Identificador persistente para citar o vincular este elemento: http://hdl.handle.net/10553/123260
Título: Isolation of Nocuolin A and Synthesis of New Oxadiazine Derivatives. Design, Synthesis, Molecular Docking, Apoptotic Evaluation, and Cathepsin B Inhibition
Autores/as: Tena Pérez, Víctor
Apaza Ticona, Luis
H. Cabanillas, Alfredo
Maderuelo Corral, Santiago
Rosero Valencia, Diego Fernando
Martel Quintana, Antera 
Ortega Domenech, Montserrat
Rumbero Sánchez, Ángel
Clasificación UNESCO: 339001 Biotecnología de microalgas
241707 Algología (ficología)
320907 Fitofármacos
Palabras clave: Anti-Tumoural
Cathepsins
Nostoc
Oxadiazines
Fecha de publicación: 2023
Publicación seriada: Marine Drugs 
Resumen: Nocuolin A (1), an oxadiazine, was isolated from the cyanobacterium Nostoc sp. Its chemical structure was elucidated using NMR and mass spectroscopic data. From this compound, two new oxadiazines, 3-[(6R)-5,6-dihydro-4,6-dipentyl-2H-1,2,3-oxadiazin-2-yl]-3-oxopropyl acetate (2) and 4-{3-[(6R)-5,6-dihydro-4,6-dipentyl-2H-1,2,3-oxadiazin-2-yl]-3-oxopropoxy}-4-oxobutanoic acid (3), were synthesised. The chemical structures of these two compounds were elucidated by a combination of NMR and MS analysis. Compound 3 showed cytotoxicity against the ACHN (0.73 ± 0.10 μM) and Hepa-1c1c7 (0.91 ± 0.08 μM) tumour cell lines. Similarly, compound 3 significantly decreased cathepsin B activity in ACHN and Hepa-1c1c7 tumour cell lines at concentrations of 1.52 ± 0.13 nM and 1.76 ± 0.24 nM, respectively. In addition, compound 3 showed no in vivo toxicity in a murine model treated with a dose of 4 mg/kg body weight.
URI: http://hdl.handle.net/10553/123260
ISSN: 1660-3397
DOI: 10.3390/md21050284
Fuente: Marine Drugs[EISSN 1660-3397],v. 21 (5), 284, (Mayo 2023)
Colección:Artículos
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