Boron neutron capture therapy system
A treatment system, boron neutron technology, applied in the field of radioactive ray irradiation treatment system, can solve the problems of normal tissue damage and poor treatment effect
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Embodiment 1
[0073] Example 1Phe-BF 3 preparation
[0074] reaction route
[0075]
[0076] Add benzyl borate (15mg, 0.05mmol), KF (0.15mmol, 0.05mL) solution, HCl (0.2mmol, 0.03mL) solution, 0.1mLMeCN solution into a 1.5mL microreactor, and react for 2h at room temperature, Get Phe-BF 3 Crude. The crude product was further purified by HPLC to obtain Phe-BF 3 . 1 H NMR (300MHz, MeOD): δppm 7.30 (m, 5H), 3.04 (d, J = 9.8Hz, 1H), 2.67 (t, J = 9.8Hz, 1H), 2.42 (brs, 1H); [M-H] - 188.0901, Found: 188.0589.
[0077] In vitro studies of compounds according to the invention
[0078] To the purification material of present embodiment 1 (hereinafter referred to as Phe-BF 3 ) conducted in vitro experiments using four different human-derived tumor cell lines U343mga, human liver cancer cell line Hep3B, human breast cancer cell line MCF7 and human sarcoma cell line 4SS. Cells were plated on uncoated tissue culture dishes and incubated at 37 °C with 5% CO 2 Culture was carried out in an in...
Embodiment 2
[0079] Example 2Phe-BF 3 cellular uptake of
[0080] U343mga cells were plated on Petri dishes at a cell density of 75% and treated with 1,4-dihydroxyboronphenylalanine (BPA) or Phe-BF dissolved in tissue culture medium 3 Incubate for 6 hours. Both boron-containing compounds are relative to the boron content (5 × 10 -4 mol / L boron) at an equimolar concentration and dissolved in tissue culture medium. The incubation was terminated by removing the boron-containing tissue culture medium and adding cold phosphate buffered saline (PBS buffer) to wash excess medium from the cells. Cells were harvested immediately by scooping off the dishes with a rubber spatula, collected in cold PBS and pelleted by centrifugation.
[0081] Cell samples were analyzed for total protein according to standard Bradford procedures. Boron analysis of pelleted cells was performed by direct current protoplast atomic emission spectroscopy (DCP-AES). Samples (50-130 mg) were digested with sulfuric acid / ...
Embodiment 3
[0085] Embodiment 3 different tumor cells to Phe-BF 3 intake
[0086] Four different tumor cell lines of human origin: U343mga, Hep3B, MCF7, and 4SS were plated on Petri dishes at 40-50% (low) and 90-100% (high) cell densities, and treated with solvent as above. Phe-BF in tissue culture medium 3 Incubate for 6 hours. The incubation was terminated by removing the boron-containing medium and adding cold PBS buffer to wash excess medium from the cells. Cells were harvested immediately by scooping off the dishes with a rubber spatula, collected in cold PBS and pelleted by centrifugation. Cell samples were analyzed for total protein according to Bradford standard procedures (supra). The results are shown in Table 2 below. In a comparison of all four human tumor cell lines (glioblastoma (U343mga), liver cancer (Hep3B), breast cancer (MCF7), sarcoma (4SS)) tested at low and high cell densities, Phe-BF 3 It is an efficient boron carrier.
[0087] Table 2: Phe-BF 3 cellular upt...
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