Therapeutic radiopharmaceuticals have been researched extensively in the last decade as a result of the growing research interest in personalized medicine to improve diagnostic accuracy and intensify intensive therapy while limiting side effects. Radiometal-based drugs are of substantial interest because of their greater versatility for clinical translation compared to non-metal radionuclides. This paper comprehensively discusses various components commonly used as chemical scaffolds to build radiopharmaceutical agents, i.e., radionuclides, pharmacokinetic-modifying linkers, and chelators, whose characteristics are explained and can be used as a guide for the researcher.
Accelerated cancer cell growth requires a massive intake of amino acids. Overexpression of L-type (large) amino acid transporter 1 (LAT1) on the cancer cell membrane facilitates such a demand, which is limited in normal organs. Therefore, LAT1 overexpression is ideal as a molecular cancer therapeutic target. JPH203, a LAT1-selective non-transportable blocker, had demonstrated LAT1 inhibition in <10 µM IC50 values and effectively suppressed cancer cell growth in studies involving several types of cancer cell lines and tumor xenograft models. A limited phase I clinical trial was performed on five different solid tumors and showed that JPH203 is well-tolerated and has a promising activity for the treatment of bile duct cancer. This review details the development and prospect of JPH203 as a LAT1-targeting cancer therapy.
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.
A large excess of unlabeled ligands over gallium-67 (Ga) provides Ga-labeled probes with high radiochemical yields in a short reaction time. However, the unlabeled ligands hinder target accumulation of radiolabeled probes by competing for target molecules. To circumvent the problem, we investigated the way to prepareGa-labeled multivalent probes from monovalent ligands. The reaction of a bi- or tridentate ligand with [Ga]Ga-citrate resulted in Ga-labeled probes of insufficient stability. However, the reaction of [Ga]Ga-citrate with a mixture of RGD-conjugated salicylaldehyde and triamine provided a Ga-labeled trivalent probe with stability sufficient for in vivo applications. Since the free Schiff base ligand decomposed rapidly upon injection, theGa-labeled trivalent probe visualized the murine tumor without postlabeling purification, which was not achieved with a Ga-labeled trivalent probe from a trivalent ligand. These findings indicate the availability of Schiff base ligands to prepareGa-labeled trivalent probes by a simple radiolabeling procedure.
Objective: In this study, various types of pharmacokinetic modifying linkers and chelators are combined with JPH203 to obtain the best-docked molecule for prospective radiopharmaceutical kits.
Methods: AutoDock 4.2.6 and AutoDockTools 1.5.6 programs was used to do the molecular docking simulation and ADMET prediction was done using VNN-ADMET to predict the pharmacokinetics and toxicity of the ligand.
Results: The result of this study showed that JPH203-linker K-NOTA has the best affinity with a docking score of about-10.7 kcal/mol and shows hydrogen interaction with Tyr259, which acts as key residue of the active site.
Conclusion: Based on the results, JPH203-linker K-NOTA has good potential as a radiopharmaceutical kit of cancer.
AbstrakPermasalahan pencemaran air yang disebabkan oleh limbah krom industri penyamakan kulit di kawasan Sukaregang, Kabupaten Garut perlu diolah dengan teknik fitoremediasi dengan tanaman dari keluarga Ponteridaceae. Penelitian ini perlu dilakukan untuk mengetahui kadar penyerapan tanaman eceng-ecengan dan menentukan eceng mana yang paling efektif menyerap krom. Penelitian ini dilakukan dengan tahap pengumpulan bahan dan determinasi tanaman eceng-ecengan, pengolahan limbah dengan fitoremediasi selama 21 hari, dan analisis kadar krom dengan spektrofotometer serapan atom. Kapasitas penyerapan Eichhornia crassipes Solm., Heteranthera peduncularis, dan Monochoria vaginalis adalah 1,5395; 0,5728; dan 0,1057 µg/g. Berdasarkan uji Duncan, disimpulkan bahwa Eichhornia crassipes Solm. merupakan tanaman eceng paling efektif yang memiliki kemampuan paling tinggi dalam menyerap logam krom limbah penyamakan kulit.Kata kunci: Eichhornia crassipes Solm., fitoremediasi, Heteranthera peduncularis, krom,
Monochoria vaginalis
Utilization of Ponteridaceae as Phytoremediation Agent in Chrome Waste Treatment AbstractWater pollution caused by waste chrome leather tanning industry at Sukaregang, Garut Regency should be done by phytoremediation technique using plants from Ponteridaceae family. This research needs to know the level of absorption of Ponteridaceae plants and determine which one is the most effective to absorb chrome. The phase of this research is by gathering materials and determination of the Ponteridaceae plants, waste treatment with phytoremediation in 21 days, and analysis of chromium levels with an atomic absorption spectrophotometer. The absorption capacity of Eichhornia crassipes Solm., Heteranthera peduncularis and Monochoria vaginalis are 1.5395; 0.5728, and 0.1057 µg/g. Based on the Duncan test, it is concluded that Eichhornia crassipes Solm. is the most effective among them with the highest ability to absorb metal chrome tannery wastes.
This review aimed to inform about the magnetic nanoparticle functionalization and solid magnetic phase extraction application to separate analytes in various types of samples. The review was conducted by analyzing several articles published in 2010 until 2021 obtained through search engines, such as Science Direct, Google Scholar and PubMed, using the keyword “magnetic phase extraction” and “magnetic nanoparticle”. The magnetic nanoparticle can be functionalized with organic, inorganic, and metal-organic framework compounds to obtain good selectivity and extraction capability. The Magnetic Solid Phase Extraction (MSPE) can be applied to separate analytes in biological, food, environmental samples. The MSPE can be used in various biological, food, and environmental samples resulting in high enrichment factor value, good recovery, and the magnetic adsorbent has excellent reusability.
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