Novel ellagic tannins alpha-glucosidase inhibitor and preparation method thereof

A technology of ellagitannins and glucosidase, which is applied in the field of medicine to achieve the effect of great medical care value

Active Publication Date: 2019-08-20
TIANJIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The purpose of the present invention is to provide a new type of ellagitannin α-glucosidase inhibitor and its preparation method, to solve the problem of high-efficiency α-glucosidase inhibitor type antidiabetic drug source and traditional Chinese medicine raspberry in the prior art. Modern Application Issues

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  • Novel ellagic tannins alpha-glucosidase inhibitor and preparation method thereof
  • Novel ellagic tannins alpha-glucosidase inhibitor and preparation method thereof
  • Novel ellagic tannins alpha-glucosidase inhibitor and preparation method thereof

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Embodiment 1

[0043] A novel ellagitannin α-glucosidase inhibitor and a preparation method thereof, which are prepared by the following method:

[0044] (1) After pulverizing immature raspberry (Rubus chingii Hu) fruit, add 50% ethanol according to the ratio of liquid to material ratio of 5:1, soak for 0.5 hours, reflux extraction for 1 hour, and repeat the residue under the same conditions Extracted 3 times, combined the filtrates, concentrated under reduced pressure to an extract, and obtained raspberry ethanol extract.

[0045] (2) Add the raspberry alcohol extract into deionized water to make a suspension, extract according to the ratio of n-butanol:water=0.5:1, repeat the extraction 3 times, combine the n-butanol layers, and concentrate under reduced pressure to Extract, get n-butanol extract.

[0046] (3) Add the n-butanol extract to deionized water to make a suspension, then add it to D101 macroporous resin, elute with 10% ethanol, concentrate under reduced pressure to extract, and ...

Embodiment 2

[0050] A novel ellagitannin α-glucosidase inhibitor and a preparation method thereof, which are prepared by the following method:

[0051](1) After pulverizing the immature raspberry (Rubus chingii Hu) fruit, add 80% ethanol according to the ratio of liquid to solid 10:1, soak for 1 hour, reflux extraction for 1 hour, and repeat the residue under the same conditions Extracted 3 times, combined the filtrates, concentrated under reduced pressure to an extract, and obtained raspberry ethanol extract.

[0052] (2) Add the raspberry alcohol extract into deionized water to make a suspension, extract according to the ratio of n-butanol: water=1:1, repeat the extraction 3 times, combine the n-butanol layers, and concentrate under reduced pressure to Extract, get n-butanol extract.

[0053] (3) Add the n-butanol extract to deionized water to make a suspension, then add it to D101 macroporous resin, elute with 20% ethanol, concentrate under reduced pressure to extract, and obtain macro...

Embodiment 3

[0057] A novel ellagitannin α-glucosidase inhibitor and a preparation method thereof, which are prepared by the following method:

[0058] (1) After pulverizing immature raspberry (Rubus chingii Hu) fruit, add 70% ethanol according to the ratio of liquid to material ratio of 15:1, soak for 1.5 hours, reflux extraction for 2 hours, and repeat the same conditions for the residue Extracted 3 times, combined the filtrates, concentrated under reduced pressure to an extract, and obtained raspberry ethanol extract.

[0059] (2) Add the raspberry alcohol extract into deionized water to make a suspension, extract according to the ratio of n-butanol: water=2:1, repeat the extraction 3 times, combine the n-butanol layers, and concentrate under reduced pressure to Extract, get n-butanol extract.

[0060] (3) Add the n-butanol extract to deionized water to make a suspension, then add it to D101 macroporous resin, elute with 50% ethanol, concentrate under reduced pressure to extract, and o...

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Abstract

The invention discloses a novel ellagic tannins alpha-glucosidase inhibitor and a preparation method thereof. The method comprises the following steps: (1), crushing an immature rubus chingii hu fruit, using ethyl alcohol with certain concentration for reflux extraction, and performing filtering to obtain a rubus chingii hu extraction solution; (2), performing concentration on the extraction solution, adding deionized water to prepare a suspension, using n-butanol for extraction, and obtaining a n-butanol extract; (3), performing concentration on the n-butanol extract to concrete, after redissolving the concrete in the deionized water, adding a product to a macroporous resin column, using the ethyl alcohol for elution, and obtaining an ethyl alcohol eluent; (4), after the concentration ofthe ethyl alcohol eluent, redissolving a product in methyl alcohol, adding the product to an OSD column, using methyl alcohol for elution, collecting the eluent, performing concentration, and obtaining a methyl alcohol concentrated solution; and (5), adjusting the methyl alcohol concentrated solution to suitable concentration, adopting PHPLC (preparative high performance liquid chromatography) topreparation, and obtaining the new ellagic tannins alpha-glucosidase inhibitor. The new ellagic tannins alpha-glucosidase inhibitor is an ellagic tannins compound, which is isolated and identified forthe first time. Compared with common alpha-glucosidase inhibitor hypoglycemic drug-acarbose, the new ellagic tannins alpha-glucosidase inhibitor has significant higher inhibitory activity on alpha-glucosidase, and has great value in drug development.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a novel ellagitannin α-glucosidase inhibitor and a preparation method thereof. Background technique [0002] Diabetes is a chronic metabolic disease that endangers health. It is caused by insufficient insulin secretion or damage to islet secreting cells in the body, and is mainly characterized by high blood sugar. Its onset is usually closely related to a series of factors such as eating habits, living habits, genetic factors and acquired organ lesions. Long-term high blood sugar concentration in the body of diabetic patients will cause a series of diabetic complications, thus reducing blood sugar levels. Content plays an important role in the treatment of diabetes and the prevention and treatment of diabetic complications. The current antidiabetic drugs mainly include insulin and insulin analogues, α-glucosidase inhibitors and so on. α-glucosidase is a hydrolase that plays ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H13/08C07H1/08A61P3/10
CPCC07H13/08C07H1/08A61P3/10
Inventor 陈海霞陈玥
Owner TIANJIN UNIV
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