CN101219183A - Application of mangosteen rind extract in preparing medicament for treating myocardial ischemia - Google Patents
Application of mangosteen rind extract in preparing medicament for treating myocardial ischemia Download PDFInfo
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- CN101219183A CN101219183A CNA2007103005986A CN200710300598A CN101219183A CN 101219183 A CN101219183 A CN 101219183A CN A2007103005986 A CNA2007103005986 A CN A2007103005986A CN 200710300598 A CN200710300598 A CN 200710300598A CN 101219183 A CN101219183 A CN 101219183A
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Abstract
The invention discloses an application of a mangosteen pericarp extraction in preparing medicines for the anti-myocardial ischemia, the coronary heart disease treatment and the angina pectoris treatment. The mangosteen pericarp is smashed and then extracted by 30 to 95 percent of ethanol which is recovered to obtain a raw material medicine used in the new herbal-drug research. The mangosteen pericarp extraction extracted and purified by the invention has the effects on the anti-myocardial ischemia, the coronary heart disease treatment and angina pectoris treatment.
Description
The present invention is dividing an application of Chinese patent application " peel of Carcinia mangostana L. extract and extracting method thereof and medicinal usage thereof ", number of patent application 200610016501.4.
Technical field
The present invention relates to extract and extracting method and medicinal usage thereof in a kind of new Chinese medicine material.
Background technology
Garcinia mangostana (mangosteen Carcinia mangostana L.), the original name mangosteen.Originate in Malaysian archipelago, modern Guangxi, Hainan abound with.Belong to the evergreen medium-sized arbor of Guttiferae, height of tree 10-20 rice, the tree type is attractive in appearance.Single leaf is to life, oval, keratin, Hua Dingsheng, the petal redness, the 2-4 month blooms, aubergine during fruit maturation, in seed 1-2 grain is arranged, brown, sarcocarp white is transparent, the fresh and sweet soft cunning of distinguishing the flavor of.Effect: the Cortex Garciniae growth is slow, plants just result of back 8-10, and the fructescence 6-7 month, sarcocarp contains soluble solid 16.8%, citric acid 0.63%, also contains other vitamin B1, B2, C4 and mineral, is typical tropical fruit (tree).
Garcinia mangostana is the aiphyllium with dense tree crown, height of tree 10-25 rice.The fruit parthenogenetic reproduction, the diameter 6-7 centimetre epidermis of fruit is solid smooth, be green during the color of the leather immaturity, transfers black purple or pink when ripe to, in the edible sarcocarp of 4-8 lobe is arranged, local flavor delicate fragrance is sweet and a bit sour.1-2 grain seed is arranged in each fruit.
The general plantation of Garcinia mangostana just began the result in 10 years, and is very strict to environmental requirement, therefore is genuine green fruit, and very famous and precious, its delicate fragrance gas is refreshing, and lubricious and oiliness stagnating is equally celebrated for their achievements with Durio Zibethinus murr, is known as " queen in the fruit ".Effect: purify the blood, cholesterol reducing.
Garcinia mangostana sarcocarp accounts for about the 20-30% of gross weight, and remainder is a peel, throws away as garbage.Show through preliminary chemistry and pharmacodynamic study: contain a large amount of flavone compounds in the peel of Carcinia mangostana L., have stronger biological activity aspect the reduction hyperlipidemia.Resourceful peel of Carcinia mangostana L. exploitation is become atorvastatin, and the hyperlipemic patients crowd at vast is with a wide range of applications.
At present, relevant peel of Carcinia mangostana L. total extract and extracting method thereof and medicinal usage thereof are not seen report.
Summary of the invention
Purpose of the present invention provides peel of Carcinia mangostana L. extract to be used for lipidemia disease in preparation, has resisted myocardial ischemia, treated the application of coronary heart disease, anginal medicine.The extraction process for purification of peel of Carcinia mangostana L. extract of the present invention is:
A. peel of Carcinia mangostana L. is pulverized, under 30-80 ℃ of condition, doubly measured the 30%-95% ethanol extraction 3 times, be respectively 3h, 2h, 1h at every turn, filter merge extractive liquid, with 20-25;
B. on the extracting solution that step a is obtained, reclaim ethanol to extractum, drying.
Because of Cortex Garciniae is grown slow, 8-10 ability result after kind, the fructescence 6-7 month, sarcocarp contains soluble solid only 16.8%, and peel accounts for more than the 70%-80% of fruit, and resource is very abundant, through studies show that it is rich in effective ingredient such as total flavones, be very precious new medical material, do not see report, its blood lipid-lowering medicine purposes belongs to first to be found.Peel of Carcinia mangostana L. extract is characterized by light yellow to brown, and is Powdered, bitter in the mouth, water soluble, ethanol etc.This peel of Carcinia mangostana L. extract content of total flavone accounts for more than 2% of peel of Carcinia mangostana L. dry weight.
When the present invention is used for preparation when resisting myocardial ischemia, treating coronary heart disease, anginal medicine, its oral or parenteral, all be safe, under oral situation, it can any conventionally form administration, as powder, granule, tablet, capsule, pill, solution, suspension, syrup, buccal tablets, sublingual lozenge etc.: when this medicine parenteral, can take any conventionally form, for example injection: as intravenous injection, ointment, suppository, percutaneous dosing, inhalant etc.
It is to be made of effective ingredient monomer or the effective ingredient excipient with solid or liquid that the present invention preparation resists myocardial ischemia, treats coronary heart disease, anginal medicine, the excipient of solid used herein or liquid is well known in the art, lift several object lessons below, powder is the powder agent that takes orally, its excipient has lactose, starch, paste essence, calcium carbonate, synthetic or puritan filler aluminum, magnesium oxide, magnesium stearate, sodium bicarbonate, dry yeast etc.; The excipient of solution has water, glycerol, propylene glycol, simple syrup, ethanol, ethylene glycol, Polyethylene Glycol, Sorbitol etc.; The excipient of ointment can use fatty oil, and agnolin, vaseline, glycerol, Cera Flava, wood are cured, white oil, resin, senior water-repelling agent or the hydrophilizing agent that is combined into such as cured.
The invention has the beneficial effects as follows that peel of Carcinia mangostana L. extract belongs to the new medicinal substances extract of Garcinia mangostana, its medicinal usage belongs to first to be found, for resist myocardial ischemia, treat coronary heart disease, new medicine source has been found in angina pectoris.
The dosage of active substance can be according to the mode of taking, patient's age and body weight and be in a bad way degree and other similar factor and change, and oral dose is: 70～120mg/ time, take for 1～2 time every day: inject 30～70mg/ time, once a day.
The specific embodiment
The present invention can further specify by following experimental example.Peel of Carcinia mangostana L. extract is hereinafter to be referred as SZGPT.
The preliminary test of experimental example one, SZGPT prevention and treatment hyperlipidemia
1, materials and methods
1.1 animal SD rat, 40, male and female half and half, body constitution amount 130g-150g is available from this school Experimental Animal Center.
1.2 medicine peel of Carcinia mangostana L. extract SZGPT: self-control; Radix Oenotherae erythrosepalae oil, Pharmaceutical Factory, Bethune Medical Univ. produces.Cholesterol powder (AR) provides (lot number F20030410) by China Medicine (Group) Shanghai Chemical Reagent Co..
1.3 the preparation high lipid food of high lipoprotein rabbit feedstuff and various pastille object height fat feedstuffs preparation: add cholesterol 0.4g, Adeps Sus domestica 2mL among the normal feedstuff 100g; The medicine that adds different content on the basis of high lipid food is mixed with the high lipid food that contains medicine and feeds for experiment.
2,40 of rats are got in the influence of normal rat fat level, male and female half and half, fasting feedwater 12h, claim the body constitution amount, be divided into 4 groups (each 10) at random: the normal control group (normal saline, 1ml/100g), positive controls (Radix Oenotherae erythrosepalae oil 1.2g/100g), the heavy dose of group of peel of Carcinia mangostana L. extract (0.84g/kg), middle dosage group (0.42g/kg) and small dose group (0.21g/kg).Said medicine is all irritated stomach (ig) administration, and every day 1 time, 15d claims body constitution amount 1 time weekly in the experimentation altogether, extracts rat eye on the 16th day, and eye socket is got blood 2-3ml, send the blood biochemical analysis, surveys TG and TC content in the serum.
3, peel of Carcinia mangostana L. extract extract blood fat reducing result of the test sees Table 1.
Table 1 peel of Carcinia mangostana L. extract blood fat reducing result of the test
| Grouping | TC(mmol/L) | TG(mmol/L) |
| The heavy dose of group of dosage group in the normal control group positive controls peel of Carcinia mangostana L. extract small dose group | 2.260±0.225 1.920±0.177 * 1.960±0.292 * 1.835±0.214 * 1.637±0.205 * | 1.513±0.351 1.241±0.235 1.073±0.365 * 1.040±0.173 * 1.035±0.154 * |
4, the conclusion experimental result shows that peel of Carcinia mangostana L. extract has tangible effect for reducing blood fat.
Experimental example two, SZGPT resist myocardial ischemia, treat coronary heart disease, anginal preliminary test
1. materials and methods
1.1 the animal health mongrel dogs, female, male dual-purpose, body weight 16.23 ± 1.87kg.
1.2 medicine and reagent peel of Carcinia mangostana L. extract (medicated powder), character: shallow rice-pudding toner end, purity: the peel of Carcinia mangostana L. extract general flavone content is no less than 2% in the sample, lot number: 031007, provide by regenerative medicine Science Institute of Jilin University; Positive control drug: Folium Ginkgo, specification: the 12mg/ sheet, contain total flavonoid glycoside 9.6mg, terpenoid lactone 2.4mg, lot number: 20031212, Guizhou Xinbang Pharmacy Stock Co., Ltd's product; Pentobarbital sodium, specification: analytical pure (25g/ bottle), lot number: 950427, Tong County, Beijing Fine Chemical Works product of cultivating people of ability; Heparin sodium injection, specification: 12500U:2ml, lot number: 0104108, Wanbang Biochemically Pharmaceutical Co Ltd, Xuzhou's product; The chlorination nitro blue tetrazolium, specification: analytical pure, lot number: F20020830, China Medicine's product; Glutamic oxaloacetic transaminase, GOT (AST) detection kit, specification: 10ml * 10, lot number: 020151, creatine kinase (CK) detection kit, specification: 10ml * 10, lot number: 090151, lactic acid dehydrogenase (LDH-L) detection kit, specification: 10ml * 10, lot number: 130081, Zhongsheng Beikong Biological Science ﹠ Technology Co., Ltd.'s product; Malonaldehyde (MDA) detection kit, specification: the 50T/ box, lot number: 20040322, superoxide dismutase (SOD) detection kit, specification: the 50T/ box, lot number: 20040323, bio-engineering research institute product is built up in Nanjing.
1.3 instrument CBI-8000 laser-Doppler blood flow instrument (U.S. BIOPAC company product) selects to be fit to bore blood flow probe according to laboratory animal coronary artery and aorta diameter; Powerlab/8s type eight derivatives are monitor and related accessories (Australian Ai De company product) according to one's analysis; SC-3 type artificial respirator (Shanghai Medical Equipment Factory's product); HL-2 type constant flow pump (Shanghai City Hu Xi instrument plant product); TU-1800S type ultraviolet-uisible spectrophotometer (Beijing Puxi General Instrument Co., Ltd's product); BI-2000 medical images analyser (Chengdu TME Technology Co., Ltd.'s product).
2. experimental technique
2.1 grouping and dosage are divided into matched group at random with experimental dog; Positive control drug Folium Ginkgo group (24mg/kg); Three dosage groups of peel of Carcinia mangostana L. extract 24mg/kg, 12mg/kg and 6mg/kg.Every group 6.Control drug and be subjected to the reagent thing to be mixed with the desired concn suspension with distilled water.
2.2 the operation method laboratory animal is anaesthetized with 3% pentobarbital sodium (30mg/kg) intravenous injection.Operation on neck, tracheal intubation connects artificial respirator, separates left carotid, and intubate writes down arteriotony through pressure transducer; Separate femoral vein, intubate is for liquid make-up or anaesthetic; Separate right common femoral artery and intubate to left ventricle, connect pressure transducer and measure left ventricular pressure and whole last pressure of left ventricular diastolic, measure the left ventricular pressure rate of change through differentiator again; Duodenal intubation is done in abdominal operation, for duodenal administration; Open breast, vertically cut off pericardium, do the fixing heart that holds up of pocket, isolate LCA and aortic root, place the laser-Doppler probe that is fit to bore, measure coronary artery blood flow and ABF (cardiac output) respectively.
3. observation index and detection method thereof
3.1 the foundation of myocardial infarction and ischemia model operation finishes, and stablize 30min, treat that every physical signs steadily after, the normalized curve that writes down every index earlier contrasts before as administration.Begin administration subsequently, positive control drug Folium Ginkgo and be subjected to the reagent YANGSHENGUO GUANXIN PIAN through duodenal administration, control animals gives the equal-volume distilled water through duodenum.45min after the administration, sets up the acute myocardial ischemia model by in the ligation left coronary artery left anterior descending branch following 1/3 section.During respectively at 2min, 5min after the ligation, 10min, 20min, 30min, 60min, 90min, 120min, 180min, 240min, 300min and 360min, 6h cardiac muscle three enzymes, SOD, MDA, myocardial infarction area percentage ratio after the surveying record coronary artery ligation.
3.2 cut heart when the experiment of myocardial infarction area measuring method finishes, clean with physiology salt is long, remove blood stains, reject non-cardiac muscular tissues such as blood vessel fat, inhale the branch that anhydrates with absorbent paper, claim weight in wet base whole-heartedly.Cut off the above atrium of coronary sulcus, satisfactory chamber is heavy.Along coronary sulcus is parallel from the apex of the heart to the heart base portion ventricle is cut into the cardiac muscle section that thickness is 1cm, cleans with normal saline.The cardiac muscle section is positioned in 0.025% nitro blue tetrazolium (NBT) solution, and temperature is incubated 15min dyeing in 37 ℃ of water-baths, constantly stirs dyeing liquor in the dyeing course and makes it with cardiac muscle sufficient touch opportunity is arranged.The unnecessary dyestuff of water flushing immediately after the dyeing, normal myocardium is dyed blueness, and infarcted myocardium is not colored.Video device by BI-2000 medical images analytical system is taken in computer with each group cardiac muscle section with the picture form, determine the area and the monoblock myocardial area of calculating myocardium infarction again by the software of BI-2000 medical images analysis system processes area, available formula: myocardial infarction area=be unstained area and/the myocardium sheet gross area and * 100%.
4. result and discussion
Peel of Carcinia mangostana L. extract is to the influence of myocardial ischemia dog myocardial infarction area
6h after the coronary artery ligation, cut into slices by cardiac muscle, substantially specimen calculates the percentage ratio that myocardial infarction area accounts for the myocardium gross area through chlorination nitro blue tetrazolium (NBT) dyeing, can reflect the prophylactic treatment effect to heart infarction of the size of myocardial infarction area after the ligation and medicine intuitively.As can be seen from Table 2: 6h after the coronary artery ligation, the myocardial infarction area of matched group are 25.7 ± 4.0%; The myocardial infarction area of positive control phase medicine Folium Ginkgo 24mg/kg group was 18.1 ± 2.0% (comparing P＜0.01 with matched group): the myocardial infarction area that is tried new drug peel of Carcinia mangostana L. extract 24mg/kg, 12mg/kg and 6mg/kg dosage group is respectively 13.1 ± 2.9%, 19.1 ± 1.5% and 23.6 ± 1.5% (relatively being respectively P＜0.001, P＜0.01 and P＞0.05 with matched group).In addition, the myocardial infarction area that is tried new drug peel of Carcinia mangostana L. extract 24mg/kg dosage group also is significantly less than the positive control drug Folium Ginkgo (P＜0.01) of identical dosage.Above-mentioned experimental result shows, is tried the new drug peel of Carcinia mangostana L. extract under the myocardial ischemia condition, can coronary blood flow increasing, improve blood supply of cardiac muscle oxygen supply situation, treatment and prevention coronary heart disease, angina pectoris, minimizing myocardial infarction area.And this effect obviously is better than the positive control drug Folium Ginkgo of same dose.Detailed results sees Table 2.
Table 2. peel of Carcinia mangostana L. extract to the influence of myocardial ischemia dog cardiac muscle three enzymes, SOD, MDA and myocardial infarction area (
N=6)
| Group | Contrast | Folium Ginkgo (24mg/kg) | Peel of Carcinia mangostana L. extract (24mg/kg) | Peel of Carcinia mangostana L. extract (12mg/kg) | YANGSHENGUO GUANXIN PIAN (6mg/kg) | |
| Before the administration | LDH (U/L) CK (U/L) AST (U/L) SOD (U/ml) MDA (nmol/ml) | 362.6±44.7 1012.2±149.5 120.9±26.2 88.6±5.5 9.9±1.6 | 326.5±62.2 1038.9±232.0 120.0±25.2 91.4±7.9 10.2±2.1 | 346.6±30.0 1127.1±180.2 124.2±20.4 89.6±9.2 9.3±1.7 | 350.9±86.4 1010.3±185.3 114.2±32.6 96.4±8.7 8.7±2.1 | 335.1±58.0 996.1±317.5 121.2±31.5 97.1±7.9 9.1±2.1 |
| Behind the coronary ligation 6 hours | LDH (U/L) CK (U/L) AST (U/L) SOD (U/ml) MDA (nmol/ml) heart infarction area (%) | 712.6±116.4 2146.2±205.2 289.8±59.7 43.1±9.0 20.2±3.1 25.7±4.0 | 419.9±127.9 *** 1639.3±397.6 ** 218.0±59.4 * 52.1±7.0 * 14.5±3.1 ** 18.1±2.0 ** | 443.5±164.7 ** 1304.3±376.2 *** 197.0±44.6 ** 68.0±8.1 ***▲▲ 13.5±3.4 ** 13.1±2.9 ***▲▲ | 505.2±154.4 * 1524.4±500.2 ** 228.4±77.9 55.4±8.5 * 15.1±3.9 * 19.1±1.5 ** | 594.8±172.4 1741.3±471.6 * 244.7±77.8 47.5±9.5 17.2±4.6 23.6±1.5 |
Annotate: compare with matched group
*P＜0.05;
*P＜0.01;
* *P＜0.001.Compare with positive control drug Folium Ginkgo group
▲ ▲P＜0.01.
The embodiment 1 of extracting method:
A. peel of Carcinia mangostana L. is pulverized, under 80 ℃ of conditions,, be respectively 3h, 2h, 1h, filtration, merge extractive liquid, at every turn with 25 times of amount 30% ethanol extractions 3 times;
B. on the extracting solution that step a is obtained, reclaim ethanol to extractum, drying.
The embodiment 2 of extracting method:
A. peel of Carcinia mangostana L. is pulverized, under 30 ℃ of conditions,, be respectively 3h, 2h, 1h, filtration, merge extractive liquid, at every turn with 20 times of amount 95% ethanol extractions 3 times;
B. on the extracting solution that step a is obtained, reclaim ethanol to extractum, drying.
The embodiment 3 of extracting method:
A. peel of Carcinia mangostana L. is pulverized, under 50 ℃ of conditions,, be respectively 3h, 2h, 1h, filtration, merge extractive liquid, at every turn with 22 times of amount 60% ethanol extractions 3 times;
B. on the extracting solution that step a is obtained, reclaim ethanol to extractum, drying.
The embodiment 1 of preparation medicament:
Get peel of Carcinia mangostana L. extract 50g, add medical starch 250g, the two fully mixes, and makes 1000 capsules, and every heavy 0.3g contains mangosteen extract 50mg.
The embodiment 2 of preparation medicament:
Get peel of Carcinia mangostana L. extract 60g, add medical starch 240g, the two fully mixes, and makes 1000, and every heavy 0.3g contains peel of Carcinia mangostana L. extract 60mg.
Claims (1)
1. peel of Carcinia mangostana L. extract is used for resisting myocardial ischemia, treating the application of coronary heart disease, anginal medicine in preparation.
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104207206A (en) * | 2014-06-30 | 2014-12-17 | 彭靖媛 | Making method of seafood in clay pot |
| CN113892645A (en) * | 2021-10-11 | 2022-01-07 | 北京合正道科技有限公司 | Composition for protecting heart and application thereof |
-
2006
- 2006-01-05 CN CNA2007103005986A patent/CN101219183A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104207206A (en) * | 2014-06-30 | 2014-12-17 | 彭靖媛 | Making method of seafood in clay pot |
| CN113892645A (en) * | 2021-10-11 | 2022-01-07 | 北京合正道科技有限公司 | Composition for protecting heart and application thereof |
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Open date: 20080716 |