%0 Journal Article %1 abdelmohsen2012antioxidant %A Abdelmohsen, Usama Ramadan %A Szesny, M %A Othman, E M %A Schirmeister, T %A Grond, S %A Stopper, H %A Hentschel, Ute %D 2012 %J Mar Drugs %K Micromonospora actinomycetes anti-protease antioxidant diazepinomicin myown %N 10 %P 2208-2221 %T Antioxidant and anti-protease activities of diazepinomicin from the sponge-associated Micromonospora strain RV115 %U http://dx.doi.org/10.3390/md10102208 %V 10 %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 IC50 of 70–90 µM. It also showed antiparasitic activity against trypomastigote forms of Trypanosoma brucei with an IC50 of 13.5 µM. These results showed unprecedented antioxidant and anti-protease activities of diazepinomicin, thus further highlighting its potential as a future drug candidate.

@article{abdelmohsen2012antioxidant, abstract = {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 IC50 of 70–90 µM. It also showed antiparasitic activity against trypomastigote forms of Trypanosoma brucei with an IC50 of 13.5 µM. These results showed unprecedented antioxidant and anti-protease activities of diazepinomicin, thus further highlighting its potential as a future drug candidate.}, added-at = {2013-02-27T11:53:18.000+0100}, author = {Abdelmohsen, Usama Ramadan and Szesny, M and Othman, E M and Schirmeister, T and Grond, S and Stopper, H and Hentschel, Ute}, biburl = {https://www.bibsonomy.org/bibtex/2712221242e31b91e9f3d265f3f07bda2/abdelmohsen}, interhash = {a943f6ae43a67c1600194648b2b985e3}, intrahash = {712221242e31b91e9f3d265f3f07bda2}, journal = {Mar Drugs}, keywords = {Micromonospora actinomycetes anti-protease antioxidant diazepinomicin myown}, number = 10, pages = {2208-2221}, timestamp = {2013-02-27T12:33:07.000+0100}, title = {Antioxidant and anti-protease activities of diazepinomicin from the sponge-associated Micromonospora strain RV115}, url = {http://dx.doi.org/10.3390/md10102208}, volume = 10, year = 2012 }