Isobenzofuranone compounds as well as preparation method and application thereof
A compound, furanone technology, applied in the field of preparation of pharmaceutical compounds, can solve the problem of lack of specific drugs, achieve significant inhibitory activity, broad application prospects, and simple methods
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Embodiment 1
[0026] Compounds 1 and 2 of the present invention can be obtained from marine fungi Penicillium It is isolated from the fermentation broth of sp.HN29-3B1. Penicillium marine fungus Penicillium sp.HN29-3B1 was isolated from the stem of the mangrove plant Cerbera manghas in Dongzhaigang Mangrove National Nature Reserve, Hainan Island. Penicillium marine fungus Penicillium The sp. HN29-3B1 strain was deposited in the China Center for Type Culture Collection on December 8, 2013 at Wuhan University, Wuhan, China, with the accession number CCTCC M 2013637.
[0027] Specific steps are as follows:
[0028] S1. Seed cultivation:
[0029] S11. Prepare seed medium: glucose 40g, peptone 4g, yeast extract 4g, sea salt 5g, tap water 2000mL, evenly distribute in 8 500mL Erlenmeyer flasks, extinguish at 121°C for 25 minutes.
[0030] S12. Cultivation of seeds: the marine fungi Penicillium The sp.HN29-3B1 strain was inoculated into the seed culture medium, and cultured on a sha...
Embodiment 2
[0036] The compound in embodiment 1 is carried out structural analysis test, obtains following physical and chemical property data:
[0037] Compound 1: white solid, melting point >195-197oC (thermometer uncalibrated), EI-MS (m / z): 288 [M] + ; HR-EI-MS (m / z): 288.0626[M] + (theoretical value 288.0628).
[0038]Compound 2: white solid, melting point 157-158oC (thermometer uncalibrated), EI-MS (m / z): 346 [M] + , HR-EI-MS (m / z): 346.1056[M] + (Theoretical value 346.1047).
[0039] The NMR data of compounds 1 and 2 are shown in Table 1.
[0040] Table 1 NMR data of compounds 1 and 2 (100MHz / 400MHz, TMS, ppm)
[0041]
[0042] After the above data analysis, the structural formulas of compound 1 and compound 2 are obtained, and the structural formulas of compound 1 and compound 2 are shown in formula (I):
[0043] .
[0044] The single crystal of compound 2 was analyzed by single crystal-X diffraction, and the crystal structure of compound 2 was measured as figure...
Embodiment 3
[0048] Compound 1,2 in embodiment 1 is carried out α-glucosidase inhibition test:
[0049] Using p-nitrophenol-α-glucoside (pNPG) as the substrate, carried out in 0.01M phosphate buffer (pH7.0). 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 400nm with a UV-visible spectrophotometer. Both the sample and the positive control (resveratrol) were made into DMSO solution (both 10 μmol / mL), and the enzyme and substrate were made into a suitable concentration solution with 0.01M phosphate buffer, and 1 mL of the initial reaction system contained 0.1 unit of enzyme. 20 μL substrate, 20 μL DMSO. Take an appropriate amount of enzyme solution, add the blank DMSO solution or sample DMSO solution, mix well, keep the temperature at 37°C for 20 minutes, add the substrate, mix well, and immediately detect the change value of the absorbance of the system within 1min at a...
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