Abstract
Due to the unique biodiversity and the physical-chemical properties of their environment, marine microorganisms have evolved defense and signaling compounds that often have no equivalent in terrestrial habitats. The aim of this study was to screen extracts of the dinoflagellate Amphidinium carterae for possible bioactivities (i.e., anticancer, anti-inflammatory, anti-diabetes, antibacterial and antifungal properties) and identify bioactive compounds. Anticancer activity was evaluated on human lung adenocarcinoma (A549), human skin melanoma (A2058), human hepatocellular carcinoma (HepG2), human breast adenocarcinoma (MCF7) and human pancreas carcinoma (MiaPaca-2) cell lines. Antimicrobial activities were evaluated against Gram-positive bacteria (Staphylococcus aureus MRSA and MSSA), Gram-negative bacteria (i.e., Escherichia coli and Klebsiella pneumoniae), Mycobacterium tuberculosis and the fungus Aspergillus fumigatus. The results indicated moderate biological activities against all the cancer cells lines and microorganisms tested. Bioassay-guided fractionation assisted by HRMS analysis allowed the detection of one new and two known amphidinols that are potentially responsible for the antifungal and cytotoxic activities observed. Further isolation, purification and structural elucidation led to a new amphidinol, named amphidinol 22. The planar structure of the new compound was determined by analysis of its HRMS and 1D and 2D NMR spectra. Its biological activity was evaluated, and it displayed both anticancer and antifungal activities.
Highlights
Many microalgae, including dinoflagellates, are known to produce compounds with a wide range of biological and biochemical properties [1]
After extraction of the A. carterae biomass, the crude extract was tested against a panel of different cancer cell lines, bacteria and fungi
Bioassay-guided fractionation allowed the isolation and identification of a new compound belonging to the amphidinol family, which we designated as amphidinol 22, from the dinoflagellate
Summary
Many microalgae, including dinoflagellates, are known to produce compounds with a wide range of biological and biochemical properties [1]. The biodiversity of marine phytoplankton species leads to a great metabolic variety that renders them a huge reservoir of new bioactive compounds with multiple possible pharmaceutical applications [2] (e.g. cytotoxic, anticancer, antibiotic, antifungal, immunosuppressant and neurotoxic activities [3,4,5,6,7,8,9,10]). Bioactive compounds of microalgal origin can be sourced directly from primary metabolism (e.g. proteins, fatty acids, vitamins and pigments) or. Mar. Drugs 2019, 17, 385 can be synthesized from secondary metabolism. Microalgae are excellent sources/producers of carotenoids, polysaccharides, vitamins, lipids as well as potent neurotoxins [11]. An increasing number of studies have focused their attention on microalgal compounds for the treatment of various human pathologies or for nutraceutical applications [12,13]
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