Synthesis of 131I Labeled Quercetin through Oxidation Method Using Chloramine-T for Cancer Radiopharmaceuticals

Maula Eka Sriyani (National Nuclear Energy Agency, Jl. Tamansari No. 71 Bandung 40132, Indonesia)
Dian Ayu Utami (Jenderal Achmad Yani University, Jl. Terusan Jenderal Sudirman Cimahi, Indonesia)
Mega Susilo Dwike (Jenderal Achmad Yani University, Jl. Terusan Jenderal Sudirman Cimahi, Indonesia)
Eva Maria Widyasari (National Nuclear Energy Agency, Jl. Tamansari No. 71 Bandung 40132, Indonesia)
Muharram Marzuki (Jenderal Achmad Yani University, Jl. Terusan Jenderal Sudirman Cimahi, Indonesia)
Rizky Juwita Sugiharti (National Nuclear Energy Agency, Jl. Tamansari No. 71 Bandung 40132, Indonesia)
Witri Nuraeni (National Nuclear Energy Agency, Jl. Tamansari No. 71 Bandung 40132, Indonesia)

Indonesian Journal of Chemistry
Vol 19, No 4 (2019)

Quercetin is one of the flavonoid groups with antioxidant activity. The objective of this study was to achieve the labeled compound of 131I-quercetin as a radiotracer for diagnosis and cancer therapy with high labeling efficiency and radiochemical purity. The labeling procedure was conducted by the oxidation reaction using chloramine-T. The effect of pH, reaction time, amount of oxidizing agent and ligand were evaluated in this research. Quercetin was successfully labeled with iodine-131 at pH 11 at room temperature for 10 min mixed in 1000 rpm with the amount of quercetin and chloramine-T is 0.4 and 0.3 mg, respectively. The results demonstrated that the ratio of quercetin/Na131I was 2 × 105. The 131I-quercetin labeling efficiency was 92.03 ± 2.20%, and radiochemical purity of 131I-quercetin was 99.34 ± 0.58%. The results showed that 131I-quercetin could be a radiotracer candidate for diagnosis and cancer therapy.