Application of isotope-labeled dianthrone compounds in the preparation of antitumor drugs
An isotope-labeled, anti-tumor drug technology, applied in the field of anti-tumor drugs and drugs, can solve the problems of difficult control of patients, infection, reduction of targeting and therapeutic effect, etc.
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Embodiment 1-2131I
[0022] Example 1-2 131 Preparation of I-labeled prohypericin
[0023] Weigh 1.0 mg of powdered protohypericin, dissolve it in 2.0 ml of DMSO, oscillate to obtain a 0.5 mg / ml protohypericin DMSO solution. Add 400 μl of protohypericin DMSO solution with a concentration of 0.5 mg / ml into the coated tube with a prepared lodogen content of 40 μg, and add 100 μl of 200 μCi Na 131 I solution, shake well, react at 20-25°C for about 60 minutes, take out the reaction solution to terminate the reaction, measure the labeling rate, and the labeling rate is greater than 90%, indicating that the labeling is successful. Measurement method of labeling rate: The labeling rate of the reaction solution was determined by paper chromatography, Whatman filter paper was used as the carrier, and 0.1mol / L HCl was used as the mobile phase for development. The labeling rate was measured by paper chromatography, and the free 131 I is distributed at the solvent front, while 131 I marks pro-hypericin to...
Embodiment 1-3131I
[0024] Example 1-3 131 Preparation of I-labeled sennoside A
[0025] Weigh 2.0mg of powdered sennoside A, dissolve in 1.0ml DMSO, shake well, and obtain 2.0mg / ml sennoside ADMSO solution. Add 400 μl of sennoside A DMSO solution with a concentration of 2.0 mg / ml into the coated tube with a prepared lodogen content of 40 μg, and add 100 μl of 200 μC Na 131 I solution, oscillate and shake well, heat in a water bath at 45°C, react for about 90 minutes, take out the reaction solution to terminate the reaction, measure the labeling rate, and the labeling rate is greater than 90%, indicating that the labeling is successful. Measurement method of labeling rate: The labeling rate of the reaction solution was determined by paper chromatography, Whatman filter paper was used as the carrier, and O.1mol / L HCl was used as the mobile phase for development. The labeling rate was measured by paper chromatography, and the free 131 I is distributed at the solvent front, while 131 I labeled s...
Embodiment 1-4131I
[0026] Example 1-4 131 Preparation of I-labeled sennoglycogen A
[0027] Weigh 2.0mg of powdered sennoglycogen A, dissolve in 1.0ml DMSO, shake and shake well to obtain 2.0mg / ml sennoglycogen A DMSO solution. Add 400 μl of sennoglycoside A DMSO solution with a concentration of 2.0 mg / ml to the prepared coated tube with a lodogen content of 40 μg, and add 100 μl of 200 μCI Na 131 I solution, oscillate and shake well, heat in a water bath at 45°C, react for about 90 minutes, take out the reaction solution to terminate the reaction, measure the labeling rate, and the labeling rate is greater than 90%, indicating that the labeling is successful.
[0028] Measurement method of labeling rate: The labeling rate of the reaction solution was determined by paper chromatography, Whatman filter paper was used as the carrier, and 0.1mol / L HCl was used as the mobile phase for development. The labeling rate was measured by paper chromatography, and the free 131 I is distributed at the sol...
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