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Application and preparation method of fluorenone compounds in dendrobium in the preparation of anti-diabetic drugs

The technology of a diabetes drug and compound is applied in the field of fluorenone compounds in the preparation of diabetes prevention and treatment drugs, and the preparation of diabetes prevention and treatment drugs, and achieves the effects of being easy to obtain, widely distributed and high in purity.

Active Publication Date: 2020-07-24
INST OF QUALITY STANDARD & DETECTION TECH YUNNAN ACAD OF AGRI SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are no relevant reports on the inhibition of α-glucosidase activity by polyphenolic compounds in this genus.

Method used

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  • Application and preparation method of fluorenone compounds in dendrobium in the preparation of anti-diabetic drugs
  • Application and preparation method of fluorenone compounds in dendrobium in the preparation of anti-diabetic drugs
  • Application and preparation method of fluorenone compounds in dendrobium in the preparation of anti-diabetic drugs

Examples

Experimental program
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preparation example Construction

[0057] The present invention also provides a preparation method of the above-mentioned compound of formula I, the method comprising preparing the compound from a plant of the genus Dendrobium (such as Dendrobium officinale, Dendrobium nobile or Dendrobium tympani). Preferably, the 1,4,7-trihydroxy-5-methoxyfluorenone, 2,5-di Hydroxy-4-methoxyfluorenone and 2,4,7-trihydroxy-5-methoxyfluorenone. Preferably, the method has the steps of:

[0058] (1) clean the fresh dendrobium candidum strips and dry them;

[0059] (2) Place the fresh strips of Dendrobium officinale in (1) in a drying box, dry them at 95-100°C for 3.0-3.5 hours, make their moisture content 20-25%, and cut them into short strips of 3.0-4.0 cm ;

[0060] (3) the short strips of Dendrobium candidum in (2) are obtained by microwave puffing and breaking; Wall products;

[0061] (4) extracting with solvent after crushing the puffed broken wall product, and merging the extract;

[0062] (5) concentrating under redu...

Embodiment 1

[0077] Inhibitory activity of Dendrobium officinale extract on α-glucosidase

[0078] Source of materials: Dendrobium officinale, Dendrobium nobile and Dendrobium chrysanthemum, which belong to the genus Dendrobium, were collected in Maitreya, Yunnan, and identified as Dendrobium officinale Kimura et Migo, D.nobile Lindl. .. The specimens are preserved in the Herbarium of the School of Medicine for Nationalities, Yunnan University for Nationalities.

[0079]The preparation of Dendrobium officinale extract: clean the fresh strips of Dendrobium officinale, and dry them; place the fresh strips of Dendrobium officinale in a drying oven, and dry them at 95°C for 3.0 hours to make the moisture content 20-25%, cut into short strips of 3.5 cm; under the conditions of 850 watts of power and 40 seconds of puffing and breaking time, the short strips of Dendrobium candidum are puffed and broken by microwave to obtain puffed and broken products; the expanded and broken products are pulver...

Embodiment 2

[0089] Further experiments with Dendrobium officinale

[0090] Example 1 was repeated using 95% methanol / water, 70% ethanol / water and 70% acetone / water as extraction solvents respectively. The results are shown in Table 3. The experimental results show that 95% methanol extract of Dendrobium candidum, 70% ethanol extract of Dendrobium candidum and 70% acetone are obtained by using 95% methanol / water, 70% ethanol / water and 70% acetone / water as extraction solvents respectively. The extract of / water has significant inhibitory effect to α-glucosidase equally, therefore can obtain the α-glucosidase in Dendrobium officinale equally with different concentrations of ethanol / water, methanol / water or acetone / water as extraction solvent Inhibitory ingredients. The results are shown in Table 2.

[0091] Table 2. The inhibitory effect of different solvent extracts of Dendrobium officinale on α-glucosidase (IC 50 ).

[0092]

[0093]

[0094] n=3

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Abstract

The invention provides application of fluorenone compounds in dendrobe for preparing a drug for treating diabetes, and particularly provides application of a fluorenone compound shown in a formula I.The compound can be used for a hypoglycemic drug, a hypoglycemic healthcare food or a hypoglycemic food. In the formula I, R1 and R2 are -H or -OH or -OCH3. The fluorenone compound is a natural compound existing in dendrobe and has the high alpha-glucosidase inhibitory activity, and the compound is adopted as the active ingredient and prepared into the hypoglycemic drug or the drug compound with pharmaceutically-acceptable carriers or accessories.

Description

technical field [0001] The invention relates to the use of fluorenone compounds in Dendrobium in the preparation of anti-diabetic drugs, in particular to the preparation of fluorenone compounds that can be isolated from Dendrobium candidum (such as Dendrobium candidum, Dendrobium nobile and Dendrobium chrysalis) Use in prevention and treatment of antidiabetic drugs. Background technique [0002] Diabetes has become a common and frequently-occurring disease that seriously affects human health. According to the statistics of the International Diabetes Federation (IDF), in 2015, about 415 million people aged 20-79 in the world suffered from diabetes (8.8% prevalence rate), and another 318 million people had impaired glucose tolerance (6.7% prevalence rate in the early stage). ). China is the country with the largest number of diabetic patients in the world. In 2015, the number of patients reached 109.6 million, and 1.3 million people died of diabetes and its complications. A...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/122A61P3/10A61P9/10A61P13/12A61P27/12A61P25/02A61P25/00A61P9/00A61K36/8984
CPCA61K31/122A61K36/8984A61P3/10A61P9/00A61P9/10A61P13/12A61P25/00A61P25/02A61P27/12
Inventor 刘宏程黄相中黎其万杨淬田凯李育晓
Owner INST OF QUALITY STANDARD & DETECTION TECH YUNNAN ACAD OF AGRI SCI
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