Abstract
The marine ecosystem is an extraordinary reserve of pharmaceutically important, bioactive compounds even in this “synthetic age”. Marine algae-associated endophytic fungi have gained prominence as an important source of bioactive compounds. This study was conducted on secondary metabolites of Chaetomium globosum-associated with marine green alga Chaetomorpha media from the Konkan coastline, India. Its ethyl acetate extract (CGEE) exhibited an IC50 value of 7.9 ± 0.1 µg/mL on MCF-7 cells. CGEE exhibited G2M phase cell cycle arrest, ROS production and MMP loss in MCF-7 cells. The myco-components in CGEE contributing to the cytotoxicity were found by Gas Chromatography/Mass Spectrometry analyses. Chrysin, a dihydroxyflavone was one of the forty-six myco-components which is commonly found in honey, propolis and passionflower extracts. The compound was isolated and characterized as fungal chrysin using HPLC, UV–Vis spectroscopy, LC–MS, IR and NMR analyses by comparing with standard chrysin. The purified compound exhibited an IC50 value of 49.0 ± 0.6 µM while that of standard chrysin was 48.5 ± 1.6 µM in MCF-7 cells. It induced apoptosis, G1 phase cell cycle arrest, MMP loss, and ROS production. This is the first report of chrysin from an alternative source with opportunities for yield enhancement.
Highlights
The marine ecosystem is an extraordinary reserve of pharmaceutically important, bioactive compounds even in this “synthetic age”
The fungus was associated with the green alga C. media and had a lemony yellow color when grown on a PDA plate (Fig. 1B)
HeLa, A-431 and MCF-7 cells were vulnerable to the extract and their IC50 values were 8.1 ± 0.1, 4.7 ± 0.1 and 7.9 ± 0.1 μg/mL respectively, indicating significant cytotoxicity
Summary
The marine ecosystem is an extraordinary reserve of pharmaceutically important, bioactive compounds even in this “synthetic age”. The purified compound exhibited an IC50 value of 49.0 ± 0.6 μM while that of standard chrysin was 48.5 ± 1.6 μM in MCF-7 cells It induced apoptosis, G1 phase cell cycle arrest, MMP loss, and ROS production. Flavonoids are a ubiquitous class of secondary metabolites, commonly found in flowers, fruits, and to a lesser extent in fungi[4] It is well established through epidemiological, clinical, and animal studies that flavonoids and its derivatives display shielding effects against cancer by interacting with the nucleotide-binding sites of kinases, phospholipases, ATPase, lipooxygenases, cyclooxygenases, and phosphodiesterases[5]. Its anti-angiogenic activity was reported to be associated with a reduction in levels of MMP-2 and MMP-911,12 It induced a significant loss in mitochondrial membrane potential and an increase in reactive oxygen species. Maruhashi et al.[14] reported that chrysin enhances the anticancer potential of drugs in lung squamous cell carcinoma, suggesting its use as an adjuvant in chemotherapy
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