Synthesis, characterization, antioxidant activity of Quercetin, Rutin and Quercetin-Rutin incorporated β-cyclodextrin inclusion complexes and determination of their activity in NIH-3T3, MDA-MB-231 and A549 cell lines    
Yazarlar (5)
A. Alper Öztürk
Anadolu Üniversitesi, Türkiye
Ebru Başaran
Anadolu Üniversitesi, Türkiye
Behiye Şenel
Anadolu Üniversitesi, Türkiye
Müzeyyen Demirel
Anadolu Üniversitesi, Türkiye
Prof. Dr. Şenay SARICA Tokat Gaziosmanpaşa Üniversitesi, Türkiye
Makale Türü Özgün Makale
Makale Alt Türü SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale
Dergi Adı Journal of Molecular Structure
Dergi ISSN 0022-2860 Wos Dergi Scopus Dergi
Dergi Tarandığı Indeksler SCI-Expanded
Dergi Grubu Q2
Makale Dili İngilizce
Basım Tarihi 02-2023
Cilt No 1282
Sayı 1
Sayfalar 1 / 13
DOI Numarası 10.1016/j.molstruc.2023.135169
Özet
Quercetin (Q) and rutin (R) are plant-originated polyphenolic flavonoids with considerably strong antioxidant and anticancer activity. Despite their potentials, low water solubility, stability problems and oral bioavailability limit their therapeutic use. The specific purpose of our study was to formulate inclusion complexes of Q and R with β-cyclodextrin (β-CD) to improve the solubility and also antioxidant activity of the flavonoids. Therefore 12 different complexes were prepared by both evaporation and lyophilization methods with 1:1 molar ratio in ethanol:water (1:1, v/v) solvent system. The characteristics of the complexes were also evaluated by yield%, zeta potential (ZP), entrapment efficiency (EE), 1H NMR, XRD, FT-IR, DSC analyses. In vitro dissolution studies were performed in comparison with pure substances. Antioxidant activity studies were carried out with DPPH tests. Cytotoxic evaluations of complexes were conducted with MTT tests on NIH 3T3, MDA-MB-231 and A549 cell lines. 1H- NMR analyses revealed the complex formation considering the shifts of the protons of the APIs as well as β-CD. ZP values were ranged between -21.20±0.56 mV and -7.10±0.62 mV. The aqueous solubility of Q and R were increased ∼29 fold and ∼35 fold, respectively. According to the MTT analyses results it has been shown that the flavonoids loaded complexes were particularly effective in MDA-MB-231 cells and 50% cell inhibition was observed even at 5 µM. The results of the analyses have demonstrated that the formation of inclusion complexes resulted in enhanced water solubility and cytotoxicity which will enhance their potential use in pharmaceutical applications.
Anahtar Kelimeler
Quercetin | Rutin | -cyclodextrin | Inclusion complex | Cytotoxicity | Antioxidant activity