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1.
Molecules ; 28(14)2023 Jul 17.
Article in English | MEDLINE | ID: mdl-37513334

ABSTRACT

New aspects of the Ni(II)-salophen complex and salophen ligand precursor were found during deep electrochemical and optical characterization, as well as biological studies for new pharmacological applications. Physicochemical and spectroscopic methods (1H- and 13C-NMR, FT-IR and UV-Vis, electrospray ionization mass spectroscopy, thermogravimetric analysis, and molar conductance measurements) were also used to prove that the salophen ligand acts as a tetradentate and coordinates to the central metal through nitrogen and oxygen atoms. The electrochemical behavior of the free Schiff salophen ligand (H2L) and its Ni(II) complex (Ni(II)L) was deeply studied in tetrabutylammonium perchlorate solutions in acetonitrile via CV, DPV, and RDE. Blue films on the surfaces of the electrodes as a result of the electropolymerization processes were put in evidence and characterized via CV and DPV. (H2L) and Ni(II)L complexes were tested for their antimicrobial, antifungal, and antioxidant activity, showing good antimicrobial and antifungal activity against several bacteria and fungi.


Subject(s)
Anti-Infective Agents , Coordination Complexes , Antifungal Agents/pharmacology , Antifungal Agents/chemistry , Spectroscopy, Fourier Transform Infrared , Ligands , Microbial Sensitivity Tests , Anti-Infective Agents/pharmacology , Anti-Infective Agents/chemistry , Schiff Bases/chemistry , Coordination Complexes/pharmacology , Coordination Complexes/chemistry
2.
Planta Med ; 81(12-13): 1154-62, 2015 Aug.
Article in English | MEDLINE | ID: mdl-25922911

ABSTRACT

The human ether-a-go-go-related gene channel is a voltage-activated K(+) channel involved in cardiac action potential. Its inhibition can lead to QT prolongation, and eventually to potentially fatal arrhythmia. Therefore, it is considered a primary antitarget in safety pharmacology. To assess the risk of human ether-a-go-go-related gene channel inhibition by medicinal plants, 700 extracts from different parts of 142 medicinal plants collected in Southern Africa were screened on Xenopus laevis oocytes. A CH2Cl2 extract from the stems and leaves of Galenia africana (Aizoaceae) reduced the peak tail human ether-a-go-go-related gene current by 50.4 ± 5.5 % (n = 3) at a concentration of 100 µg/mL. By means of high-performance liquid chromatography-based activity profiling, nine flavonoids were identified in the active time windows. However, the human ether-a-go-go-related gene channel inhibition of isolated compounds was less pronounced than that of extract and active microfractions (human ether-a-go-go-related gene inhibition between 10.1 ± 5 and 14.1 ± 1.6 at 100 µM). The two major constituents, 7,8-methylenedioxyflavone (1) and 7,8-dimethoxyflavone (13), were quantified (4.3 % and 9.4 %, respectively, in the extract). Further human ether-a-go-go-related gene inhibition tests for compounds 1 and 13 at 300 µM showed a concentration-dependent inhibitory activity (33.2 ± 12.4 and 30.0 ± 7.4, respectively). In a detailed phytochemical profiling of the active extract, a total of 20 phenolic compounds, including six new natural products, were isolated and identified.


Subject(s)
Aizoaceae/chemistry , Ether-A-Go-Go Potassium Channels/antagonists & inhibitors , Flavonoids/chemistry , Phenols/chemistry , Plant Extracts/chemistry , Potassium Channel Blockers/chemistry , Action Potentials/drug effects , Africa, Southern , Animals , Arrhythmias, Cardiac/drug therapy , Chromatography, High Pressure Liquid , ERG1 Potassium Channel , Female , Flavonoids/isolation & purification , Flavonoids/pharmacology , Heart Conduction System/drug effects , Humans , Molecular Structure , Oocytes/drug effects , Phenols/isolation & purification , Phenols/pharmacology , Plant Extracts/isolation & purification , Plant Extracts/pharmacology , Plant Leaves/chemistry , Plant Stems/chemistry , Plants, Medicinal , Potassium Channel Blockers/isolation & purification , Potassium Channel Blockers/pharmacology , Xenopus laevis
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