Ru(II) complex with anticancer liveness and method for preparing the same
A technology of anti-cancer activity and complexes, which is applied in the direction of medical preparations containing active ingredients, organic active ingredients, and pharmaceutical formulas, etc., and can solve the problems of lifeless metal complexation and unsatisfactory anti-tumor activity
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Embodiment 1
[0023] The preparation of embodiment 1Ru (II) complex:
[0024] Step 1: Add 5 grams (25 mmol) of 1,10-phenanthroline (phen) in batches to 30 ml of concentrated sulfuric acid, and stir continuously to dissolve it, then add 2.5 grams of sodium bromide, and then slowly add 15 ml of concentrated nitric acid , after dissolving all the substances in the acidic medium, the reactants were heated to reflux for 2 hours, cooled to room temperature, slowly poured into 400 g of ice water, neutralized with 150 ml of 10M sodium hydroxide to pH = 7, left to stand for 30 min, filtered, filtered Dissolve the cake with 100ml boiling water, remove the insoluble matter, mix the two filtrates, and use 5×100ml CH 2 Cl 2 Extraction, the organic phase was washed with 50ml of water, dried in anhydrous magnesium sulfate, and rotary evaporation produced a yellow solid, which was recrystallized with methanol to obtain 2.76 grams of yellow needle-like product (1,10-phenanthroline (phen)-5,6 - diketone); ...
Embodiment 2
[0031]Example 2 Ru (II) complex anticancer activity experiment
[0032] The anticancer activity assay was carried out by cytotoxicity by using the tetrazolium salt 3-(4,5-dimethylthiazole)-2,5-diphenyltetrazolium bromide (MTT) as the dye. The complex was prepared with phosphoric acid solution and stored in a refrigerator at 4°C for later use. Serial stock solutions were prepared in culture medium in 96-well microtiter plates. The complex is added to the cell culture medium in a concentration gradient (1nM-1μM), and the medium does not need to be replaced within 24 hours. At the end of the set reaction time, the medium was transferred to 200 μL of medium containing 0.5 mg / ml MTT and the microtiter plate was placed in an incubator at 37° C. for 4 hours. 100 μl DMSO was added to the medium to increase the solubility of this purple dye. Finally, the product is obtained by measuring the optical density of each well under 595nm fluorescence. Inhibition rate (II%) was calculated ...
Embodiment 3
[0034] Example 3 Interaction experiment between Ru(II) complexes and DNA
[0035] Absorption Spectroscopy Research
[0036] figure 2 Curve a is the ultraviolet absorption spectrum of the Ru(II) complex, and curves b~h are the ultraviolet absorption spectrum of the Ru(II) complex after adding DNA. It can be seen from the figure that the absorption peak intensity of the complex decreases when DNA is added. According to literature reports [10] , when the small molecule is intercalated between the base pairs of the CT-DNA double helix, its absorption spectrum exhibits a color reduction effect; when the small molecule is electrostatically bound to the CT-DNA, its absorption spectrum exhibits a color enhancement effect ; Therefore, the interaction between Ru(II) complexes and CT-DNA at this time should be dominated by intercalation.
[0037] Effects of Complexes on the Fluorescence Spectrum of DNA-EB
[0038] Ethidium bromide (EB) is a conjugated planar molecule with weak fluor...
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