0000000000462332
AUTHOR
ÁLvaro Martínez
Landomycins as glutathione-depleting agents and natural fluorescent probes for cellular Michael adduct-dependent quinone metabolism
Landomycins are angucyclines with promising antineoplastic activity produced by Streptomyces bacteria. The aglycone landomycinone is the distinctive core, while the oligosaccharide chain differs within derivatives. Herein, we report that landomycins spontaneously form Michael adducts with biothiols, including reduced cysteine and glutathione, both cell-free or intracellularly involving the benz[a]anthraquinone moiety of landomycinone. While landomycins generally do not display emissive properties, the respective Michael adducts exerted intense blue fluorescence in a glycosidic chain-dependent manner. This allowed label-free tracking of the short-lived nature of the mono-SH-adduct followed b…
Anticancer platinum agents and light
Abstract Since the discovery of cisplatin, light activation has been employed as a strategy to switch and improve the anticancer effects of platinum compounds. This contribution highlights some of the most representative discoveries obtained in the field of platinum-based photochemotherapy over the years.