Antitumor Activity of Symmetrical Selenoesters in Doxorubicin Resistant Breast Cancer.

BACKGROUND/AIM: Previously, selenocompounds (Se-compounds) and in particular selenoesters have shown promising anticancer activities. Since molecular symmetry can enhance the anticancer activity, nine symmetrical selenoesters (Se-esters) have been designed as novel, potentially active anticancer agents against doxorubicin resistant breast cancer cells. MATERIALS AND METHODS: To assess the biological effects of the symmetrical Se-esters, the antiproliferative activity was determined on sensitive MCF-7 and doxorubicin resistant KCR breast cancer cell lines. The interaction of the derivatives with doxorubicin was evaluated by checkerboard combination assay on KCR cells. Furthermore, apoptosis induction and ATPase activity in the presence of Se-esters were also determined on KCR cells. RESULTS: The symmetrical derivatives showed a noteworthy antiproliferative activity, with two of them showing IC50 values in submicromolar concentration on MCF-7 cells. In addition, some derivatives showed selectivity towards the resistant KCR cells. The combination of most of them with doxorubicin resulted in synergistic interaction, and all Se-esters could induce early and late apoptosis in KCR cells. Finally, the compounds affected the ATPase activity of ABCB1 (P-gp). CONCLUSION: The symmetrical Se-esters showed potent anticancer activity, according to in vitro tests. Further research needs to be performed to obtain similar derivatives with a better activity and selectivity, and to ascertain the potential application of these Se-containing compounds using in vivo systems.

The Relationship between Antibiotic Susceptibility and pH in the Case of Uropathogenic Bacteria.

Urinary tract infections (UTIs) are common bacterial infections caused mainly by enteric bacteria. Numerous virulence factors assist bacteria in the colonization of the bladder. Bacterial efflux pumps also contribute to bacterial communication and to biofilm formation. In this study, the phenotypic and genetic antibiotic resistance of clinical UTI pathogens such as Escherichia coli, Klebsiella pneumoniae, and Proteus mirabilis were determined by disk diffusion method and polymerase chain reaction (PCR). Following this, different classes of antibiotics were evaluated for their antibacterial activity at pH 5, 6, 7 and 8 by a microdilution method. Gentamicin (GEN) was the most potent antibacterial agent against E. coli strains. The effect of GEN on the relative expression of marR and sdiA genes was evaluated by quantitative PCR. The slightly acidic pH (pH 6) and GEN treatment induced the upregulation of marR antibiotic resistance and sdiA QS activator genes in both E. coli strains. Consequently, bacteria had become more susceptible to GEN. It can be concluded that antibiotic activity is pH dependent and so the artificial manipulation of urinary pH can contribute to a more effective therapy of multidrug resistant bacterial infections.

Stable isotope data of daily precipitation during the period of 2013-2017 from K-puszta (regional background monitoring station), Hungary.

Precipitation was collected on daily basis at K-puszta regional background monitoring station located near Kecskemét, in the western part of the Great Hungarian Plain, between 1 April 2013 and 31 December 2017 for stable hydrogen and oxygen analyses. The sample collection period covered 24 hours, from 07:00 to 07:00 h LT (Local Time) the next day. Stable hydrogen and oxygen isotope composition of the daily precipitation samples were measured using a Liquid Water Isotope Analyser (LWIA-24d) manufactured by Los Gatos Research Ltd. The dataset includes 472 stable isotopic data representing the continuation of the beforehand monitoring started in 2012 [1]. The dataset provides a unique opportunity to combine daily meteorological data and stable isotope composition of daily precipitation which can help to improve our understanding of the processes and factors at relatively high resolution that govern δD and δ18O values of the precipitation. In addition, the dataset can be used as an isotope hydrological benchmark in comparison with stable isotope dataset obtained from surface- and groundwater or other sources (e.g. climate proxies, agricultural products). Thus, research related to isotope hydrology, agriculture, paleoclimate can benefit from this dataset. Interpretation of this dataset focusing on the relationship between meteorological factors and stable isotope composition of precipitation is in progress.