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Alkaloids from the sponge Stylissa carteri present prospective scaffolds for the inhibition of Human Immunodeficiency Virus 1 (HIV-1).
Mar. Drugs 14:28 (2016)
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.
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Publication type
Article: Journal article
Document type
Scientific Article
Keywords
Hiv-1 ; Red Sea ; Stylissa Carteri ; Marine Bioprospecting ; Reverse Transcriptase; Natural-product; Drug Discovery; Marine; Hymenialdisine; Kinases
ISSN (print) / ISBN
1660-3397
e-ISSN
1660-3397
Journal
Marine Drugs
Quellenangaben
Volume: 14,
Issue: 2,
Article Number: 28
Publisher
MDPI
Publishing Place
Basel
Non-patent literature
Publications
Reviewing status
Peer reviewed