Abstract
Five new sesterterpenes, 14,15-dehydro-6-epi-ophiobolin K (1), 14,15-dehydro- ophiobolin K (2), 14,15-dehydro-6-epi-ophiobolin G (3), 14,15-dehydro-ophiobolin G (4) and 14,15-dehydro-(Z)-14-ophiobolin G (5), together with four known ophiobolins (6–9) were isolated from the marine fungus Aspergillus flocculosus derived from the seaweed Padina sp. collected in Vietnam. The five new ophiobolins were first isolated as ophiobolin derivatives consisting of a fully unsaturated side chain. Their structures were elucidated via spectroscopic methods including 1D, 2D NMR and HR-ESIMS. The absolute configurations were determined by the comparison of chemical shifts and optical rotation values with those of known ophiobolins. All compounds (1–9) were then evaluated for their cytotoxicity against six cancer cell lines, HCT-15, NUGC-3, NCI-H23, ACHN, PC-3 and MDA-MB-231. All the compounds showed potent cytotoxicity with GI50 values ranging from 0.14 to 2.01 μM.
Highlights
The marine environment is an enormous reservoir of novel sources of biologically active metabolites, many of which display unique structural skeletons that can be used as lead structures for the development of new drugs [1,2]
The results showed that all compounds were (SRB) assay, with adriamycin as a positive control
The results showed that all compounds were strongly active against 6 cancer cell lines with GI values in the range of 0.14 to 2.01 μM (Table 3)
Summary
The marine environment is an enormous reservoir of novel sources of biologically active metabolites, many of which display unique structural skeletons that can be used as lead structures for the development of new drugs [1,2]. To adapt and live in an environment that is significantly different from terrestrial organisms, marine organisms frequently produce structurally unique chemical compounds [3,4]. Secondary metabolites from marine microorganisms are recognized as a novel chemical source for drug discovery and development. Among marine-derived microbes, marine fungi produce a wide range of promising biologically active compounds [5]. Numerous novel compounds from marine fungi have displayed a wide range of bioactivities such as antiviral, antibacterial, anticancer, antiplasmodial and anti-inflammatory [6,7,8].
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