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Cellular Uptake and Computational Analysis of [131I]-Xanthine and [131I]-Hypoxanthine in Human Prostate Cancer Cell Line (LNCaP) Wongso, Hendris; Mahendra, Isa; Setiadi, Yanuar; Rattyananda, Badra Sanditya; Rizaludin, Asep; Pranisuari, Ni Made Yuktikamura Galih; Kusumaningrum, Crhisterra Ellen
Makara Journal of Science Vol. 28, No. 3
Publisher : UI Scholars Hub

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Abstract

Potent radiolabelled compounds eligible for therapy of prostate cancer need to be developed. Hence, we developed two candidate therapeutic agents bearing the iodine-131 (131I) radionuclide, namely, [131I]-xanthine (3,7-dihydropurine-2,6-dione) and [131I]-hypoxanthine (1,9-dihydro-6H-purin-6-one). The radiolabelled compounds were subjected to a cellular uptake study, which was accomplished by incubating [131I]-xanthine and [131I]-hypoxanthine with the human prostate cancer cell line (LNCaP) for 5, 15, 30, 60, and 90 min. Results showed that the accumulation of both [131I]-xanthine and [131I]-hypoxanthine in prostate cancer cells was significantly higher than the control group (131I). [131I]-xanthine rapidly accumulated in prostate cancer cells, with the highest percentage of cellular uptake of 2.73% ± 0.40% observed at 30 min of incubation. By contrast, [131I]-hypoxanthine exhibited more efficient accumulation in prostate cancer cells, especially at 60 and 90 min of incubation, with cellular uptake values of 11.5% ± 3.14% and 11.9% ± 1.83%, respectively. Furthermore, the computational analysis showed that radioiodinated xanthine and hypoxanthine provide potential binding affinities and interaction on both androgen and prostate-specific membrane antigen receptors. Overall, this study indicates that [131I]-xanthine and [131I]-hypoxanthine can be potentially developed as therapeutic agents for prostate cancer.
Treatment of Neuroendocrine Tumors (NETs) Using Somatostatin Analogs: Current View, Clinical Achievements and Future Perspectives Wongso, Hendris
Indonesian Journal of Cancer Chemoprevention Vol 10, No 2 (2019)
Publisher : Indonesian Society for Cancer Chemoprevention

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.14499/indonesianjcanchemoprev10iss2pp101-113

Abstract

Neuroendocrine tumors (NETs), previously known as carcinoid tumors, are a heterogeneous group of neoplasms which originate from cells of the endocrine or nervous system with an overall incidence of 1–5 cases per 100,000 individuals per year. Recent studies showed that their incidence has dramatically increased worldwide over the last few years. The majority of NETs overexpress the somatostatin receptors (SSTRs) in tumor cells which are further being used as the important targets for therapy purposes using somatostatin analogs (SSAs) such as octreotide and lanreotide. Like native somatostatin, SSAs bind to SSTRs and induce a range of cellular effects, including antitumor activity. Antitumor activity of SSAs and their high binding properties for the SSTRs have become valuable tools for developing advanced treatment of NETs. Consequently, SSAs have been used widely in routine clinical practice, especially for treatment of various types of NETs. Despite treatment using SSAs have made a positive contribution, recent development suggests that the used of SSAs in combination with chemotherapy or peptide receptor radionuclide therapy (PRRT) can improve clinical outcome in patients with NETs. This review provides an overview of recent trend in the treatment of NETs using SSAs, their clinical achievements in the last few years and their potential applications in the future.Keywords: neuroendocrine tumors, treatment, somatostatin analogs, chemotherapy, PRRTNeuroendocrine tumors (NETs), previously known as carcinoid tumors, are a heterogeneous group of neoplasms which originate from cells of the endocrine or nervous system with an overall incidence of 1–5 cases per 100,000 individuals per year. Recent studies showed that their incidence has dramatically increased worldwide over the last few years. The majority of NETs overexpress the somatostatin receptors (SSTRs) in tumor cells which are further being used as the important targets for therapy purposes using somatostatin analogs (SSAs) such as octreotide and lanreotide. Like native somatostatin, SSAs bind to SSTRs and induce a range of cellular effects, including antitumor activity. Antitumor activity of SSAs and their high binding properties for the SSTRs have become valuable tools for developing advanced treatment of NETs. Consequently, SSAs have been used widely in routine clinical practice, especially for treatment of various types of NETs. Despite treatment using SSAs have made a positive contribution, recent development suggests that the used of SSAs in combination with chemotherapy or peptide receptor radionuclide therapy (PRRT) can improve clinical outcome in patients with NETs. This review provides an overview of recent trend in the treatment of NETs using SSAs, their clinical achievements in the last few years and their potential applications in the future.Keywords: neuroendocrine tumors, treatment, somatostatin analogs, chemotherapy, PRRT