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Application of compound 2alpha,3beta-dyhydroxy-23-formyl-olive-12-ene-28-acid in preparation of glycosidase inhibitor medicine

A technology of glycosidase inhibitor and compound, which is applied in the field of natural medicinal chemistry, can solve the problems such as the glycosidase inhibitor activity that has not been seen, and achieves the effect of easy storage

Active Publication Date: 2017-01-04
SOUTH CHINA BOTANICAL GARDEN CHINESE ACADEMY OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The compound 2α,3β-dihydroxy-23-aldehyde-olean-12-en-28-acid was isolated from the plant Akebiatrifoliata (Wang J., Ren H., Xu, Q.L., et al. al.Food Chem., 2015, 168, 623-629), its chemical structural formula is shown in the following formula (I), but so far there is no research report on its glycosidase inhibitor activity

Method used

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  • Application of compound 2alpha,3beta-dyhydroxy-23-formyl-olive-12-ene-28-acid in preparation of glycosidase inhibitor medicine
  • Application of compound 2alpha,3beta-dyhydroxy-23-formyl-olive-12-ene-28-acid in preparation of glycosidase inhibitor medicine
  • Application of compound 2alpha,3beta-dyhydroxy-23-formyl-olive-12-ene-28-acid in preparation of glycosidase inhibitor medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Example 1: Preparation of compound 2α, 3β-dihydroxy-23-formyl-olean-12-ene-28-acid

[0021] 1.1 Extraction and separation

[0022] The sample (dried fruit of Akebia trifoliata, weighing 2.0 kg) was pulverized and extracted three times with 95% ethanol aqueous solution at room temperature, and the combined filtrate was concentrated under reduced pressure to remove the organic solvent to obtain the crude extract of the total extract. The total extract crude extract was suspended in 500ml water, then extracted with an equal volume of petroleum ether and then extracted 3 times with ethyl acetate, and the ethyl acetate extract was concentrated under reduced pressure to obtain the total extract of ethyl acetate (170g). Dissolve the total extract of ethyl acetate with chloroform / methanol (350mL) with a volume ratio of 1:1, add normal phase silica gel (80-100 mesh) and mix the sample with a weight ratio of 1:1.5, evaporate to dryness, and dry-pack the column (200 -300 mesh, 16...

Embodiment 2

[0025] Example 2: Compound 2α, 3β-dihydroxy-23-aldehyde-olean-12-ene-28-acid inhibits α-glucosidase activity detection

[0026] 2.1 Instruments and reagents

[0027] The experiment used Genois microplate reader (Tecan GENios, Swizerland); α-glucosidase was purchased from Sigma Chemical Co. (Sigma-Aldrich, St.Louis, USA), and acarbose (Acarbose) was purchased from Tokyo Chemical Industry Co., Ltd. (Japan), 4-nitrophenol-α-D-glucopyranoside (PNPG) was purchased from Tokyo Chemical Industry Co., Ltd. (Japan); sample 2α, 3β-dihydroxy-23- Aldehyde-olean-12-en-28-acid was prepared from the above experimental example.

[0028] 2.2 Test method:

[0029]a) Preparation of drug solution: prepare 10 mg / ml of 2α, 3β-dihydroxy-23-aldehyde-olean-12-en-28-acid and acarbose from dimethyl sulfoxide (DMSO) respectively solution, and prepare 67mmol / L of phosphate buffer (prepared with ultrapure water), PNPG substrate solution (5mM, prepared with phosphate buffer), and 0.2M NaCO 3 solution (pr...

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Abstract

The invention provides application of a compound 2alpha,3beta-dyhydroxy-23-formyl -olive-12-ene-28-acid in preparation of glycosidase inhibitor medicine. The compound with highalpha-glycosidase inhibiting activity can be obtained from akebia trifoliate and other plants, monomers of the compound 2alpha,3beta-dyhydroxy-23-aldehyde-olive-12-alkene-28-acid are stable, storage is easy, the alpha-glycosidase inhibiting activity of the compound is remarkably higher than that of clinical medicine acarbose (about 8.5 times of the activity of acarbose), and the compound is highly likely to be further developed into the effective and safe alpha-glycosidase inhibitor medicine for preventing and treating II diabetes, and has good prospects.

Description

[0001] Technical field: [0002] The invention belongs to the field of natural medicinal chemistry, and in particular relates to the preparation of glycosidase inhibitors or application in medicine. [0003] Background technique: [0004] Diabetes is a clinically common endocrine and metabolic disorder disease, which has an important correlation with the annual increase of cardiovascular diseases and cancers, and is an important killer of human health. At present, there are more than 100 million people in my country with a prevalence rate, and it is increasing year by year. Diabetes is causing more and more serious losses to our people's health and national economy. Diabetes is divided into insulin-dependent type 1 diabetes (DM1) and non-dependent type 2 diabetes (DM2), and the incidence and prevalence of DM2 are much higher than DM1. Competitive α-glucosidase inhibitors can delay the digestion and absorption of carbohydrates, control the sharp rise in blood sugar after meal...

Claims

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Application Information

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IPC IPC(8): A61K31/56A61P3/10
CPCA61K31/56
Inventor 谭建文王晶徐巧林董丽梅罗碧
Owner SOUTH CHINA BOTANICAL GARDEN CHINESE ACADEMY OF SCI
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