Icaritin derivative and its preparation method and use
A technology of icariin and its derivatives, applied in the field of biomedicine, can solve the problems affecting the bioavailability of icariin and the reduction of icariin's water solubility, and achieve the effect of good water solubility and wide application prospects
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Embodiment 1
[0028] Add icariin, 2-bromoethanol, and anhydrous potassium carbonate into a round-bottomed flask at a ratio of 1:4:4, absorb an appropriate amount of dry acetone to dissolve, reflux and stir at 56°C for 8 hours, and use a thin layer Chromatography was detected with chloroform-acetone developer with a volume ratio of 20:1, and the completion of the reaction was judged by the presence of no reactant icariin on the thin-layer chromatography plate. After the reaction was completed, the solution was concentrated to dryness under reduced pressure at 30-40°C, dissolved in ethyl acetate, and then extracted with 1% aqueous hydrochloric acid and distilled water successively, the ethyl acetate layer was dried with anhydrous sodium sulfate and filtered, and the filtrate was concentrated to obtain Crude product 1.5 g.
[0029] Put the crude product on a 200-300 mesh silica gel column, elute with a gradient of chloroform-acetone volume ratio 40:1, 20:1, and 10:1, and develop the chloroform...
Embodiment 2
[0038] Add icariin, 3-bromopropanol, and anhydrous potassium carbonate in a molar ratio of 1:4:4 into a round-bottomed flask, absorb an appropriate amount of dry acetone to dissolve, reflux and stir at 56°C for 8 hours, and use thin-layer chromatography Chromatography was detected with chloroform-acetone developer with a volume ratio of 20:1, and the completion of the reaction was judged by the absence of the reactant icariin on the thin-layer chromatography plate. After the reaction was completed, the solution was concentrated to dryness under reduced pressure at 30-40°C, dissolved in ethyl acetate, and then extracted with 1% aqueous hydrochloric acid and distilled water successively, the ethyl acetate layer was dried with anhydrous sodium sulfate and filtered, and the filtrate was concentrated to obtain Crude product 1.8 g.
[0039] Put the crude product on a 200-300 mesh silica gel column, elute with a gradient of chloroform-acetone volume ratio 40:1, 20:1, and 10:1, and de...
Embodiment 3
[0048]The logarithmic growth of human breast cancer cells MCF-7, MDA-MB-435s, lung cancer cells A549 and African green monkey kidney cells Vero was added to a 96-well plate, and 100 μL per well contained about 1000 cells. Then add compound 1 and compound 2 obtained in the above examples 1-2 respectively, and add icariin and tamoxifen as controls, set 3 parallel wells in each group, and culture them in a carbon dioxide incubator at 37°C for 72 hours, before the end of the experiment Add 20 μL of MTT (5 mg / mL) solution for 4 hours, cultivate for another 4 hours, discard the culture solution and add 0.15 mL of DMSO. After the crystals are dissolved, detect the OD value of each well at a wavelength of 570 nm on an enzyme-linked detector. Calculate the growth inhibition rate according to the following formula, and then calculate the half inhibitory concentration (IC) by SPSS (13.0) software 50 value).
[0049]
[0050] The results are shown in Table 1, where IC 50 Expressed as...
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