Εξειδίκευση τύπου :	Άρθρο σε επιστημονικό περιοδικό
Τίτλος:	Adamantylidene-substituted alkylphosphocholine TCAN26 is more active against Sporothrix schenckii than miltefosine
Δημιουργός/Συγγραφέας:	Borba-Santos L.P. Ishida K. [EL] Καλογεροπούλου, Θεοδώρα[EN] Calogeropoulou, Theodora De Souza W. Rozental S.
Εκδότης:	Fundacao Oswaldo Cruz
Ημερομηνία:	2016
Γλώσσα:	Αγγλικά
ISSN:	0074-0276
DOI:	10.1590/0074-02760160088
Άλλο:	PubMed ID: 27581121
Περίληψη:	Sporotrichosis is the most frequent subcutaneous mycosis in the world and its increasing incidence has led to the search for new therapeutic options for its treatment. In this study, we demonstrated that three structural analogues of miltefosine (TCAN26, TC19, and TC70) showed inhibitory activity against Sporothrix schenckii sensu stricto and that TCAN26 was more active in vitro than miltefosine against several isolates. Scanning electron microscopy showed that S. schenckii exposure to TCAN26 resulted in cells that were slightly more elongated than untreated cells. Transmission electron microscopy showed that TCAN26 treatment induced loss of the regular cytoplasmic electron-density and altered the cell envelope (disruption of the cell membrane and cell wall, and increased cell wall thickness). Additionally, TCAN26 concentrations required to kill S. schenckii cells were lower than concentrations that were cytotoxic in mammalian cells, and TCAN26 was more selective than miltefosine. Thus, the adamantylidene-substituted alkylphosphocholine TCAN26 is a promising molecule for the development of novel antifungal compounds, although further investigations are required to elucidate the mode of action of TCAN26 in S. schenckii cells.
Τίτλος πηγής δημοσίευσης:	Memorias do Instituto Oswaldo Cruz
Τόμος/Κεφάλαιο:	111
Τεύχος:	8
Σελίδες:	523-527
Θεματική Κατηγορία:	[EL] Φαρμακευτική χημεία[EN] Pharmaceutical chemistry
Λέξεις-Κλειδιά:	Antifungal Miltefosine analogue Sporothrix schenckii
Αξιολόγηση από ομότιμους (peer reviewed):	Ναι
Κάτοχος πνευματικών δικαιωμάτων:	© 2016, Fundacao Oswaldo Cruz. All rights reserved.
Όροι και προϋποθέσεις δικαιωμάτων:	All Open Access, Gold, Green
Εμφανίζεται στις συλλογές:	Ινστιτούτο Χημικής Βιολογίας - Επιστημονικό έργο