RESUMEN
This study investigates the presence of the different classes of micro-pollutants such as pharmaceutical active compounds (PhACs) (20 antibiotics, 8 analgesics and anti-inflammatories, 5 cytostatic agents, 7 ß-blockers, 4 lipid regulators, 13 psychiatrics, 1 antidiabetic, 1 receptor antagonist, 1 local anaesthetic, 1 antihypertensive and their 5 metabolites), hormones (8 compounds), X-ray contrast agents (6 compounds), benzotriazoles (3 compounds) and pesticides (6 compounds), and antibiotic resistance in hospital wastewater (HWW) of a medical faculty in Istanbul, Turkey. In addition, the seasonal variations of the selected PhACs and X-ray contrast agents and antibiotic resistance were evaluated for 2 years in a total of eight samples. In the PhACs, sulfamethoxazole and its metabolite (4 N-acethyl-sulfamethoxazole) in the antibiotic group and paracetamol in the analgesic and anti-inflammatory group were found at 100% of frequency and the highest concentrations as 35, 43 and 210 µg/L, respectively. The mean concentrations of psychiatric compounds were found less than 0.25 µg/L except carbamazepine (1.36 µg/L). Bisphenol A in hormone group had the highest concentration up to 14 µg/L. In the hormone group compounds, 17-α-Ethinylestradiol and 17-ß-Estradiol were detected at lower mean concentrations of 0.2 and 0.05 µg/L, respectively. 1H-benzotriazole had the highest concentration with the mean concentration of 24.8 µg/L in benzotriazole group compounds. The compounds in X-ray contrast agents group were noted as compounds detected at the highest concentration in HWW up to 3000 µg/L. Antibiotic resistance against azithromycin, clindamycin and trimethoprim-sulfamethoxazole antibiotics was observed around 50% in the winter period. The seasonal variation was detected for the most of the investigated PhACs, especially in antibiotic group which was in line with those significant differences in antibiotic resistance rates in the studied antibiotics between winter and summer seasons.
Asunto(s)
Preparaciones Farmacéuticas , Contaminantes Químicos del Agua , Antibacterianos/análisis , Farmacorresistencia Microbiana , Monitoreo del Ambiente , Hospitales , Estaciones del Año , Turquía , Aguas Residuales/análisis , Contaminantes Químicos del Agua/análisisRESUMEN
Infectious diseases are the significant global health problem because of drug resistance to most classes of antimicrobials. Interest is growing in the development of new antimicrobials in pharmaceutical discovery. For that reason, the urgency for scientists to find and/or develop new important molecules is needed. Many natural active molecules that exhibit various biological activities have been isolated from the nature. For the present research, a new selected set of aminobenzoquinones, denoted as plastoquinone analogs (PQ1-24), was employed for their in vitro antimicrobial potential in a panel of seven bacterial strains (three Gram-positive and four Gram-negative bacteria) and three fungi. The results revealed PQ analogs with specific activity against bacteria including Staphylococcus epidermidis and pathogenic fungi, including Candida albicans. PQ8 containing methoxy group at the ortho position on the phenylamino moiety exhibited the highest growth inhibition against S. epidermidis with a minimum inhibitory concentration of 9.76 µg/mL. The antifungal profile of all PQ analogs indicated that five analogs (while PQ1, PQ8, PQ9, PQ11, and PQ18 were effective against Candida albicans, PQ1 and PQ18 were effective against Candida tropicalis) have potent antifungal activity. Selected analogs, PQ1 and PQ18, were studied for biofilm evaluation and time-kill kinetic study for better understanding.
Asunto(s)
Antiinfecciosos/farmacología , Candida albicans/efectos de los fármacos , Plastoquinona/análogos & derivados , Plastoquinona/farmacología , Staphylococcus epidermidis/efectos de los fármacos , Antiinfecciosos/química , Biopelículas/efectos de los fármacos , Biopelículas/crecimiento & desarrollo , Candida albicans/crecimiento & desarrollo , Halogenación , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Plastoquinona/química , Staphylococcus epidermidis/crecimiento & desarrollo , Relación Estructura-ActividadRESUMEN
Four methoxy substitute salicylidene thiosemicarbazones were synthesized. The reaction of both thione and thioalkylated thiosemicarbazones with PdCl2 in ethanol yields ONS-coordinated chelate complexes with general formula [Pd(L)Cl]. The structures of eight compounds were characterized by using analytical and spectroscopic methods. Electrochemistry of the Pd(II) complexes was studied using cyclic voltammetric technique. The CVs of the complexes were quite complicate because of some oxidative responses of the ligands which proceed by forming conjugated -N=CH-, -HC=CH- and -N=CH-HC=CH- groups. Two cathodic responses attributed to one electron reduction of Pd(II)/(I) and Pd(I)/(0) were observed for the central ion coordinated with S atom of H3C-S- group whereas only one reduction peak appeared when the Pd(II) coordinated with S atom of >C=S group of thiosemicarbazone ligand. The latter also showed an additional anodic response assigned to Pd(II)/(III) oxidation. Thermogravimetric analysis (TGA) technique was used to investigate and compare the thermal properties of the ligands and their metal complexes. In vitro antimicrobial activity of thiosemicarbazones and their complexes was evaluated against four Gram-negative bacteria, three Gram-positive bacteria, and antifungal activity against three fungi.