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Applications of four kaurane diterpene compounds in preparation of glycosidase inhibitor medicines

A glycosidase inhibitor, kaurine-type technology is applied to the application field of four kaurine diterpenoid compounds in the preparation of glycosidase inhibitor drugs, and the preparation process is easy to operate, high in safety and rich in sources.

Active 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] Compounds 3α-hydroxy-ent-kauran-19-oic acid (1), 3α-tigloyloxy-9β-hydroxy-ent-kaur-16-en-19-oic acid (2), 3α-cinnamoyloxy-ent-kaur-16 -en-19-oic acid (3), 3α-cinnamoyloxy-9β-hydroxy-ent-kaur-16-en-19-oic acid (4) are all kaurane diterpene compounds, these compounds have been obtained from three Split leaf Wedelia (Wedelia trilobata (L.) Hitchc) isolated from (Qiang et al., Helvetica Chimica Acta2011,94:817-823; Bohlmann et al., Phytochemistry1981,20:751-756; Ma et al., Natural Products and Bioprospecting, 2013, 3:107-111), 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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  • Applications of four kaurane diterpene compounds in preparation of glycosidase inhibitor medicines
  • Applications of four kaurane diterpene compounds in preparation of glycosidase inhibitor medicines
  • Applications of four kaurane diterpene compounds in preparation of glycosidase inhibitor medicines

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Embodiment 1

[0017] Embodiment 1: Preparation of four kinds of diterpene compounds in Wedelia chinensis

[0018] 1.1 Plant source and identification

[0019] 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.

[0020] 1.2 Extraction and separation

[0021] The whole plant of Wedelia chinensis (dry weight 2kg) was pulverized, 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 were combined; the ethanol in the extract was drained by concentration under reduced pressure, and then an appropriate amount of water was added to make it It became a suspension, which was extracted 4 times with petroleum ether; the petroleum ether fraction (45 g) was obtained after concentration under reduced pressu...

Embodiment 2

[0026] Embodiment 2: The α-glucosidase inhibitory activity detection of described four kinds of diterpene compounds

[0027] 2.1 Instruments and reagents

[0028] Experimental instrument: Genois microplate reader (Tecan GENios, Swizerland)

[0029] 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); Phenylphenol-α-D-glucopyranoside (PNPG) was purchased from Tokyo Chemical Industry Co., Ltd. (Japan); four diterpene compounds α-hydroxy-ent-kauran-19-oic acid (compound 1), 3α-tigloyloxy-9β-hydroxy-ent-kaur-16-en-19-oic acid (compound 2), 3α-cinnamoyloxy-ent-kaur-16-en-19-oic acid (compound 3), 3α-cinnamoyloxy- 9β-hydroxy-ent-kaur-16-en-19-oic acid (compound 4) is prepared from the above experimental example 1 or can also refer to the literature Qiang et al., Helvetica Chimica Acta2011, 94:817-823; Bohlmann et al ., Phytochemistry1981, 20:751-756; Ma et al., N...

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Abstract

The invention provides applications of four kaurane diterpene compounds in preparation of glycosidase inhibitor medicines. The four compounds capable of highly inhibiting alpha-glycosidase activity are natural compounds which are high in safety and capable of rapid natural degradation without residue in the environment. The four compounds are obtained by separation from wedelia trilobata, and other plant materials. The plant materials are rich in source. A preparation process is easy in operation. Monomers of the four compounds are stable and liable to store. The alpha-glucosidase inhibition activity of the four compounds is obviously higher than or equivalent to that of acarbose that is a clinic medicine. The four compounds are extremely likely developed into effective and safe alpha-glucosidase inhibitor medicines used for preventing and treating type II diabetes, and have good prospects.

Description

technical field [0001] The invention belongs to the field of natural medicinal chemistry, in particular to four kaurane diterpene compounds 3α-hydroxy-ent-kaura n-19-oic acid (1), 3α-tigloyloxy-9β-hydroxy-ent-kaur-16-en -19-oic acid (2), 3α-cinnamoyloxy-ent-kaur-16-en-19-oic acid (3), 3α-cinnamoyloxy-9β-hydroxy-ent-kaur-16-en-19-oic acid ( 4) Application of the pharmaceutically acceptable salt thereof in the preparation of glycosidase inhibitors or medicines. Background of the invention [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 eco...

Claims

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Application Information

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IPC IPC(8): A61K31/19A61K31/22A61K31/216A61P3/10
Inventor 谭建文任慧周忠玉徐巧林董丽梅
Owner SOUTH CHINA BOTANICAL GARDEN CHINESE ACADEMY OF SCI
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