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Mar. Drugs 2016, 14(2), 28;

Alkaloids from the Sponge Stylissa carteri Present Prospective Scaffolds for the Inhibition of Human Immunodeficiency Virus 1 (HIV-1)

Red Sea Research Center, Division of Biological and Environmental Science and Engineering, King Abdullah University of Science and Technology (KAUST), Thuwal 23955-6900, Saudi Arabia
Research Unit Analytical BioGeoChemistry, Helmholtz Zentrum Muenchen, 85764 Neuherberg, Germany
Institute of Virology, Helmholtz Zentrum Muenchen, German Research Center for Environmental Health, Ingolstädter Landstraße 1, D-85764 Neuherberg, Germany
Analytical Food Chemistry, Technical University of Munich, 85354 Freising Weihenstephan, Germany
Scripps Institution of Oceanography and Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego, 9500 Gilman Drive, La Jolla, CA 92093, USA
Author to whom correspondence should be addressed.
Academic Editor: Paul Long
Received: 21 July 2015 / Revised: 18 December 2015 / Accepted: 14 January 2016 / Published: 4 February 2016
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The sponge Stylissa carteri is known to produce a number of secondary metabolites displaying anti-fouling, anti-inflammatory, and anti-cancer activity. However, the anti-viral potential of metabolites produced by S. carteri has not been extensively explored. In this study, an S. carteri extract was HPLC fractionated and a cell based assay was used to evaluate the effects of HPLC fractions on parameters of Human Immunodeficiency Virus (HIV-1) infection and cell viability. Candidate HIV-1 inhibitory fractions were then analyzed for the presence of potential HIV-1 inhibitory compounds by mass spectrometry, leading to the identification of three previously characterized compounds, i.e., debromohymenialdisine (DBH), hymenialdisine (HD), and oroidin. Commercially available purified versions of these molecules were re-tested to assess their antiviral potential in greater detail. Specifically, DBH and HD exhibit a 30%–40% inhibition of HIV-1 at 3.1 μM and 13 μM, respectively; however, both exhibited cytotoxicity. Conversely, oroidin displayed a 50% inhibition of viral replication at 50 μM with no associated toxicity. Additional experimentation using a biochemical assay revealed that oroidin inhibited the activity of the HIV-1 Reverse Transcriptase up to 90% at 25 μM. Taken together, the chemical search space was narrowed and previously isolated compounds with an unexplored anti-viral potential were found. Our results support exploration of marine natural products for anti-viral drug discovery. View Full-Text
Keywords: Stylissa carteri; marine bioprospecting; HIV-1; reverse transcriptase; Red Sea Stylissa carteri; marine bioprospecting; HIV-1; reverse transcriptase; Red Sea

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O’Rourke, A.; Kremb, S.; Bader, T.M.; Helfer, M.; Schmitt-Kopplin, P.; Gerwick, W.H.; Brack-Werner, R.; Voolstra, C.R. Alkaloids from the Sponge Stylissa carteri Present Prospective Scaffolds for the Inhibition of Human Immunodeficiency Virus 1 (HIV-1). Mar. Drugs 2016, 14, 28.

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