Application of alkaloid compound in preparation of anti-obesity medicine

A technology of alkaloids and compounds, applied in biochemical equipment and methods, microorganisms, drug combinations, etc., can solve the problem of no research report on biological activity, and achieve the effect of inhibiting fat accumulation and good anti-obesity function.

Active Publication Date: 2020-11-24
ZHOUKOU NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there are few literature reports on the biological activities of these compounds, especially the biological activities in regulating lipid metabolism and anti-obesity.

Method used

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  • Application of alkaloid compound in preparation of anti-obesity medicine
  • Application of alkaloid compound in preparation of anti-obesity medicine
  • Application of alkaloid compound in preparation of anti-obesity medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Example 1: Microbial fermentation culture and preparation of compounds

[0044] 1. Fermentation culture and extraction of fermented product

[0045] 1) Production strains

[0046] In this example, the strain used to produce compound I by fermentation is Aspergillus terreus isolated from the digestive tract of Pacific oyster ( Aspergillus terreus ) ML-44 strain, which is preserved in China General Microorganism Culture Collection Center (CGMCC), and the preservation number is CGMCC No. 15664.

[0047] 2) Fermentation culture

[0048] According to the routine method of microbial culture, take out Aspergillus from the refrigerator at 4°C ( Aspergillus terreus ) ML-44 test tube slant, scrape appropriate amount of spores with an inoculation loop under sterile conditions, and inoculate them in 5 newly prepared PDA solid medium (composition: glucose 2%, agar 2%, NaCl 1.5%, with 20 % potato boiled liquid) on the plate, activated and cultured in an incubator at 28°C for 5 da...

Embodiment 2

[0058] Example 2: Compound I inhibits the adipogenic differentiation of C3H10T1 / 2 cells

[0059] 1) The growth inhibitory effect of compound I on C3H10T1 / 2 cells

[0060] The effect of compound I on the viability of C3H10T1 / 2 cells was detected by MTT assay. Take C3H10T1 / 2 cells in the logarithmic growth phase, and use fresh DMEM medium to prepare a cell density of 2×10 5 cells / ml cell suspension, inoculated in 96-well plate, 200 μl per well, after 12 hours of incubation at 37°C, 2 μl of sample solution was added to each well of the sample group, and 2 μl of methanol was added to each well of the blank control group. Treat at 37°C for 48 h. Add 20 μl of pre-cooled 5 mg / ml MTT solution (prepared in PBS solution) to each well, incubate at 37°C for 4 h, centrifuge at 4°C and 2000 rpm for 10 min, suck off the supernatant, and add 150 μl to each well μl DMSO, placed on a microplate reader and oscillated sufficiently to completely dissolve the purple MTT product, and measure the ...

Embodiment 3

[0063] Example 3: Compound I inhibits the occurrence of obesity in male Drosophila induced by high fat

[0064] Three-day-old male Drosophila were divided into three groups. The control group was cultured with basic medium, the HFD-induced group was given high-fat medium (basic medium with 15% lard), and the treatment group was given high-fat medium supplemented with compound I. Lipid medium (final concentration 0.1mg / ml) was treated continuously for 20 days, and the body weight of Drosophila in each group was detected. Depend on figure 2 The results of the middle test show that the weight of Drosophila can be significantly increased by culturing in high-fat medium to form obese Drosophila; at the same time, the treatment of compound I can significantly inhibit the obesity of Drosophila induced by HFD.

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Abstract

The invention relates to a use of an alkaloid compound in preparing an anti-obesity drug. The alkaloid compound or a pharmaceutically acceptable salt thereof is of a structure shown as a formula I; and the invention relates to a use of structural analogs alone or in the form of a composition in preparing the anti-obesity drug. Fermentation culture is performed on aspergillus terreus ML-44 from seato acquire a leavening containing a compound shown in the formula I, and separation and purification are performed on the leavening to obtain the compound shown in the formula I, wherein as for the aspergillus terreus ML-44, a preservation number is CGMCC No. 15664, a preservation date is 17 April, 2018, and a preservation place is China General Microbiological Culture Collection Center (CGMCC).By adopting the use provided by the invention, the compound and the structural analogs thereof have the anti-obesity activity, a lead compound is provided to develop a novel anti-obesity drug. (The formula I is described in the description).

Description

technical field [0001] The invention relates to the use of an alkaloid compound in the preparation of anti-obesity medicine. Background technique [0002] With the development of society and economy, the incidence of obesity in my country is increasing year by year, and the number of patients has increased from 2.4 million in 1975 to more than 90 million in 2014, accounting for 14.3% of the obese population in the world (NCD Risk Factor Collaboration, Trends in adult body- mass index in 200 countries from 1975 to 2014: a pooled analysis of 1698 population-based measurement studies with 19•2 million participants. The Lancet, 2016, 387, 1377–1396). Obesity is closely related to the occurrence of a series of chronic diseases such as type II diabetes, cardiovascular and cerebrovascular diseases, and cancer (Smith and Minson, Obesity and adipokines: effects on sympathetic overactivity. J Physiol, 2012, 590, 1787–1801; Singer and Lumeng, The initiation of metabolic inflammation in...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D213/82A61K31/455A61P3/04C12P17/12C12R1/66
CPCA61P3/04C07D213/82C12P17/12
Inventor 刘晓萌吴长景杨明生崔香毛建航李凤
Owner ZHOUKOU NORMAL UNIV
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