CN105534990A - Application of cardiospermum halicacabum extract in preparation of medicinal preparations for treating diabetes - Google Patents
Application of cardiospermum halicacabum extract in preparation of medicinal preparations for treating diabetes Download PDFInfo
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- CN105534990A CN105534990A CN201510880543.1A CN201510880543A CN105534990A CN 105534990 A CN105534990 A CN 105534990A CN 201510880543 A CN201510880543 A CN 201510880543A CN 105534990 A CN105534990 A CN 105534990A
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- cardiospermum halicacabum
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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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
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Abstract
The invention discloses an application of a cardiospermum halicacabum extract in the preparation of medicinal preparations for treating diabetes. The cardiospermum halicacabum extract comprises taraxerol and/or 3[beta]-alnusonol. The results of alpha-glucosidase inhibition experiment show that taraxerol and 3[beta]-alnusonol can both inhibit the activity of alpha-glucosidase, the inhibition performance of taraxerol and 3[beta]-alnusonol is highly similar with that of a reference substance (acarbose), and thus the cardiospermum halicacabum extract can be used to treat diabetes.
Description
Technical field
The present invention relates to the application in a kind of Cardiospermum halicacabum extract.More particularly, the present invention relates to the application of a kind of Cardiospermum halicacabum extract in the pharmaceutical preparation of preparation treatment diabetes.
Background technology
Cardiospermum halicacabum is sapindaceous plant Cardiospermum halicacabum (CardiospermumhalicacabumL.) dry herb, has another name called Herba Cardiospermi Halicacabi, Herba Clerodendri fortunati, triangle lantern, is born in wilderness, Tian Bian, shrubbery.The southwestern various places such as main distribution Guangdong, Guangxi, Fujian, Taiwan, among the people being used for treats diabetes, pneumonia, jaundice, gonorrhea, rheumatism, traumatic injury, venom etc.Find when this seminar is studied the hypoglycemic pharmacological action of Cardiospermum halicacabum, its ethanol extraction obviously can reduce the blood glucose value of alloxan diabetes mice and the sick mice of epinephrine glycosuria, filter out ethyl acetate and n-butanol portion is hypoglycemic effective site, be separated from effective site and identify 11 compounds, comprising chemical compositions such as taraxerol, 3 β-Folium Et Cacumen Alni Japonicae alcohol.Alpha-glucosidase (α-glucosidase) can catalytic starch or sucrose digestion final step and produce abundant glucide, be one of major target class for the treatment of diabetes at present.The alpha-glucosidase inhibitor being used for the treatment of diabetes clinically mainly contains acarbose, voglibose, miglitol etc., but these compounds have certain side effect, therefore, the natural drug looking for a kind of safety, curative effect reliably to treat diabetes has important practical significance.Therefore, this research for object of study, take alpha-glucosidase as target spot with the main component taraxerol of Cardiospermum halicacabum effective site, 3 β-Folium Et Cacumen Alni Japonicae alcohol, screens further its external diabetes effect.
Summary of the invention
An object of the present invention is to solve at least the problems referred to above, and the advantage will illustrated at least is below provided.
A further object of the invention is to provide the application of a kind of Cardiospermum halicacabum extract in the pharmaceutical preparation of preparation treatment diabetes, Cardiospermum halicacabum extract, namely all energy Inhibiting α-glucosidase is active for taraxerol and 3 β-Folium Et Cacumen Alni Japonicae alcohol, its inhibition is close with reference substance acarbose height, can be used for treat diabetes etc. disease.
In order to realize according to these objects of the present invention and other advantage, provide the application of a kind of Cardiospermum halicacabum extract in the pharmaceutical preparation of preparation treatment diabetes.
Preferably, the application of described Cardiospermum halicacabum extract in the pharmaceutical preparation of preparation treatment diabetes, described Cardiospermum halicacabum extract is taraxerol or 3 β-Folium Et Cacumen Alni Japonicae alcohol.
Preferably, the application of described Cardiospermum halicacabum extract in the pharmaceutical preparation of preparation treatment diabetes, described pharmaceutical preparation is the Cardiospermum halicacabum extract and the pharmaceutically acceptable adjuvant composition that include effective amount.
Preferably, the application of described Cardiospermum halicacabum extract in the pharmaceutical preparation of preparation treatment diabetes, described pharmaceutical preparation is injection, tablet, pill, capsule, suspending agent or Emulsion.
The present invention at least comprises following beneficial effect: Cardiospermum halicacabum extract-taraxerol of the present invention and 3 β-Folium Et Cacumen Alni Japonicae alcohol are expected to be used for the treatment of the relevant disease that diabetes etc. take alpha-glucosidase as target spot, show through alpha-glucosidase Inhibition test, all energy Inhibiting α-glucosidase is active for taraxerol and 3 β-Folium Et Cacumen Alni Japonicae alcohol, its inhibition is close with reference substance acarbose height, can be used for treat diabetes etc. disease; This medicine can make common dosage forms pharmaceutically, comprises and makes injection, tablet, pill, capsule, suspending agent or Emulsion.
By the Inhibition test of external alpha-glucosidase, demonstrate Cardiospermum halicacabum extract-taraxerol and 3 β-Folium Et Cacumen Alni Japonicae alcohol has very strong inhibit activities to alpha-glucosidase, to the IC of alpha-glucosaccharase enzyme level
50value is respectively 0.82mg/ml and 0.78mg/ml.
Part is embodied by explanation below by other advantage of the present invention, target and feature, part also will by research and practice of the present invention by those skilled in the art is understood.
Accompanying drawing explanation
Fig. 1 is that the 3 β-Folium Et Cacumen Alni Japonicae alcohol of variable concentrations is to the suppression ratio of а-glucosidase;
Fig. 2 is that the taraxerol of variable concentrations is to the suppression ratio of а-glucosidase.
Detailed description of the invention
Below in conjunction with embodiment, the present invention is described in further detail, can implement according to this with reference to description word to make those skilled in the art.
It should be noted that experimental technique described in following embodiment if no special instructions, is conventional method, described reagent and material, if no special instructions, all can obtain from commercial channels.
The structural formula of 3 β-Folium Et Cacumen Alni Japonicae alcohol is:
One, leaching process
1, raw material prepares
Cardiospermum halicacabum herb is adopted in suburb, Nanning, is accredited as the dry herb of sapindaceous plant Cardiospermum halicacabum CardiospermumhalicacabumL. through Colleges Of Traditional Chinese Medicine Of Guangxi TCD identification teaching and research room Liao Yue certain herbaceous plants with big flowers senior experimentalist.Specimen is stored in Chemistry for Chinese Traditional Medicine teaching and research room of Colleges Of Traditional Chinese Medicine Of Guangxi.
2 Extraction and isolation
Cardiospermum halicacabum dry herb coarse powder 25kg, uses 95% ethanol percolate extraction, collects 10 times amount percolates; 60% ethanol percolate extraction used again by medicinal residues, collects 10 times amount percolates, and merge percolate, concentrating under reduced pressure obtains total extractum.Extractum adds after suitable quantity of water suspends uses petroleum ether, chloroform, ethyl acetate, n-butanol extraction, recycling design successively, obtains the extract of corresponding site.
Petroleum ether part 140g is through silica gel column chromatography, with petroleum ether-ethyl acetate gradient elution, obtain compound 1 (1.98g) and 5 powder coarse crystallization A, B, C, D, E, A with B powder is separated through silica gel column chromatography and obtains compound 2 (30mg) and 3 (6.5mg); C, D, E, F powder through petroleum ether-ethyl acetate repeatedly recrystallization obtain compound 1 (192.4mg).
Ethyl acetate extract 80g is separated and chloroform-methanol recrystallization repeatedly through silica gel column chromatography (chloroform-acetone) repeatedly, obtains compound 2 (452mg);
Wherein, compound 1: white, needle-shaped crystals (chloroform), Liebermann-Burchard reaction is positive.EI-MSm/z:426[M]+,408,393,274,259,245,205,173,119,109,95,69,55。1H-NMR(400MHz,CDCl3)δ:1.15,1.09,1.04,1.00,0.98,0.94,0.93,0.85(3H,s,CH3×8),3.46(1H,brs,H-3),5.62(1H,d,J＝4.8Hz,H-12)；13C-NMR(100MHzCDCl3)δ:19.6(C-1),27.8(C-2),76.3(C-3),40.8(C-4),141.6(C-5),122.1(C-6),23.6(C-7),47.4(C-8),34.6(C-9),49.7(C-10),33.1(C-11),30.3(C-12),37.8(C-13),38.9(C-14),34.5(C-15),34.8(C-16),30.1(C-17),43.0(C-18),35.0(C-19),28.2(C-20),32.0(C-21),39.3(C-22),28.9(C-23),25.4(C-24),16.2(C-25),18.2(C-26),18.4(C-27),32.4(C-28),32.0(C-29),36.0(C-30)。Above data and bibliographical information basically identical, therefore authenticating compound 1 is 3 β-Folium Et Cacumen Alni Japonicae alcohol.
Compound 2: white, needle-shaped crystals (chloroform), mp248 ~ 249 DEG C, Libermann-Burchard reaction is positive.With taraxerol reference substance thin layer altogether, in 3 kinds of development systems, Rf value is completely the same, and it is identical to develop the color, therefore authenticating compound 2 is taraxerol.
Two, experimentation
1, the mensuration of external alpha-glucosidase activity
All tests are all with MicroplatereaderELX808TM type microplate reader (BioTek company of the U.S.), measure under 37 DEG C of conditions.Data analysis software uses Origin software to carry out date processing, uses acarbose product in contrast.
Selecting of 1.1 enzymatic reaction systems
Enzyme mark version adds the PBS buffer of 170ul, then adds alpha-glucosidase (1u) 10ul respectively, place 20min under reaction temperature 37 DEG C of conditions after.Add the substrate of 10ul variable concentrations, namely concentration be respectively 0.3125mg/ml, 0.625mg/ml, 1.25mg/ml, 2.5mg/ml, 5mg/ml to nitrocresol heteroside (pNPG), after rapid mix homogeneously after reaction temperature 37 DEG C places 20min, measure mixed solution at 400nm place absorbance (OD), by regulating concentration of substrate different, the absorbance of mixed liquor is detected, filters out suitable concentration of substrate, to be made into best enzymatic system.
The OD value of mixed solution during table 1 substrate variable concentrations
As shown in Table 1, the absorbance OD value of mixed solution finds to increase along with the increase of concentration of substrate, and OD value is too high or too low, it is inaccurate that capital causes measuring the data come, best OD value is about 0.7-1.0, therefore can determine that best concentration of substrate is 1.25mg/ml, therefore selected enzymatic reaction system is: the 1. PBS buffer of 170ul; 2. the alpha-glucosidase (1u) of 10ul; 3. the substrate (concentration be 1.25mg/ml to nitrocresol heteroside) of 10ul, under this kind of enzymatic system, is conducive to the carrying out of enzymatic reaction.
1.2IC
50the calculating of value
Experimentally result, is decided to be 100% by enzyme activity when not adding sample, and so adding the enzyme activity after variable concentrations sample is relative activity percent (i.e. remaining vigor percent):
Map known, time when relative activity is 50% by counter sample concentration, be IC
50value;
Wherein, by be generally used on the market treat diabetes a kind of oral antidiabetic drug-acarbose as a comparison;
The IC of 1.2.13 β-Folium Et Cacumen Alni Japonicae alcohol
50calculating
Can be known by Fig. 1, at mensuration Folium Et Cacumen Alni Japonicae alcohol in the inhibitory action of а-glucosidase, the IC of 3 β-Folium Et Cacumen Alni Japonicae alcohol
50value is 0.75mg/ml, compares reference substance acarbose (IC
50=0.8mg/ml) to get well, and along with the increase suppression ratio of 3 β-Folium Et Cacumen Alni Japonicae determining alcohol is also along with rising, it is positioned at the various alpha-glucosidases of small intestinal by competitive inhibition, the speed making starch based be decomposed into glucose slows down, thus slow down the absorption of glucose in intestinal, reduce postprandial hyperglycemia, thus reach the object of effectively treatment diabetes.
1.2.2 taraxerol IC
50calculating
At mensuration taraxerol in the inhibitory action of а-glucosidase, can be known by Fig. 2, the IC of taraxerol
50value is 0.82mg/ml, with reference substance acarbose (IC
50=0.8mg/ml) close, and along with the increase suppression ratio of taraxerol concentration is also along with rising, it is positioned at the various alpha-glucosidases of small intestinal by competitive inhibition, the speed making starch based be decomposed into glucose slows down, thus slow down the absorption of glucose in intestinal, reduce postprandial hyperglycemia, thus reach the object of effectively treatment diabetes.
Table 2. compound is to the IC of alpha-glucosaccharase enzyme inhibition activity
50value
In sum, taraxerol, 3 β-Folium Et Cacumen Alni Japonicae alcohol are close with reference substance acarbose to the inhibit activities of alpha-glucosidase.The present invention is that the new antidiabetic medicine of research and development provides new thinking.
Although embodiment of the present invention are open as above, but it is not restricted to listed in description and embodiment utilization, it can be applied to various applicable the field of the invention completely, for those skilled in the art, can easily realize other amendment, therefore do not deviating under the general concept that claim and equivalency range limit, the present invention is not limited to specific details and illustrates here and the embodiment described.
Claims (4)
1. the application of Cardiospermum halicacabum extract in the pharmaceutical preparation of preparation treatment diabetes.
2. the application of Cardiospermum halicacabum extract as claimed in claim 1 in the pharmaceutical preparation of preparation treatment diabetes, it is characterized in that, described Cardiospermum halicacabum extract is taraxerol or 3 β-Folium Et Cacumen Alni Japonicae alcohol.
3. the application of Cardiospermum halicacabum extract as claimed in claim 1 in the pharmaceutical preparation of preparation treatment diabetes, is characterized in that, described pharmaceutical preparation is the Cardiospermum halicacabum extract and the pharmaceutically acceptable adjuvant composition that include effective amount.
4. the application of Cardiospermum halicacabum extract as claimed in claim 1 in the pharmaceutical preparation of preparation treatment diabetes, it is characterized in that, described pharmaceutical preparation is injection, tablet, pill, capsule, suspending agent or Emulsion.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510880543.1A CN105534990A (en) | 2015-12-04 | 2015-12-04 | Application of cardiospermum halicacabum extract in preparation of medicinal preparations for treating diabetes |
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| CN201510880543.1A CN105534990A (en) | 2015-12-04 | 2015-12-04 | Application of cardiospermum halicacabum extract in preparation of medicinal preparations for treating diabetes |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107446009A (en) * | 2017-09-05 | 2017-12-08 | 广西中医药大学 | The O β D glucuronic acid methyl esters of chrysoeriol 7 and its extracting method and purposes |
| CN107501367A (en) * | 2017-09-05 | 2017-12-22 | 广西中医药大学 | The O β D glucuronic acids butyl esters of chrysoeriol 7 and its extracting method and purposes |
-
2015
- 2015-12-04 CN CN201510880543.1A patent/CN105534990A/en active Pending
Non-Patent Citations (4)
| Title |
|---|
| KADAPAKKAM NANDABALAN SANGEETHA ETAL: "3β-taraxerol of Mangifera indica, a PI3K dependent dual activator of glucose transport and glycogen synthesis in 3T3-L1 adipocytes", 《BIOCHIMICA ET BIOPHYSICA ACTA (BBA) - GENERAL SUBJECTS》 * |
| YAN DING ETAL: "The regulation of inflammatory cytokine secretion in macrophage cell line by the chemical constituents of Rhus sylvestris", 《BIOORGANIC & MEDICINAL CHEMISTRY LETTERS》 * |
| 苗伟生: "倒地铃降血糖作用及化学成分研究", 《万方数据硕士学位论文》 * |
| 韦建华等: "倒地铃化学成分研究", 《中草药》 * |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107446009A (en) * | 2017-09-05 | 2017-12-08 | 广西中医药大学 | The O β D glucuronic acid methyl esters of chrysoeriol 7 and its extracting method and purposes |
| CN107501367A (en) * | 2017-09-05 | 2017-12-22 | 广西中医药大学 | The O β D glucuronic acids butyl esters of chrysoeriol 7 and its extracting method and purposes |
| CN107501367B (en) * | 2017-09-05 | 2020-06-16 | 广西中医药大学 | Haloeriol-7-O- β -D-glucuronic acid butyl ester and extraction method and application thereof |
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Application publication date: 20160504 |
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