Labeling of Piperine with Iodine-131 as Radiotracer in the Development of Cancer Drugs from Indonesia’s Natural Products

Piperine, as one of the secondary metabolites of pepper, shows many pharmacological activities in
various studies, including as antiinflammatory, antimicrobial, hepatoprotective, antioxidant, and
potentially anticancer agents. Cancer is still one of the leading causes of death in the world due to the
absence of specific symptoms in early-stage of cancer. The development of drugs for early diagnosis
and selective treatment of cancer cells is considered one of the best solutions to reduce mortality. The
activity of piperine that could induce apoptosis of 4T1 breast cancer cells and HT-29 colon cancer
cells at in vivo trials prove it as a potential compound that can carry radioactive atoms (as labeledcompound) to cancer cells. This study was conducted to determine the optimal conditions of labeling
of piperine with iodine-131 in order to obtain a 131I-piperine which can later be used as a radiotracer in
the development of cancer drugs. The labeling of piperine was performed by Chloramine-T iodination
method and followed by purification with ion exchange chromatography. The optimal labeling
results of piperine with 43.99% ± 1.23 radiochemical purity were obtained with piperine 3mg/300μL,
chloramine-T 50 μg as an oxidizer, incubation time 30 min at room temperature, and 100 μg sodium
metabisulphite as a reductor. To improve the purity of the preparation, purification by ion exchange
chromatography method with Dowex 1X8 mesh 100-200 as resin was used until obtained 93.26%
± 0.94 of radiochemical purity. Further research is necessary before 131I-piperine can be used as a
radiotracer for cancer diagnosis in nuclear medicine.
Keywords: cancer, iodine-131, 131I-piperine, labeled-compound, radiotracer