Applications of compound ent-kaur-16-en-19-oic acid in preparation of glycosidase inhibitor medicines

A technology for glycosidase inhibitors and compounds, which is applied in the field of natural medicinal chemistry, can solve problems such as no research reports on glycosidase inhibitors, and achieve the effects of easy storage, good economic benefits, and easy preparation process.

Inactive Publication Date: 2014-10-08
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

[0004] The compound ent-kaur-16-en-19-oic acid is a kaurane diterpenoid, which was isolated from Wedelia trilobata (L.) Hitchc (Qiang Y, Du D-L, Chen Y-J, Gao K.ent-Kaurane diterpenes and further constituents from Wedeli

Method used

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  • Applications of compound ent-kaur-16-en-19-oic acid in preparation of glycosidase inhibitor medicines
  • Applications of compound ent-kaur-16-en-19-oic acid in preparation of glycosidase inhibitor medicines
  • Applications of compound ent-kaur-16-en-19-oic acid in preparation of glycosidase inhibitor medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] Embodiment 1: Preparation of diterpene compound ent-kaur-16-en-19-oic acid in Wedelia chinensis

[0015] 1.1 Plant source and identification

[0016] The plant material for extraction, Sphagneticola trilobata (L.) Pruski, was collected from the South China Botanical Garden in Guangdong Province in September 2009 and identified by Xing Fuwu, a researcher at the South China Botanical Garden, Chinese Academy of Sciences.

[0017] 1.2 Extraction and separation

[0018] The whole plant of Wedelia chinensis (dry weight: 2kg) is crushed, soaked and extracted with ethanol with a volume fraction of 95% at room temperature for 3 times, each time for 2 days, and the extracts are combined; after vacuum concentration, the ethanol in the extract is drained and then an appropriate amount of water is added Make it into a suspension, and sequentially extract four times with petroleum ether and ethyl acetate respectively; after concentrating under reduced pressure, the petroleum ether f...

Embodiment 2

[0022] Example 2: Detection of α-glucosidase inhibitory activity of the compound ent-kaur-16-en-19-oic acid

[0023] 2.1 Instruments and reagents

[0024] Experimental instrument: Genois microplate reader (Tecan GENios, Swizerland)

[0025] Reagent samples: α-glucosidase was purchased from Sigma Chemical Co. (Sigma-Aldrich, St.Louis, USA); Acarbose was purchased from Tokyo Chemical Industry Co., Ltd. (Japan); Phenol-α-D-glucopyranoside (PNPG) was purchased from Tokyo Chemical Industry Co., Ltd. (Japan); the sample ent-kaur-16-en-19-oic acid was prepared from the above experimental examples, and could also be prepared according to Document Qiang Y, Du D-L, Chen Y-J, Gao K. ent-Kaurane diterpenes and further constituents from Wedelia trilobata. Helvetica Chimica Acta2011, 94:817-823 preparation method.

[0026] 2.2 Test method:

[0027] a) Preparation of drug solution: Compound ent-kaur-16-en-19-oic acid and acarbose were prepared with dimethyl sulfoxide (DMSO) to prepare 10 mg...

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Abstract

The invention discloses applications of a compound ent-kaur-16-en-19-oic acid in preparation of glycosidase inhibitor medicines. The compound ent-kaur-16-en-19-oic acid has high alpha-glucosidase inhibition activity, and the alpha-glucosidase inhibition activity of the compound is even higher than that of acarbose that is a first-line medicine for diabetes, and therefore the compound can be used for development and preparation of potential medicine candidates used for preventing and treating physiological changes or diseases caused by or related to alpha-glucosidase, wherein the physiological changes or diseases caused by or related to the alpha-glucosidase include but is not limited to type II diabetes.

Description

Technical field: [0001] The invention belongs to the field of natural medicine chemistry, and in particular relates to the preparation of glycosidase inhibitors or medicines by using a kaurene-type diterpene compound ent-kaur-16-en-19-oic acid or a pharmaceutically acceptable salt or an esterified derivative thereof in the application. Background technique: [0002] Diabetes is a clinically common endocrine and metabolic disorder disease, which has an important correlation with the annual increase in cardiovascular diseases and cancers, and is an important killer of human health. At present, the incidence of diabetes is increasing worldwide. In my country, the prevalence of diabetes is more than 100 million, and it shows a trend of increasing year by year. Diabetes is causing more and more serious losses to our people's health and national economy. [0003] Diabetes in western medicine is divided into type Ⅰ diabetes (or insulin-dependent, DM1) and type Ⅱ diabetes (or non-...

Claims

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Application Information

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IPC IPC(8): A61K31/19A61P3/10
Inventor 谭建文任慧徐巧林周忠玉罗应
Owner SOUTH CHINA BOTANICAL GARDEN CHINESE ACADEMY OF SCI
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