CN109045045A - A kind of active ingredient of Chinese herbs composition for treating cardiovascular and cerebrovascular disease - Google Patents

A kind of active ingredient of Chinese herbs composition for treating cardiovascular and cerebrovascular disease Download PDF

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Publication number
CN109045045A
CN109045045A CN201810921299.2A CN201810921299A CN109045045A CN 109045045 A CN109045045 A CN 109045045A CN 201810921299 A CN201810921299 A CN 201810921299A CN 109045045 A CN109045045 A CN 109045045A
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composition
active ingredient
cerebrovascular disease
treating cardiovascular
chinese herbs
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CN109045045B (en
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缪国鹏
韩娟
张际峰
童贯和
武以海
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SUZHOU LICHEN BIOTECHNOLOGY Co.,Ltd.
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Huainan Normal University
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/575Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/045Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • A61K31/05Phenols
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/12Ketones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines Containing Plant Substances (AREA)

Abstract

The invention discloses a kind of active ingredient of Chinese herbs composition for treating cardiovascular and cerebrovascular disease, the composition is gone obtained by two or three of mixing in the peppery diketone of hydroxyl ginger by pachymic acid, honokiol and 10-.The present invention is under the combination of optimal compatibility, and compatibility or three component compatibilities can significantly reduce TC, TG and LDL-C content and increase the content of HDL-C two-by-two.Two-by-two after compatibility, blank control group level cannot be fully achieved in four kinds of indexs, but is on close level with blank control group.Four kinds of finger target values can then be reduced or be increased to blank control level by three component compatibilities.

Description

A kind of active ingredient of Chinese herbs composition for treating cardiovascular and cerebrovascular disease
Technical field
The present invention relates to field of traditional Chinese medicine preparations, and in particular to a kind of active ingredient of Chinese herbs combination for treating cardiovascular and cerebrovascular disease Object.
Background technique
Atherosclerosis (atherosclerosis, AS) refers to deposited fat on ductus arteriosus wall, because of interior film outward appearance It is yellow-white, similar congee sample, therefore it is atherosis.The deposition of these lipids makes artery wall thickening, flexibility decrease, to make Blood vessel is hardened, therefore referred to as atherosclerosis.Cholesterol metabolism abnormity be cause the significant risk of atherosclerotic lesions because Element, epidemiological study have confirmed that low-density lipoprotein (LDL) or low density lipoprotein cholesterol (LDL-C) are artery congee The important pathogenic factor of sample hardening, and the horizontal generation with atherosclerosis of plasma hdl cholesterol (HDL-C) Negatively correlated, triglyceride (TG) and total cholesterol (TC) raising are the independent hazard factors for causing coronary heart disease.Nowadays, recognize It is existed simultaneously for the abnormal reduction increased with HDL-C of LDL-C, TG, TC, is a kind of blood lipoprotein syndrome of high risk, Referred to as atherogenic lipoprotein phenotype.Atherosclerosis is coronary heart disease, cerebral infarction, peripheral vascular disease and high blood The main reason for cardiovascular and cerebrovascular diseases such as pressure.
The Western medicine lipid-lowering effects such as existing Statins (Statin), fibrates (Fibrate) are obvious, but long-term administration is to liver It is big (only about 28% crowd is applicable in) with musclar toxicity effect.Ezetimibe (Ezetimibe) and bile acid sequestrant etc. due to The mechanism of action is single, and target user is then less.And compound of Chinese herbal medicine hyperlipidemia and its complication have a good effect, but by It is complex in traditional Chinese medicine compound ingredient, there is the action character of more compositions, too many levels, multiple target point, quality is difficult to control, from And limit popularization and use of the Chinese traditional medicines depressing lipid in wider scope.The single active ingredient of Chinese herbs of ingredient is although quality controllable, but It is that therapeutic effect has a long way to go compared with Chinese medicine compound prescription.In recent years, tcm components are with its " with strong points, safe and effective, quality controllable " As the research tendency of the modernization of Chinese medicine, the main active of ingredients in Chinese medicine compound prescription is combined, not using it Same mechanism of action plays the curative effect of preferable even better than Chinese medicine compound prescription.
Poria cocos is one of common traditional Chinese medicine ingredients in China, and the civil saying for having " ten medicines, nine Poria cocos ", Poria cocos is Polyporaceae The dry sclerotia of fungi Poria cocos, traditional Chinese medicine theory think that Poria cocos has effects that inducing diuresis for removing edema, invigorating the spleen excreting dampness, antitoxic heart-soothing and sedative.Fu Siberian cocklebur chemical component mainly has pachymaran and su-fuling etc., and su-fuling is one group of tetracyclic triterpenes small molecule compound, with acid Form exists, and pachymic acid (pachymic acid, PA) is one of its most important ingredient.Researches show that PA can be by directly pressing down Phospholipase A2 processed
(phospholipase A2, PLA2) limits OxLDL ELISA modification, and then inhibits atherosclerosis Formation.
Cortex Magnoliae Officinalis is a kind of traditional Chinese medicine in China, there is certain long history, with significant antibacterial activity, cardiovascular protection The extensive effect such as function, antidepression.Data at home and abroad report about its main component HK effect mainly have antibacterial, antiulcer, Calm nervous centralis, relaxed muscle, extend sleep, decompression, treatment gastrointestinal disease, antianxiety, it is antitumor the effects of.Research is aobvious Show, honokiol (honokoil, HK) can be by binding directly simultaneously peroxide activator enzyme body proliferator activated receptor γ (peroxisome
Proliferators-activated receptors, PPAR γ), to show the function such as hypoglycemic, reducing blood lipid Effect.
It is a kind of natural that 10- present in ginger, which removes the peppery diketone of hydroxyl ginger (10-dehydrogingerdione, DHG), CETP inhibitor, cholesterol ester transfer protein (cholesterol ester transfer protein, CETP) are that one kind exists The important molecule to play the role of a nucleus in HDL metabolism, HDL-C level can be increased up to 50% after being inhibited, and can be significantly changed The pathologic process of atherosclerosis.
Although the related pharmacological mechanism of three kinds of active constituents has been reported that, however, not carried out reasonable compatibility still.
Summary of the invention
To solve the above problems, the present invention provides a kind of active ingredient of Chinese herbs composition for treating cardiovascular and cerebrovascular disease, Lipid-loweringing purpose is realized by carrying out reasonable compatibility to PA, HK and DHG, can reduce side effect, while remaining Chinese medicine multiple groups Divide disease-resistant pharmacological mechanism.
To achieve the above object, the technical scheme adopted by the invention is as follows:
A kind of active ingredient of Chinese herbs composition for treating cardiovascular and cerebrovascular disease, the composition is by pachymic acid (PA), magnolia obovata Phenol (HK) and 10- are gone obtained by two or three of mixing in the peppery diketone of hydroxyl ginger (DHG).
Further, the composition is made of the raw material of following mass percent:
Pachymic acid (PA), honokiol (HK) and 10- remove the quality percentage of the peppery diketone of hydroxyl ginger (DHG) in the composition Than being respectively 20~50%, 5~30% and 10~40%.
Preferably, the composition is by pachymic acid (PA), honokiol (HK) 3:1 in mass ratio mixing gained.
Preferably, the composition goes the peppery diketone of hydroxyl ginger (DHG) 3:2 in mass ratio to mix institute by pachymic acid (PA), 10- ?.
Preferably, the composition goes the peppery diketone of hydroxyl ginger (DHG) 1:2 in mass ratio to mix institute by honokiol (HK), 10- ?.
Preferably, the composition goes the peppery diketone of hydroxyl ginger (DHG) by quality by pachymic acid (PA), honokiol (HK), 10- Gained is mixed than 3:1:2.
The invention has the following advantages:
Optimal compatibility combination under, two-by-two compatibility or three component compatibilities can significantly reduce TC, TG and LDL-C content with And increase the content of HDL-C.Two-by-two after compatibility, four kinds of indexs cannot be fully achieved blank control group level, but with blank pair According to being on close level for group.Four kinds of finger target values can then be reduced or be increased to blank control level by three component compatibilities.
Specific embodiment
In order to which objects and advantages of the present invention are more clearly understood, the present invention is carried out with reference to embodiments further It is described in detail.It should be appreciated that the specific embodiments described herein are merely illustrative of the present invention, it is not used to limit this hair It is bright.
Kun Ming mice is after 4 weeks feed, fasting 12h.Blank control group (feeding basal feed), hyperlipidemia pair are set According to group (feeding high lipid food), one pack system experimental group and component compatibility experimental group.Free water and feed during experiment, daily with 8mg/kg dosage in early morning and at dusk respectively carry out intraperitoneal injection 1 time (0.2mL), continuous 2 weeks.After the last administration, all animals are prohibited 12h is eaten, eyeground vein takes blood, and blood the water-bath 30min at 37 DEG C, 3500r/min are centrifuged 15min, separate serum, use kit Measure TC, TG, HDL-C, LDL-C content.Medicament is all made of aqueous dissolution or the suspension of Tween 80 and ethyl alcohol, wherein tween 80 and ethyl alcohol final concentration less than 0.1%.
1 one pack system of table and component compatibility experimental result (n=10)
Note: variance analysis and Duncan Multiple range test are carried out using SPSS ver.16.0 software (IBM, the U.S.);Each component Ratio be mass ratio.
Seen from table 1, above-mentioned compatibility combination under, two-by-two compatibility or three component compatibilities can significantly reduce TC, TG and LDL-C content and the content for increasing HDL-C.Two-by-two after compatibility, blank control group level cannot be fully achieved in four kinds of indexs, but It is on close level with blank control group.Four kinds of finger target values can then be reduced or be increased to blank control water by three component compatibilities It is flat.
The above is only a preferred embodiment of the present invention, it is noted that for the ordinary skill people of the art For member, without departing from the principle of the present invention, it can also make several improvements and retouch, these improvements and modifications are also answered It is considered as protection scope of the present invention.

Claims (6)

1. a kind of active ingredient of Chinese herbs composition for treating cardiovascular and cerebrovascular disease, which is characterized in that the composition by pachymic acid and Magnolol, 10- are gone obtained by two or three of mixing in the peppery diketone of hydroxyl ginger.
2. a kind of active ingredient of Chinese herbs composition for treating cardiovascular and cerebrovascular disease as described in claim 1, which is characterized in that should Composition is made of the raw material of following mass percent:
Pachymic acid 20~50%;Honokiol 5~30%;10- removes the peppery diketone 10~40% of hydroxyl ginger.
3. a kind of active ingredient of Chinese herbs composition for treating cardiovascular and cerebrovascular disease as described in claim 1, which is characterized in that should Composition is by pachymic acid (PA), honokiol (HK) 3:1 in mass ratio mixing gained.
4. a kind of active ingredient of Chinese herbs composition for treating cardiovascular and cerebrovascular disease as described in claim 1, which is characterized in that should Composition removes the peppery diketone of hydroxyl ginger (DHG) 3:2 in mass ratio mixing gained by pachymic acid (PA), 10-.
5. a kind of active ingredient of Chinese herbs composition for treating cardiovascular and cerebrovascular disease as described in claim 1, which is characterized in that should Composition removes the peppery diketone of hydroxyl ginger (DHG) 1:2 in mass ratio mixing gained by honokiol (HK), 10-.
6. a kind of active ingredient of Chinese herbs composition for treating cardiovascular and cerebrovascular disease as described in claim 1, which is characterized in that should Composition removes the peppery diketone of hydroxyl ginger (DHG) 3:1:2 in mass ratio mixing gained by pachymic acid (PA), honokiol (HK), 10-.
CN201810921299.2A 2018-08-14 2018-08-14 A Chinese medicinal composition for treating cardiovascular and cerebrovascular diseases Active CN109045045B (en)

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Cited By (1)

* Cited by examiner, † Cited by third party
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CN112138053A (en) * 2020-11-05 2020-12-29 西北民族大学 A pharmaceutical composition for treating cardiovascular and cerebrovascular diseases, and its preparation method

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CN104000876A (en) * 2014-06-18 2014-08-27 青岛市市立医院 Composition of mangnolia officinalis and gingerol and application thereof
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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112138053A (en) * 2020-11-05 2020-12-29 西北民族大学 A pharmaceutical composition for treating cardiovascular and cerebrovascular diseases, and its preparation method

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