Synthesis, radiolabeling and In Vivo tissue distribution of an anti-oestrogen glucuronide compound, (99m)Tc-TOR-G.
Toremifene (TOR) has been used as an anti-oestrogen drug for the treatment and prevention of human breast cancer. The aim of this study was the addition of the hydrophilic groups diethylenetriamine pentaacetic acid (DTPA) and glucuronic acid to the starting substance TOR and to label it with technetium-99m ((99m)Tc) radionuclide and to investigate radiopharmaceutical potential of the new compound. The synthesis reactions are completed in four steps, including enzymatic reaction, with the following substeps; preparation of microsomal fraction from Hutu 80 cell line and subsequent purification of UDP-glucuronyl transferase (UDPGT), estimation of protein quantity in microsomal samples and glucuronidation reaction. The results indicate that (99m)Tc-TOR-G may be proposed as a new anti-oestrogen glucuronide imaging agent for ovarian tumours.
Department of Nuclear Applications, Institute of Nuclear Sciences, Ege University, Izmir, Turkey. fazilet.zumrut.biber@ege.edu.tr
F Z Biber
FZ
Muftuler
P
P
Unak
S
S
Yolcular
A Yurt
AY
Kilcar
C
C
Ichedef
H
H
Enginar
S
S
Sakarya
D000818:Animals; D045744:Cell Line, Tumor; D004379:Duodenal Neoplasms / Q000000981:diagnostic imaging / Q000378:metabolism; D020847:Estrogen Receptor Modulators / Q000097:blood / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D005260:Female; D020723:Glucuronic Acid / Q000737:chemistry; D006801:Humans; D007553:Isotope Labeling / Q000379:methods; D009132:Muscles / Q000000981:diagnostic imaging / Q000378:metabolism; D015609:Organotechnetium Compounds / Q000097:blood / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D010053:Ovary / Q000000981:diagnostic imaging / Q000378:metabolism; D004369:Pentetic Acid / Q000737:chemistry; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000097:blood / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D051381:Rats; D017208:Rats, Wistar; D017556:Technetium Compounds / Q000097:blood / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D014018:Tissue Distribution; D017312:Toremifene / Q000031:analogs & derivatives* / Q000737:chemistry
C550377:99mTc-TOR-G; D020847:Estrogen Receptor Modulators; D015609:Organotechnetium Compounds; D019275:Radiopharmaceuticals; D017556:Technetium Compounds; D004369:Pentetic Acid; D017312:Toremifene; D020723:Glucuronic Acid