Organometallic half-sandwich complexes (η5-Cp)IrCl(L)PF6 (1) and (η5-Cp)RhCl(L)PF6 (2) were prepared using pentamethylcyclopentadienyl chloride dimers of iridium(III) or rhodium(III) with the ...4-amino-N-(2,2′-bipyridin-5-yl)benzenesulfonamide ligand (L) and ammonium hexafluorophosphate. The crystal structures of L, 1, and 2 were analyzed in detail. The coordination reactions of the ligand with the central ions were confirmed using various spectroscopic techniques. Additionally, the interactions between sulfaligand, Ir(III), and Rh(III) complexes with carbonic anhydrase (CA), human serum albumin (HSA), and CT-DNA were investigated. The iridium(III) complex (1) did not show any antiproliferative properties against four different cancer cell lines, i.e., nonsmall cell lung cancer A549, colon cancer HCT-116, breast cancer MCF7, lymphoblastic leukemia Nalm-6, and a nonmalignant human embryonic kidney cell line HEK293, due to high binding affinity to GSH. The sulfonamide ligand (L) and rhodium(III) complex (2) were further studied. L showed competitive inhibition toward CA, while complexes 1 and 2, uncompetitive. All compounds interacted with HSA, causing a conformational change in the protein’s α-helical structure, suggesting the induction of a more open conformation in HSA, reducing its biological activity. Both L and 2 were found to induce cell death through a caspase-dependent pathway. These findings position L and 2 as potential starting compounds for pharmaceutical, therapeutic, or medicinal research.
Recently, a new Chronic Kidney Disease Epidemiology Collaboration (CKD-EPI) formula was presented as a better alternative to the modification of diet in renal disease (MDRD) formula for GFR ...estimation (eGFR) in patients with relatively well-preserved kidney function. The main objective of our study was to compare the eGFR results arrived by the new CKD-EPI to the older MDRD equation in antiretroviral (ARV)-naive and ARV-treated HIV-1-infected patients. The study was performed in 287 adult HIV-1-infected patients and was an evaluation comparing eGFR results based on age, gender, race, and serum creatinine. The biggest difference in estimated glomerular filtration rate (eGFR) measured by the two formulas was seen in ARV-naive men with well-preserved kidney function (p = 0.001). Moreover, we found a significant negative correlation between mean difference in eGFR measured by the two equations and the age of the studied subjects (r = -0.37, p < 0.001). No correlation was observed between mean difference in eGFR and HIV viral load (r = -0.15, p = 0.2). Independent of the equation used, a significant decrease of eGFR in ARV-treated in comparison to ARV-untreated HIV-1-infected patients was seen (p < 0.001). In conclusion, in HIV-1-infected subjects, especially in ARV-naive men with well-preserved kidney function, eGFR measured by MDRD and CKD-EPI formulas varies strongly following the method used. Such discrepancies may be important in everyday clinical practice and must be confirmed by additional studies using GFR measured with a reference method.
Glacier retreat is an eminent consequence of exacerbating climate change. In the Svalbard archipelago, most of the glaciers are discharging fresh and turbid waters directly to the sea, substantially ...impacting the coastal Arctic marine ecosystems. This study attempted to characterise the environmental conditions (hydrography, turbidity, marine aggregates) in the glacial-influenced waters and relate them to the abundance and species composition of protists and zooplankton. The study was conducted in the summer of 2016 in two Svalbard fjords (Wijdefjorden and Rijpfjorden) as well as in coastal waters close to glacier terminations on two islands (Nordaustlandet and Edgeøya). Well-recognised gradients in seawater salinity, turbidity, and particle aggregates that spread from glacier fronts towards open waters were not directly associated with the corresponding horizontal gradients in plankton communities. However, the studied environmental parameters explained the high overall variability in protists and zooplankton abundance (70 and 62% of explained variation, respectively). Different vertical distribution patterns and composition of plankton and marine aggregates were observed between fjords compared to open sea island locations suggesting different origin and transport of pelagic organisms and aggregate suspensions among study locations. The results do not support the hypothesis of synchronised horizontal change in environmental and biological components, which indicates that the relation between glacier meltwaters and plankton dynamics is a derivative of complex interactions driven by several physical and ecological processes that occur at different spatiotemporal scales. Nevertheless, this investigation provides new data pertaining to particle and plankton concentrations and structure in coastal waters near glaciers, which is essential for further understanding of the future coastal Arctic ecosystems functioning under rapid glacier retreat caused by climate change.
•Marine-terminating glaciers produce strong environmental gradients in Svalbard waters.•Climate-induced coastal water darkening will create hindered conditions for plankton.•The response of plankton to glacier discharge is not straightforward.•Various spatiotemporal scales result in different bio-physical interactions.•Composition of plankton and aggregates differs between fjords and shelfs of islands.
The measurement of oxygen consumption is an important element in the understanding of an organism's metabolic state. Oxygen is also a phosphorescence quencher, which allows the evaluation of ...phosphorescence emitted by oxygen sensors. Two Ru(II)-based oxygen-sensitive sensors were used to study the effect of chemical compounds (
) = CoCl
(dap)
Cl, and (
) = CoCl
(en)
Cl (AmB = amphotericin B) against reference and clinical strains of
. The
-(4,7-diphenyl-1,10-phenanthroline)ruthenium(II) chloride (Ru(DPP)
Cl
) (Box) adsorbed onto the Davisil
silica gel was embedded in the silicone rubber Lactite NuvaSil
5091 and the coating on the bottom of 96-well plates. The water-soluble oxygen sensor (BsOx =
-(4,7-diphenyl-1,10-phenanthrolinedisulphonic acid disodium)ruthenium(II) chloride 'x' hydrate = {RuDPP(SO
Na)
}Cl
= water molecules were omitted in the BsOx formula) was synthesized and characterized by RP-UHPLC, LCMS, MALDI, elemental analysis, ATR, UV-Vis,
H NMR, and TG/IR techniques. The microbiological studies were performed in the environment of RPMI broth and blood serum. Both Ru(II)-based sensors turned out to be useful in the study of the activity of Co(III) complexes and the commercial antifungal drug amphotericin B. In addition, a new activity of the oxygen sensor, the soluble Ru(II) complex BsOx, was demonstrated, which is a mixture with amphotericin B that caused a significant increase in its antifungal activity. Thus, it is also possible to demonstrate the synergistic effect of compounds active against the microorganisms under study.
Background
Evaluation of skin condition on the basis of parametrization and objective measurements of the parameters has become obligatory. The aim of this study was to assess sex‐related changes in ...skin topography and structure using the skin testing equipment.
Materials and Methods
The study was carried out on the group of 40 volunteers (20 females and 20 males) of the mean age 24 ± 3 years. The skin parameters were measured using 3 devices: Visioscan® VC 98 (skin topography), Visioline® VL 650 (skin macro relief) and Ultrascan UC22 (ultrasound imaging of the skin). All measurements were performed on the inner part of the left forearm.
Results
The skin parameters measured revealed significant differences in skin surface and structure between females and males. The skin of all women subjects was more homogenous in its structure with the presence of more abundant superficial skin lines and wrinkles in comparison to male skin. The higher number of skin furrows in the skin of women is in agreement with literature reports claiming that men's skin has lower number of wrinkles which are deeper and more pronounced. Ultrasound imaging of the skin indicated greater thickness and lower density of the dermis of men subjects compared to those of females.
Conclusion
Non‐invasive methods of skin testing using new and advanced equipment have provided a possibility of objective parametrization and evaluation of sex‐related changes in skin topography and structure.
Fungal pathogens are considered as serious factors for deadly diseases and are a case of medical concern. Invasive fungal infections also complicate the clinical course of COVID-19, leading to a ...significant increase in mortality. Furthermore, fungal strains' multidrug resistance has increased the demand for antifungals with a different mechanism of action. The present study aimed to identify antifungal compounds targeting yeast topoisomerase II (yTOPOII) derived from well-known human topoisomerase II (hTOPOII) poisons C-1305 and C-1311. Two sets of derivatives: triazoloacridinones (IKE1-8) and imidazoacridinones (IKE9-14) were synthetized and evaluated with a specific emphasis on the molecular mechanism of action. Our results indicated that their effectiveness as enzyme inhibitors was not solely due to intercalation ability but also as a result of influence on catalytic activity by the formation of covalent complexes between plasmid DNA and yTOPOII. Lysine conjunction increased the strength of the compound's interaction with DNA and improved penetration into the fungal cells. Triazoloacridinone derivatives in contrast to starting compound C-1305 exhibited moderate antifungal activity and at least twice lower cytotoxicity. Importantly, compounds (IKE5-8) were not substrates for multidrug ABC transporters whereas a derivative conjugated with lysine (IKE7), showed the ability to overcome C. glabrata fluconazole-resistance (MIC 32-64 µg mL
).
Human DNA topoisomerases are essential for crucial cellular processes, including DNA replication, transcription, chromatin condensation, and maintenance of its structure. One of the significant ...strategies employed in cancer treatment involves the inhibition of a specific type of topoisomerase, known as topoisomerase II (Topo II). Carbazole derivatives, recognised for their varied biological activities, have recently become a significant focus in oncological research. This study assesses the efficacy of three symmetrically substituted carbazole derivatives: 2,7-Di(2-furyl)-9H-carbazole (
), 3,6-Di(2-furyl)-9H-carbazole (
), and 3,6-Di(2-thienyl)-9H-carbazole (
) - as anticancer agents. Among investigated carbazole derivatives, compound 3,6-di(2-furyl)-9H-carbazole bearing two furan moieties emerged as a novel catalytic inhibitor of Topo II. Notably, 3,6-di(2-furyl)-9H-carbazole effectively selectively inhibited the relaxation and decatenation activities of Topo IIα, with minimal effects on the IIβ isoform. These findings underscore the potential of compound 3,6-Di(2-furyl)-9H-carbazole as a promising lead candidate warranting further investigation in the realm of anticancer drug development.
Celotno besedilo
Dostopno za:
DOBA, IZUM, KILJ, NUK, PILJ, PNG, SAZU, UILJ, UKNU, UL, UM, UPUK
ABSTRACT
Background Recent studies in rodents revealed that regulatory T cells (T reg cells) with CD4+CD25+ phenotype can exert suppressive effects on experimentally‐induced allergic airway ...inflammation and airway hyper‐reactivity. It is unclear however, whether modulations of bronchoconstriction responses in human subjects might be related to T reg cells. We report here for the first time the changes in frequency of circulating lymphocytes with putative T reg cell phenotype (CD4+CD25+CD127low) in relation to bronchoconstriction phenotype following an intrabronchial allergen challenge.
Material and methods Thirty‐one house dust mite sensitive patients were challenged with Dermatophagoides pteronyssinus extract (Dp). Eleven isolated early responders (IER) were compared with nine dual (early and late) responders (DR) and to 11 non‐responders (NR). Frequencies of peripheral blood CD4+CD25+CD127low lymphocytes were assessed in all groups of patients by using three‐parameter flow cytometry before, and six and 24 h, after allergen inhalation.
Results At baseline, frequencies of CD4+CD25+CD127low lymphocytes were not statistically different among NR, IER and DR. When all individuals were analyzed together, a statistically significant decrease in frequency of CD4+CD25+CD127low lymphocytes was observed 6 h after the bronchial challenge. Interestingly, such a pattern was found consistently only in NR, while IER and DR displayed varying responses resulting in a trend similar to that of NR. Twenty‐four hours after the bronchial challenge, frequencies of CD4+CD25+CD127low lymphocytes in all groups tended to return to baseline values.
Conclusions Our data indicate that bronchial allergen inhalation in sensitive patients (predominantly in those who did not develop significant bronchoconstriction) is associated with a decrease of proportion of peripheral lymphocytes with regulatory T cell phenotype.
Pt(II)-imprinted thiocyanato-functionalized SBA-15 materials were prepared by co-condensation of tetraethoxysilane with various amounts of thiocyanatopropyltriethoxysilane in the presence of ...Pluronic123 and Pt(II) ions. The obtained materials were characterized by physicochemical methods. The adsorption behaviour of the Pt(II)-imprinted thiocyanato-functionalized SBA-15 with respect to Pt(II) ions was studied. Ion-imprinted materials were found to show a high adsorption capacity in a wide range of solution pH and fast Pt(II) adsorption rate. The maximum static adsorption capacity of the ion-imprinted sorbent synthesized of tetraethoxysilane and thiocyanatopropyltriethoxysilane in molar ratio of 18/2 for Pt(II) were 76.4 mg/g. The obtained Pt(II)-imprinted materials show a high selectivity towards Pt(II) ions in the presence of Au(III), Ru(II) and Pd(II) ions. Acidified thiourea solution was found to be the most effective medium for platinum species desorption from the synthesized ion-imprinted sorbents for 5 adsorption/desorption cycles. Each time 92% of platinum species were leached from the material in 1 mol/L thiourea solution without significantly decreasing of its adsorption capacity. The results showed that obtained ion-imprinted mesoporous organosilica could be employed as an effective material for the recovery of platinum from hospital wastewater.
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•Pt(II)-imprinting affects on porosity and morphology of functionalized SBA-15.•Adsorption of Pt(II) onto functionalized ion-imprinted SBA-15 reached 78 mg g−1.•Pt(II)-imprinted SBA-15 provides fast Pt(II) removal.•Adsorption of Pt(II) in the presence of Pd(II), Au(III) and Ru(III) was selective.•It allows for effective removal of Pt(II) species from hospital wastewater.
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