%0 Journal Article
%T Antioxidant and Anti-Protease Activities of Diazepinomicin from the Sponge-Associated Micromonospora Strain RV115
%A Usama Ramadan Abdelmohsen
%A Matthias Szesny
%A Eman Maher Othman
%A Tanja Schirmeister
%A Stephanie Grond
%A Helga Stopper
%A Ute Hentschel
%J Marine Drugs
%D 2012
%I MDPI AG
%R 10.3390/md10102208
%X Diazepinomicin is a dibenzodiazepine alkaloid with an unusual structure among the known microbial metabolites discovered so far. Diazepinomicin was isolated from the marine sponge-associated strain Micromonospora sp. RV115 and was identified by spectroscopic analysis and by comparison to literature data. In addition to its interesting preclinical broad-spectrum antitumor potential, we report here new antioxidant and anti-protease activities for this compound. Using the ferric reducing antioxidant power (FRAP) assay, a strong antioxidant potential of diazepinomicin was demonstrated. Moreover, diazepinomicin showed a significant antioxidant and protective capacity from genomic damage induced by the reactive oxygen species hydrogen peroxide in human kidney (HK-2) and human promyelocytic (HL-60) cell lines. Additionally, diazepinomicin inhibited the proteases rhodesain and cathepsin L at an IC 50 of 70¨C90 ¦ÌM. It also showed antiparasitic activity against trypomastigote forms of Trypanosoma brucei with an IC 50 of 13.5 ¦ÌM. These results showed unprecedented antioxidant and anti-protease activities of diazepinomicin, thus further highlighting its potential as a future drug candidate.
%K diazepinomicin
%K anti-protease
%K antioxidant
%K actinomycetes
%K Micromonospora
%U http://www.mdpi.com/1660-3397/10/10/2208