Bischalcone compound as well as preparation method and application thereof
A technology of bis-chalcones and compounds, which is applied in the field of extraction and separation of traditional Chinese medicine, can solve problems such as the difficulty in finding active compounds in licorice and the complex chemical composition of licorice, and achieve good prospects, novel structure, and the effect of inhibiting the activity of carboxylesterase 2
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Embodiment 1
[0038] Embodiment 1: the preparation of compound 6 and compound 15
[0039]Take 10 kg of dry rhizome of licorice, add 50% volume fraction of methanol after pulverization, and reflux extract 3 times, each time for two hours, the amount of each extraction solvent is 10, 8, 6 times of the amount of medicinal materials, combine the extracts, and recover under reduced pressure The solvent was evaporated to dryness to obtain the extract, and the extract was redissolved in methanol with a volume fraction of 50% to obtain an extraction concentrate; 2 times the volume of the extraction concentrate was added to extract with n-heptane for 3 times, and after the organic solvent layers were combined, Concentrate to dryness under reduced pressure to obtain the n-heptane extract; the n-heptane extract was separated by normal phase silica gel column chromatography, and gradient eluted with dichloromethane:methanol at a volume ratio of 50:1-1:1, and the volume Fractions eluted at a ratio of 20...
Embodiment 2
[0050] Embodiment 2: activity screening experiment
[0051] Mix compound 6 and compound 15 with human carboxylesterase 2 respectively, and incubate with shaking at 37°C for 20 min, add the probe substrate to start the reaction, incubate with shaking at 37°C for 40 min, add an equal volume of acetonitrile, and stop the reaction after shaking vigorously. The 96-well plate was placed on a fluorescent microplate reader for fluorescence detection (Ex=308nm, Em=392, 528nm), and the fluorescence intensity was calculated. The fluorescence intensity ratio of the DMSO group was used to calculate the inhibitory intensity of human carboxylesterase 2 ( Figure 5 ).
[0052] Both compound 6 and compound 15 showed strong inhibitory activity against human carboxylesterase 2 (residual activity < 20%), and had good application prospects in adjuvant cancer therapy.
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