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Alpha-glucosidase inhibitor and application thereof

A technology of glucosidase and inhibitor, which is applied in the field of medicine to achieve the effects of inhibitory activity, low toxicity and enhanced inhibitory activity

Active Publication Date: 2020-11-06
WUYI UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no relevant report on the application of cinnamic acid and magnolol derivatives to inhibit glucosidase.

Method used

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  • Alpha-glucosidase inhibitor and application thereof
  • Alpha-glucosidase inhibitor and application thereof
  • Alpha-glucosidase inhibitor and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Embodiment 1: α-glucosidase inhibitor and its preparation

[0047] The α-glucosidase inhibitors in the embodiments of the present invention are all cinnamic acid-magnolol derivatives, and the structural formula of cinnamic acid-magnolol derivatives is:

[0048]

[0049] Among them, R 1 independently selected from a hydrogen atom, an alkyl group, an alkoxy group, a halogen, a haloalkyl group or a hydroxyl group; R 1 Located in the ortho, meta or para position of the benzene ring.

[0050] Specifically, in the embodiments of the present invention, the compounds listed in the following Table 1 are included (respectively denoted as 4a~4j and 5a~5j):

[0051] Table 1. Cinnamic Acid-Magnolol Derivatives

[0052]

[0053] In the present invention, "2-" corresponds to the ortho position of the benzene ring, "3-" corresponds to the meta position of the benzene ring, and "4-" corresponds to the para position of the benzene ring.

[0054] The compound of 4a~4j in table 1...

Embodiment 2

[0086] Embodiment 2: α-glucosidase inhibitory activity test of compound

[0087] 1. Microplate method to verify the inhibitory activity of α-glucosidase in vitro:

[0088] 1.1 Principle: α-glucosidase catalyzes the hydrolysis of 4-nitrophenyl-α-D-glucopyranoside (PNPG) to produce nitrophenol (PNP, yellow substance with maximum absorption at 405nm), α-glucosidase The inhibitor can inhibit the combination of α-glucosidase and the substrate to reduce the release of PNP, and the enzyme inhibitory activity of the extract is calculated by the change of PNP content in the reaction system within a certain period of time.

[0089] (1) Preparation of 100mM phosphate buffer solution (PBS) with pH 6.8: Mix and dissolve 17.907g of disodium hydrogen phosphate and 6.804g of potassium dihydrogen phosphate respectively, then add deionized water to make up to 1L, and use a pH meter to Measure the pH.

[0090] (2) Preparation of cinnamic acid-magnolol series derivative solution: Weigh a certai...

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Abstract

The invention discloses an alpha-glucosidase inhibitor and application thereof. The alpha-glucosidase inhibitor comprises a compound with the following structural formula: R1 is independently selectedfrom a hydrogen atom, an alkyl group, an alkoxy group, halogen, a halogenated alkyl group or a hydroxyl group; R1 is located at the ortho-position, meta-position or para-position of a benzene ring. The active component of the inhibitor is a cinnamate-magnolol derivative, and the cinnamate-magnolol derivative has relatively strong alpha-glucosidase inhibition activity which can be about 25-50 times that of acarbose, and the inhibitor can be used for treating or adjunctively treating diabetes mellitus II, and has good potential medical and health-care values.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to alpha-glucosidase inhibitors and applications thereof. Background technique [0002] Diabetes is a metabolic, lifelong disease, and its complications seriously threaten human health. Diabetes is a series of metabolic disorders of protein, fat, water and electrolytes caused by insufficient insulin secretion and other reasons, among which hyperglycemia is the main symbol. In recent years, the prevalence of diabetes has been relatively high, and it has become the third largest chronic disease that seriously endangers human health after tumors and cardiovascular diseases. With the rapid development of my country's economy and society, changes in dietary structure and lifestyle, and the acceleration of population aging, the prevalence of diabetes is also showing a trend of rapid increase. While the prevalence of diabetes is rising rapidly, the awareness rate, treatment rate and con...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): B01J20/24B01J20/30C02F1/28C02F101/30
CPCB01J20/24C02F1/286B01J2220/485B01J2220/4812B01J2220/4806C02F2101/308
Inventor 徐学涛陈洁邓旭阳梁园赵曼宁李冬利张焜
Owner WUYI UNIV
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