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001-es BibID:	BIBFORM118039
035-os BibID:	(cikkazonosító)107 (WoS)001152973300001 (Scopus)85183155490
Első szerző:	Hermenean, Anca
Cím:	Chrysin Directing an Enhanced Solubility through the Formation of a Supramolecular Cyclodextrin-Calixarene Drug Delivery System : A Potential Strategy in Antifibrotic Diabetes Therapeutics / Anca Hermenean, Eleftheria Dossi, Alex Hamilton, Maria Consiglia Trotta, Marina Russo, Caterina Claudia Lepre, Csilla Sajtos, Ágnes Rusznyák, Judit Váradi, Ildikó Bácskay, István Budai, Michele D'Amico, Ferenc Fenyvesi
Dátum:	2024
ISSN:	1424-8247
Megjegyzések:	Calixarene 0118 (OTX008) and chrysin (CHR) are promising molecules for the treatment of fibrosis and diabetes complications but require an effective delivery system to overcome their low solubility and bioavailability. Sulfobutylated beta-cyclodextrin (SBECD) was evaluated for its ability to increase the solubility of CHR by forming a ternary complex with OTX008. The resulting increase in solubility and the mechanisms of complex formation were identified through phase-solubility studies, while dynamic light-scattering assessed the molecular associations within the CHR-OTX008-SBECD system. Nuclear magnetic resonance, differential scanning calorimetry, and computational studies elucidated the interactions at the molecular level, and cellular assays confirmed the system's biocompatibility. Combining SBECD with OTX008 enhances CHR solubility more than using SBECD alone by forming water-soluble molecular associates in a ternary complex. This aids in the solubilization and delivery of CHR and OTX008. Structural investigations revealed non-covalent interactions essential to complex formation, which showed no cytotoxicity in hyperglycemic in vitro conditions. A new ternary complex has been formulated to deliver promising antifibrotic agents for diabetic complications, featuring OTX008 as a key structural and pharmacological component.
Tárgyszavak:	Orvostudományok Gyógyszerészeti tudományok idegen nyelvű folyóiratközlemény külföldi lapban folyóiratcikk OTX008 chrysin sulfobutylatedβ-cyclodextrin ternary complex solubilization mechanism molecular simulation fibrosis
Megjelenés:	Pharmaceuticals. - 17 : 1 (2024), p. 1-20. -
További szerzők:	Dossi, Eleftheria Hamilton, Alex Trotta, Maria Consiglia Russo, Marina Lepre, Caterina Claudia Sajtos Csilla Rusznyák Ágnes (1995-) (gyógyszerész) Váradi Judit (1973-) (gyógyszerész, gyógyszertechnológus) Bácskay Ildikó (1969-) (gyógyszerész, gyógyszertechnológus) Budai István (1977-) (folyamatmérnök) D'Amico, Michele Fenyvesi Ferenc (1977-) (gyógyszerész, gyógyszertechnológus)
Pályázati támogatás:	TKP2021-EGA-18 Egyéb GINOP-2.3.1-20-2020-00004 GINOP
Internet cím:	Szerző által megadott URL DOI Intézményi repozitóriumban (DEA) tárolt változat
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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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