Application of 12,15-dioxo-α-ostendene in pharmaceuticals
A kind of ostene, action technology, applied in the field of medicine
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Embodiment 1
[0017] Preparation process of compound PFC-37:
[0018] The dried agarwood (heartwood of Aquilaria sinensis (Lour.) Spreng.; 2.9kg) was pulverized, 90% ethanol was ultrasonically extracted at 60°C for 30min, and finally a concentrated crude extract (459.3g) was obtained. Then the extract was suspended in water, extracted with equal volumes of petroleum ether, ethyl acetate and n-butanol in turn, and the solvent was recovered to obtain 0.7 g of petroleum ether extract, 374.8 g of ethyl acetate extract, and 52.5 g of n-butanol extract .
[0019] The ethyl acetate extraction part (374.8g) was mixed with an equal amount of 80-100 mesh silica gel, and was segmented by normal phase silica gel column chromatography, the eluent was petroleum ether-ethyl acetate system (50:1, 30:1 , 20:1, 10:1, 5:1, 3:1, 2:1, 1:1, 0:1, v / v) gradient elution, followed by ethyl acetate-methanol system ( 5:1, 3:1, 2:1, 1:1, 0:1, v / v), the same components were combined by TLC to obtain 5 parts (Fr.Y-1~Fr...
Embodiment 2
[0025] The neuroprotective activity test method of compound PFC-37 is as follows:
[0026] 1. PC12 poorly differentiated cells were cultured in DMEM high glucose + 10% FBS + 100U / mL double antibody medium, incubator temperature 37°C, 5% CO 2 ;
[0027] 2. When PC12 poorly differentiated cells grow to an appropriate number, trypsin digestion to prepare a cell suspension;
[0028] 3. Aspirate the cell suspension into a 15mL centrifuge tube, 800rpm, 5min;
[0029] 4. After centrifugation, the centrifuge tube is sterilized with alcohol and taken into the ultra-clean bench, and the supernatant is poured into the waste liquid tank;
[0030]5. Add 5 mL of new complete medium, pipette ten times, and blow away the cells as much as possible, but not too hard;
[0031] 6. Take 0.02mL of cell suspension, add it to the cell counting plate, and count;
[0032] 7. Adjust the cell concentration to 1 × 10 5 cells / mL, added to 96-well plate, 0.1 mL per well, and cultured in a cell incubato...
Embodiment 3
[0041] Effect of neuroprotective activity of compound PFC-37:
[0042] The neuroprotective activity data of the compound PFC-37 are shown in Table 1. At the compound concentration of 1 μM and 2 μM, MPP + The induced PC12 cell injury had significant protective activity (P<0.001).
[0043] Table 1. Compound PFC-37 vs MPP + Protective effect of induced PC12 cell injury
[0044]
[0045] Notes to Table 1: Compared with the model group, **P<0.01, ***P<0.001.
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