CN101301403B - Clerodendrum bungei extract and use thereof for treating airway hyperreactivity - Google Patents
Clerodendrum bungei extract and use thereof for treating airway hyperreactivity Download PDFInfo
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- CN101301403B CN101301403B CN2008100316988A CN200810031698A CN101301403B CN 101301403 B CN101301403 B CN 101301403B CN 2008100316988 A CN2008100316988 A CN 2008100316988A CN 200810031698 A CN200810031698 A CN 200810031698A CN 101301403 B CN101301403 B CN 101301403B
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Abstract
The invention provides a clerodendron bungei extractive which is used for curing the airway hyperresponsiveness disease. A triterpenes extractive which is about 0.7 percent by weight percentage of the clerodendron bungei raw pesticide is obtained by a complete stool of the clerodendron bungei; the research shows that the triterpenes compound in the clerodendron bungei can relieve the pathological changes in airway and alveolus, reduce the inflammation reaction and the airway hyperresponse, has the effect similar to the glucocorticoid, has the evident functions of reducing the airway hyperresponsiveness and relieving the airway and lung injury caused by the ozone stress, and can cure the effective part of the airway hyperresponsiveness disease; moreover, the experiment shows that the clerodendron bungei total extractive does not have the toxicity to the peripheral leukocytes, the liver and kidney and has good safety.
Description
Technical field
The present invention relates to a kind of medical usage of natural plant extracts, particularly Caulis et folium clerodendri bungei extract and be used for the treatment of the purposes of airway hyperreactivity disease.
Background technology
Airway hyper-reaction is a kind of common clinical manifestation, is mainly seen in acute and chronic respiratory tract diseases such as bronchial asthma, chronic obstructive pulmonary disease, viral upper respiratory tract infection.Pathogenesis that now it is generally acknowledged airway hyper-reaction is an airway inflammation, so class of medications mainly is to prevent and treat from antiinflammatory and symptomatic treatment both direction.The medicine of treatment airway hyper-reaction commonly used has anti-inflammatory drug and bronchodilator two classes at present, more sure in the anti-inflammatory drug have two classes: corticosteroid and sodium cromoglicate Buddhist nun polyacid sodium, and wherein the corticosteroid of imbedibility has become a line medicine of treatment asthma; Commonly used in the bronchodilator have aminophylline, a diprophylline.Though airway hyper-reaction can be treated or alleviate to these medicines, can not solve the state of an illness and show effect repeatedly and block air passage structure and reinvent and problems such as pulmonary function decline process.Simultaneously, these medicines have in various degree side effect to human body, and the patient increases year by year to the toleration of these medicines.Therefore, from natural plants, isolate and have the antagonism airway inflammation and reduce airway hyper-reaction, and the little ingredient of toxic and side effects, will help the clinical treatment of such disease, have bigger social benefit.
Caulis et folium clerodendri bungei, formal name used at school: Clerodendrum bungei Steud, English name: Rose Glorybower, section's name: Verenaceae Verbenaceae undershrub, be distributed widely in North China, south China, northwest and southwestern each province, be born in by hillside, border or the ditch.It is extensive use of and accumulates its abundant medicinal experience already as medicinal plants by various nationalities, be used for the treatment of carbuncle in traditional medicine, furuncle, mastitis, arthritis, eczema, headache, diseases such as toothache.But at present considerably less, and all do not relate to airway inflammation or airway hyper-reaction disease about the research of its active component.
Summary of the invention
The objective of the invention is to from Caulis et folium clerodendri bungei, extract triterpene extracts, and research obtains, and this extract can be used for the treatment of airway inflammation or the airway hyper-reaction disease has significant curative effect.
Another object of the present invention is to prepare the various pharmacy that contain the Caulis et folium clerodendri bungei triterpene extracts and can accept the various pharmaceutical preparatioies of form.
The present invention extracts triterpene extracts by following method from Caulis et folium clerodendri bungei: add 50wt% ethanol after the Caulis et folium clerodendri bungei Herb is shredded, place 82 ℃ of water-bath internal heating to reflux, extract backflow, concentrate evaporate to dryness, add distilled water and stir into suspension, use petroleum ether extraction then, reuse chloroform extraction behind the isolated for disposal extract, reclaim chloroform extraction liquid, concentrate evaporate to dryness, obtain accounting for the triterpene extracts of former medicine 0.7% left and right sides weight ratio of Caulis et folium clerodendri bungei.
The inventor further studies confirm that, triterpenoid compound can alleviate ozone attack institute's air flue that causes and alveolar pathological change, inflammatory reaction and airway hyper-reaction in the Caulis et folium clerodendri bungei, its effect is near glucocorticoid, have and very significantly reduce airway hyper-reaction and alleviate air flue that ozone stress cause and the function of injury of lung, be the effective site of treatment airway hyperreactivity disease, and do not observe the Caulis et folium clerodendri bungei total extract to peripheral blood leucocyte and Liver and kidney toxicity, safety is good.
Press practice of pharmacy, triterpenoid compound in the Caulis et folium clerodendri bungei extract of the present invention is prepared into the medicament as treatment airway hyperreactivity disease of acceptable multiple pharmaceutical dosage form on the clinical pharmacy, said medicament comprises said dosage form on present any pharmaceutics, comprises any in aerosol in the oral formulations, oral liquid, tablet, granule, pellet, the capsule.
Description of drawings
Fig. 1: Caulis et folium clerodendri bungei triterpene extracts airway of mice responsiveness curve figure (n=8);
P＜0.05vs normal control group #P＜0.05vs model group
Fig. 2: the active bar diagram of Caulis et folium clerodendri bungei triterpene extracts mice lactic acid dehydrogenase (LDH) (n=8);
P＜0.05vs normal control group #P＜0.05vs model group
Fig. 3: each experimental mice lungs pathological section figure (HE * 100);
Fig. 4: each experimental mice lungs pathological section figure (HE * 400);
Fig. 5: each experimental mice hepatopathy reason slice map (HE * 400).
The specific embodiment
Embodiment 1: the separation preparation of Caulis et folium clerodendri bungei triterpene extracts
Wild Caulis et folium clerodendri bungei Herb is cleaned, dries, and takes by weighing 100 grams, shreds the back and adds in the 2L round-bottomed flask, adds 50% ethanol 1L; Round-bottomed flask is placed 82 ℃ of water-bath internal heating reflux, extract, 4 hours, reclaim backflow.And then add 1L50% ethanol, repeat aforesaid operations once.Merge extractive liquid, is poured into and is concentrated evaporate to dryness in the beaker then; Add distilled water 200ml again, stir into suspension; Use 200ml petroleum ether extraction secondary then, reuse chloroform 200ml divides reextraction behind the isolated for disposal extract, reclaims chloroform extraction liquid.From chloroform extraction liquid, get 0.1ml and do the prerun inspection of its composition, remaining concentrated evaporate to dryness, concentrate is weighed, and is about 0.7 gram.
Then concentrate is made emulsifying agent, method is as follows: concentrate is placed beaker, add vegetable oil 1.5 grams, place 75 ℃ of water-baths, it is stand-by that continuous stirring is fully melted it.Other gets a clean beaker, adds arabic gum 0.375 gram, adds distilled water 5ml, places 95 ℃ of water-baths, stirs 20 minutes, be cooled to then 70 ℃ stand-by.Then oil phase and water are mixed, be ground to no bulky grain state, and then adding distilled water, to transfer to cumulative volume be 25ml, and then use ultrasonic grinding 5min with mortar.Place the cold preservation of sealed glass bottle stand-by then.
The prerun inspection of ingredient: utilize silica gel thin-layer plate to carry out the chemical constituent prerun inspection of extract.With capillary pipette inhale a small amount of said extracted thing respectively point sample on first block of lamellae, spray vanillin-concentrated sulphuric acid then in three silica gel thin-layer plates; On second block of lamellae, spray 1% ferric chloride; On the 3rd block of lamellae, spray bismuth potassium iodide, observe change color.The qualification result of extract sees Table 1:
Table 1: extract is made the result that the prerun of thin layer silica gel is checked
Thin layer silica gel prerun inspection is the method for composition in a kind of qualitative reaction natural drug, and its cardinal principle is to identify the existence of a certain classification of medicine by the change color that some chemical reactions cause.Triterpene substance is under the effect at vanillin-concentrated sulphuric acid behind the chloroform extraction, generate orange to blue material, its shade is directly proportional with triterpene content, aldehydes matter can become indigo plant, dark green or bluish violet with 1% ferric chloride reaction, and alkaloid can present salmon pink or yellow with the bismuth potassium iodide reaction.Extract obtained the reacting with vanillin-concentrated sulphuric acid only of this experiment becomes navy blue, illustrates and contains a large amount of triterpene substances, no phenols and alkaloid.
Embodiment 2: the Caulis et folium clerodendri bungei triterpene extracts is to the effect of the high reaction model of airway of mice
1. animal grouping and processing: 50 of kunming mices are divided into 5 groups at random.Administering mode is for irritating stomach, and irritating the stomach amount is the 1ml/100g body weight.
1. normal control group: irritate stomach once with normal saline every day, continuous 7 days;
2. Caulis et folium clerodendri bungei triterpenes matched group group: irritate stomach once, continuous 7 days with Caulis et folium clerodendri bungei triterpene extracts emulsifying agent every day;
3. airway hyper-reaction model group: irritate stomach with normal saline every night, continuous 7 days, irritates stomach beginning in the 3rd day and attacked 20 minutes continuous 5 days with ozone every afternoon;
4. steroid group (positive control): irritate stomach with the glucocorticoid of 0.5mg/ml every night, continuous 7 days, irritates stomach beginning in the 3rd day and attacked 20 minutes continuous 5 days with ozone every afternoon;
5. Caulis et folium clerodendri bungei triterpenes treatment group: irritate stomach once with Caulis et folium clerodendri bungei triterpene extracts emulsifying agent every night, continuous 7 days, irritates stomach beginning in the 3rd day and attacked 20 minutes continuous 5 days with ozone every afternoon.
2. observation index
1. airway resistance (Buxco toy lung function system)
Chloral hydrate anesthesia mice (dosage is 0.3ml/100g) is cut the mice trachea then, connects Buxco toy lung function system after the intubate, measures the airway resistance of mice under base state; Use 0.39mg/ml then successively, 0.78mg/ml, 1.56mg/ml and the methacholine (Mch) of 3.12mg/ml excites, measure the airway resistance of mice under these four kinds of different excited states, be airway resistance ratio divided by the airway resistance value gained relative value of this mice under base state respectively.
Exciting concentration with methacholine is abscissa, and airway resistance ratio is vertical coordinate, draws the airway of mice responsiveness curve.The rising amplitude of curve is big more, and the expression mice is obvious more to the reaction of Mch, and airway reactivity is high more.
The result is shown in accompanying drawing 1 (n=8), and model group presents tangible airway hyper-reaction, and the Caulis et folium clerodendri bungei triterpene extracts has the effect of the airway hyper-reaction that the reduction ozone with hormone analog stress be caused.Caulis et folium clerodendri bungei triterpene extracts effect separately influences the reactive nothing of airway of mice.
2. numeration of leukocyte and the classification in the broncho-pulmonary irrigating solution (BALF)
Open breast knot and prick a side lung and cut the back with 4% paraformaldehyde preservation, the opposite side lung is preserved irrigating solution after with the lavation of PBS liquid.The lavation method is to insert in the airway of mice with plastic tube earlier, tightens with stitching thread, extracts the PBS of 0.5ml then with the 1ml syringe, slowly injects in the mice one laterobronchus lung, and slowly pumpback then three times repeatedly, is reclaimed irrigating solution.
With the rotating speed centrifugal limb trachea lung-douching fluid of 1500r/min, centrifugal 5min gets supernatant and measures lactic acid dehydrogenase (LDH) content, and measuring method is with reference to lactic dehydrogenase enzyme reagent kit (bio-engineering research institute is built up in Nanjing) description; Precipitate adds the numeration of leukocyte liquid mixing of 500 μ l, counts quantity of leucocyte with counting chamber; And then centrifugal (1500r/min * 5min), taking precipitate is made the cell smear, Rui-Ji dyeing liquor dyeing, differential counting.Each experimental group numeration of leukocyte is referring to accompanying drawing 3.
Table 1: each organizes the leukocyte count of BALF in the mice and differential counting thereof (* 106/L x ± s)
N=8, P＜0.05vs normal control group #P＜0.05vs model group
Results suggest: model group ozone is attacked and can be caused in the bronchoalveolar lavage fluid total white blood cells and lymphocyte, granulocyte quantity increases, the Caulis et folium clerodendri bungei triterpene extracts is effect and normal control group zero difference separately, but can reduce following total white blood cells of ozone attack and lymphocyte, granulocyte quantity, present the effect that suppresses airway inflammation, its effect and steroid group are close.
3. lactic acid dehydrogenase (LDH) determination of activity in the broncho-pulmonary irrigating solution (BALF)
Lactic acid dehydrogenase is an important enzyme in the energy i (in vivo) metabolic process.This enzyme almost be present in the institute in a organized way in.When a small amount of tissue necrosis, this enzyme promptly discharges blood and the vigor of mensuration is raise.
Show from accompanying drawing 2: model group ozone is attacked and can be caused that the LDH activity increases the bronchoalveolar lavage fluid, and the reflection cytoclasis increases, and triterpene extracts can reduce the LDH activity, points out its cytoprotection indirectly.
4. the lungs of each group experiment mice are done pathology section and dyeing, observe the lesion degree of air flue and lung tissue, each is organized pathological section and sees accompanying drawing 3 (HE * 100) and accompanying drawing 4 (HE * 400).Wherein Fig. 3-A is the normal control group, and section shows the airway epithelia structural integrity, and alveolar structure is normal, and NIP changes; Fig. 3-B is a Caulis et folium clerodendri bungei triterpene extracts matched group, and section shows the airway epithelia structural integrity, and alveolar structure is normal, and airway walls has light inflammation to change; Fig. 3-C is the airway hyper-reaction model group, and section shows that airway epithelia comes off, and mucous secretion is arranged in the air flue, and alveolar structure is consolidation, has a large amount of inflammatory cells to ooze out; Fig. 3-D is a Caulis et folium clerodendri bungei triterpene extracts treatment group, and section shows the airway epithelia structural integrity, and most of alveolar structure is normal, and fraction has hyperemia, and airway walls has light inflammation to change; Fig. 3-E is a steroid group, and section shows the airway epithelia structural integrity, and most of alveolar structure is normal, and fraction is in edema, and airway walls has light inflammation to change.Accompanying drawing 4 is visual down for high power lens, and Fig. 4-A is the normal control group, and section shows the airway epithelia structural integrity, and alveolar structure is normal, and NIP changes; Fig. 4-B is the airway hyper-reaction model group, and section shows that airway epithelia comes off, and airway walls has big amount lymphocyte to ooze out, intra-alveolar edema, hyperemia; Fig. 4-C is an extract triterpenes treatment group, and section shows the airway epithelia structural integrity, and alveolar structure is normal, and NIP changes; By accompanying drawing 3 and accompanying drawing 4 as can be seen: the Caulis et folium clerodendri bungei triterpene extracts can alleviate ozone and attack institute's air flue that causes and alveolar pathological change, and reaction reduces inflammation.
5. the numeration of leukocyte in the peripheral blood
Leukocyte in each group mice peripheral blood is counted, and the result shows: Caulis et folium clerodendri bungei extract does not have obvious the change to the peripheral blood leucocyte sum, does not find the general toxic and side effects that extracting solution has leukocyte to suppress.
6. the pathological section of liver, nephridial tissue
Liver, the nephridial tissue of each experimental mice are done the pathology section.Hepatopathy reason section microgram sees that accompanying drawing 5: Fig. 5-A is the airway hyper-reaction model group, and the section display structure is normal, and NIP changes; Fig. 5-B is a Caulis et folium clerodendri bungei total extract treatment group, and the section display structure is normal, and NIP changes; Fig. 5-C is a steroid group, and the section display structure is normal, and NIP changes; Liver, the section of nephropathy reason do not find that all the Caulis et folium clerodendri bungei extracting solution has tangible toxic action to liver, nephridial tissue.
Embodiment 3: contain the preparation of the pharmaceutical preparation of Caulis et folium clerodendri bungei triterpene extracts
Get the Caulis et folium clerodendri bungei triterpene extracts among the embodiment 1, prepare various pharmaceutically acceptable various forms of pharmaceutical compositions by conventional method known in the art:
Granule: get the Caulis et folium clerodendri bungei triterpene extracts respectively, mix homogeneously after microcrystalline Cellulose, starch solidify is the binding agent wet granulation with the hypromellose, with 80 degrees centigrade of oven dry of granule, promptly gets the granule that contains the Caulis et folium clerodendri bungei triterpene extracts.
Pellet: get the Caulis et folium clerodendri bungei triterpene extracts, evenly mixed with adjuvant after microcrystalline Cellulose, starch solidify respectively, be binding agent with the hypromellose, be that substrate prepares the micropill of diameter between 0.5～1.4 with blank pill nuclear.
Capsule: get the Caulis et folium clerodendri bungei triterpene extracts, solidify the back mix homogeneously through microcrystalline Cellulose, starch respectively, drying, the soft capsule of packing into after pulverizing, sieving promptly get Caulis et folium clerodendri bungei triterpenoid compound capsule.
Aerosol: get the Caulis et folium clerodendri bungei triterpene extracts, mixed with normal saline and other known aerosol formulations additives respectively, get Caulis et folium clerodendri bungei triterpenoid compound aerosol.
Tablet: get the Caulis et folium clerodendri bungei triterpene extracts, the Caulis et folium clerodendri bungei triterpene extracts of recipe quantity, evenly mixed with known tablet formulation adjuvant, tabletting behind the wet granulation.
When above-mentioned various preparation was used for the treatment of the disease treatment of people's air flue high response, dosage was for comprising 2800～5600mg effective ingredient every day.
Claims (1)
1. the Caulis et folium clerodendri bungei triterpene extracts is preparing the purposes for the treatment of in the airway hyperreactivity disease medicament, described Caulis et folium clerodendri bungei triterpene extracts is prepared from by following method: add 50wt% ethanol after the Caulis et folium clerodendri bungei Herb shreds, place 82 ℃ of water-bath internal heating to reflux, extract backflow, concentrate evaporate to dryness; Add water and stir into suspension, use petroleum ether extraction then, reuse chloroform extraction behind the isolated for disposal extract reclaims chloroform extraction liquid, concentrates evaporate to dryness, obtains accounting for the triterpene extracts of former medicine 0.7% left and right sides weight ratio of Caulis et folium clerodendri bungei.
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| CN1425401A (en) * | 2002-12-27 | 2003-06-25 | 叶彬 | Medicine for curing foot and skin itch |
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| CN1425401A (en) * | 2002-12-27 | 2003-06-25 | 叶彬 | Medicine for curing foot and skin itch |
Non-Patent Citations (3)
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| 王国荣等.臭牡丹化学成分和药理作用的研究进展.齐鲁药事.2006,25(1),第42-44页. * |
| 董晓萍等.臭牡丹全草化学成分的研究(一).天然产物研究与开发.1999,11(5),第8-10页. * |
| 高黎明等.臭牡丹化学成分的研究.中国中药杂志.2003,28(11),第1042-1044页. * |
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