A series of six/five member (E/Z)-Goniothalamin analogs were synthesized from commercially available (3,4-dihydro-2H-pyran-2-yl)methanol/5-(hydroxymethyl)dihydrofuran-2(3H)-one in three steps with good to moderate overall yields and their cytotoxicity against lymphoblastic leukemic T cell line (Jurkat E6.1) have been evaluated. Among the synthesized analogs, (Z)-Goniothalamin appeared to be the most active in cytotoxicity (IC50 = 12 μM). Structure-activity relationship study indicates that introducing substituent in phenyl ring or replacing phenyl ring by pyridine/naphthalene, or decreasing the ring size of lactones (from six to five member) do not increase the cytotoxicity.
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http://dx.doi.org/10.1007/s12272-013-0099-1 | DOI Listing |
Water Res
December 2024
The Ministry of Education Key Laboratory of Northwest Water Resource, Environment and Ecology, Xi'an University of Architecture and Technology, Xi'an, 710055, PR China; Shaanxi Key Laboratory of Environmental Engineering, Xi'an University of Architecture and Technology, Xi'an, 710055, PR China. Electronic address:
Permanganate (Mn(VII)) is a traditional reagent used for water purification, but it is mild to deal with refractory organic contaminants of emerging concern. There is great interest in combination with effective and low-cost biochar to improve reaction kinetics of Mn(VII). Until recently, it still unclear how biomass composition and carbon structure of biochar influence the Mn(VII) oxidation performance.
View Article and Find Full Text PDFPhys Chem Chem Phys
January 2025
School of Chemistry and Molecular Biosciences, University of Queensland, St Lucia QLD 4072, Australia.
Steroids are organic compounds found in all forms of biological life. Besides their structural roles in cell membranes, steroids act as signalling molecules in various physiological processes and are used to treat inflammatory conditions. It has been hypothesised that in addition to their well-characterised genomic and non-genomic pathways, steroids exert their biological or pharmacological activities an indirect, nonreceptor-mediated membrane mechanism caused by steroid-induced changes to the physicochemical properties of cell membranes.
View Article and Find Full Text PDFFront Pharmacol
December 2024
Department of Orthodontics, State Key Laboratory of Oral Diseases, West China School of Stomatology, Sichuan University, Chengdu, Sichuan, China.
Neprilysin (NEP), a zinc-dependent membrane-bound metallopeptidase, regulates various bioactive peptides, particularly in kidneys, vascular endothelium, and the central nervous system. NEP's involvement in metabolizing natriuretic peptides, insulin, and enkephalins makes it a promising target for treating cardiovascular and Alzheimer's diseases. Several NEP inhibitors, such as sacubitril and omapatrilat, have been approved for clinical use, which inhibit NEP activity to prolong the bioactivity of beneficial peptides, thereby exerting therapeutic effects.
View Article and Find Full Text PDFNuclear DNA is organized into a compact three-dimensional (3D) structure that impacts critical cellular processes. High-throughput chromosome conformation capture (Hi-C) is the most widely used method for measuring 3D genome architecture, while linear epigenomic assays, such as ATAC-seq, DNase-seq, and ChIP-seq, are extensively employed to characterize epigenomic regulation. However, the integrative analysis of chromatin interactions and associated epigenomic regulation remains challenging due to the pairwise nature of Hi-C data, mismatched resolution between Hi-C and epigenomic assays, and inconsistencies among analysis tools.
View Article and Find Full Text PDFSmall
January 2025
Faculty of Materials Science and Engineering, Analysis and Testing Research Center, Kunming University of Science and Technology, Kunming, 650093, P. R. China.
Modulating electronic structure to balance the requirement of both hydrogen evolution reaction (HER) and oxygen evolution reaction (OER) is crucial for developing bifunctional catalysts. Herein, phase transformation engineering is utilized to separately regulate catalyst structure, and the designed NiFe@Ni/Fe-MnOOH schottky heterojunction exhibits remarkable bifunctional electrocatalytic activity with low overpotentials of 19 and 230 mV at 10 mA cm for HER and OER in 1M KOH, respectively. Meanwhile, an anion-exchange membrane water electrolyzer employing NiFe@Ni/Fe-MnOOH as electrodes shows low voltages of 1.
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