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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
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001-es BibID:	BIBFORM117746
035-os BibID:	(cikkazonosító)1332212 (Scopus)85181199885 (WoS)001133248900001
Első szerző:	Trotta, Maria Consiglia
Cím:	Chrysin-based supramolecular cyclodextrin-calixarene drug delivery system : a novel approach for attenuating cardiac fibrosis in chronic diabetes / Maria Consiglia Trotta, Hildegard Herman, Alina Ciceu, Bianca Mladin, Marcel Rosu, Caterina Claudia Lepre, Marina Russo, Ildikó Bácskay, Ferenc Fenyvesi, Raffaele Marfella, Anca Hermenean, Cornel Balta, Michele D`Amico
Dátum:	2023
ISSN:	1663-9812
Megjegyzések:	Introduction: Cardiac fibrosis is strongly induced by diabetic conditions. Both chrysin (CHR) and calixarene OTX008, a specific inhibitor of galectin 1 (Gal-1), seem able to reduce transforming growth factor beta (TGF-?)/SMAD pro-fibrotic pathways, but their use is limited to their low solubility. Therefore, we formulated a dual-action supramolecular system, combining CHR with sulfobutylated ?-cyclodextrin (SBECD) and OTX008 (SBECD + OTX + CHR). Here we aimed to test the anti-fibrotic effects of SBECD + OTX + CHR in hyperglycemic H9c2 cardiomyocytes and in a mouse model of chronic diabetes. Methods: H9c2 cardiomyocytes were exposed to normal (NG, 5.5 mM) or high glucose (HG, 33 mM) for 48 h, then treated with SBECD + OTX + CHR (containing OTX008 0.75?1.25?2.5 ?M) or the single compounds for 6 days. TGF-?/SMAD pathways, Mitogen-Activated Protein Kinases (MAPKs) and Gal-1 levels were assayed by Enzyme-Linked Immunosorbent Assays (ELISAs) or Real-Time Quantitative Reverse Transcription Polymerase chain reaction (qRT-PCR). Adult CD1 male mice received a single intraperitoneal (i.p.) administration of streptozotocin (STZ) at a dosage of 102 mg/kg body weight. From the second week of diabetes, mice received 2 times/week the following i.p. treatments: OTX (5 mg/kg)-SBECD; OTX (5 mg/kg)-SBECD-CHR, SBECD-CHR, SBECD. After a 22-week period of diabetes, mice were euthanized and cardiac tissue used for tissue staining, ELISA, qRT-PCR aimed to analyse TGF-?/SMAD, extracellular matrix (ECM) components and Gal-1. Results: In H9c2 cells exposed to HG, SBECD + OTX + CHR significantly ameliorated the damaged morphology and reduced TGF-?1, its receptors (TGF?R1 and TGF?R2), SMAD2/4, MAPKs and Gal-1. Accordingly, these markers were reduced also in cardiac tissue from chronic diabetes, in which an amelioration of cardiac remodeling and ECM was evident. In both settings, SBECD + OTX + CHR was the most effective treatment compared to the other ones. Conclusion: The CHR-based supramolecular SBECD-calixarene drug delivery system, by enhancing the solubility and the bioavailability of both CHR and calixarene OTX008, and by combining their effects, showed a strong anti-fibrotic activity in rat cardiomyocytes and in cardiac tissue from mice with chronic diabetes. Also an improved cardiac tissue remodeling was evident. Therefore, new drug delivery system, which could be considered as a novel putative therapeutic strategy for the treatment of diabetes-induced cardiac fibrosis.
Tárgyszavak:	Orvostudományok Gyógyszerészeti tudományok idegen nyelvű folyóiratközlemény külföldi lapban folyóiratcikk chrysin cyclodextrin calixarene drug delivery system cardiac fibrosis chronic diabetes
Megjelenés:	Frontiers in Pharmacology. - 14 (2023), p. 1-17. -
További szerzők:	Herman, Hildegard Ciceu, Alina Mladin, Bianca Rosu, Marcel Lepre, Caterina Claudia Russo, Marina Bácskay Ildikó (1969-) (gyógyszerész, gyógyszertechnológus) Fenyvesi Ferenc (1977-) (gyógyszerész, gyógyszertechnológus) Marfella, Raffaele Hermenean, Anca Balta, Cornel D'Amico, Michele
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001-es BibID:	BIBFORM105881
035-os BibID:	(Scopus)85135203181 (WOS)000839762100001 (cikkazonosító)4785
Első szerző:	Trotta, Maria Consiglia
Cím:	Effects of the Calix[4]arene Derivative Compound OTX008 on High Glucose-Stimulated ARPE-19 Cells : focus on Galectin-1/TGF-β/EMT Pathway / Maria Consiglia Trotta, Francesco Petrillo, Carlo Gesualdo, Settimio Rossi, Alberto Della Corte, Judit Váradi, Ferenc Fenyvesi, Michele D'Amico, Anca Hermenean
Dátum:	2022
ISSN:	1420-3049
Tárgyszavak:	Orvostudományok Gyógyszerészeti tudományok idegen nyelvű folyóiratközlemény külföldi lapban folyóiratcikk
Megjelenés:	Molecules. - 27 : 15 (2022), p. 1-15. -
További szerzők:	Petrillo, Francesco Gesualdo, Carlo Rossi, Settimio Corte, Alberto Della Váradi Judit (1973-) (gyógyszerész, gyógyszertechnológus) Fenyvesi Ferenc (1977-) (gyógyszerész, gyógyszertechnológus) D'Amico, Michele Hermenean, Anca
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