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Mangrove endophytic fungi-derived bisabolane sesquiterpenoids, preparation method thereof and application in anti-type II diabetes drugs

A technology of bisabolane sesquiterpenes and endophytic fungi, which can be applied in the fields of drug combination, metabolic diseases, organic chemistry, etc., can solve the problems of high preparation cost and side effect limitation.

Active Publication Date: 2018-12-28
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Because the high preparation cost and adverse side effects limit their clinical application, it is imperative to design or screen out less side effects, easy to synthesize, and low-cost α-glucosidase inhibitors

Method used

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  • Mangrove endophytic fungi-derived bisabolane sesquiterpenoids, preparation method thereof and application in anti-type II diabetes drugs
  • Mangrove endophytic fungi-derived bisabolane sesquiterpenoids, preparation method thereof and application in anti-type II diabetes drugs
  • Mangrove endophytic fungi-derived bisabolane sesquiterpenoids, preparation method thereof and application in anti-type II diabetes drugs

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0011] The compounds 1 and 2 of the present invention are isolated from the fermentation liquid of the mangrove endophytic fungus Aspergillus flavusQQSG-3. Aspergillus flavusQQSG-3, an endophytic fungus of mangrove forests, was isolated from the trunk of mangrove plant Kandeliaobovata in Huizhou, Guangdong. The preservation unit of the marine fungus Aspergillus flavusQQSG-3 strain is the Guangdong Provincial Microbiological Culture Collection Center, the preservation address is the Guangdong Institute of Microbiology, China, the preservation number is GDMCC No: 60380, and the preservation date is May 25, 2018 . Specific steps are as follows:

[0012] 1. Seed culture:

[0013] (1) Preparation of seed culture medium: Weigh 72g of potato dextrose water and 1800mL of tap water, distribute them evenly in six 500mL Erlenmeyer flasks, and extinguish at 121°C for 25 minutes.

[0014] (2) Seed cultivation: the mangrove endophytic fungus Aspergillus flavusQQSG-3 was inserted into the...

Embodiment 2

[0021] The compound in embodiment 1 is carried out structural analysis test, obtains following physical and chemical property data:

[0022] Compound 1: Pale yellow oil, EI-MS (m / z): 339[M-H] - ; HR-EI-MS (m / z): 339.19631[M-H] - (theoretical value 339.19657).

[0023] Compound 2: Pale yellow oil, EI-MS (m / z): 485 [M-H] - ; HR-EI-MS (m / z): 485.32715[M-H] - (theoretical value 485.32725).

[0024] The NMR data of compounds 1 and 2 are shown in Table 1 and Table 2.

[0025] NMR data of compound 1 in table 1 (125MHz / 500MHz, TMS, ppm)

[0026]

[0027]

[0028] Table 2 NMR data of compound 2 (125MHz / 500MHz, TMS, ppm)

[0029]

Embodiment 3

[0031] Compound 1 and 2 in embodiment 1 are carried out α-glucosidase inhibition experiment:

[0032] Using p-nitrophenol-α-glucoside (pNPG) as a substrate, it was carried out in 0.01M phosphate buffer (pH=7.0). pNPG was enzymatically hydrolyzed into p-nitrophenol by α-glucosidase, and the enzyme activity was calculated by measuring the change of its absorbance at a wavelength of 405nm with a UV-Vis spectrophotometer. Both the sample and the positive control (acarbose) were made into DMSO solution (both 5000 μM), and the enzyme and substrate were made into 0.2 units / ml and 5 mM with 0.01M phosphate buffer, respectively.

[0033] Method: Add 60 μl phosphate buffer solution, 20 μl glucosidase solution, and 10 μl sample (DMSO) to 100 μl reaction system in sequence. After standing at 37° C. for 10 minutes, 10 μl of substrate was added, and then standing at 37° C. for 20 minutes, and the absorbance of the system was detected immediately at a wavelength of 405 nm. Use the followin...

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Abstract

The invention discloses mangrove endophytic fungi-derived bisabolane sesquiterpenoids, a preparation method thereof and an application in anti-type II diabetes drugs. The structural formula of the bisabolane sesquiterpenoids is shown as the formula (I). Compounds 1 and 2 can significantly inhibit the activity of alpha-glucosidase with IC50 values of 4.5 MuM and 3.1 MuM respectively, and the positive control acarbose IC50 is 840.2 MuM. Therefore, such compounds can be used for developing alpha-glucosidase inhibitor drugs for prevention and treatment of type II diabetes.

Description

technical field [0001] The invention relates to the field of pharmaceutical compounds, in particular to the application of bisabolyl sesquiterpenoids in the preparation of α-glucosidase inhibitor drugs. Background technique [0002] Diabetes is a metabolic disease characterized by hyperglycemia and hyperlipidemia. According to the IDF Diabetes Atlas, about 425 million adults worldwide suffer from diabetes in 2017, which is a recognized worldwide disease. According to different pathogenesis, it is generally divided into type I diabetes (insulin-dependent) and type II diabetes (non-insulin dependent). α-Glucosidase is a hydrolase, which is an important target for the treatment of type II diabetes. Its function is to catalyze the last step in the digestion process of carbohydrates in the body, and hydrolyze oligosaccharides into monosaccharides, which in turn leads to blood sugar in the human body. level of improvement. Therefore, inhibiting the activity of α-glucosidase, pre...

Claims

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Application Information

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IPC IPC(8): C07C39/21C07C43/178A61P3/10
CPCA61P3/10C07C39/21C07C43/1783
Inventor 佘志刚吴颖楠刘昭明黄锡山
Owner SUN YAT SEN UNIV
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