CN106806365B - Purposes of the psoralen in preparation treatment hyperlipidemia - Google Patents
Purposes of the psoralen in preparation treatment hyperlipidemia Download PDFInfo
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- CN106806365B CN106806365B CN201710073710.0A CN201710073710A CN106806365B CN 106806365 B CN106806365 B CN 106806365B CN 201710073710 A CN201710073710 A CN 201710073710A CN 106806365 B CN106806365 B CN 106806365B
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/365—Lactones
- A61K31/366—Lactones having six-membered rings, e.g. delta-lactones
- A61K31/37—Coumarins, e.g. psoralen
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Abstract
The invention belongs to pharmaceutical technology fields, are related to psoralen in the purposes of preparation treatment hyperlipidemia, first passage pharmacological testing discovery psoralen of the present invention has therapeutic effect well to olive Antihyperlipidemia capsule.The therapeutic effect for feeding the hyperlipidemia disorders of lipid metabolism rat model established to high lipid food for psoralen carries out system research, as the result is shown: psoralen has the therapeutic effect of significant ground to olive Antihyperlipidemia capsule, psoralen can be such that the total cholesterol (TC), triglycerides (TG), low density lipoprotein cholesterol (LDL-C) of hyperlipidemia rats reduces, high-density lipoprotein cholesterol (HDL-C) increases, and has the function of while reducing hyperlipidemia rats cholesterol and triglycerides.
Description
Technical field
The present invention relates to a kind of purposes of psoralen in preparation treatment hyperlipidemia.
Background technique
Dyslipidemia is the abbreviation of blood lipid metabolic disorder, refer mainly to triglycerides (Triglyceride, abridge TG),
Low density lipoprotein cholesterol (abbreviation LDL-C), total cholesterol (total cholesterol, abridge TC) are more than normal range (NR)
And (or) high-density lipoprotein cholesterol (abbreviation HDL-C) is low；The hyperlipidemia often claimed in clinic, generally refer to TC and
(or) LDL-C and (or) TG increase.In recent years, human lives' condition and life style have great improvement, and diet type is numerous
It is more and full of nutrition, and move and rest accordingly and do not increase, cause metabolism class disease more and more, hyperlipidemia is exactly
One of which, disease incidence increasingly increase.Modern research shows that the diseases such as atherosclerosis, diabetes, cardiovascular and cerebrovascular disease with
Dyslipidemia has close relationship.As one of risk factor, adjust blood lipid level, correct disorders of lipid metabolism can be with
Effectively prevention even mitigates artery sclerosis, the incidence of cardiovascular and cerebrovascular disease.Epidemiology shows, the total illness of China's dyslipidemia
Rate is 18.6%, and dyslipidemia crowd has reached 1.6 hundred million within 18 years old or more.With the development of society, the accelerating rhythm of life, diet
The change etc. of structure, disease incidence is in rising trend, greatly affected the quality of life of patient, it has also become major disease problem.
Therefore, there is an urgent need to seek practicable control method.Common treatment hyperlipidemia has at present: (1) hydroxyl
First glutaryl CoA reductase inhibitor (Statins): i.e. hydroxy-3-methylglutaryl CoA reductase inhibitor, at present clinical application
Widest one kind drug.It there is now following statins: Simvastatin, Atorvastatin, Rosuvastatin, general recommendations
It takes at night.(2) phenoxy acetic acid class fat regulation medicine (fibrates): such as clofibrate, Bezafibrate, fenofibrate top grade.
Statins (statins) can mainly reduce Blood Cholesterol, and main mechanism is that it is methylol penta
Two acyl coenzyme A (HMG-CoA) reductase inhibitors, such drug synthesize rate-limiting enzyme by Reverse transcriptase endogenous cholesterol
(HMG-CoA) reductase blocks intracellular hydroxyl first valeric acid metabolic pathway, reduces intracellular cholesteryl synthesis, thus feedback
Stimulate cell membrane surface (predominantly liver cell) low-density lipoprotein (low density lipoprotein, LDL) acceptor quantity
Increase with activity, reduce serum cholesterol removing increase, level.Fibrate can pass through the activity of enhancing lipoprotein lipase
Accelerate the decomposition of lipoprotein, while also can be reduced the synthesis of lipoprotein in liver, to reduce blood lipid.The prominent of this kind of drug is made
With being substantial reduction in triglycerides.
To sum up, currently used treatment hyperlipidemia statins action character is can to reduce Blood Cholesterol, shellfish
Special class drug can reduce triglycerides in blood.In addition the derivable liver enzyme exception of existing statins and rhabdomyolysis etc.
Adverse reaction, or even cause the generation of hepatic injury, while taking fibrates and both lipid-regulation medicines of Statins, liver kidney damage occurs
Harmful and rhabdomyolysis danger will obviously increase.Therefore, exploitation has while reducing gallbladder in hyperlipidemia patient blood
The research of the drug of sterol and triglycerides is of great significance.
Psoralen (Psoralen) is the important composition ingredient of Effects of Bu Gu rouge (Psoralea corylifolia L.)
One of, it can be separated from the seed of psoralea corylifolia, belong to furocoumarin class active skull cap components, bioactivity is a variety of more
Sample.Pharmacological research shows that psoralen has the effects that anticancer, anti-oxidant, anti-leukocythemia, antidepression, antiviral, antibacterial；It is clinical
Upper psoralen joint UVA Radiation (PUVA) can be used for treating psoriasis, leucoderma, skin T cell lymphoma and
The diseases such as graft versus host disease(GVH disease).Psoralen (Psoralen) chemical name is 7H- furans simultaneously [3,2-G] chromene -7-
Ketone, and psoralen or Methoxypsoralen can be referred to as.Colorless needle crystals (crystallize) in ethanol, and molecular formula is C11H6O3, phase
It is 186.16 to molecular mass, fusing point is 189-190 DEG C, can be dissolved in ethyl alcohol, chloroform, be slightly soluble in water, ether and petroleum ether, Psoralen
The structural formula of rouge element are as follows:
Therefore, first passage pharmacological testing of the present invention shows: psoralen has olive Antihyperlipidemia capsule to be controlled well
Treatment effect.For psoralen to high lipid food feed establish hyperlipidemia disorders of lipid metabolism rat model therapeutic effect into
Row system research, the results show that psoralen can make the total cholesterol (TC) of hyperlipidemia rats, triglycerides (TG), low close
Spending lipoprotein cholesterol (LDL-C) reduces, and high-density lipoprotein cholesterol (HDL-C) increases, and has while reducing hyperlipidemia
The effect of Rat Cholesterol and triglycerides.
Summary of the invention
Present invention aims at provide a kind of purposes of psoralen in preparation treatment hyperlipidemia.The present invention
First passage pharmacological testing discovery psoralen has therapeutic effect well to olive Antihyperlipidemia capsule.For psoralen pair
The therapeutic effect that high lipid food feeds the hyperlipidemia disorders of lipid metabolism rat model established carries out system research, as the result is shown:
Psoralen has the therapeutic effect of significant ground to olive Antihyperlipidemia capsule, and psoralen can make the total cholesterol of hyperlipidemia rats
(TC), triglycerides (TG), low density lipoprotein cholesterol (LDL-C) reduce, and high-density lipoprotein cholesterol (HDL-C) rises
Height has the function of while reducing hyperlipidemia rats cholesterol and triglycerides.
A kind of purposes of the psoralen of the present invention in preparation treatment hyperlipidemia.
A kind of psoralen of the present invention preparation treatment hyperlipidemia in purposes, involved in mend
Bone fat cellulose content >=98% is purchased from Nanjing Jing Zhu Biotechnology Co., Ltd, lot number 20151117.
Specific embodiment
Embodiment
Experimental study of the psoralen to hyperlipidemia rats effect for reducing fat:
Purpose: influence of the research psoralen to hyperlipidemia rats blood lipid；Method: foundation is fed by high lipid food
Hyperlipidemia disorders of lipid metabolism rat model measures its four items of blood lipid tests after receiving oral gastric infusion psoralen and treating 4 weeks.
As a result: compared with model group, psoralen can make the total cholesterol (TC) of hyperlipidemia rats, triglycerides (TG), low-density
Lipoprotein cholesterol (LDL-C) reduces, and high-density lipoprotein cholesterol (HDL-C) increases.Conclusion: psoralen is to hyperlipidemia
The lipid metaboli of rat has certain adjustment effect.
Keyword: psoralen；Hyperlipidemia；Rat；
1 material:
1.1 experimental animals: healthy SD male rat, weight 180-220g；Xinjiang Animal Experimental Study center provides, experiment
Animal productiong licensing number: SCXK (new) 2011-0001；
1.2 laboratory apparatus and main agents: four items of blood lipid tests reagent steps auspicious offer by Shenzhen, full-automatic biochemical analyzer:
7100 types, Hitachi, Ltd；
1.3 tested materials: psoralen, content >=98% are purchased from Nanjing Jing Zhu Biotechnology Co., Ltd, lot number
20151117,2-8 DEG C of temperature preservation；
1.4 high lipid foods: by Beijing Australia, section pull together feed corporation,Ltd provide；
1.5 positive control drugs: simvastatin piece, manufacturer: Jiangsu Huang He Pharmaceutical Co., Ltd, lot number:
20150820, authentication code: national drug standard H20067793；
2. method:
2.1 modelings and grouping: to adapt to environment, 10 rats are extracted out at random as Normal group within SD rat feeding 1 week
(A group) is fed with normal diet (protein account for 23%, carbohydrate account for 53%, fat account for 5%), remaining rat feeds with high in fat
Feed, high lipid food is by 10% lard, and 20% sucrose, 10% yolk powder, 1% cholesterol, 59% basestocks form, after 1 month,
Successful 50 rats of modeling are randomly divided into 4 groups: B model group, C positive drug control group, D psoralen low dose group, E Psoralen
Rouge element middle dose group, F psoralen high dose group, while Normal group is A group, gives basal feed, treatment cycle 4
Week.Each group is by 2 dosage of table oral (stomach-filling) administration, 1 time a day, continuous surrounding；
2.2 Testing index and method: rat takes blood (to take fasting before blood after high lipid food is fed 1 month, in eye socket
16h), solidification is stood, centrifugation separates serum, measures total cholesterol (TC), triglycerides (TG), low-density lipoprotein in serum
White cholesterol (LDL-C), high-density lipoprotein cholesterol (HDL-C), the data obtained carry out statistical procedures.Modeling is successfully big
After mouse is treated 1 month, abdominal aortic blood (taking fasting 16h before blood) after anesthesia, automatic clinical chemistry analyzer measures four items of blood lipid tests:
Total cholesterol (TC), triglycerides (TG), low density lipoprotein cholesterol (LDL-C), high-density lipoprotein cholesterol (HDL-
C)；
2.3 data processings: four items of blood lipid tests data are indicated with means standard deviation；Comparison among groups are carried out with SPSS20.0, are adopted
With one-way analysis of variance (ANOVA): first carrying out each group totally relatively, determine between each group if without significance,statistical meaning
Difference on no statistical significance；Otherwise the many-one continued between administration group and control group compares, and is examined according to homogeneity of variance
It tests as a result, variance uses LSD method together, heterogeneity of variance uses Tamhane ' sT2 method；Statistical check significance level is 0.05；
3 results:
3.1 general status: weight is apparently higher than blank control group, the state of mind behind rat 1 month of high lipid food nursing
Well, it is quick on the draw, fur gloss, activity reduction, is shown no obvious abnormalities in administration process；
3.2 modeling results: it is shown in Table 1:
Influence of 1 high lipid food of table to rat fat
Seen from table 1: total cholesterol (TC) in the serum of control rats high in fat, sweet after high lipid food is fed 1 month
Oily three esters (TG), the more general food group of low density lipoprotein cholesterol (LDL-C) significantly increase (P < 0.01), high-density lipoprotein
The more general food group of cholesterol (HDL-C) is substantially reduced (P < 0.01), high blood lipid model modeling success.
Influence of 3.3 psoralens to hyperlipidemia rats four items of blood lipid tests:
Compared with Normal group, total cholesterol (TC), the triglycerides (TG), low density lipoprotein cholesterol of model group
(LDL-C) significant to increase, statistically significant (P < 0.01), high-density lipoprotein cholesterol (HDL-C) is remarkably decreased, has
Statistical significance (P < 0.01)；Compared with model group, positive control simvastatin piece group total cholesterol (TC), glycerol after treatment
Three esters (TG), low density lipoprotein cholesterol (LDL-C) significantly reduce (P < 0.01), high-density lipoprotein cholesterol (HDL-C)
It is significant to increase (P < 0.01)；Psoralen low dose group total cholesterol (TC), triglycerides (TG), low-density lipoprotein gallbladder are solid
Alcohol (LDL-C) is substantially reduced (P < 0.05), high-density lipoprotein cholesterol (HDL-C) apparent increase (P < 0.05)；Psoralea corylifolia
The middle and high dosage group total cholesterol (TC) of element, triglycerides (TG), low density lipoprotein cholesterol (LDL-C) significantly reduce (P <
0.01), high-density lipoprotein cholesterol (HDL-C) significantly increases (P < 0.01), and acts on the reduction of triglycerides (TG) bright
It is aobvious to be shown in Table 2 better than positive control simvastatin piece group (P < 0.05):
2 psoralen of table to rat fat influence (N=10)
Note: compared with Normal group#P < 0.05,##P < 0.01；The * P < 0.05 compared with model group, * * P < 0.01；
Compared with positive controls▲P < 0.05.
4 discuss:
The hypolipidemic activity of psoralen is evaluated using the method being administered after first modeling, the more preferable simulation clinic of energy is answered
With.Originally the experimental results showed that, after high lipid food is fed 1 month, rat fat four are obviously increased, and are given psoralen and controlled
The rat for the treatment of, metabolism disorder of blood lipid have obtained good improvement, show that psoralen has the work of good prevention hyperlipidemia
With it is horizontal to reduce related blood lipids index, finally improves hyperlipidemic conditions.This is mentioned for this medicine of hyperlipidemia clinical treatment early application
For strong experimental evidence.And it may indicate that psoralen all has obviously hyperlipemia rat TG, TC from its action character
Ground reduction acts on, its effect for reducing TC and simvastatin piece have no notable difference, and its effect for reducing TG under Isodose
It is substantially better than simvastatin piece.Show that psoralen can make the total cholesterol (TC) of hyperlipidemia rats, triglycerides (TG), low
Density lipoprotein-cholesterol (LDL-C) reduces, and high-density lipoprotein cholesterol (HDL-C) increases, and has while reducing high in fat
The effect of mass formed by blood stasis Rat Cholesterol and triglycerides.
Claims (1)
1. a kind of purposes of psoralen as sole active agent in preparation treatment hyperlipidemia.
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| CN106234714A (en) * | 2016-09-09 | 2016-12-21 | 安徽省怡果生态科技有限公司 | A kind of concocting method of Fructus Fici leaf tea |
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| CN106234714A (en) * | 2016-09-09 | 2016-12-21 | 安徽省怡果生态科技有限公司 | A kind of concocting method of Fructus Fici leaf tea |
Non-Patent Citations (2)
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| 水迷宫法测定补骨脂素对去卵巢痴呆大鼠行为学的影响;潘永梅等;《深圳中西医结合杂志》;20161031;第26卷(第20期);第8-10页，尤其是第10页左栏第2段 |
| 荷丹片治疗高脂血症的临床疗效;魏家军;《天津药学》;20161231;第28卷(第3期);第41，78页，尤其是第78页右栏第1-2段 |
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Effective date of registration: 20190808 Address after: 830049 No. 776 Yan'an Road, Urumqi City, Xinjiang Uygur Autonomous Region Patentee after: Xinjiang Uygur Autonomous Region Uighur Medical Research Institute Address before: 830049 No. 776 Yan'an Road, Urumqi City, Xinjiang Uygur Autonomous Region Co-patentee before: Slain Aibai Patentee before: Xinjiang Uygur Autonomous Region Uighur Medical Research Institute Co-patentee before: Li Zhijian |