Due to interesting therapeutic properties of ^(153)Sm and antineoplastic antibiotic,bleomycin(BLM), ^(153)Sm-bleomycin(^(153)Sm-BLM) was developed as a possible therapeutic compound using ^(153)SmCl_3 and BLM.The ^(15...Due to interesting therapeutic properties of ^(153)Sm and antineoplastic antibiotic,bleomycin(BLM), ^(153)Sm-bleomycin(^(153)Sm-BLM) was developed as a possible therapeutic compound using ^(153)SmCl_3 and BLM.The ^(153)SmCl_3 was obtained by thermal neutron flux(5×10^(13)n·cm^(-2)·s^(-1))of an enriched ^(152)Sm_2O_3 sample,dissolved in acidic media.Under optimized conditions(room temperature,45 min,0.1 mg bleomycin for 740-3700 MBq ^(153)SmCl_3) a radiochemical purity over 98%was obtained shown by HPLC(Specific activity = 55 TBq/mM).The ^(153)SmCl_3 and ^(153)Sm-BLM were administered into wild-type rats up to 96 h followed by biodistribution.The SPECT imaging of labeled compound in wild-type rats was performed and significant image pattern was observed for a radiolabeled bleomycin compound.The ^(153)Sm-BLM is a potential therapeutic compound and our experiments on this compound have shown satisfactory quality,and stability suitable for future therapeutic studies.展开更多
This work was conducted for radiolabeling of an anticancer antibiotic, i.e. doxorubicin with 61Cu for production of possible tracer used in PET oncology. 61Cu was prepared with natural zinc target and 22 MeV150 μA pr...This work was conducted for radiolabeling of an anticancer antibiotic, i.e. doxorubicin with 61Cu for production of possible tracer used in PET oncology. 61Cu was prepared with natural zinc target and 22 MeV150 μA protons via natZn(p, xn)61Cu reaction with a yield of 123.2 MBq·μA-1·h-1. Optimization reactions were performed for pH, temperature and concentration. Biodistribution of the tracer was studied in normal and fibrosarcoma bearing mice. At the optimized conditions, ITLC showed that radiochemical purity was over 97% with a specific activity of 2.22× 103MBq ·mmol-1·L-1. This was kept unchanged even with presence of human serum as well as room temperature for 5 h. Biodistribution of the tracer in fibrosarcoma bearing mice demonstrated significant tumor uptake after 2 h. This tracer can be used in the detection of various tumors responding to doxorubicin chemotherapy using PET scan and/or determination of tumor therapy response to doxorubicin chemotherapy.展开更多
基金support of the International Atomic Energy Agency(IAEA) support under IRA/2/006 and IRA/2/007
文摘Due to interesting therapeutic properties of ^(153)Sm and antineoplastic antibiotic,bleomycin(BLM), ^(153)Sm-bleomycin(^(153)Sm-BLM) was developed as a possible therapeutic compound using ^(153)SmCl_3 and BLM.The ^(153)SmCl_3 was obtained by thermal neutron flux(5×10^(13)n·cm^(-2)·s^(-1))of an enriched ^(152)Sm_2O_3 sample,dissolved in acidic media.Under optimized conditions(room temperature,45 min,0.1 mg bleomycin for 740-3700 MBq ^(153)SmCl_3) a radiochemical purity over 98%was obtained shown by HPLC(Specific activity = 55 TBq/mM).The ^(153)SmCl_3 and ^(153)Sm-BLM were administered into wild-type rats up to 96 h followed by biodistribution.The SPECT imaging of labeled compound in wild-type rats was performed and significant image pattern was observed for a radiolabeled bleomycin compound.The ^(153)Sm-BLM is a potential therapeutic compound and our experiments on this compound have shown satisfactory quality,and stability suitable for future therapeutic studies.
文摘This work was conducted for radiolabeling of an anticancer antibiotic, i.e. doxorubicin with 61Cu for production of possible tracer used in PET oncology. 61Cu was prepared with natural zinc target and 22 MeV150 μA protons via natZn(p, xn)61Cu reaction with a yield of 123.2 MBq·μA-1·h-1. Optimization reactions were performed for pH, temperature and concentration. Biodistribution of the tracer was studied in normal and fibrosarcoma bearing mice. At the optimized conditions, ITLC showed that radiochemical purity was over 97% with a specific activity of 2.22× 103MBq ·mmol-1·L-1. This was kept unchanged even with presence of human serum as well as room temperature for 5 h. Biodistribution of the tracer in fibrosarcoma bearing mice demonstrated significant tumor uptake after 2 h. This tracer can be used in the detection of various tumors responding to doxorubicin chemotherapy using PET scan and/or determination of tumor therapy response to doxorubicin chemotherapy.
