Next Article in Journal
Anti-Human Rhinoviral Activity of Polybromocatechol Compounds Isolated from the Rhodophyta, Neorhodomela aculeata
Previous Article in Journal
Marine Cyanobacteria Compounds with Anticancer Properties: A Review on the Implication of Apoptosis
Mar. Drugs 2012, 10(10), 2208-2221; doi:10.3390/md10102208
Article

Antioxidant and Anti-Protease Activities of Diazepinomicin from the Sponge-Associated Micromonospora Strain RV115

1,†,* , 2
,
3,‡
,
4
,
2
,
3
 and
1
1 Julius-von-Sachs-Institute for Biological Sciences, University of Würzburg, Julius-von-Sachs-Platz 3, Würzburg 97082, Germany 2 Institute of Organic Chemistry, Eberhard-Karls-Universität, Auf der Morgenstelle 18, Tübingen 72076, Germany 3 Department of Toxicology, University of Würzburg, Würzburg 97078, Germany 4 Institute of Pharmacy and Biochemistry, University of Mainz, Staudinger Weg 5, Mainz 55128, Germany Permanent address: Department of Pharmacognosy, Faculty of Pharmacy, Minia University, Minia 61519, Egypt. Permanent address: Department of Analytical Chemistry, Faculty of Pharmacy, Minia University, Minia 61519, Egypt.
* Author to whom correspondence should be addressed.
Received: 24 July 2012 / Revised: 6 September 2012 / Accepted: 17 September 2012 / Published: 8 October 2012
View Full-Text   |   Download PDF [337 KB, uploaded 24 February 2015]   |   Browse Figures

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.
Keywords: diazepinomicin; anti-protease; antioxidant; actinomycetes; Micromonospora diazepinomicin; anti-protease; antioxidant; actinomycetes; Micromonospora
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Share & Cite This Article

Further Mendeley | CiteULike
Export to BibTeX |
EndNote
MDPI and ACS Style

Abdelmohsen, U.R.; Szesny, M.; Othman, E.M.; Schirmeister, T.; Grond, S.; Stopper, H.; Hentschel, U. Antioxidant and Anti-Protease Activities of Diazepinomicin from the Sponge-Associated Micromonospora Strain RV115. Mar. Drugs 2012, 10, 2208-2221.

View more citation formats

Related Articles

Article Metrics

For more information on the journal, click here

Comments

Cited By

[Return to top]
Mar. Drugs EISSN 1660-3397 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert