1472-93-1Relevant articles and documents
PH-responsive dendritic core-multishell nanocarriers
Fleige, Emanuel,Achazi, Katharina,Schaletzki, Karolina,Triemer, Therese,Haag, Rainer
, p. 99 - 108 (2014)
In this paper we describe novel pH-responsive core-multishell (CMS) nanocarrier (pH-CMS), obtained by introducing an aromatic imine linker between the shell and the core. At a pH of 5 and lower the used imine linker was rapidly cleaved as demonstrated by NMR studies. The CMS nanocarriers were loaded with the dye Nile red (NR) and the anticancer drug doxorubicin (DOX), respectively. The transport capacities were determined using UV/Vis spectroscopy, and the sizes of the loaded and unloaded CMS nanocarriers were investigated using dynamic light scattering (DLS). We could show that CMS nanocarriers efficiently transported NR in supramolecular aggregates, while DOX was transported in a unimolecular fashion. After cellular uptake the DOX-loaded pH-responsive nanocarriers showed higher toxicities than the stable CMS nanocarriers. This is due to a more efficient DOX release caused by the cleavage of the pH-labile imine bond at lower pH within the intracellular compartments.
Cysteine-Targeted Insecticides against A. gambiae Acetylcholinesterase Are Neither Selective nor Reversible Inhibitors
Gorecki, Lukas,Andrys, Rudolf,Schmidt, Monika,Kucera, Tomas,Psotka, Miroslav,Svobodova, Barbora,Hrabcova, Veronika,Hepnarova, Vendula,Bzonek, Petr,Jun, Daniel,Kuca, Kamil,Korabecny, Jan,Musilek, Kamil
, p. 65 - 71 (2019/12/25)
Acetylcholinesterase cysteine-targeted insecticides against malaria vector Anopheles gambia and other mosquitos have already been introduced. We have applied the olefin metathesis for the preparation of cysteine-targeted insecticides in high yields. The prepared compounds with either a succinimide or maleimide moiety were evaluated on Anopheles gambiae and human acetylcholinesterase with relatively high irreversible inhibition of both enzymes but poor selectivity. The concept of cysteine binding was not proved by several methods, and poor stability was observed of the chosen most potent/selective compounds in a water/buffer environment. Thus, our findings do not support the proposed concept of cysteine-targeted selective insecticides for the prepared series of succinimide or maleimide compounds.
Direct interaction, instrumental for signaling processes, between LacCer and Lyn in the lipid rafts of neutrophil-like cells
Chiricozzi, Elena,Ciampa, Maria Grazia,Brasile, Giuseppina,Compostella, Federica,Prinetti, Alessandro,Nakayama, Hitoshi,Ekyalongo, Roudy C.,Iwabuchi, Kazuhisa,Sonnino, Sandro,Mauri, Laura
, p. 129 - 141 (2015/03/05)
Lactosylceramide [LacCer; β-Gal-(1-4)-β-Glc-(1-1)-Cer] has been shown to contain very long fatty acids that specifically modulate neutrophil properties. The interactions between LacCer and proteins and their role in cell signaling processes were assessed
