Inonotus obliquus alcohol F and application thereof in preparation of alpha-glucosidase inhibitor drugs

A technology of Inonotus obliquus alcohol and glucosidase, applied in the preparation of α-glucosidase inhibitor drugs, in the field of triterpenoids, can solve problems such as toxic side effects and heart system risks, and achieve postprandial control blood sugar effect

Active Publication Date: 2021-03-19
GUANGDONG INST OF MICROBIOLOGY GUANGDONG DETECTION CENT OF MICROBIOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The α-glucosidase inhibitors currently on the market are mainly acarbose, voglibose, miglitol, etc., but it is worth noting that these inhibitors currently used have brought different Degree of toxic side effects, such as gastrointestinal side effects, urticaria, liver dysfunction, cardiac system risk, etc.

Method used

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  • Inonotus obliquus alcohol F and application thereof in preparation of alpha-glucosidase inhibitor drugs
  • Inonotus obliquus alcohol F and application thereof in preparation of alpha-glucosidase inhibitor drugs
  • Inonotus obliquus alcohol F and application thereof in preparation of alpha-glucosidase inhibitor drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Embodiment 1: the preparation of inonotofaciol F

[0027] Take 5 kg of dried sclerotia of Polyporaceae fungus Ganoderma lucidum (Inonotus obliquus), crush it, and heat (80°C) reflux extraction with 10 times the amount (mass / volume, g / mL) of 95% ethanol for 2 times. After 2 hours, the extracts were combined and concentrated under reduced pressure to 1 / 20 of the original volume to obtain IO; 3 times the amount of ethyl acetate was added to extract twice to obtain the ethyl acetate extract IO-EA. IO-EA was dissolved with 2 times the amount (mass / volume, g / mL) of chloroform methanol (1:1 v / v) solution, and evenly mixed into the silica gel. After the solvent was evaporated, the adsorbed ethyl acetate extract IO-EA Silica gel is added to the top of the adsorbent in the chromatographic column for silica gel column chromatography separation, with chloroform-methanol at a volume ratio of 100:0, 98:2, 95:5, 90:10, 80:20, 70:30 , 50:50 and 0:100 as the eluent gradient elution, co...

Embodiment 2

[0028] Embodiment 2: the preparation of inonotofaciol F

[0029] Inonotus obliquus mycelium was inoculated on PDB medium, and cultured at 25°C with 200r / min shaking for 7 days to prepare seed liquid, and then inoculated into 20 Erlenmeyer flasks containing rice medium according to 5% inoculation amount, and cultured statically at 25°C On 45d, the fermented product was obtained. The rice culture medium is composed of the following components: 70g / bottle of rice, 100mL / bottle of purified water, which is prepared by adding 70g of rice into a bottle filled with 100ml of water and sterilizing. The fermented product was added to ethyl acetate for soaking and ultrasonic extraction for 3 times, and the extract was concentrated to dryness under reduced pressure to obtain a crude extract. The crude extract was passed through a silica gel column, eluted with cyclohexane and methanol, and the fraction eluted with methanol was collected and concentrated to dryness. Then carry out medium ...

Embodiment 3

[0036] Example 3: In vitro inhibition of α-glucosidase activity test of Inonotolidinol F

[0037] Prepare a series of test sample solutions with different concentrations in advance (dissolve in a small amount of DMSO, dilute to the corresponding concentration with distilled water, control the final volume fraction of DMSO2 CO 3 (1M) Terminate the reaction, and measure the absorbance at a wavelength of 405 nm. A blank group was set up in the experiment at the same time: use 10 μL of phosphate buffer (50 mM, pH7.0) instead of the test sample solution; blank control group: use 10 μL of phosphate buffer (50 mM, pH7.0) instead of the test sample solution, At the same time, 50 μL of phosphate buffer (50 mM, pH 7.0) was used to replace the aqueous solution of α-glucosidase; sample control group: 50 μL of phosphate buffer (50 mM, pH 7.0) was used to replace the aqueous solution of α-glucosidase. Each of the above experimental groups was repeated three times, and the results were aver...

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Abstract

The invention discloses inonotus obliquus alcohol F and application thereof in preparation of an alpha-glucosidase inhibitor drug. The structural formula of the inonotus obliquus alcohol F is shown asa formula (I). The inonotus obliquus alcohol F is separated from inonotus obliquus or a fermentation culture of the inonotus obliquus, the inonotus obliquus alcohol F has remarkable alpha-glucosidaseinhibition activity, the inhibition mode of the inonotus obliquus alcohol F on the alpha-glucosidase activity is a typical non-competitive inhibitor, and the inonotus obliquus alcohol F is more beneficial to control of postprandial blood sugar of diabetics compared with a competitive inhibitor. Therefore, the compound can be used for preparing medicines for treating diabetes.

Description

Technical field: [0001] The invention belongs to the field of natural medicines, and in particular relates to the triterpenoid compound obliqurol F and its application in the preparation of α-glucosidase inhibitor drugs. Background technique: [0002] Diabetes is a common clinical disease caused by the lack or relative lack of insulin in the human body. The World Health Organization (WHO) divides diabetes into two types: type I diabetes (or insulin-dependent, IDDM) and type II diabetes (or insulin-dependent diabetes mellitus). called non-insulin-dependent, NIDDM). Among them, type 2 diabetes accounts for the majority. There are more than 20 million diabetic patients in my country, and nearly 90% of them are type 2 diabetes, and it appears multiple and younger, which seriously threatens national health. [0003] α-glucosidase is a hydrolase of maltose, sucrose or other oligosaccharides in the small intestine. The hydrolysis eventually produces glucose, which is absorbed into...

Claims

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Application Information

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IPC IPC(8): C07J19/00A61P3/10A61K31/585
CPCC07J19/00A61P3/10
Inventor 陈少丹吴清平雍天乔高雄关小莺谢意珍肖春李向敏胡惠萍陈地灵潘鸿辉
Owner GUANGDONG INST OF MICROBIOLOGY GUANGDONG DETECTION CENT OF MICROBIOLOGY
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