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001-es BibID:	BIBFORM072239
035-os BibID:	(WoS)000428512500010 (Scopus)85042051752
Első szerző:	Nacereddine, Abdelhamid
Cím:	Self-Assembled Supramolecular Nanoparticles Improve the Cytotoxic Efficacy of CK2 Inhibitor THN7 / Abdelhamid Nacereddine, Andre Bollacke, Eszter Róka, Christelle Marminon, Zouhair Bouaziz, Ferenc Fenyvesi, Ildikó Katalin Bácskay, Joachim Jose, Florent Perret, Marc Le Borgne
Dátum:	2018
ISSN:	1424-8247
Megjegyzések:	Since the approval of imatinib in 2001, kinase inhibitors have revolutionizedcancer therapies. Inside this family of phosphotransferases, casein kinase 2 (CK2) is ofgreat interest and numerous scaffolds have been investigated to design CK2 inhibitors.Recently, functionalized indeno[1,2-b]indoles have been revealed to have high potency againsthuman cancer cell lines such as MCF-7 breast carcinoma and A-427 lung carcinoma.4-Methoxy-5-isopropyl-5,6,7,8-tetrahydroindeno[1,2-b]indole-9,10-dione (THN7), identified as apotent inhibitor of CK2 (IC50 = 71 nM), was selected for an encapsulation study in order to evaluate itsantiproliferative activity as THN7-loaded cyclodextrin nanoparticles. Four ?-cyclodextrins (?-CDs)were selected to encapsulate THN7 and all experiments indicated that the nanoencapsulation of thisCK2 inhibitor in ?-CDs was successful. No additional surface-active agent was used during thenanoformulation process. Nanoparticles formed between THN7 and ?-C6H13 amphiphilic derivativegave the best results in terms of encapsulation rate (% of associated drug = 35%), with a stabilityconstant (K11) of 298 mol?L?1 and a size of 132 nm. Hemolytic activity of the four ?-CDs wasdetermined before the in cellulo evaluation and the ?-C6H13 derivative gave the lowest value ofhemolytic potency (HC50 = 1.93 mol?L?1). Only the THN7-loaded cyclodextrin nanoparticles showingless toxicity on human erythrocytes (?-C6H13, ?-C8H17 and ?-C4H9) were tested against A-427 cells.All drug-loaded nanoparticles caused more cytotoxicity against A-427 cells than THN7 alone. Basedon these results, the use of amphiphilic CD nanoparticles could be considered as a drug deliverysystem for indeno[1,2-b]indoles, allowing an optimized bioavailability and offering perspectives forthe in vivo development of CK2 inhibitors.
Tárgyszavak:	Orvostudományok Gyógyszerészeti tudományok idegen nyelvű folyóiratközlemény külföldi lapban folyóiratcikk indeno[1,2-b]indole CK2 inhibitor cyclodextrin nanoparticles in cellulo human erythrocytes A427 cells
Megjelenés:	Pharmaceuticals. - 11 : 1 (2018), p. 1-11. -
További szerzők:	Bollacke, Andre Róka Eszter (1989-) (gyógyszerész, gyógyszertechnológus) Marminon, Christelle Bouaziz, Zouhair Fenyvesi Ferenc (1977-) (gyógyszerész, gyógyszertechnológus) Bácskay Ildikó (1969-) (gyógyszerész, gyógyszertechnológus) Jose, Joachim Perret, Florent Le Borgne, Marc
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