Abstract
A new α-pyrone merosesquiterpenoid possessing an angular tetracyclic carbon skeleton, ochraceopone F (1), and four known secondary metabolites, aspertetranone D (2), cycloechinulin (3), wasabidienone E (4), and mactanamide (5), were isolated from the marine fungus Aspergillus flocculosus derived from a sponge Stylissa sp. collected in Vietnam. The structures of Compounds 1–5 were elucidated by analysis of 1D and 2D NMR spectra and MS data. All the isolated compounds were evaluated for anti-proliferation activity and their suppression effects on receptor activator of nuclear factor κB ligand (RANKL)-induced osteoclast differentiation using tartate-resisant acid phosphatase (TRAP). Compounds 1–5 had no anti-proliferative effect on human cancer cell lines up to 30 μg/mL. Among these compounds, aspertetranone D (2) and wasabidienone E (4) exhibited weak osteoclast differentiation inhibitory activity at 10 μg/mL. However, mactanamide (5) showed a potent suppression effect of osteoclast differentiation without any evidence of cytotoxicity.
Highlights
Bone remodeling is the regulation to maintain the quality and mass of bone by undergoing a resorption and formation cycle repetitively [1,2]
High-resolution ESIMS was recorded on a hybrid ion-trap time-of-flight mass spectrometer (SYNAPT G2, Wasters Corporation, Milford, CT, USA)
All compounds had no cytotoxic effect on human cancer cell lines (HCT 15, NUGC-3, NCI-H23, ACHN, PC-3, and MDA-MB-231) up to 30 μg/mL
Summary
Bone remodeling is the regulation to maintain the quality and mass of bone by undergoing a resorption and formation cycle repetitively [1,2]. The cells responsible for the skeleton resorption are the osteoclasts. Osteoclasts are multinucleated cells generated from their mononuclear precursor cells derived from the monocyte/macrophage lineage [3]. Osteoclasts are induced by two putative promoters, macrophage colony stimulating factor (M-CSF) and receptor activator of nuclear factor-κB ligand (RANKL). The excessive formation of osteoclasts causes abnormal bone remodeling, Mar. Drugs 2018, 16, 14; doi:10.3390/md16010014 www.mdpi.com/journal/marinedrugs
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