Cationic quaternized aminocalix[4]arenes: cytotoxicity, haemolytic and antibacterial activities

Biomedical Applications of Calixarenes: State of the Art and Perspectives

“…[51] Loftsson et al examined the cytotoxicity and hemolytic effect of an amphiphilic tetraalkylammonium-modified C4A (12), revealing the absence of cytotoxicity up to 200 mm in tests on mouse macrophage RAW 264.7 cells. [52] In terms of hemolytic activity toward rabbit red blood cells, 12 was not active at concentrations of up to 100 mm.I na ddition, assemblies based on amphiphilic CAs (13, 14,a nd 15)w ere shown to exhibit no or negligible cytotoxicity and in vivo toxicity by us and other groups. [53] Thet oxicity of some CA derivatives can be useful in certain cases.S ebti and Hamilton reported significantly cytotoxic C4A derivatives that could inhibit tumor growth and angiogenesis,w ith the lowest IC 50 observed for 16.…”

“…Loftsson et al. examined the cytotoxicity and hemolytic effect of an amphiphilic tetraalkylammonium‐modified C4A ( 12 ), revealing the absence of cytotoxicity up to 200 μ m in tests on mouse macrophage RAW 264.7 cells [52] . In terms of hemolytic activity toward rabbit red blood cells, 12 was not active at concentrations of up to 100 μ m .…”

Biomedizinische Anwendungen von Calixarenen: Stand der Wissenschaft und Perspektiven

“…[51] Loftsson et al untersuchten die Zytotoxizitätu nd den hämoly-tischen Effekt eines amphiphilen Te traalkylammonium-modifizierten C4A (12)u nd zeigten das Fehlen einer Zytotoxizitätbis zu 200 mm in Te sts an RAW264.7 Mausmakrophagenähnlichen Zellen. [52] In Bezug auf die hämolytische Aktivität gegenüber roten Blutkçrperchen von Kaninchen war 12 bei Konzentrationen von bis zu 100 mm nicht aktiv.D arüber hinaus wurde von uns und anderen Arbeitsgruppen gezeigt, dass Anordnungen, die auf amphiphilen CAs (13, 14 und 15) basieren, keine oder eine vernachlässigbare Zytotoxizitätund In-vivo-Toxizitäta ufwiesen. [53] Die Toxizitäte iniger CA-Derivate kann in bestimmten Fällen nützlich sein.…”

Calixarene Derivatives for (Nano)Biotechnologies

“…[24] Another deep investigation of calixarenes 33a,b also confirmed previously described results. [25] Calixarene-based Nanoparticles for Gene Transfection and Bio-Imaging A series of amphiphilic calixarenes 32b, 33a-d, 34b bearing cationic groups at the upper rim and the alkyl chains at the lower rim were synthesized. [26][27][28] The molecular design of these calixarenes was directed to increase their affinity for DNA (compared to 35-39 [29] ) due to formation of the additional hydrogen bonds between the hydroxyl group of choline residues and the carbohydrate and phosphate groups of DNA in the case of 33 or additional electrostatic interaction between protonated aminogroups of 34b and phosphate groups of DNA or to improve π-stacking interaction with the nucleic bases of DNA in the case of 32b.…”