Tumour targeting fluorescent probe and application in tumour NO test
A fluorescent probe and tumor-targeting technology, applied in molecular probes for tumor-targeted fluorescence imaging, and the application field of tumor NO detection, can solve the problems of lack of tumor targeting, difficult time and space distribution and expression, etc. , to achieve the effects of long fluorescence retention time, low synthesis cost and simple synthesis steps
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Embodiment 1
[0053] Example 1: The synthetic route of probe 1 and probe 2:
[0054] (1) Synthesis of 2-(2-hydroxyphenyl)-benzimidazole: mix equimolar (5~15mmol) of salicylaldehyde, sodium bisulfite and 25mL of absolute ethanol, stir at room temperature for 3~6h, then Equimolar o-phenylenediamine was dissolved in 25mL DMF and added dropwise to the previous solution and heated to reflux for 2~3h. After the reaction, the reactant is poured into 10 times cold water, the precipitate is separated out, filtered with suction, dried, and recrystallized twice with anhydrous ethanol;
[0055] (2) Synthesis of 2-(2-hydroxy-5-nitro)-benzimidazole: Dissolve 0.01~0.05g of 2-(2-hydroxyphenyl)-benzimidazole in 10 times the amount of concentrated sulfuric acid and use Cool to -10°C in an ice-salt bath, add dropwise the pre-prepared and cooled mixed acid (concentrated HNO) made from the calculated amount of nitric acid and equal volume of sulfuric acid. 3 1.0~5.0g; concentrated H 2 SO 4 1.2~6.0g) and keep the ...
Embodiment 2
[0062] Example 2: Tumor targeting study of probe 1 in mice bearing S180 sarcoma
[0063] Inoculate S180 sarcoma cells (concentration of 10 6 cells / ml) to the armpit of Balb / c mice (male, 6-8 weeks, 18-22g), and 200μl of S180 cells were subcutaneously injected into the armpit of each mouse. After 1 week of inoculation, take 200μl of probe 1 in PBS (concentration of 10 9 Top10 / ml), injected into S180 tumor-bearing mice via tail vein. Two days after tail vein injection, the mice were sacrificed, and major organs (heart, liver, spleen, lung, kidney, brain, blood) and tumor tissues were taken, homogenized and dissolved in 800 μl DMSO, and the organ fluorescence distribution of probe 1 was measured In order to determine whether it has tumor targeting, the excitation light is 330nm, and the fluorescence intensity value at 505nm is measured. The results of each organ are shown in fluorescence intensity / gram of tissue. Results can be seen figure 2 .
[0064] In order to visualize the re...
Embodiment 3
[0066] Example 3: Fluorescence changes of probe 2 reacting with NO
[0067] Suspend probe 2 in 1×PBS, the final concentration is 10 9 Topl0 / ml, take 200μl to react with 1.8mM NO for 1,5min, then measure the fluorescence intensity change of the suspension, the excitation wavelength is 330nm, see the result Figure 4 , Fluorescence intensity are all normalized. The results of fluorescence photos before and after the reaction between probe 2 and NO can be found Figure 5 .
[0068] From Figure 4 It can be seen that the background fluorescence intensity of probe 2 is very low. After reacting with NO, the fluorescence intensity increases rapidly (within 1 minute). After five minutes of reaction, the fluorescence intensity tends to be stable, and the enhancement factor . The rapid and obvious increase in fluorescence after reacting with NO indicates that probe 2 can be used as a fluorescent probe for NO detection for the determination of NO. Figure 5 The fluorescence photographs provi...
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