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- Title
Antioxidant and Anti-Protease Activities of Diazepinomicin from the Sponge-Associated Micromonospora Strain RV115.
- Authors
Abdelmohsen, Usama Ramadan; Szesny, Matthias; Othman, Eman Maher; Schirmeister, Tanja; Grond, Stephanie; Stopper, Helga; Hentschel, Ute
- 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.
- Subjects
THERAPEUTIC use of alkaloids; THERAPEUTIC use of antioxidants; MICROMONOSPORA; SPONGES (Invertebrates); METABOLITES; SPECTROSCOPIC imaging; ANTINEOPLASTIC agents; CELL lines; THERAPEUTICS
- Publication
Marine Drugs, 2012, Vol 10, Issue 10, p2208
- ISSN
1660-3397
- Publication type
Article
- DOI
10.3390/md10102208