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23-Norursane triterpene compound and its preparation method and application in the preparation of glycosidase inhibitor drugs

A technology of glycosidase inhibitors and triterpenoids, applied in the field of natural medicinal chemistry, can solve the problems of allergy and anaphylactic shock in patients, and achieve the effects of high safety, abundant sources and easy operation

Active Publication Date: 2021-04-20
GUANGDONG ACAD OF FORESTRY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the important α-glucosidase inhibitors that have been developed and marketed and are being clinically tested for the treatment of type 2 diabetes include first-line drugs acarbose (acarbose), voglibose and miglitol, etc., which can effectively control diabetes and lower blood sugar, but they all have obvious Including side effects such as gastrointestinal dysfunction (such as stomach distension, abdominal distension, diarrhea, abdominal pain, etc.), and occasionally some patients may also have allergic reactions, and severe anaphylactic shock may occur

Method used

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  • 23-Norursane triterpene compound and its preparation method and application in the preparation of glycosidase inhibitor drugs
  • 23-Norursane triterpene compound and its preparation method and application in the preparation of glycosidase inhibitor drugs
  • 23-Norursane triterpene compound and its preparation method and application in the preparation of glycosidase inhibitor drugs

Examples

Experimental program
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Embodiment 1

[0024]Example 1: Three-leaf Tongxin New Compound 2-Hydroxy-3-Carbonyl-23-Preparation 1.1 Plant Source of Trichon-28-Acid

[0025]The fruit samples of akebia trifoliata (thumb.) Koidz. The fruit samples were collected from Hunan Province in September 2017.

[0026]1.2 extraction and separation

[0027]Sample (three-herafly fruit dry product, 2.0 kg) Crushing, extract three times with a volume fraction of 95% ethanol solution, combined with filtrate to remove organic solvents to give a total extract. The total dipper was suspended in 500 ml of water, then extracted with an equal volume of petroleum ether, and the extract was concentrated under reduced pressure to obtain a petroleum ether total extract (31 g). The total extract of the petroleum ether was dissolved with a volume ratio of 1: 1 chloroform / methanol (100 mL), and the positive phase silica gel (80-100 mesh) was shaped at a weight ratio of 1: 1.5, and the dried column (200- 300 mesh, 800 grams), dry method, use petroleum ether / ace...

Embodiment 2

[0038]Example 2: Compound 2-Hydroxy-3-Carbonyl-23-Degradation of Umowa-1,4,12-Trivadiene-28-Glycosidase Inhibitory Activity Detection 2.1 Instruments & Reagents

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PUM

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Abstract

The invention discloses 23-norursane triterpene compound, its preparation method and its application in the preparation of glycosidase inhibitor drugs. The present invention separates and obtains the 23-norursane triterpene compound represented by the formula I with strong inhibitory activity of α-glucosidase from Akebia trifoliate, which has low potential toxic and side effects, rich source of plant materials, and when plant fruit is used for extraction It can also make the plant itself not too damaged and can be used for a long time, and the monomer compound is stable and easy to store, and its activity of inhibiting α-glucosidase is significantly stronger than that of clinical drug acarbose, which is likely to be further developed into an effective and safe The α-glucosidase inhibitor drugs for the prevention and treatment of type Ⅱ diabetes have good prospects.

Description

Technical field:[0001]The present invention belongs to the field of natural drug chemistry, and more particularly to a new drop triterpene compound obtained from three-leaf wood separation, i.e., 2-hydroxy-3-carbonyl-23-decoison-1,4,12-tri-tri-1 28-acid, and the compound or a pharmaceutically acceptable salt thereof in the preparation of glycosidase inhibitors or drugs.Background technique:[0002]Diabetes is a common endocrine metabolic disorder disease in the clinic, which is an important killer that threatens human health. With the improvement of people's living standards, diabetes has become more and more young, and many children will suffer this disease. The incidence of diabetes in the current global global is raised, and there is more than 100 million people in my country and presents a year increasing trend. Diabetes is positively lost to my country's health and national economies.[0003]Diabetes Western Medical is divided into type I diabetes (or insulin-dependent, DM1) and ty...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J63/00A61K31/56A61P3/10
CPCA61P3/10C07J63/008
Inventor 徐巧林谭建文曾雷王颂
Owner GUANGDONG ACAD OF FORESTRY
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