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ARS Home » Southeast Area » Oxford, Mississippi » Natural Products Utilization Research » Research » Publications at this Location » Publication #330988
Research Project: Discovery and Development of Natural Products for Pharmaceutical and Agrochemical Applications II

Location: Natural Products Utilization Research

Title: Polybrominated diphenyl ethers from the marine organisms Lendenfeldia dendyi and Sinularia dura with anti-MRSa activity

Author
item RADWAN, MOHAMED - University Of Mississippi
item WANAS, AMIRA - University Of Mississippi
item FRONCZEK, FRANK - Louisiana State University
item JACOB, MELISSA - University Of Mississippi
item ROSS, SAMIR - University Of Mississippi

Submitted to: Medical Chemistry Research
Publication Type: Peer Reviewed Journal
Publication Acceptance Date: 6/22/2015
Publication Date: 7/1/2015
Citation: Radwan, M., Wanas, A.S., Fronczek, F.R., Jacob, M.R., Ross, S.A. 2015. Polybrominated diphenyl ethers from the marine organisms Lendenfeldia dendyi and Sinularia dura with anti-MRSa activity. Medical Chemistry Research. 24:3398-3404.

Interpretive Summary: For many years, infectious diseases have been a worldwide problem and have affected quality of life and caused economic hindrance for millions of people. Resistance to antimicrobials has become an important problem in virtually all areas of infectious diseases, not just bacterial infections, including fungal and parasitic diseases as well. Methicillin-resistant Staphylococcus aureus (MRSa) is one of the most common causes of healthcare-associated infections reported to the National Nosocomial Infections Surveillance System (NNIS). This organism is resistant not only to methicillin but also to other penicillins and cephalosporins. The lack of new drug classes that act against this resistant microorganism gives us the opportunity to explore natural products with potential biomedical applications. In this study, we report the antibacterial and antifungal activities of five polybrominated diphenyl ethers (1–5), in particular activity against MRSa from the marine sponge Lendenfeldia dendyi and the soft coral Sinularia dura. The isolated compounds displayed significant and selective activity against methicillin-resistant Staphylococcus aureus (MRSa) with IC50 values of 0.1 – 1.18 µM. Compound 5 exhibited very potent and a significant antibacterial activity against MRSa with IC50 value of 0.04 µM, compared to that of the drug control ciprofloxacin (0.23 µM). Also, the isolated compounds showed no toxicity.

Technical Abstract: Bioassay-guided fractionation of the marine sponge Lendenfeldia dendyi and the soft coral Sinularia dura resulted in the isolation of five polybrominated diphenyl ethers (1-5). The structures of the isolated compounds were determined using spectroscopic methods(lD and 2D NMR) and HRMS analyses. The absolute structures of compound s 1 and 2 were confirmed by X-ray analysis. Antimicrobial testing of the isolated compounds along with the acetylated derivative of compound 2 (2a) indicated that they displayed a significant and selective activity against methicillin-resistant Staphylococcus aureus (MRSa) with IC50 values of <0.04-1.18 pM. The antimalarial and antileishmanial activities of the isolated compounds were also evaluated.