CN106236815A - Resina garciniae extract application in preventing and treating diabetes - Google Patents
Resina garciniae extract application in preventing and treating diabetes Download PDFInfo
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- CN106236815A CN106236815A CN201610628680.0A CN201610628680A CN106236815A CN 106236815 A CN106236815 A CN 106236815A CN 201610628680 A CN201610628680 A CN 201610628680A CN 106236815 A CN106236815 A CN 106236815A
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- resina garciniae
- diabetes
- garciniae extract
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- medicine
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- 238000002360 preparation method Methods 0.000 claims description 12
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- MZOFCQQQCNRIBI-VMXHOPILSA-N (3s)-4-[[(2s)-1-[[(2s)-1-[[(1s)-1-carboxy-2-hydroxyethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-[[2-[[(2s)-2,6-diaminohexanoyl]amino]acetyl]amino]-4-oxobutanoic acid Chemical compound OC[C@@H](C(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(O)=O)NC(=O)CNC(=O)[C@@H](N)CCCCN MZOFCQQQCNRIBI-VMXHOPILSA-N 0.000 claims description 8
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/38—Clusiaceae, Hypericaceae or Guttiferae (Hypericum or Mangosteen family), e.g. common St. Johnswort
-
- 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
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
- A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs
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- Health & Medical Sciences (AREA)
- Natural Medicines & Medicinal Plants (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Mycology (AREA)
- Microbiology (AREA)
- Medical Informatics (AREA)
- Botany (AREA)
- Biotechnology (AREA)
- Alternative & Traditional Medicine (AREA)
- Medicines Containing Plant Substances (AREA)
Abstract
The present invention relates to pharmaceutical engineering field, specifically disclose Resina garciniae extract application in preparing the medicine and/or food preventing and treating diabetes.The present invention also provides for Resina garciniae extract application in the medicine preparing body inflammatory factor TNF α and IL 6 process LAN that suppression causes because of overnutrition.Present invention firstly discovers that Resina garciniae extract has effect for the treatment of diabetes, new medicament screen and clinical treatment for preventing and treating secondary diabetes provide theoretical foundation and target, provide solid foundation for diabetes mellitus prevention measure and Therapeutic Method optimization.
Description
Technical field
The present invention relates to pharmaceutical engineering field, specifically, relate to Resina garciniae extract application in preventing and treating diabetes.
Background technology
Diabetes are one of principal diseases that harm modern is healthy, and diabetes are in China's adult male and the morbidity of women
Rate is 11% and 10.5% respectively, the current diabetics of China more than 100,000,000, the most also 1.39 hundred million belong to diabetes " after
Standby army ".China has replaced India, becomes whole world diabetes the first big country.Disclosing according to World Health Organization (WHO), global every 10 seconds just
Having 1 people to die from diabetes, within every 30 seconds, just have 1 people because of complication such as diabetes amputation, the most blind, cardiovascular and cerebrovascular vessel, diabetes are
Become serious public health problem.And along with the aggravation of whole world aging trend, the trend in cumulative year after year.It is currently used for
The means for the treatment of diabetes include insulin treatment and Drug therapy, and the kind of its Chinese medicine mainly includes sulfonylurea drugs, double
Guanidine antidiabetic drug, alpha-glucosidase inhibitor, euglycemic agent, Insulin secretagogues etc..In order to preferably resist disease
Disease, medical circle attempts all the time to develop and new has blood sugar reducing function and the medicine for the treatment of diabetes effect and treatment means.
Summary of the invention
In order to solve problems of the prior art, it is an object of the invention to provide a kind of therapeutic effect definite, control
Treat the Remedies for diabetes of low cost.
In order to realize the object of the invention, technical scheme is as follows:
First aspect, the invention provides Resina garciniae extract application in preparation preventing and treating diabetes medicament and/or food,
Medicine and/or the food of diabetes is prevented and treated using Resina garciniae extract as active component preparation.
Further, described application is using Resina garciniae extract as the medicine of sole active agent preparation treatment diabetes.
As preferably, it is particularly suitable for treating type ii diabetes.
Present invention also offers Resina garciniae extract at preparation suppression body inflammatory factor TNF-α and the medicine of IL-6 process LAN
In application.
Further, described body inflammatory factor TNF-α and IL-6 process LAN are caused by overnutrition.
Further, described Resina garciniae extract at least includes that the compound A shown in structure formula I (also can claim Resina garciniae to carry
Take thing A) and/or structure formula II shown in compound B (also can claim Resina garciniae extract B):
It should be noted that described Resina garciniae extract can be by conventional method such as alcohol extraction, the chromatography etc. of this area from Resina garciniae
(Garcinia morella Desv) etc. extract and obtains.
Described compound A and compound B can be bought by commercial sources or utilize marketable material, by prior art
(described extracting method can be found in the Chinese patent Shen of Publication No. CN105213366A in traditional compou nd synthesis method synthesis
Please).Can be further purified by modes such as column chromatography, high performance liquid chromatography or crystallizations after synthesis.
The present invention still further provides the compound A shown in structure formula I and the compound B shown in structure formula II and exists
Application in preparation preventing and treating type ii diabetes medicine and/or food.
As preferably, described medicine is oral formulations.The present invention finds through test, by described Resina garciniae extract or structural formula
(I) mice that medicine per os gavage prepared by the compound A shown in or the compound B shown in structure formula II suffers from diabetes, tool
There is obvious therapeutic effect.
The present invention also provides for a kind of pharmaceutical composition for treating diabetes, and its effective ingredient is Resina garciniae extract.
As preferably, its effective ingredient is Resina garciniae extract A (i.e. aforesaid compound A).
When described pharmaceutical composition uses, the single dose unit of Resina garciniae extract A is: 0.1-300mg/kg body weight, excellent
Select 0.5-100mg/kg body weight, more preferably 5-20mg/kg body weight.
The dosage form of described pharmaceutical composition includes tablet, sugar coated tablet, film coated tablet, enteric coated tablet, capsule, hard
Capsule, soft capsule, oral liquid, suck agent, granule, electuary, pill, powder, unguentum, sublimed preparation, suspensoid, powder, molten
Liquor, injection, suppository, ointment, plaster, cream, spray, drop, patch；Preferred oral dosage form, such as capsule, sheet
Agent, oral liquid, granule, pill, powder, sublimed preparation, unguentum etc..Described peroral dosage form can be containing conventional excipient, such as bonding
Agent, filler, diluent, tablet agent, lubricant, disintegrating agent, coloring agent, flavoring agent and wetting agent etc., if desired can be to tablet
It is coated.
The filler being suitable for includes the filler that cellulose, mannitol, lactose are similar with other；The disintegrating agent bag being suitable for
Include starch, polyvinylpyrrolidone and starch derivatives etc., such as sodium starch glycollate；The lubricant being suitable for includes magnesium stearate
Deng.The wetting agent being suitable for includes sodium lauryl sulphate etc..
The pharmaceutical composition that the present invention provides can significantly decrease the blood glucose caused because of high fat diet and raise, suppress because of
Insulin resistant that obesity causes and hyperglycemia.
As preferably, Resina garciniae extract A is dissolved in edible oil (such as Semen Maydis oil) and makes oral formulations.Per os gavage
Suffer from the mice of diabetes, there is obvious therapeutic effect.
Present invention firstly discovers that Resina garciniae extract and Resina garciniae extract A and B therein have effect for the treatment of diabetes, for
New medicament screen and the clinical treatment of preventing and treating secondary diabetes provide theoretical foundation and target, for diabetes mellitus prevention measure and treatment
Method optimization provides solid foundation.
Accompanying drawing explanation
Fig. 1 is the inhibitory action knot of the mice obesity that in the embodiment of the present invention 1, high fat material is induced by Resina garciniae extract A, B
Really.
Fig. 2 is the result that in the embodiment of the present invention 1, mouse glucose tolerance is tested by Resina garciniae extract A, B.
Fig. 3 is Resina garciniae extract A, B result to mouse islets element tolerance test in the embodiment of the present invention 1.
Fig. 4 is macrophage TNF-α and the IL-6 of Resina garciniae extract A, B suppression Palmic acid induction in the embodiment of the present invention 2
Expression of results.
Detailed description of the invention
Following example are used for illustrating the present invention, but are not limited to the scope of the present invention.If not specializing, embodiment
In the conventional means that is well known to those skilled in the art of technological means used, raw materials used be commercial goods.
The foundation of embodiment 1 diabetes mice model and the process of Resina garciniae extract
Male C57BL/6 mice is randomly divided into 6 groups, often group 8.First group feeds normal diet (normal diet is purchased from
Jun Ke institute, allows mice free choice feeding every day)；Second group feeds high lipid food+Semen Maydis oil (each mice gives 0.1mL Semen Maydis every day
Oil) matched group；3rd group feeds high lipid food+Resina garciniae extract A (5mg/Kg body weight/day)；4th group feeds high lipid food+rattan
Yellow extract A (20mg/Kg body weight/day), the 5th group feeds high lipid food+Resina garciniae extract B (5mg/Kg body weight/day)；6th
Group feeds high lipid food+Resina garciniae extract B (20mg/Kg body weight/day), allows mice free choice feeding every day, every every balance of mice
The most always take food 1.70-2.00g.Wherein, the 3rd-six group is that Resina garciniae extract A or B is dissolved in Semen Maydis oil, takes 0.1mL every day beautiful
Miyou feeds mice.
Process 14 weeks, measure weekly each group of Mouse Weight and fasting glucose, and mice is carried out glucose-tolerant and islets of langerhans
Element resistance test.Result is the most as Figure 1-3.
Glucose tolerance detects: mice overnight fasting, and next day is to 20% glucose of mouse peritoneal injection 2g/Kg body weight
(Sigma company).Before injectable dextrose monohydrate, mouse tail vein takes blood 10 μ L, respectively at 15 minutes after to glucose, and 30 minutes,
60 minutes, 120 minutes each tail venous blood sampling 10 μ L, with the change of commercially available Roche blood glucose meter (ACCU-CHEK) detection blood glucose.
Insulin tolerance detects: mice fasting 5 hours, to the recombinant human insulin of mouse peritoneal injection 0.75U/Kg body weight
(Eli Lilly drugmaker).Before insulin injection, mouse tail vein takes blood 10 μ L, respectively at 15 points after to insulin
Clock, 30 minutes, 60 minutes, 120 minutes each tail venous blood sampling 10 μ L, with commercially available Roche blood glucose meter (ACCU-CHEK) detection blood
The change of sugar.
Fig. 1 shows, the mice obesity that high fat material is induced by Resina garciniae extract A and B is inhibited.Resina garciniae extract A
With B process group can dose-dependent suppression high fat material induction obesity, high dose process group (20mg/Kg/ days) significantly presses down
Make the obesity (p < 0.05) of high fat material induction.
Fig. 2 is the result that mouse glucose tolerance is tested by Resina garciniae extract A and B.Resistance at the glucose that mice is carried out
In being tested, wherein Resina garciniae extract A process group can significantly reduce the content (P < 0.05) of glucose in blood at 30 and 60 minutes.
Fig. 3 is Resina garciniae extract A and the B result to mouse islets element tolerance test.Resistance at the insulin that mice is carried out
In being tested, Resina garciniae extract A process group can significantly reduce the content (P < 0.05) of glucose in blood at 30 and 60 minutes.
Embodiment 2 Resina garciniae extract processes the experiment in vitro of the macrophage of Palmic acid induction
Utilize macrophage system Raw264.7 (RAW 264.7 purchased from American Type Culture Collection,
The ATCC U.S.) carry out following experiment: being randomly divided into eight groups, first group is culture medium negative control；Second group with the palm fibre of 100 μMs
Palmitic acid acid (Sigma company) matched group；3rd group is 1ng/mL LPS (Sigma company) matched group；4th group with the Petiolus Trachycarpi of 100 μMs
Acid and 1ng/mL LPS Combined Treatment matched group, simulate body fat fibrosis models.Five to eight group is guidance model (Palmic acid
100uM+LPS 1ng/mL) add Resina garciniae extract process group.The Resina garciniae extract A of the 5th group 25 μMs；The 6th group of rattan adding 50 μMs
Yellow extract A.The 7th group of Resina garciniae extract B adding 25 μMs；The 8th group of Resina garciniae extract B adding 50 μMs.Receive after processing 24 hours
Collection culture medium, utilizes the secreting, expressing change of ELISA kit each group of cellular inflammation factor TNF-α of detection and IL-6.Result is such as
Shown in Fig. 4, it is RPM1640 (Sigma company) for cultivating the culture medium of macrophage.From fig. 4, it can be seen that Resina garciniae extract
A and B can dose dependent significantly inhibit the inflammatory factor TNF-α and the expression of IL-6 caused because of overnutrition.Therefore,
Resina garciniae extract A and B of high concentration can be applied and be used for, in preparation, the body inflammatory factor TNF-α that suppression causes because of overnutrition
With (* P < 0.05, * * P < 0.01) in the medicine of IL-6 process LAN.
Although, the present invention is described in detail the most with a general description of the specific embodiments, but
On the basis of the present invention, can make some modifications or improvements it, this will be apparent to those skilled in the art.Cause
This, these modifications or improvements without departing from theon the basis of the spirit of the present invention, belong to the scope of protection of present invention.
Claims (10)
1. Resina garciniae extract application in the medicine and/or food of preparation preventing and treating type ii diabetes.
2. Resina garciniae extract application in the medicine of preparation suppression body inflammatory factor TNF-α and IL-6 process LAN.
Application the most according to claim 2, it is characterised in that the body inflammatory factor caused because of overnutrition for suppression
Application in the medicine of TNF-α and IL-6 process LAN.
4. according to the application described in any one of claims 1 to 3, it is characterised in that described Resina garciniae extract at least includes structure
Compound A shown in formula I and/or the compound B shown in structure formula II:
5. the application in preparation preventing and treating type ii diabetes medicine and/or food of the compound A shown in structure formula I.
6. the application in preparation preventing and treating type ii diabetes medicine and/or food of the compound B shown in structure formula II.
7. for preventing and treating the pharmaceutical composition of diabetes, it is characterised in that its effective ingredient is Resina garciniae extract.
Pharmaceutical composition the most according to claim 7, it is characterised in that the dosage form of described pharmaceutical composition include powder,
Tablet, granule, capsule, suspensoid, Emulsion, effervescent tablet or injection.
Pharmaceutical composition the most according to claim 8, it is characterised in that it is to be dissolved in edible oil by Resina garciniae extract
The oral formulations made.
Pharmaceutical composition the most according to claim 9, it is characterised in that described edible oil includes Semen Maydis oil.
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