IN VIVO INTERACTION OF PROPYLTHIOURACIL WITH SODIUM IODIDE (Na131I) RADIOPHARMACEUTICAL IN RATS (Rattus norvegicus)

IN VIVO INTERACTION OF PROPYLTHIOURACIL WITH SODIUM IODIDE (Na131I) RADIOPHARMACEUTICAL IN RATS (Rattus norvegicus).. The aim of this research is to determine the effect of propylthiouracil (PTU) treatment to pharmacokinetics interaction and biodistribution profile of Na131I radiopharmaceuticals. Three groups of animal model were used in this experiment, i.e. experimental animals which given PTU for 1 time (onset or A groups), PTU for six days (B Groups) and without treatment (control or C Groups). Pharmacokinetics and biodistribution test were conducted by giving PTU per oral and  after 24 hours, continued by giving Na131I solution per oral. In pharmacokinetics test, percentage of injection dose/gram of blood (%ID/g) was calculated to determine the absorption, distribution and elimination half time. In biodistribution test, percentage of injection dose/gram of organs was calculated to determine the accumulation of Na131I in spesific organs. The results showed that the absorption half time of A, B and C groups were 3.14 ± 1.42, 2.49 ± 0.49 and 2.52 ± 0.7 hours, respectively. The distribution half time of A, B and C groups were 10.58 + 5.85, 12.92 + 3.75 and 11.42 + 3.15 hours, respectively. The elimination half time of A, B and C groups were 113.03 + 46.03, 96.57+ 47.76 and 196.71 + 145.21 hours, respectively. Biodistribution test results showed that the accumulation of Na131I in thyroid of A, B and C groups were 1.31 + 0.45, 5.03 + 0.55 and 4.45 + 2.24 % respectively. This research was concluded that PTU treatment cannot alter absorption, distribution and elimination half time Na131I, but the accumulation in thyroid was decrease in A group to control

Evaluasi Spesifisitas Radiofarmaka 99mtc-ketokonazol Pada Infeksi Yang Disebabkan Oleh Candida Albicans, Staphylococcus Aureus Dan Escherichia Coli

EVALUASI SPESIFISITAS RADIOFARMAKA 99mTc-KETOKONAZOL PADA INFEKSI YANG DISEBABKAN OLEH Candida albicans, Staphylococcus aureus dan Escherichia coli. Penyakit infeksi masih menjadi masalah kesehatan utama dan penyebab kematian di seluruh dunia, terutama di negara berkembang. Diagnosis infeksi dengan metode pencitraan di kedokteran nuklir memerlukan sensitivitas dan spesifitas yang baik. 99mTc-ketokonazol adalah radiofarmaka antibiotik yang disintesis dengan menandai ketokonazol dengan radionuklida teknesium-99m. Radiofarmaka ini diharapkan dapat digunakan untuk mendeteksi infeksi di kedokteran nuklir, sehingga 99mTc-ketokonazol harus selektif dapat terakumulasi di daerah infeksi. Oleh karena itu, pada penelitian ini dilakukan evaluasi spesifitas 99mTc-ketokonazol untuk mendeteksi infeksi yang disebabkan oleh beberapa mikroorganisme. Hasil uji biodistribusi 99mTc-ketokonazol menunjukkan akumulasi 99mTc-ketokonazol di paha yang diinfeksi pada 1 jam setelah injeksi dengan rasio target/non target (T/NT) sebesar 3,40 untuk Candida albicans; 1,93 untuk Staphylococcus aureus dan 2,81 untuk Escherichia coli. Studi ini menunjukkan bahwa 99mTc-ketokonazol adalah radiofarmaka yang menjanjikan untuk deteksi infeksi dengan cepat dan memiliki sensitivitas dan spesifisitas yang baik

Preclinical Evaluation of Chicken Egg Yolk Antibody (IgY) Anti-RBD Spike SARS-CoV-2—A Candidate for Passive Immunization against COVID-19

The coronavirus disease 2019 (COVID-19) has become a substantial threat to the international health sector and the global economy. As of 26 December 2021, the number of mortalities resulting from COVID-19 exceeded 5.3 million worldwide. The absence of an effective non-vaccine treatment has prompted the quest for prophylactic agents that can be used to combat COVID-19. This study presents the feasibility of chicken egg yolk antibody (IgY) anti-receptor-binding domain (RBD) spike SARS-CoV-2 as a strong candidate to neutralize the virus for application in passive immunization. For the purpose of preclinical studies, we radiolabeled IgY anti-RBD spike SARS-CoV-2 with radionuclide iodine-131. This allowed us to evaluate several biological characteristics of IgY in vitro, in vivo, and ex vivo. The preclinical data suggest that IgY anti-RBD spike SARS-CoV-2 could specifically bind to the SARS-CoV-2 antigens; however, little uptake was observed in normal cells (MRC-5) (<2%). Furthermore, the ex vivo biodistribution study revealed that IgY predominantly accumulated in the trachea of normal mice compared to other organs. We also found that IgY possessed a good safety profile when used as an intranasal agent. Taken together, we propose that IgY anti-RBD spike SARS-CoV-2 has the potential for application in passive immunization against COVID-19

Molecular Docking Study of Pramipexole Derivatives as Radiopharmaceutical Candidates for Brain Imaging

Neurodegenerative diseases are a global priority disease. According to the World Health Organization (WHO), it is estimated that by 2050, there will be 152 million people with neurodegenerative diseases. Currently, the method used for brain imaging is PET/CT, with the most widely used radiopharmaceutical being 18F-FDG [7,8]. 18F-FDG is used to determine brain glucose metabolism, however the 18F-FDG does not have a specific receptor. Pramipexole compounds can cross the blood-brain barrier and have high specificity for dopamine receptors. By modifying and labelling the structure of pramipexole derivatives, it is expected to obtain pramipexole derivatives with a good affinity to the dopamine receptor. In order to reduce the risk of failure, radiation hazard, and research funds, in this research, a molecular docking study was carried out using the targeted docking method between dopamine receptor proteins and 22 pramipexole derivatives using AutoDock 4, GaussView software for structure preparation, Gaussian software for energy calculation, and Biovia Discovery Studio for structure visualization. The experimental results showed that the free binding energy of pramipexole derivatives for the dopamine receptor was obtained in the range of -2.81 to -5.84 kcal/mol. The best free binding energy value was obtained for compound PD-7, with a free binding energy value of -5.84 kcal/mol, while the RMSD value obtained was 0.6 A°, and amino acid residues that interacted with compound PD-7 among others: Leu347, Leu343, Tyr198, Leu199, Glu202, Phe201, and Val203 with hydrophobic and hydrogen bond interactions. The PD-7 compound was labeled using the radioisotope iodine-131 based on the free binding energy value. From the experimental results, compound 131I-PD-7 showed a free binding energy value of -4.66 kcal/mol and interacts with the similar amino acid residues as compound PD-7. These results indicate that the compound 131I-PD-7 is a potential candidate to be studied further as a radiopharmaceutical candidate for brain imaging

Preclinical Evaluation of Chicken Egg Yolk Antibody (IgY) Anti-RBD Spike SARS-CoV-2—A Candidate for Passive Immunization against COVID-19

The coronavirus disease 2019 (COVID-19) has become a substantial threat to the international health sector and the global economy. As of 26 December 2021, the number of mortalities resulting from COVID-19 exceeded 5.3 million worldwide. The absence of an effective non-vaccine treatment has prompted the quest for prophylactic agents that can be used to combat COVID-19. This study presents the feasibility of chicken egg yolk antibody (IgY) anti-receptor-binding domain (RBD) spike SARS-CoV-2 as a strong candidate to neutralize the virus for application in passive immunization. For the purpose of preclinical studies, we radiolabeled IgY anti-RBD spike SARS-CoV-2 with radionuclide iodine-131. This allowed us to evaluate several biological characteristics of IgY in vitro, in vivo, and ex vivo. The preclinical data suggest that IgY anti-RBD spike SARS-CoV-2 could specifically bind to the SARS-CoV-2 antigens; however, little uptake was observed in normal cells (MRC-5) (&lt;2%). Furthermore, the ex vivo biodistribution study revealed that IgY predominantly accumulated in the trachea of normal mice compared to other organs. We also found that IgY possessed a good safety profile when used as an intranasal agent. Taken together, we propose that IgY anti-RBD spike SARS-CoV-2 has the potential for application in passive immunization against COVID-19.</jats:p

Translocator Protein 18 kDa (TSPO): A Promising Molecular Target for Image-Guided Surgery of Solid Cancers

The translocator protein 18-kDa (TSPO) is a mitochondrial membrane protein that is previously identified as the peripheral benzodiazepine receptor (PBR). Furthermore, it plays a significant role in a diverse range of biochemical processes, including steroidogenesis, mitochondrial cholesterol transport, cell survival and death, cell proliferation, and carcinogenesis. Several investigations also reported its roles in various types of cancers, including colorectal, brain, breast, prostate, and lung cancers, as well as melanoma. According to a previous study, the expression of TSPO was upregulated in cancer cells, which corresponds to an aggressive phenotype and/or poor prognosis. Consequently, the potential for crafting diagnostic and prognostic tools with a focus on TSPO holds great potential. In this context, several radioligands designed to target this protein have been identified, and some of the candidates have advanced to clinical trials. In recent years, the use of hybrid probes with radioactive and fluorescence molecules for image-guided surgery has exhibited promising results in animal and human studies. This indicates that the approach can serve as a valuable surgical navigator during cancer surgery. The current hybrid probes are built from various molecular platforms, including small molecules, nanoparticles, and antibodies. Although several TSPO-targeted imaging probes have been developed, their development for image-guided surgery of cancers is still limited. Therefore, this review aims to highlight recent findings on the involvement of TSPO in carcinogenesis, as well as provide a new perspective on the potential application of TSPO-targeted hybrid probes for image-guided surgery