Hydrophilic bis-MPA hyperbranched dendritic scaffolds as nanocarriers of a fully characterized flavonoid morin-Zn(II) complex for anticancer applications

Halevas, Eleftherios; Mavroidi, Barbara; Kaplanis, Michael; Hatzidimitriou, Antonios G.; Moschona, Alexandra; Litsardakis, G.; Pelecanou, Maria

doi:10.1016/j.jinorgbio.2022.111832

Cited by 9 publications

(5 citation statements)

References 69 publications

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“… Compound 1 (Morin or 2-(2,4-dihydroxyphenyl)-3,5,7-trihydroxy-4 H -chromen-4-one) showed NMR spectra identical to those reported in the literature [ 38 ]. Compound 2 (Quercetin or 2-(3,4-dihydroxyphenyl)-3,5,7-trihydroxy-4 H -chromen-4-one) showed NMR spectra identical to those reported in the literature [ 39 ].…”

Section: Figuresupporting

confidence: 58%

Natural Flavonoid Derivatives Have Pan-Coronavirus Antiviral Activity

et al. 2023

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The SARS-CoV-2 protease (3CLpro) is one of the key targets for the development of efficacious drugs for COVID-19 treatment due to its essential role in the life cycle of the virus and exhibits high conservation among coronaviruses. Recent studies have shown that flavonoids, which are small natural molecules, have antiviral activity against coronaviruses (CoVs), including SARS-CoV-2. In this study, we identified the docking sites and binding affinity of several natural compounds, similar to flavonoids, and investigated their inhibitory activity towards 3CLpro enzymatic activity. The selected compounds were then tested in vitro for their cytotoxicity, for antiviral activity against SARS-CoV-2, and the replication of other coronaviruses in different cell lines. Our results showed that Baicalein (100 mg/mL) exerted strong 3CLpro activity inhibition (>90%), whereas Hispidulin and Morin displayed partial inhibition. Moreover, Baicalein, up to 25 mg/mL, hindered >50% of SARS-CoV-2 replication in Vero E6 cultures. Lastly, Baicalein displayed antiviral activity against alphacoronavirus (Feline-CoV) and betacoronavirus (Bovine-CoV and HCoV-OC43) in the cell lines. Our study confirmed the antiviral activity of Baicalein against SARS-CoV-2 and demonstrated clear evidence of its pan-coronaviral activity.

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Section: Figuresupporting

confidence: 58%

Natural Flavonoid Derivatives Have Pan-Coronavirus Antiviral Activity

et al. 2023

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“…Previous studies have shown that morin encapsulation significantly enhanced its anticancer properties by improving its intracellular delivery when compared to free morin, inducing cell death in different cancer cell lines, such as lung [ 79 , 108 , 109 ], cervical [ 46 ] and breast cancer [ 70 , 110 ]. However, there is a limited amount of research on the use of mesoporous silica nanoparticles loaded with morin for melanoma treatment.…”

Section: Resultsmentioning

confidence: 99%

“…We observed a significant decrease in the viability of A375, MNT-1, and SK-MEL-28 cells when exposed to MH-MSN concentrations between 350 and 400 µg/mL after 48 and 72 h. While the differences were minor, it appears that the A375 and SK-MEL-28 cell lines, which are amelanotic (i.e., non-pigmented), were slightly more sensitive than the highly pigmented MNT-1 cells, particularly with prolonged exposure to both MH and MH-MSN treatments. Previous studies have shown that morin encapsulation significantly enhanced its anticancer properties by improving its intracellular delivery when compared to free morin, inducing cell death in different cancer cell lines, such as lung [79,108,109], cervical [46] and breast cancer [70,110]. However, there is a limited amount of research on the use of mesoporous silica nanoparticles loaded with morin for melanoma treatment.…”

Section: Effect Of Morin Hydrate and Morin-loaded Msns On Cell Viabil...mentioning

confidence: 99%

Morin Hydrate Encapsulation and Release from Mesoporous Silica Nanoparticles for Melanoma Therapy

et al. 2023

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Melanoma incidence, a type of skin cancer, has been increasing worldwide. There is a strong need to develop new therapeutic strategies to improve melanoma treatment. Morin is a bioflavonoid with the potential for use in the treatment of cancer, including melanoma. However, therapeutic applications of morin are restrained owing to its low aqueous solubility and limited bioavailability. This work investigates morin hydrate (MH) encapsulation in mesoporous silica nanoparticles (MSNs) to enhance morin bioavailability and consequently increase the antitumor effects in melanoma cells. Spheroidal MSNs with a mean size of 56.3 ± 6.5 nm and a specific surface area of 816 m2/g were synthesized. MH was successfully loaded (MH-MSN) using the evaporation method, with a loading capacity of 28.3% and loading efficiency of 99.1%. In vitro release studies showed that morin release from MH-MSNs was enhanced at pH 5.2, indicating increased flavonoid solubility. The in vitro cytotoxicity of MH and MH-MSNs on human A375, MNT-1 and SK-MEL-28 melanoma cell lines was investigated. Exposure to MSNs did not affect the cell viability of any of the cell lines tested, suggesting that the nanoparticles are biocompatible. The effect of MH and MH-MSNs on reducing cell viability was time- and concentration-dependent in all melanoma cell lines. The A375 and SK-MEL-28 cell lines were slightly more sensitive than MNT-1 cells in both the MH and MH-MSN treatments. Our findings suggest that MH-MSNs are a promising delivery system for the treatment of melanoma.

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“…The cytotoxicities of zinc( ii ) coordination complexes DQ1–DQ20 were evaluated via a cell counting kit-8 (CCK-8) assay against SK-OV-3CR cancer cells, with HL-7702 normal cells as a comparison. 32,33 The cytotoxicity of zinc( ii ) coordination complexes DQ1–DQ20 toward SK-OV-3CR cancer cells was considerably higher than that of free H-Q1–H-Q6, D1–D10 ligands, and Zn(NO 3 ) 2 ·6H 2 O (Tables 1 and S61†) and other 8-hydroxyquinoline zinc( ii ) metal complexes. 29 Additionally, the key roles of the bathophenanthroline (D4) group as the secondary ligand and the 5- and 7-dichloro-substituted group of the 8-hydroxyquinoline moiety endowed the DQ6 complex with significantly more antiproliferative activity than that of DQ1–DQ5 , DQ7–DQ20 , and the well-known standard anticancer drug cisplatin (Tables 1 and S61†).…”

Section: Resultsmentioning

confidence: 99%