Antioxidant and Anti-Protease Activities of Diazepinomicin from the Sponge-Associated Micromonospora Strain RV115
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- 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 antioxidantDiazepinomicin 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.…
Autor(en): | Usama Ramadan Abdelmohsen, Matthias Szesny, Eman Maher Othman, Tanja Schirmeister, Stepanie Grond, Helga Stopper, Ute Hentschel |
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URN: | urn:nbn:de:bvb:20-opus-76279 |
Dokumentart: | Artikel / Aufsatz in einer Zeitschrift |
Institute der Universität: | Fakultät für Biologie / Julius-von-Sachs-Institut für Biowissenschaften |
Sprache der Veröffentlichung: | Englisch |
Erscheinungsjahr: | 2012 |
Originalveröffentlichung / Quelle: | In: Marine Drugs (2012) 10: 10, 2208-2221, doi:10.3390/md10102208 |
Allgemeine fachliche Zuordnung (DDC-Klassifikation): | 5 Naturwissenschaften und Mathematik / 57 Biowissenschaften; Biologie / 570 Biowissenschaften; Biologie |
Normierte Schlagworte (GND): | Biologie |
Freie Schlagwort(e): | Micromonospora; actinomycetes; anti-protease; antioxidant; diazepinomicin |
Datum der Freischaltung: | 30.04.2013 |
Sammlungen: | Open-Access-Publikationsfonds / Förderzeitraum 2012 |
Lizenz (Deutsch): | CC BY: Creative-Commons-Lizenz: Namensnennung |