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A kind of sesquiterpene compound and its preparation and application

A sesquiterpene and compound technology, applied in the field of α-glucosidase inhibitors, can solve the problems of weak activity and high adverse reaction rate, and achieve the effect of small molecular weight and low dosage

Active Publication Date: 2018-02-02
ZHEJIANG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The purpose of the present invention is to overcome the shortcomings of existing α-glucosidase inhibitors such as weak activity and high adverse reaction rate, and provide two compounds with strong α-glucosidase inhibitory activity and their preparation and application

Method used

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  • A kind of sesquiterpene compound and its preparation and application
  • A kind of sesquiterpene compound and its preparation and application
  • A kind of sesquiterpene compound and its preparation and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] The preparation method of embodiment 1 compound 1

[0021] 1. Preparation of Penicillium extensa ferment by fermentation culture

[0022] 1) Strain: Penicillium expansum, purchased from China Agricultural Microorganism Culture Collection and Management Center, the strain number is 1511C0001ACCC37275.

[0023] 2) Cultivation and storage on slant

[0024] Solid medium: glucose 3g, potato extract powder 0.5g, KH 2 PO 4 0.2g, 1.5g agar, add water to 100mL, pH value is natural.

[0025] Solid culture method: Penicillium expanses strains are inoculated on a solid medium slant, and cultivated at 28°C for 5-7 days. After the solid culture is over, place the slant at 4-10°C and refrigerate for later use. Preparation of 30% glycerol cryovials: Under aseptic conditions, wash the slant of the test tube with 6ml of sterilized 30% glycerin, dispense into glycerol tubes (3ml / branch), and store at -20°C for later use.

[0026] 3) Shake flask seed culture

[0027] Medium: glucose...

Embodiment 2

[0044] Physicochemical properties and spectral data of embodiment 2 compound 1

[0045] Compound 1: white amorphous powder; molecular formula is C 15 h 20 o 4 ;Optical rotation [α] -36.7 (c0.15, MeOH); infrared v max 3441,2923,2583,1745,1649,1462,1356,1266,1208,1144,1064,996,923,883,848,762,722,690cm -1 ; Hydrogen spectrum and carbon spectrum are shown in Table 1; High resolution mass spectrum (ESI) m / z: 265.1426[M+H] + .

[0046] Table 1 NMR data of compound 1

[0047]

[0048]

Embodiment 3

[0049] The α-glucosidase inhibitory activity of embodiment 3 compound 1

[0050] 25 μL, 0.085U / mL α-glucosidase potassium phosphate buffer solution (pH 6.8) and 100 μL potassium phosphate buffer solution (pH 6.8) containing different concentrations (0.48, 0.24, 0.12, 0.06, 0.03mg / mL) of compound 1 Add it into a 96-well plate, mix well, (add 80 μL 1.0M Na 2 CO 3 aqueous solution to terminate the reaction), and incubated at 37°C for 15min. Add 25 μL of 5.0 mM 4-nitrophenol-β-D-glucopyranoside (pNPG) potassium phosphate buffer, incubate at 37°C for 30 min, then add 80 μL of 1.0M Na 2 CO 3 The aqueous solution terminates the reaction, reads the absorbance value at 405nm and calculates the inhibition rate with a microplate reader, and the inhibition rate=1-(A 测定 -A 测定背景 ) / (A 空白 -A 空白背景 ), where, A 测定背景 is the absorbance of the system when the sample to be tested is added but no enzymatic reaction occurs, A 空白背景 is the absorbance of the system when the sample to be tested i...

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Abstract

The invention discloses a sesquiterpenes compound and preparation and application thereof. Penicillium expansum is inoculated to a fermentation medium, fermentation cultivation is performed on the conditions of 25-28 DEG C and 150 rpm, a fermentation solution is taken for separation and purification, and the sesquiterpenes compound is obtained. The sesquiterpenes compound has the better alpha-glucosidase inhibitory activity compared with acarbose on sale, the activity is four times that of the acarbose, the molecular weight of the sesquiterpenes compound is small, and therefore the sesquiterpenes compound has the advantage of being small in dosage.

Description

(1) Technical field [0001] The present invention relates to an α-glucosidase inhibitor, in particular to a new sesquiterpene compound, its preparation method and its application in acting on α-glucosidase. (2) Background technology [0002] Diabetes mellitus is a metabolic disorder syndrome characterized by persistent hyperglycemia caused by polygenic inheritance and environmental factors. Its pathological features are manifested as insufficient insulin secretion or insulin resistance, leading to disorders of sugar, fat, protein, water, and electrolyte metabolism in the body. Surveys show that diabetes can cause acute or chronic complications such as heart, brain, liver, lung, kidney, and nerves. It is the third major disease that endangers human health after cardiovascular and cerebrovascular diseases and cancer. The high morbidity and disability rate of diabetes and its lifelong harm to human health are very serious and bring heavy economic burden to individuals and socie...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D493/10A61P3/10C12P17/18
CPCC07D493/10C12P17/181
Inventor 应优敏姚枫麒方成安占扎君单伟光
Owner ZHEJIANG UNIV OF TECH
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