CN110279690A - Purposes of the wedelolactone as slimming medicine - Google Patents
Purposes of the wedelolactone as slimming medicine Download PDFInfo
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- CN110279690A CN110279690A CN201910710411.2A CN201910710411A CN110279690A CN 110279690 A CN110279690 A CN 110279690A CN 201910710411 A CN201910710411 A CN 201910710411A CN 110279690 A CN110279690 A CN 110279690A
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- A—HUMAN NECESSITIES
- 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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P3/04—Anorexiants; Antiobesity agents
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Abstract
The present invention provides a kind of purposes of wedelolactone as slimming medicine.The experimental evidence of wedelolactone weight-reducing is provided.The wedelolactone is a kind of compound monomer.The weight-reducing includes to weight gain caused by diet or other reasons, the increase of yellow fat volume, fat inhibition or improvement result.The drug can be oral medicine.The present invention proves that wedelolactone has the function of significantly reducing body fat content, losing weight by pharmacological experiment study, can be used for obesity caused by many reasons and overweight prevention and treatment.
Description
Technical field
The present invention relates to the new applications of wedelolactone more particularly to a kind of wedelolactone as slimming medicine, subtracts body
The purposes of rouge content drug.
Background technique
According to World Health Organization's data announced in 2008, the whole world has 1,400,000,000 people overweight, wherein 5,000 ten thousand is fat.It is overweight
Still increasing with obese people ratio, it is estimated that, to the year two thousand thirty, global obese people is up to 1,000,000,000.
Obesity is the inducement of many diseases, such as type-2 diabetes mellitus, cardiovascular disease, hypertension and nonalcoholic fatty liver
Deng, these diseases not only reduce patients ' life quality, also shortening patient's service life.
Wedelolactone is eclipta (Eclipta prostrata L.), golden small cup wedelia chinensis (Wedelia
A kind of natural lactone compound present in plants such as calendulacea) has various pharmacological actions, as liver protection,
Anti- snake venom, anti-immunity inhibition, anti-inflammatory etc..
We have done years of work to the improvement result of metabolic disease and cardiovascular disease around wedelolactone, find it
Pharmacological action with improvement blood lipid, inhibition vascular remodeling, and publish an article [PLoS ONE (2015), 10 (7): e0132720；
Experimental Gerontology(2017),96:73–81]。
That is, prior art discloses the improvement blood lipid of wedelolactone, inhibit vascular remodeling effect, antiobesity action and these
Effect is different, and concrete reason is as follows:
1. it is different from obesity is improved to improve blood lipid
(1) positive connection is not present in blood fat disorder and obesity.The two is all metabolic disease, and there are certain correlations, for example,
Poor eating habits are one of blood fat disorder and fat common causes.But it in different individuals, due to self-characteristic or and deposits
Other inducements, can develop as various disease, the generation of two kinds of diseases does not have positive connection simultaneously.Data show, some blood
Rouge disorder patient has no obesity, has 30% not have blood fat disorder [J Clin Endocrinol Metab in obese patient
(2005), 90 (7): 4145-50], the people of Normal-weight but also have blood fat disorder patient [Diabetes (1998) 47 (5): 699-
713]。
(2) blood fat disorder and obesity are clinically two kinds of independent diseases or symptom, and evaluation index is different, therapeutic agent
Also different.The evaluation index of blood fat disorder is that Blood Cholesterol, triglycerides, low-density lipoprotein increase, and high density rouge
Albumen reduces；And fat evaluation index is body fat tissue content and weight and height ratio.The clinical of blood fat disorder is used
Medicine mainly has statins, fibrate, niacin etc.；And fat clinical application has orlistat, Liraglutide, green card
Color woods, Phentermine/Topiramate, naltrexone/Bupropion etc..
(3) drug for treating blood fat disorder may not be able to improve obesity.For example, statins have significant tune rouge to make
With being a line lipid-regulation medicine of clinical use.But some clinical trials are shown, statins use 1 year, on weight without influence
[Surg Obes Relat Dis(2017),13(4):674-80]；Even some clinical trials are shown, can be led using Statins
Cause fat fat [JAMA Intern Med (2014), 174 (7): 1038-45].
2. inhibiting vascular remodeling different from obesity is improved
Vascular remodeling differs greatly with fat.The wedelolactone that we deliver improves vascular remodeling effect and refers to the medicine
Object improves interventional therapy or intravascular stent operation causes vascular remodeling, luminal stenosis caused by the subsequent hair of injury of blood vessel, improvement
Target organ is blood vessel.And improving obesity is to reduce fat volume, lose weight, improved position is adipose tissue.
Summary of the invention
A kind of new application the purpose of the present invention is to provide wedelolactone as slimming medicine.
The wedelolactone is a kind of lactone compound monomer.
The weight-reducing include poor eating habits or inherent cause are drawn or other reasons caused by weight gain, fat
Inhibition or improvement result.
The weight-reducing includes reducing yellow adipose tissue to increase the intracorporal yellow fat content of type obese patient.
The drug reduces yellow fat volume by increasing energetic supersession.
The weight-reducing includes acting on overweight or obese patient's weight and body fat reduction.
The drug can be oral medicine.
The present invention proves that wedelolactone has apparent antiobesity action, and this effect is led by pharmacological experiment study
If can be used for overweight, fat and body fat caused by many reasons by reducing body fat content and increasing what fatty brownification was realized
The prevention and treatment of too high levels.Therefore the present invention is by reducing that fat volume, losing weight improves obesity, improved specific position
Setting is yellow adipose tissue.
Detailed description of the invention
Fig. 1 is influence diagram of the wedelolactone to mouse weight；
Wherein, the weight consecutive variations that (A) is 10 weeks after administration.It (B-C) is the 5th week (B) and the system of the 10th week (C) weight
Meter figure；## and ### expression obese model group (HFD) is compared with control group (NCD), p < 0.01 and p < 0.001；* and * * * table
Show administration group (WDL5, WDL10 and WDL20) compared with obese model group (HFD), p < 0.01 and p < 0.001；
Fig. 2 is influence diagram of the wedelolactone to mouse body fat；
Wherein, (A) is the statistical chart of each group body fat content, mouse systemic fat weight that body fat content measure with MRI and
The ratio calculation of weight；It (B) is the organization chart of subcutaneous yellow fat and groin yellow fat；(C) it is cut for adipose tissue paraffin
The representative figure (* 400) of piece HE dyeing；(D) it is the statistical chart of fat cell volume, calculates cell area using ImageJ software,
According to formula v=4/3 π r3Calculate cell volume；# and ### indicates obese model group (HFD) p < compared with control group (NCD)
0.05 and p < 0.001；*, * * and * * * expression administration group (WDL5, WDL10 and WDL20) is compared with obese model group (HFD), p
< 0.05, p < 0.01 and p < 0.001；
Fig. 3 is influence diagram of the wedelolactone to energetic supersession；
Wherein, (A) is the energy consumption values of CLAMS systematic survey；It (B) is the statistics to day and night energy consumption
Figure；It (C) is autonomic activities amount statistical chart；It (D) is food ration statistical chart；* * indicates WDL administration group (5mg/kg) and obese model
Group (HFD) is compared, p < 0.001；
Fig. 4 is influence diagram of the wedelolactone to fat drips quantity in the fat cell of in vitro culture；
Wherein, preceding lipocyte (preadipocyte), mature fat cell (control) and each dosage of WDL treat cell
The representative figure (left side) of HE dyeing and statistical chart (right side).### indicates mature fat cell (control) and preceding lipocyte
(preadipocyte) it compares, p < 0.001；* and * * * indicate each treatment group of WDL compared with mature fat cell control group,
P < 0.01 and p < 0.001.
Specific embodiment
Embodiment 1
Wedelolactone is to overweight and fat improvement result.
The present invention uses the mouse obesity model of high fat diet induction, observes wedelolactone to obese mouse weight and body
The influence of rouge.
Steps are as follows for pharmacodynamic experiment specific method provided by the invention:
1) experimental animal and reagent
C57BL/6 mouse 60, male 4-6 weeks, is purchased from Xiamen University's Experimental Animal Center.
Wedelolactone is purchased from Shanghai Yuan Ye Biotechnology Co., Ltd.
2) animal processing method
Mouse feeding environment: 23 ± 1 DEG C of temperature, humidity: 40%-60%, natural lighting, free water, ad lib.It is suitable
After answering 1 week, 5 groups are randomly divided into, every group 12, is denoted as control group (NCD), obese model group (HFD), wedelolactone respectively
5mg/kg group (being denoted as WDL5), wedelolactone 10mg/kg group (being denoted as WDL10), wedelolactone 20mg/kg group (are denoted as
WDL20)。
Control group fed chow diet, other groups feed high lipid food.High fat diet gives solvent or drug after 4 weeks.
It is administered by the following method:
Control group and obese model group: physiological saline is given in stomach-filling when afternoon 17 daily.
WDL5 group: gastric infusion is primary when afternoon 17 daily, dosage 5mg/kg.
WDL10 group: gastric infusion is primary when afternoon 17 daily, dosage 10mg/kg.
WDL20 group: gastric infusion is primary when afternoon 17 daily, dosage 20mg/kg.
Successive administration 10 weeks according to the method described above measure weekly weight, record food ration.CLAMS system is used after stomach-filling 1 week
Measure energy consumption, autonomic activities and food-intake.After 10 weeks, MRI measures mouse adipose weight, the ratio calculation body fat with weight
Content；All animal physiological salt water perfusions when materials take subcutaneous and groin adipose tissue, take pictures and observe subcutaneous fat and abdomen stock
Ditch fat size；HE dyeing observation fat cell size after adipose tissue paraffin section.
Statistical analysis: 5 software of Graphpad Prism (GraphPad Software Inc, USA) is used with data
Statistical analysis is carried out, comparison among groups one-way analysis of variance is further examined with t when variance analysis difference has conspicuousness
It tests and compares two-by-two.
3) result and analysis
3.1) influence of the wedelolactone to weight, as a result as shown in Figure 1.Should the result shows that:
1. high fat diet increases C57BL/6 mouse weight, illustrate modeling success.
2. the wedelolactone treatment group of three dosage is compared with obese model group, weight gradually decreases after administration, arrives
Significant difference is all had at the 5th week, and maintains significant difference during administration hereafter.Illustrate wedelolactone for
Weight gain caused by high fat diet has significant inhibiting effect.
3.2) influence of the wedelolactone to body fat, as a result as shown in Figure 2.Should the result shows that:
1. obese model group mouse is compared with normal diet controls group mouse, body fat content is obviously increased, subcutaneous fat and
Groin fat significantly increases, and the volume of fat cell also obviously becomes larger.
2. wedelolactone treatment group, compared with obese model group, the equal conspicuousness of body fat content reduces, subcutaneous yellow fat
It is obviously reduced with groin yellow fat, the volume of yellow fat cell also obviously becomes smaller.The results show, in wedelia chinensis
Ester can be substantially reduced body fat content and fat volume.
3.3) influence of the wedelolactone to energetic supersession, as a result as shown in Figure 3.Should the result shows that:
Compared with obese model group, energy consumption is dramatically increased for wedelolactone 5mg/kg treatment group, and day and night
Energy consumption increase, but on autonomic activities amount and food-intake without influence.The results show, wedelolactone mainly pass through
Increase energy consumption and reduce fat volume, lose weight, the autonomic activities and feed aspect be affected on weight are without influence.
Embodiment 2
Improvement result of the wedelolactone to fat drips in cuituring adipocytes in vitro.
The present invention uses 3T3 PECTORAL LIMB SKELETON, and adding the stimulation such as insulin, it is divided into mature fat cell, is then added not
With concentration wedelolactone, influence of the drug to fat drips quantity in fat cell is observed.
Steps are as follows for pharmacodynamic experiment specific method provided by the invention:
1) 3T3 cell culture:
3T3 cell is cultivated with complete medium (10%FBS+89%DMEM+1% is dual anti-).Cell reaches 70%-80% and melts
By cell inoculation to six orifice plates when right, fresh complete medium being replaced after cell covers with and continues to cultivate, cell contact is allowed to press down
System 2 days.Then with induced medium (in complete medium contain 10ug/ml Insulin, 0.5mM IBMX, 1 μM of Dex) and
Maturation medium (containing 10ug/ml Insulin in complete medium) is cultivated 2 days respectively, and cell induction is thin for mature fat
Born of the same parents.
2) cell experiment step:
The fat cell of induced maturation, be divided into tri- dosage groups of control group (control) and WDL (respectively be incubated for 0.2 μM,
0.5 μM and 1.0 μM of WDL, is accordingly denoted as WDL0.2, WDL0.5 and WDL1.0).Cell, oil red O stain are fixed after being incubated for six days
It shows fat drips, takes pictures under microscope.Then n-butanol impregnates the oil red O in dissolution cell, and microplate reader measures absorbance OD value, fixed
Amount compares the difference of fat drips quantity between group of cells.
3) result and analysis:
Influence of the wedelolactone to fat drips quantity in fat cell, as a result as shown in Figure 4.Should the result shows that:
1. 3T3 PECTORAL LIMB SKELETON, after the induced maturations such as insulin, fat drips quantity obviously increases, illustrate to induce successfully.
2. wedelolactone treatment group compared with mature fat cell control group, fat drips quantity reduce, WDL 0.2 μM,
It can significantly reduce fat drips quantity at 0.5 μM and 1.0 μM.
Particular embodiments described above, pair present invention solves the technical problem that, technical scheme and beneficial effects carry out
It is further described, it should be understood that the above is only a specific embodiment of the present invention, is not limited to this
Invention, all within the spirits and principles of the present invention, any modification, equivalent substitution, improvement and etc. done should be included in this hair
Within bright protection scope.
Claims (5)
1. purposes of the wedelolactone as slimming medicine.
2. purposes as described in claim 1, it is characterised in that: the weight-reducing includes drawing to poor eating habits or inherent cause
Weight gain, fat inhibition or the improvement result risen.
3. purposes as described in claim 1, it is characterised in that: the weight-reducing includes reducing yellow adipose tissue to increase type obesity
The yellow fat content of patient's body.
4. purposes as claimed in claim 3, it is characterised in that: the drug reduces yellow fat by increasing energetic supersession
Volume.
5. purposes as described in claim 1, it is characterised in that: the drug is oral medicine.
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| CN201910710411.2A CN110279690A (en) | 2019-08-02 | 2019-08-02 | Purposes of the wedelolactone as slimming medicine |
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| CN201910710411.2A CN110279690A (en) | 2019-08-02 | 2019-08-02 | Purposes of the wedelolactone as slimming medicine |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN114224882A (en) * | 2021-12-22 | 2022-03-25 | 天津中医药大学 | Application of wedelolactone in preparation of medicine for activating NK cells |
| CN116672338A (en) * | 2023-07-19 | 2023-09-01 | 中国医学科学院皮肤病医院(中国医学科学院皮肤病研究所) | Application of wedelolactone in preparation of medicines for treating systemic lupus erythematosus |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105832721A (en) * | 2015-02-03 | 2016-08-10 | 稳达生技股份有限公司 | Method for treating hypertriglyceridemia with a Wedelia chinensis extract |
| CN109820848A (en) * | 2019-04-04 | 2019-05-31 | 南通大学附属医院 | The new application of wedelolactone |
-
2019
- 2019-08-02 CN CN201910710411.2A patent/CN110279690A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105832721A (en) * | 2015-02-03 | 2016-08-10 | 稳达生技股份有限公司 | Method for treating hypertriglyceridemia with a Wedelia chinensis extract |
| CN109820848A (en) * | 2019-04-04 | 2019-05-31 | 南通大学附属医院 | The new application of wedelolactone |
Non-Patent Citations (2)
| Title |
|---|
| SEYOUNG LIM ET AL.: "Wedelolactone Inhibits Adipogenesis Through the ERK Pathway in Human Adipose Tissue-Derived Mesenchymal Stem Cells", 《JOURNAL OF CELLULAR BIOCHEMISTRY》 * |
| 何昌善等: "《临症用药纲目》", 31 August 2017, 中国医药科技出版社 * |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN114224882A (en) * | 2021-12-22 | 2022-03-25 | 天津中医药大学 | Application of wedelolactone in preparation of medicine for activating NK cells |
| CN116672338A (en) * | 2023-07-19 | 2023-09-01 | 中国医学科学院皮肤病医院(中国医学科学院皮肤病研究所) | Application of wedelolactone in preparation of medicines for treating systemic lupus erythematosus |
| CN116672338B (en) * | 2023-07-19 | 2023-12-19 | 中国医学科学院皮肤病医院(中国医学科学院皮肤病研究所) | Application of wedelolactone in preparation of medicines for treating systemic lupus erythematosus |
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Application publication date: 20190927 |