Bioactive Potential of Marine Macroalgae from the Central Red Sea (Saudi Arabia) Assessed by High-Throughput Imaging-Based Phenotypic Profiling.
Marine algae represent an important source of novel natural products. While their bioactive potential has been studied to some extent, limited information is available on marine algae from the Red Sea. This study aimed at the broad discovery of new bioactivities from a collection of twelve macroalgal species from the Central Red Sea. We used imaging-based High-Content Screening (HCS) with a diverse spectrum of cellular markers for detailed cytological profiling of fractionated algal extracts. The cytological profiles for 3 out of 60 algal fractions clustered closely to reference inhibitors and showed strong inhibitory activities on the HIV-1 reverse transcriptase in a single-enzyme biochemical assay, validating the suggested biological target. Subsequent chemical profiling of the active fractions of two brown algal species by ultra-high resolution mass spectrometry (FT-ICR-MS) revealed possible candidate molecules. A database query of these molecules led us to groups of compounds with structural similarities, which are suggested to be responsible for the observed activity. Our work demonstrates the versatility and power of cytological profiling for the bioprospecting of unknown biological resources and highlights Red Sea algae as a source of bioactives that may serve as a starting point for further studies.
Red Sea Research Center, Division of Biological and Environmental Science and Engineering (BESE), King Abdullah University of Science and Technology (KAUST), 23955-6900 Thuwal, Saudi Arabia. sk6225@nyu.edu.
Stephan
S
Kremb
Research Unit Analytical Biogeochemistry, Helmholtz Zentrum München, Ingolstaedter Landstrasse 1, D-85764 Neuherberg, Germany. constanze.mueller@helmholtz-muenchen.de.
Constanze
C
Müller
Research Unit Analytical Biogeochemistry, Helmholtz Zentrum München, Ingolstaedter Landstrasse 1, D-85764 Neuherberg, Germany. schmitt-kopplin@helmholtz-muenchen.de.|Chair of Analytical Food Chemistry, Technische Universität München (TUM), 85354 Freising-Weihenstephan, Germany. schmitt-kopplin@helmholtz-muenchen.de.
Philippe
P
Schmitt-Kopplin
Red Sea Research Center, Division of Biological and Environmental Science and Engineering (BESE), King Abdullah University of Science and Technology (KAUST), 23955-6900 Thuwal, Saudi Arabia. christian.voolstra@kaust.edu.sa.
Christian R
CR
Voolstra
D001688:Biological Products / Q000737:chemistry* / Q000494:pharmacology; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors; D019156:Indian Ocean; D013058:Mass Spectrometry / Q000379:methods; D012529:Saudi Arabia; D012624:Seaweed / Q000737:chemistry*
D001688:Biological Products; C514824:reverse transcriptase, Human immunodeficiency virus 1; D054303:HIV Reverse Transcriptase
HIV; High-Content Screening; algae; bioprospecting; cytological profiling; natural products