CN104224798B - The application of aborane type triterpenoid compound antimetabolic syndrome and prepared medicine - Google Patents
The application of aborane type triterpenoid compound antimetabolic syndrome and prepared medicine Download PDFInfo
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- CN104224798B CN104224798B CN201410341055.9A CN201410341055A CN104224798B CN 104224798 B CN104224798 B CN 104224798B CN 201410341055 A CN201410341055 A CN 201410341055A CN 104224798 B CN104224798 B CN 104224798B
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Abstract
The invention discloses application and prepared medicine, the especially aborane type triterpenoid compound application in terms of blood fat reducing, blood sugar lowering of aborane type triterpenoid compound antimetabolic syndrome.Described aborane type triterpenoid compound has the rising of the triglyceride levels of suppression olive oil load mice significantly, and in suppression hepatocyte, the accumulation of triglyceride, therefore can be applicable to the preparation of fat-reducing medicament.Described aborane type triterpenoid compound can be made into pharmaceutically acceptable any preparation.The present invention has opened up the new medical application of aborane type triterpenoid compound, has the advantages that pharmacological action is strong, safety is high, provides a kind of new effective, safe drugs for vast cardiovascular patient and selects.
Description
Technical field
The invention belongs to biomedicine technical field, relate to the antimetabolic syndrome application of a kind of compound, be specifically related to the application of aborane type triterpenoid compound antimetabolic syndrome and prepared medicine.
Background technology
Raising and living-pattern preservation along with people's living standard, because the disease of the serious threat human health caused by unsound life style and environmental factors and life is increasingly severe, these diseases are referred to as " diseases due to habit disturbance ", mainly include hypertension, hyperlipidemia, disease and the obesity etc. such as hyperglycemia.Change along with people's dietary structure, the increase that animal food is taken in, suffer from hyperlipidemia and fat crowd increases year by year, and hyperlipemia is the risk factor of atherosclerosis and incidence of coronary heart disease, China dies from the number of cardiovascular and cerebrovascular disease every year more than 3,000,000, it has also become the big killer of the first of our people.The atherosclerotic topmost strategy of current preventing and treating is exactly blood fat reducing, current lipid lowerers mainly has Statins, fibrates, nicotinic acid class, resinae, cholesterol absorption inhibitor etc., but it is higher that these medicines exist price mostly, toxic and side effects is big, the shortcoming such as easy bounce-back after drug withdrawal.And natural plant amedica is widely distributed with it, toxic and side effects is little, cheap, especially has the advantages such as good efficacy to become the important sources of exploitation lipidemia medicine to various complication.
Triterpenoid compound is widely present in nature, and especially more in dicotyledon, free triterpene is primarily present in the plants such as Compositae, pulse family, Euphorbiaceae, Meliaceae, Celastraceae, Rubiaceae, Burseraceae and Labiatae.Triterpene compound structure complexity is various, the triterpenoid compound having now been found that, mostly is tetracyclic triterpene and pentacyclic triterpene, and minority is chain, monocycle, dicyclo, tricyclic triterpene compounds etc..Triterpenoid compound has diversified pharmacologically active, including antibacterial, antiinflammatory, antitumor, antiviral, antifertility, reduction cholesterol, resists myocardial ischemia, kills Mollusca etc..Having been reported that triterpene saponin has the effect reducing cholesterol, but be seldom found to reduce the triterpenoid compound of triglyceride, especially aborane type triterpenoid compound application in fat-reducing medicament have not been reported.
Summary of the invention
It is an object of the invention to provide the application of a kind of aborane type triterpenoid compound antimetabolic syndrome and prepared medicine.
The present invention is to be achieved through the following technical solutions:
The application in preparing antimetabolic syndrome medicine and/or health product of the aborane type triterpenoid compound, the chemical structural formula of described aborane type triterpenoid compound is as follows:
Wherein, R1For hydrogen atom, hydroxyl, methoxyl group or acetoxyl group；R2For hydrogen atom, hydroxyl, methoxyl group, acetoxyl group or carbonyl；R3For hydrogen atom, hydroxyl, methoxyl group or acetoxyl group.
Described antimetabolic syndrome medicine and/or health product are blood fat reducing and/or diabetes medicine and/or health product.
Described antimetabolic syndrome medicine is blood lipid-lowering medicine and/or health product.
Described blood lipid-lowering medicine and/or medicine that health product are triglyceride reducing and/or health product.
Described antimetabolic syndrome medicine is diabetes medicine and/or health product.
The described R in aborane type triterpenoid compound1For hydrogen atom, R2For carbonyl, R3For acetoxyl group.
The medicine of a kind of hypolipidemic, makes pharmaceutical dosage form by aborane type triterpenoid compound and pharmaceutic adjuvant；
The chemical structural formula of described aborane type triterpenoid compound is as follows:
Wherein, R1For hydrogen atom, hydroxyl, methoxyl group or acetoxyl group；R2For hydrogen atom, hydroxyl, methoxyl group, acetoxyl group or carbonyl；R3For hydrogen atom, hydroxyl, methoxyl group or acetoxyl group；
Described pharmaceutic adjuvant is slow releasing agent, polyvinylpyrrolidone or microcrystalline Cellulose；
Described dosage form is tablet, capsule or pill.
Described slow releasing agent is hydroxypropyl methylcellulose and/or lactose.
Described medicine is the medicine of triglyceride reducing.
Compared with prior art, the present invention has a following useful technique effect:
The invention discloses the application of aborane type triterpenoid compound anti-antimetabolic syndrome, especially aborane type triterpenoid compound application in terms of blood fat reducing, blood sugar lowering, the fat-reducing medicament prepared with aborane type triterpenoid compound has the advantages that pharmacologically active is strong, safety is high, toxic and side effects is little, and the fibrate simultaneously also overcoming the main triglyceride reducing applied clinically at present causes the side effect of hepatomegaly.The present invention has been the new application of developing of the class medicine of preparation prevention and treatment hyperlipidemia.
The present invention, by mice olive oil load test, demonstrates aborane type triterpenoid compound and can effectively suppress the rising of mice plasma triglyceride, and in dose-dependence, even more eager to excel in whatever one does than the effect of positive control drug orlistat.
The present invention, by testing the lipopexia of liver cancer tissue HepG2 cell, demonstrates most aborane type triterpenoid compound and has the effect of triglyceride accumulation in suppression hepatocyte, and some is even much better than than the activity of fibrate bezafibrate.
The experiment that glucose is taken in by the present invention by liver cancer tissue HepG2 cell, demonstrates aborane type triterpenoid compound and can remarkably promote the cell absorption to glucose when low dosage, and this illustrates that this compounds is likely to be of anti-diabetic activity.
The present invention uses mtt assay to carry out cellulotoxic experiment in human liver cancer cell HepG2 cell line, result display aborane type triterpenoid compound does not has any toxicity when drug level is 100 μMs, even can also increase hepatocellular vigor, by the experiment of cell in vitro poison, this explanation proves that this compounds is safe.
Accompanying drawing explanation
Fig. 1 is the compounds of this invention 13 Cyto toxic experiment showed figure；
What Fig. 2 was the compounds of this invention 13 on cellular uptake glucose affects result block diagram, and wherein, a is comparison medicine bezafibrate, and (b) is arbor alkyl-type triterpenoids 13.
Detailed description of the invention
Below in conjunction with specific embodiment, the present invention is described in further detail, and the explanation of the invention is not limited.
The aborane type triterpenoid compound of the present invention application in preparing antimetabolic syndrome medicine and/or health product, the chemical structural formula of described aborane type triterpenoid compound is as follows:
Wherein, R1For hydrogen atom, hydroxyl, methoxyl group or acetoxyl group；R2For hydrogen atom, hydroxyl, methoxyl group, acetoxyl group or carbonyl；R3For hydrogen atom, hydroxyl, methoxyl group or acetoxyl group.
The medicine of a kind of hypolipidemic, makes pharmaceutical dosage form by aborane type triterpenoid compound and pharmaceutic adjuvant；Described pharmaceutic adjuvant is slow releasing agent, polyvinylpyrrolidone or microcrystalline Cellulose；Described dosage form is tablet, capsule or pill.Described slow releasing agent is hydroxypropyl methylcellulose and/or lactose.
One, below for some structures being used for screening the arbor alkyl-type triterpenoids of cell blood fat reducing experiment of the present invention:
Two, the preparation of the blood lipid-lowering medicine of the present invention
Embodiment 1
The preparation of tablet
Weigh 10 g of compound 13,90 grams of hydroxypropyl methylcellulose, 100 grams of polyvinylpyrrolidones, 85 grams of lactose, 90 grams of micropowder silica gels, compound 13 is mixed homogeneously with the slow releasing agent of recipe quantity, add adhesive polyethylene to pelletize than pyrrolidone, at 40-70 DEG C, dry granule, dry granule adds the lubricant micropowder silica gel of recipe quantity, mixing, tabletting.
Embodiment 2
The preparation of capsule
300 g of compound 13, add dextrin in right amount, mixing, and 85% ethanol is made granule, is dried, granulate, adds micropowder silica gel 5g, and mixing loads capsule, makes 1000, obtain capsule of the present invention, every 0.35g.
Three, the aborane type triterpenoid compound effect experiment of the present invention
1, mice olive oil load test
Experimental technique: 60 mices are randomly divided into 6 groups, often organizes each 10.It is respectively normal group (N), model group (C), orlistat group (PC, 100mg/kg), sample is compound 13, it is divided into low dose group (SL, 10mg/kg), dosage group (SM, 20mg/kg) in sample, sample high dose group (SH, 40mg/kg).Often fasting 20-24h before group mouse experiment, prohibits water 3-4h before experiment, and eye socket is taken a blood sample, as the blood fat value of 0h.Determine the blood fat value of each group of mice 0h, and re-start packet according to blood fat value, make the initial blood fat value mean often organizing mice essentially identical.After packet completes, each group gastric infusion (normal group gives distilled water) respectively, after 30min, gavage to after olive oil (5mL/kg) respectively at 2h, 4h, 6h eye socket is taken a blood sample, Quick spin takes serum, 4 DEG C of preservations, uses enzymatic measurement to measure the concentration of triglyceride.Result is as shown in table 1:
Table 1 compound 13 is to Mouse oral olive oil load test result
Note: compare with matched group, * P ＜ 0.05, * * P ＜ 0.01
It can be seen that compound 13 can effectively suppress the rising of mice plasma triglyceride from table 1 result, and in dose-dependence, even more eager to excel in whatever one does than the effect of positive control drug orlistat.
2, the impact on the accumulation of HepG2 cell triglyceride
HepG2 cell is inoculated in 48 orifice plates, cultivate in the MEM culture medium containing 10% hyclone, at 37 DEG C, after 5% CO2 gas incubator is cultivated one day, change DMEM high glucose medium into, within every two days, change a not good liquor, after being further cultured for 6 days, sopping up the culture medium in plate hole, every hole adds distilled water 150 μ L, ultrasonication, uses triglyceride determination test kit (Beijing Northization safe clinical reagent company limited) to measure TG content therein.Sample is dissolved in DMSO, rejoins when changing liquid every time, and bezafibrate is as positive control.Result is as shown in table 2:
Table 2 is the arbor alkyl-type triterpenoids lipopexia inhibitory action to HepG2 cell of the present invention
Note: compare with matched group, * P ＜ 0.05, * * P ＜ 0.01
From Table 2, it can be seen that most aborane type triterpenoid compound has the effect of triglyceride accumulation, especially compound 8,10 and 13 in suppression hepatocyte, it is eager to excel a lot than the activity of positive control drug bezafibrate.
3, cellulotoxic experiment
The cytotoxic activity of reactive compound uses mtt assay to measure in human liver cancer cell HepG2 cell line, and specific practice is as follows: HepG2 cell suspension, in the DMEM culture medium containing 10% hyclone, is inoculated in 48 orifice plates, and inoculum density is 5 × 104Cells/well.The sample of the variable concentrations being dissolved in DMSO adds in hand-hole, after 37 DEG C of incubators containing 5% carbon dioxide are cultivated 4 or 6 days, sop up culture medium, every hole adds 10 μ L MTT (4mg/mL), cultivate 4 hours, after cultivation, every hole adds mensuration absorbance at the lysigenous first of DMSO, with 570nm.Result as shown in Figure 1, wherein, * P ＜ 0.01 (comparing with matched group).
From the point of view of the cytotoxic activity result of compound 13, this compound does not has any toxicity when 100 μMs, even can also increase hepatocellular vigor, by the experiment of cell in vitro poison, this explanation proves that this compound is safe.
4, the impact that glucose is taken in
HepG2 cell suspension, in the DMEM culture medium containing 10% hyclone, is inoculated in 48 orifice plates, and inoculum density is 5 × 104Cells/well, after cultivating 6 days, cell is cultivated 4 hours in serum-free medium, then cell is cleaned with KRP buffer, after adding sample, after hatching 20 minutes in the KRP buffer containing 100nM insulin, add 2-DG and 2-deoxygenates-D-(2,6-3H)-glucose (1 μ Ci/mL) continues to hatch 10 minutes, then cell is cleaned to terminate reaction with ice-cold PBS, every hole adds 200 μ L NaOH (1M) at 37 DEG C, 1M HCl is added to neutralize reactant liquor after hatching 2 hours, the radioactivity of cellular uptake glucose liquid scintillation counter (Beckman LS6500) measures, and bezafibrate is as positive control.As in figure 2 it is shown, wherein, (a) is bezafibrate to result, and (b) is compound 13, and * P ＜ 0.01 (comparing with matched group).
As can be seen from the results, compound 13 is compared with positive control drug bezafibrate, the cell absorption to glucose can be remarkably promoted when low dosage, this illustrates that this compound is likely to be of anti-diabetic activity, contrasting, bezafibrate just starts to promote cellular uptake glucose from 30 μMs.
Claims (6)
1. aborane type triterpenoid compound is preparing blood fat reducing and/or diabetes medicine and/or health care
Application in product, the chemical structural formula of described aborane type triterpenoid compound is as follows:
Wherein, R1For hydrogen atom, hydroxyl, methoxyl group or acetoxyl group；R2For hydrogen atom, hydroxyl, first
Epoxide, acetoxyl group or carbonyl；R3For hydrogen atom, hydroxyl, methoxyl group or acetoxyl group.
Apply the most as claimed in claim 1, it is characterised in that described blood lipid-lowering medicine and/or guarantor
Strong product are medicine and/or the health product of triglyceride reducing.
Apply the most as claimed in claim 1 or 2, it is characterised in that described aborane type triterpenes
R in compound1For hydrogen atom, R2For carbonyl, R3For acetoxyl group.
4. the medicine of a hypolipidemic, it is characterised in that by aborane type triterpenoid compound with medicinal
Pharmaceutical dosage form made by adjuvant；
The chemical structural formula of described aborane type triterpenoid compound is as follows:
Wherein, R1For hydrogen atom, hydroxyl, methoxyl group or acetoxyl group；R2For hydrogen atom, hydroxyl, first
Epoxide, acetoxyl group or carbonyl；R3For hydrogen atom, hydroxyl, methoxyl group or acetoxyl group；
Described pharmaceutic adjuvant is slow releasing agent, polyvinylpyrrolidone or microcrystalline Cellulose；
Described dosage form is tablet, capsule or pill.
The medicine of a kind of hypolipidemic the most according to claim 4, it is characterised in that described is slow
Releasing agent is hydroxypropyl methylcellulose and/or lactose.
The medicine of a kind of hypolipidemic the most according to claim 4, it is characterised in that described medicine
Thing is the medicine of triglyceride reducing.
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