Εξειδίκευση τύπου :	Άρθρο σε επιστημονικό περιοδικό
Τίτλος:	A novel alkyl phosphocholine-dinitroaniline hybrid molecule exhibits biological activity in vitro against Leishmania amazonensis
Δημιουργός/Συγγραφέας:	Godinho J.L.P. Georgikopoulou K. [EL] Καλογεροπούλου, Θεοδώρα[EN] Calogeropoulou, Theodora de Souza W. Rodrigues J.C.F.
Ημερομηνία:	2013
Γλώσσα:	Αγγλικά
ISSN:	0014-4894
DOI:	10.1016/j.exppara.2013.06.015
Άλλο:	PubMed ID: 23845259
Περίληψη:	Parasitic protozoa of the Leishmania genus cause leishmaniasis, an important complex of tropical diseases that affect about 12million people around the world. The drugs used to treat leishmaniasis are pentavalent antimonials, miltefosine, amphotericin B and pentamidine. In the present study, we evaluated the effect of a novel alkyl phosphocholine-dinitroaniline hybrid molecule, TC95, against Leishmania amazonensis promastigotes and intracellular amastigotes. Antiproliferative assays indicated that TC95 is a potent inhibitor of promastigotes and intracellular amastigotes with IC50 values of 2.6 and 1.2μM, respectively. Fluorescence microscopy with anti-α-tubulin antibody revealed changes in the cytoskeleton, whilst scanning electron microscopy showed alterations in the shape, plasma membrane, length of the flagellum, and cell cycle. Flow cytometry confirmed the cell cycle arrest mainly in G1 phase, however a significant population appeared in sub G0/G1 and super-G2. The alterations in the plasma membrane integrity were confirmed by fluorometric analysis using Sytox Blue. Transmission electron microscopy also revealed an accumulation of lipid bodies, confirmed by fluorescence microscopy and fluorometric analysis using Nile Red. Important lesions were also observed in organelles such as mitochondrion, endoplasmic reticulum and Golgi complex. In summary, our study suggests that TC95, an alkyl phosphocholine-trifluralin hybrid molecule, is a promising novel compound against L. amazonensis.
Τίτλος πηγής δημοσίευσης:	Experimental Parasitology
Τόμος/Κεφάλαιο:	135
Τεύχος:	1
Σελίδες:	153-165
Θεματική Κατηγορία:	[EL] Φαρμακευτική χημεία[EN] Pharmaceutical chemistry
Λέξεις-Κλειδιά:	Alkyl phospholipid analogues Chemotherapy Dinitroanilines Hybrid molecule Leishmania Ultrastructure
Αξιολόγηση από ομότιμους (peer reviewed):	Ναι
Κάτοχος πνευματικών δικαιωμάτων:	© 2013 Elsevier Inc.
Σημειώσεις:	Coordenação de Aperfeiçoamento de Pessoal de Nível Superior, CAPES; Conselho Nacional de Desenvolvimento Científico e Tecnológico, CNPq; Fundação Carlos Chagas Filho de Amparo à Pesquisa do Estado do Rio de Janeiro, FAPERJ
Εμφανίζεται στις συλλογές:	Ινστιτούτο Χημικής Βιολογίας - Επιστημονικό έργο