Bougainvillea glabra triterpenoid saponin, hpyerglycemic drugs with triterpenoid saponin as active component and preparation method and application thereof

A kind of technology of leaf leaf flower and triterpenoid saponins, which is applied in the preparation of hypoglycemic drugs.

Active Publication Date: 2015-09-16
XISHUANGBANNA TROPICAL BOTANICAL GARDEN CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Its disadvantage is that the content of compounds (1), (2), and (3) is low, and the mixed solvent system of organic solvent and water is used many times in the separation and purification, and the recovery temperature of the mixed solvent is high, which is not conducive to the recovery and utilization of solvent Conducive to industrial mass production

Method used

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  • Bougainvillea glabra triterpenoid saponin, hpyerglycemic drugs with triterpenoid saponin as active component and preparation method and application thereof
  • Bougainvillea glabra triterpenoid saponin, hpyerglycemic drugs with triterpenoid saponin as active component and preparation method and application thereof
  • Bougainvillea glabra triterpenoid saponin, hpyerglycemic drugs with triterpenoid saponin as active component and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] The triterpenoid saponins compounds oleanolic acid-3-O-β-D-glucopyranoside (1), oleanolic acid-3-O-β-D-xylopyranose (1 →3)-β-D-glucopyranose (2), oleanolic acid-3-O-β-D-xylopyranose (1→3)-β-D-glucopyranose Preparation and structure identification of methyl glucoside (3):

[0038] Take the leaves and leaves (50 kg), dry and pulverize them, and extract them by cold soaking with 90% methanol at room temperature for 3 times, the time is 7, 3, and 3 days each time, and the extract is concentrated under reduced pressure to obtain methanol extract ; After the methanol extract is suspended in water, it is fully extracted with ethyl acetate and n-butanol successively, and the equal volume is extracted three times respectively, and the solvent is recovered to obtain the ethyl acetate part, n-butanol part and water part; Column chromatography, 100:0, 20:1, 10:1, 8:1, 6:1, 2:1, 0:100 chloroform / methanol gradient elution, thin layer chromatography, combined with triterpene saponins...

Embodiment 2

[0051] The triterpene saponin compound of the present invention, glabrata saponins, oleanolic acid-3-O-β-D-glucopyranoside (1), oleanolic acid-3-O-β-D-xylopyranose ( 1→3)-β-D-glucopyranose (2), oleanolic acid-3-O-β-D-xylopyranose (1→3)-β-D-glucopyranose Acid methyl glycoside (3) has a therapeutic effect on streptozotocin (STZ)-induced hyperglycemia in mice with type 2 diabetes. The experimental principles, methods and results are as follows:

[0052] Experimental principle: Streptozotocin (STZ) selectively destroys the islet β cells of mice, causing them to develop diabetes. The mice were fed with high-calorie feed for a certain period of time and fasted for 12 hours, and STZ was injected intraperitoneally at 100 mg / kg body weight. , can prepare type Ⅱ diabetes animal model, and the model prepared according to this method has the characteristics of overweight, impaired glucose tolerance, elevated blood lipid, elevated serum insulin and decreased insulin receptor binding capac...

Embodiment 3

[0061] Compounds obtained in Example 1 Oleanolic acid-3-O-β-D-glucopyranose (1), oleanolic acid-3-O-β-D-xylopyranose (1→3) -β-D-glucopyranose (2), oleanolic acid-3-O-β-D-xylopyranose (1→3)-β-D-glucopyranose methyl (3), add 4% sulfuric acid ethanol solution, pH = 4, filter and dry to prepare sulfate compound 1-3.

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Abstract

Bougainvillea glabra triterpenoid saponin compounds comprise a triterpenoid saponin with a skeleton containing oleanolic acid, wherein the 3-site of the oleanolic acid is connected with 1'-site of beta-D-pyran glucuronic acid by an oxygen atom, and comprise other two derivates with the same skeleton structure; and the compound as shown in formula (I) is preferable, in the formula (I), R1 is methyl or hydrogen and R2 is hydrogen or beta-D-pyran xylose. The bougainvillea glabra triterpenoid saponin compounds 1-3 are new plant sourced hypoglycemic drugs. Pharmaceutical compositions with the compounds as active ingredients and a preparation method and application thereof in making the hypoglycemic drugs are provided.

Description

technical field [0001] The present invention belongs to the technical field of medicines, and in particular relates to a class of triterpene saponins in G. saponins, which can be used as hypoglycemic active compounds, pharmaceutical compositions using them as active ingredients, their preparation methods and their application in the preparation of hypoglycemic drugs. in the application. Background technique [0002] Type 2 diabetes continues to have a high incidence worldwide, and has become the third non-communicable disease that seriously threatens people's health and life after cardiovascular and cerebrovascular diseases and malignant tumors. Long-term hyperglycemia in diabetics can lead to macrovascular lesions (heart disease, hypertension, cerebrovascular accidents, and lower extremity vascular lesions), microvascular lesions (diabetic retinopathy, diabetic nephropathy), and neuropathy, endangering the heart, brain, and kidneys and other vital organs. At present, the ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J63/00C07H15/256C07H1/08A61K31/704A61P3/10
CPCA61K31/704C07H1/08C07H15/256C07J63/008
Inventor 张玉梅宋启示范青飞
Owner XISHUANGBANNA TROPICAL BOTANICAL GARDEN CHINESE ACAD OF SCI
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