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Aromatic polyol compound and preparation method and application thereof

An aromatic polyol and compound technology, which is applied in the field of medicine and achieves the effect of inhibiting the decomposition of starch into glucose in the body, with high safety and reducing postprandial blood sugar.

Pending Publication Date: 2021-12-10
国科特膳江苏生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These two drugs are chemically synthesized α-glucosidase inhibitors, which will cause obvious adverse reactions such as digestive tract

Method used

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  • Aromatic polyol compound and preparation method and application thereof
  • Aromatic polyol compound and preparation method and application thereof
  • Aromatic polyol compound and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] The aromatic polyol compounds provided in this example are compound 1 (AGI-6481) and compound 2 (AGI-4433) shown in formula I, and the molecular formula of compound 1 is C 21 h 20 o 10 , the structural formula is 1 in formula I, and the molecular formula of compound 2 is C 21 h 18 o 10 , the structural formula is 2 in formula I.

[0026]

[0027] 3 mM pNPG and p-nitrophenyl-β-D-glucopyranoside were used as reaction substrates. Add different concentrations of AGI-6481, AGI-4433, acarbose, voglibose and various sources of glucosidase into the phosphate buffer, react with the substrate at 25°C for 10 minutes, add the color reagent, Measure absorbance and calculate IC50. IC50 is defined as the concentration that inhibits glucosidase activity by 50% under the given conditions. As shown in Table 1, the aromatic polyol compound provided in this example can inhibit glucosidase from different sources, and the effect is similar to that of acarbose and voglibose.

[002...

Embodiment 2

[0037]The specific preparation process of the aromatic polyol compound in Example 1 is as follows, including the following steps: stirring and extracting 2kg of dried chili leaf powder with 20L of 70% ethanol at room temperature for 12 hours, and concentrating the extract under reduced pressure to obtain a total extract of 682.7 g. After the first extract obtained in this way was suspended in distilled water, an equal amount of methylene chloride and ethanol were added, and the mixture was fully shaken and stirred. The fractions were allowed to stand. After taking the organic solvent layer (dichloromethane-ethanol), an equal amount of dichloromethane was added and fractional distillation was carried out in the same manner. The organic solvent layer thus obtained was collected by rotary concentration under reduced pressure to obtain the first active fraction (144.6 g). A certain amount of the active part thus obtained is suspended in distilled water, only dichloromethane is a...

Embodiment 3

[0040] Such as Figure 5 As shown, 24 SD male rats were fasted for 12 hours and divided into four groups: control group, 10mg / kg AGI-4433, 30mg / kg AGI-4433, 2.5mg / kg acarbose orally, each group of rats At the same time, 2 mg / kg of sucrose was orally administered, and the rats in each group had similar fasting blood glucose levels before administration, and the blood glucose values ​​of each group were measured before administration, 30, 60, 90, and 120 minutes after administration. The aromatic polyol compound AGI-4433 in Example 1 can reduce postprandial blood sugar in rats, comparable to acarbose.

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PUM

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Abstract

The invention belongs to the technical field of medicines, and particularly relates to an aromatic polyol compound and a preparation method and application thereof. The aromatic polyol compound comprises a compound 1 and a compound 2, wherein the molecular formula of the compound 1 is C21H20O10, and the molecular formula of the compound 2 is C21H18O10. The aromatic polyol compound is a natural compound separated and extracted from plants, and early-stage research shows that the aromatic polyol compound has the effect of inhibiting alpha glycosidase to delay decomposition of starch into disaccharide, and has the effect of inhibiting sucrase and maltase to delay decomposition of disaccharide into glucose. Based on the effects, the compound can effectively inhibit the process of decomposing in vivo starch into glucose, reduces postprandial blood sugar, has extremely high safety, and does not have obvious adverse reaction.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an aromatic polyol compound and a preparation method and application thereof. Background technique [0002] After the human body eats, the starch (polysaccharide) in the food must be decomposed into glucose to be absorbed by the human body. In this process, the catalysis of α-glucosidase and disaccharidase is required to effectively complete this process. After glucose is absorbed into the blood, the postprandial blood sugar rises. Diabetic patients need to control both postprandial and fasting blood sugar at the same time. [0003] Similar hypoglycemic drugs currently on the market are acarbose (such as Bayer's Baitangping) and voglibose. These two drugs are chemically synthesized α-glucosidase inhibitors, which can cause obvious adverse reactions such as the digestive tract. Contents of the invention [0004] Aiming at the deficiencies of the above-mentioned pr...

Claims

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Application Information

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IPC IPC(8): C07H17/07C07H1/08C07D407/12A61P3/10A61K31/7048A61K31/366
CPCC07H17/07C07H1/08C07D407/12A61P3/10
Inventor 万冬梅朱雁军
Owner 国科特膳江苏生物科技有限公司
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