Percorrer por autor "Meskini, Islem"
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- Dawson- and Lindqvist-Type hybrid polyoxometalates: synthesis, characterization and Ca2+-ATPase inhibition potentialPublication . Meskini, Islem; Capet, Frédéric; Fraqueza, Gil; Necmi, Dege; Tahir, Muhammad Nawaz; Ayed, Brahim; Aureliano, ManuelPolyoxometalates (POMs) represent a broad class of anionic inorganic (V, Mo, W) clusters with versatile structures of chemical and physical properties. POMs are inhibitors of many enzymes, including P-type ATPases, well-known to be a target of several approved drugs. Herein, two new hybrid POMs with Mo and mixed V/W, namely (C2H8N1)6[V2Mo18O62].3H2O (1) and (C4H16N3)4[V2W4O19]3.12H2O (2), were synthesized via wet chemical methods in aqueous solution, and their purity was confirmed and characterized by single X-ray diffraction and infrared spectroscopy. The cations are dimethylammonium ((C2H8N)+) and diethylenetriammonium ((C4H16N3)3+), respectively. POMs biological activities were investigated, specifically their inhibitory potential against Ca2+-ATPase. The sarcoplasmic reticulum Ca2+-ATPase activities were measured spectrophotometrically using the coupled enzyme pyruvate kinase/lactate dehydrogenase assay. For the Ca2+-ATPase activity, Dawson (1) showed an IC50 value of 3.4 μM, whereas Lindqvist (2) displayed a value of 45.1 μM. The Ca2+-ATPase inhibitory potential of these POMs can be correlated with the net charge (namely 6- and 4-) and the charge density (namely 0.33 and 0.67). A structure–activity-relationship was established for a series of 17 POMs Ca2+-ATPase inhibitors correlating IC50 values and POMs net charge and POMs charge density. The described features make Dawson (1) and Lindqvist (2) attractive POMs in a wide range of chemistry fields as well as in biomedical applications.
- Dawson- and lindqvist-type hybrid polyoxometalates: synthesis, characterization and Ca2+-ATPase inhibition potentialPublication . Meskini, Islem; Capet, Frédéric; Fraqueza, Gil; Dege, Necmi; Tahir, Muhammad Nawaz; Ayed, Brahim; Aureliano, ManuelPolyoxometalates (POMs) represent a broad class of anionic inorganic (V, Mo, W) clusters with versatile structures of chemical and physical properties. POMs are inhibitors of many enzymes, including P-type ATPases, well-known to be a target of several approved drugs. Herein, two new hybrid POMs with Mo and mixed V/W, namely (C2H8N1)6[V2Mo18O62].3H2O (1) and (C4H16N3)4[V2W4O19]3.12H2O (2), were synthesized via wet chemical methods in aqueous solution, and their purity was confirmed and characterized by single X-ray diffraction and infrared spectroscopy. The cations are dimethylammonium ((C2H8N)+ ) and diethylenetriammonium ((C4H16N3) 3+), respectively. POMs biological activities were investigated, specifically their inhibitory potential against Ca2+-ATPase. The sarcoplasmic reticulum Ca2+-ATPase activities were measured spectrophotometrically using the coupled enzyme pyruvate kinase/lactate dehydrogenase assay. For the Ca2+-ATPase activity, Dawson (1) showed an IC50 value of 3.4 µM, whereas Lindqvist (2) displayed a value of 45.1 µM. The Ca2+-ATPase inhibitory potential of these POMs can be correlated with the net charge (namely 6- and 4-) and the charge density (namely 0.33 and 0.67). A structure–activity-relationship was established for a series of 17 POMs Ca2+-ATPase inhibitors correlating IC50 values and POMs net charge and POMs charge density. The described features make Dawson (1) and Lindqvist (2) attractive POMs in a wide range of chemistry fields as well as in biomedical applications.
- Synthesis, characterization, hirshfeld surface analysis of V-substituted keggin polyoxotungstates and Ca2+-ATPase inhibiting potentialPublication . Meskini, Islem; Fraqueza, Gil; Capet, Frédéric; Aureliano, Manuel; Ayed, BrahimPolyoxometalates (POMs) biological and biomedical applications have attracted increasing attention over the past decades. Polyoxometalates are inorganic transition metal oxygen clusters characterized by having multiple structures and tunable electronic properties that are well-known to be effective inhibitors of many enzymes, such as ATPases. Herein, a new hybrid POM of the Keggin type, Vanadium-substituted Keggin polyoxotungstate, namely (C₆H₁₅N)₄(C₆H₁₆N)₆(VW₁₂O₄₀)₂⋅4H₂O, was synthesized via wet-chemical methods in aqueous solution. Its purity was confirmed, and the compound was fully characterized by single-crystal X-ray diffraction, infrared spectroscopy, UV–visible spectroscopy, and thermogravimetric analysis. The Keggin-type compound exhibited a half maximal inhibitory concentration (IC50) value of 8.25 μM toward calcium adenosine triphosphatase (Ca2+- ATPase) inhibition, as measured spectrophotometrically using a coupled pyruvate kinase/lactate dehydrogenase enzyme assay. Hirshfeld surface analysis was employed to investigate intermolecular interactions within the crystal structure, revealing differences in hydrogen bonding and oxygen-based contacts. These structural features may suggest a possible relationship with the observed biological activity; however, no direct correlation with Ca2+-ATPase inhibition can be firmly established from the present data. Therefore, the observed relationships should be considered preliminary and structural in nature, rather than mechanistic. Further computational and biological studies are required to clarify the role of these interactions in enzyme inhibition.