A kind of ruthenium-artesunate complex and its preparation method and application
A technology of artesunate and complexes, which are applied in the field of ruthenium-artesunate complexes and their preparation methods and their antitumor effects, can solve the problems of poor water solubility, low bioavailability and limited application of artesunate tablets. and other problems, to achieve good anti-tumor activity and increase the effect of intake
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Embodiment 1
[0031] 7.6729mmol DIP, 3.836mmol RuCl 3 ·nH 2 O and 38.36mmol lithium chloride were placed in a three-necked flask, and 11mL of N,N-dimethylformamide was added, and reacted at 153°C for 8h under nitrogen protection. After the reaction was completed, the reaction solution was added dropwise to 150mL of ice acetone, , placed in a 4°C refrigerator overnight, suction filtered, and washed alternately with 4°C pre-cooled water and acetone to obtain cis-[Ru(DIP) 2 Cl 2 ]·2H 2 O;
[0032] Take 0.3144mmol cis-[Ru(DIP) 2 Cl 2 ]·2H 2O and 0.3144mmol 4-hydroxymethyl-4'-methyl-2-2'-bipyridine were placed in a three-necked flask, and 100mL of ethanol aqueous solution with a volume fraction of 75% was added, and reacted at 85°C for 8h under nitrogen protection, and the reaction was completed Afterwards, the reaction solution was fully concentrated to 10 mL, and 1.2576 mmol of ammonium hexafluorophosphate solid was added, and a large amount of precipitate was precipitated by ultrasonic...
Embodiment 2
[0037] Experimental test for antitumor activity of ruthenium-artesunate complex:
[0038] HepG2, A549R, and HeLa cells were respectively treated with DMEM medium containing 10% fetal bovine serum and 1% penicillin-streptomycin solution (10% fetal bovine serum and 1% penicillin-streptomycin were volume percentages), at 37°C , 5% CO 2 Cultured in a cell incubator, the cells were digested with 0.25% trypsin by mass percentage into a single cell suspension, and the viable cells were counted with a hemocytometer, and the concentration of viable cells was adjusted to 5×10 4 / mL was inoculated in 96-well culture plate, 160 μL per well, and after 24 hours of culture, different amounts of drugs were added respectively. °C, with 5% CO 2 Incubate in an incubator for 48 hours, add MTT (20 μL / well) 4 hours before the end, discard the supernatant after 4 hours, add DMSO (150 μL / well), shake for 15 minutes, and then measure the absorbance at a wavelength of 570 nm.
[0039] The cells were...
Embodiment 3
[0046] The uptake of ruthenium-artesunate complexes in HeLa cells was studied. In this example, the uptake of ruthenium-artesunate complexes in HeLa cells was observed by laser confocal microscopy:
[0047] HeLa cells were cultured in a 35mm Corning laser confocal culture dish. When the density was 70%, 5μM Ru-2 was added to incubate for 1h, 2h, 3h, and 4h respectively. After that, they were washed twice with PBS, and immediately washed with laser light. Confocal microscope observation.
[0048] Research results such as Figure 5 As shown, the uptake of Ru-2 by cells increased in a time-dependent manner.
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