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A sesquiterpene compound, fungal secondary metabolite extract containing it and use thereof

A technology of secondary metabolites and sesquiterpenoids, which is applied in the field of medicine, can solve problems such as lipase inhibition that has not been seen yet, achieve good research and development prospects, inhibit lipase activity, and achieve high yield effects

Active Publication Date: 2021-11-09
INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Some polyspiroidal sesquiterpenoids with peculiar skeletons are rarely reported, and the research on the biological activity of such components mainly focuses on antibacterial and α-glucosidase inhibitory activities. Reports of lipase inhibition

Method used

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  • A sesquiterpene compound, fungal secondary metabolite extract containing it and use thereof
  • A sesquiterpene compound, fungal secondary metabolite extract containing it and use thereof
  • A sesquiterpene compound, fungal secondary metabolite extract containing it and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] The preparation of fungal secondary metabolite extract comprises the steps:

[0027] (1).

[0028] Preparation of strain liquid seed solution: The formula of the culture solution is 200g of potatoes, 10g of yeast extract, 6g of peptone, 30g of glucose, KH 2 PO 4 2g, MgSO 4 0.5g, dilute to 1L, adjust pH to 6.8. Pack into 500mL Erlenmeyer flasks, fill each bottle with about 150mL, sterilize at 115°C, 68kPa for 30 minutes. After being inoculated with the Penicillium purpurogenum IMM003 strain, culture it for 3 days at 28°C and 155 rpm. Then the culture solution was diluted 100 times and used as seed solution for future use.

[0029] (2) Strain solid fermentation: put 150g rice and 180mL purified water into a 1L Erlenmeyer flask, sterilize at 115°C, 68kPa for 30 minutes, inoculate Penicillium purpurogenum IMM003 seed solution, and cultivate at 28°C for 40 days. After soaking in 500 mL of ethyl acetate for 30 minutes, it was extracted three times by ultrasonic extrac...

Embodiment 2

[0031] The preparation of sesquiterpene compound comprises the steps:

[0032] The extract obtained in Example 1 was eluted by medium-pressure silica gel column chromatography (petroleum ether-acetone 50:1, 20:1, 5:1, 3:1, 0:1) to obtain components A-F. Select component B and then normal pressure silica gel column chromatography (petroleum-ether acetone 100:1, 50:1, 20:1, 10:1, 7:1, 5:1, 3:1, 2:1, 1:1 , acetone, methanol) to obtain component B1-11. Component B5 via Flash C 18 Column chromatography (20%, 30%, 50%, 70%, 90% methanol-water gradient elution) yielded components B5-1 to B5-5. B5-1 was purified by Sephadex LH-20 column chromatography to obtain compound 1 (45.0 mg). Component B7 via Flash C 18 Column chromatography (20%, 30%, 50%, 70%, 90% methanol-water gradient elution) yielded components B7-1 to B7-5. Component B7-1 was separated by HPLC semi-preparative chromatography (ES-C18 column, 75% methanol-water, 205 nm) to obtain compound 3 (19 min, 6.0 mg). B7-2 was...

experiment example 1

[0048] Experimental example 1: Evaluation of the inhibitory effect of fungal secondary metabolite extracts and compounds on pancreatic lipase activity

[0049] Instruments: metal incubator, vortex shaker, microplate reader

[0050] Reagent: including 0.1M Buffer (citric acid-disodium hydrogen phosphate) buffer (pH 7.4), 0.25mM 4-MUO (4-methylumbelliferone) and 1mg / ml lipase (dissolved in buffer)

[0051] Experimental steps:

[0052] 1) The microsome incubation system contains the following components (total volume 200μl):

[0053]

[0054] Table 3 lipase incubation system and addition amount

[0055]

[0056] 2) Add lipase+buffer+Inhibitor / DMSO to a black 96-well plate, shake and mix well, then place in a metal bath / water bath at 37°C for 10 minutes for pre-incubation;

[0057] 3) After adding 2 μl 4-MUO to start the reaction, perform fluorescence analysis, that is, kinetic detection with a fluorescent microplate reader, and the time is 30 minutes;

[0058] 4) Set up...

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PUM

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Abstract

The invention discloses a sesquiterpene compound with lipase inhibitory effect. This type of sesquiterpene compound has the structures shown in formula (I) and formula (II): experiments have proved that formula (I) and formula (II) of the present invention The lipase activity of the sesquiterpenoids shown in formula (II) has significant inhibitory effect, suggesting that the sesquiterpenoids shown in formula (I) and formula (II) can be used as blood lipid-lowering, anti-obesity drugs or health products, with Good prospects for research and development.

Description

technical field [0001] The invention belongs to the technical field of medicine, in particular to a sesquiterpene compound and a fungal secondary metabolite extract containing the sesquiterpene compound, and their use in the preparation of blood lipid-lowering, anti-obesity drugs or health care products. Background technique [0002] Obesity is one of the "diseases of civilization" brought about by the gradual improvement of people's material living conditions. Obesity and a series of cardiovascular diseases such as hypertension and hyperlipidemia caused by obesity have become one of the main hazards affecting people's health. . There are many reasons for obesity, such as genetic factors, environmental factors, eating habits, etc., among which high-fat diet is an important cause of obesity. Most weight-loss drugs on the market act on the brain and reduce the intake of food by controlling appetite, but because these drugs may affect the brain or nervous system, adverse react...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D493/20A61K31/365A61P3/06A61P3/04C12P17/18A23L33/10C12R1/80
CPCA23V2002/00A23L33/10A61P3/04A61P3/06C07B2200/07C07D493/20C12P17/181A23V2200/3262A23V2200/332A23V2250/208
Inventor 林生夏桂阳王玲燕张景芳王亚男夏欢
Owner INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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