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Article

Delivery of Thyronamines (TAMs) to the Brain: A Preliminary Study

1
Smart Bio-Interfaces, Istituto Italiano di Tecnologia, Viale Rinaldo Piaggio 34, 56025 Pontedera, Italy
2
The Biorobotics Institute, Scuola Superiore Sant’Anna, Viale Rinaldo Piaggio 34, 56025 Pontedera, Italy
3
Department of Clinical & Experimental Medicine, University of Pisa, Via Savi 10, 56126 Pisa, Italy
4
Laboratory of Biochemistry, Department of Pathology, University of Pisa, 56100 Pisa, Italy
5
Department of Chemistry and Pharmacy, University of Sassari, 07100 Sassari, Italy
*
Author to whom correspondence should be addressed.
Academic Editors: Barbara De Filippis and Gunter Peter Eckert
Molecules 2021, 26(6), 1616; https://doi.org/10.3390/molecules26061616
Received: 11 February 2021 / Revised: 5 March 2021 / Accepted: 12 March 2021 / Published: 14 March 2021
Recent reports highlighted the significant neuroprotective effects of thyronamines (TAMs), a class of endogenous thyroid hormone derivatives. In particular, 3-iodothyronamine (T1AM) has been shown to play a pleiotropic role in neurodegeneration by modulating energy metabolism and neurological functions in mice. However, the pharmacological response to T1AM might be influenced by tissue metabolism, which is known to convert T1AM into its catabolite 3-iodothyroacetic acid (TA1). Currently, several research groups are investigating the pharmacological effects of T1AM systemic administration in the search of novel therapeutic approaches for the treatment of interlinked pathologies, such as metabolic and neurodegenerative diseases (NDDs). A critical aspect in the development of new drugs for NDDs is to know their distribution in the brain, which is fundamentally related to their ability to cross the blood–brain barrier (BBB). To this end, in the present study we used the immortalized mouse brain endothelial cell line bEnd.3 to develop an in vitro model of BBB and evaluate T1AM and TA1 permeability. Both drugs, administered at 1 µM dose, were assayed by high-performance liquid chromatography coupled to mass spectrometry. Our results indicate that T1AM is able to efficiently cross the BBB, whereas TA1 is almost completely devoid of this property. View Full-Text
Keywords: 3-iodothyronamine (T1AM); multi-target directed ligand; neurodegeneration; blood–brain barrier; high-performance liquid chromatography coupled to mass spectrometry 3-iodothyronamine (T1AM); multi-target directed ligand; neurodegeneration; blood–brain barrier; high-performance liquid chromatography coupled to mass spectrometry
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MDPI and ACS Style

di Leo, N.; Moscato, S.; Borso', M.; Sestito, S.; Polini, B.; Bandini, L.; Grillone, A.; Battaglini, M.; Saba, A.; Mattii, L.; Ciofani, G.; Chiellini, G. Delivery of Thyronamines (TAMs) to the Brain: A Preliminary Study. Molecules 2021, 26, 1616. https://doi.org/10.3390/molecules26061616

AMA Style

di Leo N, Moscato S, Borso' M, Sestito S, Polini B, Bandini L, Grillone A, Battaglini M, Saba A, Mattii L, Ciofani G, Chiellini G. Delivery of Thyronamines (TAMs) to the Brain: A Preliminary Study. Molecules. 2021; 26(6):1616. https://doi.org/10.3390/molecules26061616

Chicago/Turabian Style

di Leo, Nicoletta, Stefania Moscato, Marco Borso', Simona Sestito, Beatrice Polini, Lavinia Bandini, Agostina Grillone, Matteo Battaglini, Alessandro Saba, Letizia Mattii, Gianni Ciofani, and Grazia Chiellini. 2021. "Delivery of Thyronamines (TAMs) to the Brain: A Preliminary Study" Molecules 26, no. 6: 1616. https://doi.org/10.3390/molecules26061616

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