A nitric oxide donor small molecule and its preparation and application
A technology of nitric oxide and small molecules, applied in the chemical and biological fields, can solve the problems of inability to be directly transported and inconvenient to handle, and achieve the effect of inhibiting tumor cell activity and good anti-tumor cell activity
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Embodiment 1
[0033] The synthesis of embodiment 1 donor small molecules (I)
[0034] 1. Synthesis of compound (S-2)
[0035]
[0036] Phenylthiourea (6.57 mmol, purchased from Anaiji), sodium molybdate dihydrate (0.10 mmol, purchased from Anaiji) and deionized water (100 mL) were added into a 100 mL round bottom flask. 30% hydrogen peroxide (2.24mL, 19.73mmol) was added dropwise to the mixture at 0°C. After the drop was complete, the mixture was reacted at room temperature for 4 hours, and the reaction was monitored by TLC. After the reaction was completed, the solid precipitate was collected by suction filtration, and the precipitate was washed three times with deionized water (100 mL). The solid mixture was then dissolved in methanol (120 mL), precipitated with petroleum ether (50 mL), and filtered to dryness to obtain 1.38 mmol of compound (S-2), with a yield of 21%.
[0037] 1 H NMR(500MHz,DMSO)δ9.61(s,1H),7.51(dd,J=10.7,4.8Hz,2H),7.41(t,J=7.4Hz,1H),7.32-7.28(m,2H) .
[0038] 2...
Embodiment 2
[0051] Example 2 Evaluating the Ability of Donor Small Molecules to Release Nitric Oxide
[0052] 1) Sample to be tested:
[0053] Group A: donor small molecule (I) (500 μM)+PBS (pH=7.4);
[0054] Group B: donor small molecule (I) (5 μM)+NTR (50 μg / mL)+NADH (500 μM)+PBS (pH=7.4);
[0055] Group C: donor small molecule (I) (50 μM)+NTR (50 μg / mL)+NADH (500 μM)+PBS (pH=7.4);
[0056] Group D: donor small molecule (I) (500 μM)+NTR (50 μg / mL)+NADH (500 μM)+PBS (pH=7.4);
[0057] Control group: PBS (pH=7.4);
[0058] Wherein, NTR is nitroreductase, and NADH is nicotinamide adenine dinucleotide. Two parallels per set. Place it on a mixer at 25°C and shake at 1000rpm, which is the sample to be tested.
[0059] 2) Standard substance: the sodium nitrite standard substance was diluted with PBS (pH=7.4), and six concentration gradients of the standard substance were set up, and the final concentrations were 2.5, 5, 10, 20, 40, and 80 μM.
[0060] 3) Take out Griess Reagent I and Gr...
Embodiment 3
[0065] Example 3 Evaluating the anti-tumor cell proliferation activity of the donor small molecule (I)
[0066] 1. Cell culture conditions
[0067] Human prostate cancer cell PC-3 was selected and purchased from ATCC Company. Use cell culture medium (DMEM high glucose medium containing 10% fetal bovine serum, 0.1mg / mL streptomycin and 100U / mL penicillin (purchased from Hangzhou Zeheng Biotechnology Co., Ltd.)), at 37°C / 5% CO 2 , culture cells in a cell incubator with saturated humidity.
[0068] 2. Detection of the anti-tumor cell proliferation activity of the donor small molecule (I)
[0069] Inoculate well-growing human prostate cancer cell PC-3 (containing 100 μL cell culture medium) at an inoculation volume of 5000 cells / well in a 96-well cell culture plate, and place at 37°C / 5% CO 2 Incubate for 16-20 hours in an incubator.
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