Can topographic features of debris cones (SW Spitsbergen) be geoindicators of environmental changes?

Evidence of recent geomorphic processes within debris cones, their spatial distribution and diversification on cones surface are interpreted in the context of contemporary slope morphogenesis. The detailed inventory of relief features on debris cones in the SW Spitsbergen revealed their great spatial diversity. It is linked with a dominance of different morphological processes in adjacent areas. Spatial and temporal diversity of process-relief assemblages on cones is strongly related with local factors, like bedrock lithology, slope aspect and inclination, local circulation and climatic conditions. However, the potential role of debris cones and their topographic features as geoindicators archiving information about the environmental impact of global changes, cannot be explicitly estimated. Local constraints obscure the regional expression of any global trends, which could be detected on the basis of process-relief assemblages on debris cones in polar regions

The Former Gestapo Headquarters and the Provincial Office of Public Security in Anstadt Avenue in Łódź Interdisciplinary Site Research

The paper discusses the research me­thods and the most important results of the interdisciplinary project “The Former Gestapo Headquarters and the Provincial Office of Public Security in Anstadt Avenue in Łódź. Interdisciplinary Site Research” conducted in 2019–2021. Considering the challenges faced by the archaeology of the contemporary past, a subdiscipline of archaeology, an attempt was made to link the results of archaeological research to the relatively well-known historical context of structural and functional transformations of the site explored, mostly the establishment of a Jewish school in Anstadt Avenue at the end of the 1930s, the operation of the Gestapo headquarters during the Second World War and of the communist Provincial Office of Public Security after the war, and the division of the site into police and school sections in 1957, which has been preserved to date. Also ethno­graphic research was carried out, which identified sources referring to the forms of remembrance and commemoration of places, events, and people. The Authors hope that the archaeological research will be soon resumed on account of the planned investments, allowing to publish a complementary and interdisciplinary monograph of the site explored

Molecular structure, in vitro anticancer study and molecular docking of new phosphate derivatives of betulin

A series of 30-diethylphosphate derivatives of betulin were synthesized and evaluated for their in vitro cytotoxic activity against human cancer cell lines, such as amelanotic melanoma (C-32), glioblastoma (SNB-19), and two lines of breast cancer (T47D, MDA-MB-231). The molecular structure and activities of the new compounds were also compared with their 29-phosphonate analogs. Compounds 7a and 7b showed the highest activity against C-32 and SNB-19 cell lines. The IC50 values for 7a were 2.15 and 0.91 M, and, for 7b, they were 0.76 and 0.8 M for the C-32 and SNB-19 lines, respectively. The most potent compounds, 7a and 7b, were tested for their effects on markers of apoptosis, such as H3, TP53, BAX, and BCL-2. For the whole series of phosphate derivatives, a lipophilicity study was performed, and the ADME parameters were calculated. The most active products were docked to the active site of the EGFR protein. The relative binding affinity of selected phosphate betulin derivatives toward EGFR was compared with standard erlotinib on the basis of ChemScore and KDEEP score. Positively, all derivatives docked inside the cavity and showed significant interactions. Moreover, a molecular dynamics study also reveals that ligands 7a,b form stable complexes and the plateau phase started after 7 ns

Quinolinesulfonamides: Interaction between bovine serum albumin, molecular docking analysis, and antiproliferative activity against human breast carcinoma cells

<p>The complex formation of bovine serum albumin (BSA) with library of all seven regioisomeric quinolinesulfonamides (QSAs) under physiological condition is studied in this paper. The fluorescence quenching mechanism of BSA by QSAs was discussed and the association constants, as well as the number of binding sites, were calculated. In addition, a molecular docking study of the tested sulfamoylquinolines on the active site of serum albumin is performed. The experimental data and molecular docking studies reveal that sulfamoylquinolines bind in the large hydrophobic cavity of subdomain IB, and in the hydrophobic pockets of BSA subdomains IIA and IIIA by hydrophobic interactions with tryptophanyl (Trp-213) and tyrosyl residues. Moreover, the antiproliferative activity of QSAs against two human breast cancer cell lines (human adenocarcinoma (MCF-7) and human ductal carcinoma (MDA-MB-231)) and a human normal fibroblast is also studied in this paper. The antiproliferative activity of the tested QSAs was comparable to those of cisplatin. The returned data indicate that some of the tested quinolinesulfamoyl derivatives display significant cytotoxic activity.</p