae extract pulmonary artery bar that significantly diastole potassium chloride shrinks; The high pulmonary artery pressure of rat due to the reduction monocrotaline that Radix Scutellariae extract can concentration relies on as shown in Figure 2; As shown in table 1,2, Radix Scutellariae extract can suppress film smooth muscle cell proliferation in pulmonary artery, promote its apoptosis.
The impact of the Rats of Pulmonary Hypertension right heart index of table 1. variable concentrations baicalin extract on monocrotaline induction, tunica media Thickness Ratio, lumen of vessels Area Ratio (%,
)
The blank group of #p < 0.01vs; * p < 0.01vs model group
The impact that table 2. variable concentrations baicalin extract is transferred to associated protein BAX, BCL-2 to the Rats of Pulmonary Hypertension of monocrotaline induction
The blank group of #p < 0.01vs; * p < 0.01vs model group
The invention has the beneficial effects as follows: the present invention has excavated a kind of new medical application to known compound Radix Scutellariae glycosides, opened up a new application.Research has found that baicalin extract has the effect of good reduction pulmonary artery pressure, can reduce Rats of Pulmonary Hypertension hypertrophy of right heart index, reverse film reconstruct in pulmonary artery, baicalin extract can raise arterial smooth muscle cell apoptosis-related protein Bax, lowers Bcl-2.Can be used for preventing and treating the natural medicine of pulmonary hypertension.The advantages of nontoxic raw materials that this product is used, low price, with low cost, safe and efficient, market prospect is wide, and expection economic benefit and social benefit are considerable.
Brief description of the drawings
Fig. 1 is that the baicalin extract of variable concentrations is to the diastole effect of the pre-shrunk vascular strip of potassium chloride.
Fig. 2 is the average Pulmonic impact of Rats of Pulmonary Hypertension that the baicalin extract of variable concentrations is induced monocrotaline.
Detailed description of the invention
Below in conjunction with accompanying drawing, the present invention is elaborated.
In the present invention, the extraction of baicalin used is prepared according to purgation:
Baicalin extracts: take ethanol reflux extraction, get baicalin decoction pieces 100g, pulverized 10 mesh sieves, extract at twice with 10 times, 8 times amounts with 60% ethanol, each 1 hour, filter, filtrate decompression reclaims ethanol to the greatest extent and becomes extractum, and calculating paste-forming rate is 39-40g/100g crude drug.
The extractum content obtaining by other extraction methods is at 18-41g/100g crude drug
Embodiment 1
Baicalin tablet: get baicalin extract extractum 5g, make solid dispersion with polyethylene glycol 6000 with the ratio of 1: 6, add polyvinylpolypyrrolidone, sodium carboxymethyl cellulose, carboxymethyl starch sodium, pregelatinized Starch, magnesium stearate, micropowder silica gel, mix homogeneously tabletting, to obtain final product.
Embodiment 2
Baicalin capsules agent: conventional dropping preparation method is made soft capsule.Get baicalin extract extractum, dry, pulverize, granulation, incapsulates, and remembers.
Embodiment 3
Baicalin pill: get baicalin extract extractum, dry, pulverize, with water pill, cold drying, sugar coating, film-coat or bag charcoal clothing, to obtain final product.
More than show and described ultimate principle of the present invention and principal character and advantage of the present invention.The technical staff of the industry should understand; the present invention is not restricted to the described embodiments; that in above-described embodiment and description, describes just illustrates principle of the present invention; without departing from the spirit and scope of the present invention; the present invention also has various changes and modifications, and these changes and improvements all fall in the claimed scope of the invention.The claimed scope of the present invention is defined by appending claims and equivalent thereof.
Claims (3)
1. the application of Radix Scutellariae extract in the medicine of preparation treatment pulmonary hypertension.
2. Radix Scutellariae extract reverses the application in pulmonary artery reconstruct medicine in preparation.
3. Radix Scutellariae extract according to claim 1 and 2, is characterized in that, containing baicalin 50%-95% (percentage by weight).
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310072178.2A CN104027392A (en) | 2013-03-07 | 2013-03-07 | Application of Radix Scutellariae extract in pharmacy |
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| Application Number | Priority Date | Filing Date | Title |
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| CN201310072178.2A CN104027392A (en) | 2013-03-07 | 2013-03-07 | Application of Radix Scutellariae extract in pharmacy |
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| CN104027392A true CN104027392A (en) | 2014-09-10 |
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20030166583A1 (en) * | 2002-02-22 | 2003-09-04 | Oliver Yoa-Pu Hu | Dermal cytochrome P450 1A inhibitors and enhancers |
| CN101953980A (en) * | 2010-10-14 | 2011-01-26 | 江苏省中医院 | Allium macrostemon and pepperweed seed mixture for treating chronic obstructive pulmonary disease (COPD) by adopting phlegm removing and turbidity resolving method |
-
2013
- 2013-03-07 CN CN201310072178.2A patent/CN104027392A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20030166583A1 (en) * | 2002-02-22 | 2003-09-04 | Oliver Yoa-Pu Hu | Dermal cytochrome P450 1A inhibitors and enhancers |
| CN101953980A (en) * | 2010-10-14 | 2011-01-26 | 江苏省中医院 | Allium macrostemon and pepperweed seed mixture for treating chronic obstructive pulmonary disease (COPD) by adopting phlegm removing and turbidity resolving method |
Non-Patent Citations (4)
| Title |
|---|
| 卢园园等: "黄芩苷抑制低氧性肺动脉平滑肌细胞增殖的机制", 《实用医学杂志》 * |
| 周晓红等: "黄芩甙抗内毒素休克的实验研究", 《河北中医药学报》 * |
| 杜海燕等: "HPLC法测定黄芩提取物中黄芩苷的含量", 《中草药》 * |
| 王伟等: "5种中药黄酮对血管平滑肌细胞凋亡的交互作用", 《北京中医药大学学报》 * |
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Application publication date: 20140910 |
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