Kremb Stephan, Müller Constanze, Schmitt-Kopplin Philippe, Voolstra Christian R
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.
Research Unit Analytical Biogeochemistry, Helmholtz Zentrum München, Ingolstaedter Landstrasse 1, D-85764 Neuherberg, Germany.
Mar Drugs. 2017 Mar 20;15(3):80. doi: 10.3390/md15030080.
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.
海洋藻类是新型天然产物的重要来源。尽管它们的生物活性潜力已在一定程度上得到研究，但关于红海海洋藻类的信息却很有限。本研究旨在从红海中部的12种大型藻类中广泛发现新的生物活性。我们使用基于成像的高内涵筛选（HCS）和多种细胞标记物，对分级分离的藻类提取物进行详细的细胞学分析。在60个藻类组分中，有3个的细胞学分析结果与参考抑制剂密切聚类，并在单酶生化分析中对HIV-1逆转录酶显示出强大的抑制活性，从而验证了所提出的生物学靶点。随后，通过超高分辨率质谱（FT-ICR-MS）对两种褐藻的活性组分进行化学分析，揭示了可能的候选分子。对这些分子进行数据库查询，使我们找到了具有结构相似性的化合物组，这些化合物被认为是导致观察到的活性的原因。我们的工作证明了细胞学分析在未知生物资源生物勘探中的多功能性和强大作用，并突出了红海藻类作为生物活性物质来源的地位，这可能为进一步研究提供一个起点。
