The mangrove forests are a complex ecosystem occurring at tropical and subtropical intertidal estuarine zones and nourish a variety of fungi that produce 1387 secondary metabolites with the feature of source, chemical and bioactive diversity.
Since the 1960s, more than 20,000 compounds were discovered from marine organisms. In this paper we performed a quantitative analysis for the novel marine natural products reported between 1985 and 2008. The data was extracted mainly from the reviews of Faulkner and Blunt [1–26]. The organisms producing these marine natural products are divided into three major biological classes: marine microorganisms (including phytoplankton), marine algae and marine invertebrate. The marine natural products are divided into seven classes based on their chemical structure: terpenoids, steroids (including steroidal saponins), alkaloids, ethers (including ketals), phenols (including quinones), strigolactones, and peptides. The distribution and the temporal trend of these classes (biological classes and chemical structure classes) were investigated. We hope this article provides a comprehensive perspective on the research of marine natural products.
Four new bisabolane-type sesquiterpenoids, aspergiterpenoid A (1), (−)-sydonol (2), (−)-sydonic acid (3), and (−)-5-(hydroxymethyl)-2-(2′,6′,6′-trimethyltetrahydro-2H- pyran-2-yl)phenol (4) together with one known fungal metabolite (5) were isolated from the fermentation broth of a marine-derived fungus Aspergillus sp., which was isolated from the sponge Xestospongia testudinaria collected from the South China Sea. Four of them (1–4) are optically active compounds. Their structures and absolute configurations were elucidated by using NMR spectroscopic techniques and mass spectrometric analysis, and by comparing their optical rotations with those related known analogues. Compounds 1–5 showed selective antibacterial activity against eight bacterial strainswith the MIC (minimum inhibiting concentrations) values between 1.25 and 20.0 µM. The cytotoxic, antifouling, and acetylcholinesterase inhibitory activities of these compounds were also examined.
9 February 2010 in British Journal of Pharmacology
Background and purpose: The aims of this study were to investigate the anti‐cancer activity of SZ‐685C, an anthracycline analogue isolated from marine‐derived mangrove endophytic fungi, and to explore the molecular mechanisms underlying such activity.Experimental approach: The effect of SZ‐685C on the viability of cancer cell lines was investigated using the 3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyl tetrazolium bromide (MTT) assay. SZ‐685C‐induced apoptosis was assessed by Annexin V‐fluorescein isothiocyanate/propidium iodide staining, terminal deoxynucleotidyl transferase‐mediated dUTP nick end labelling assay and analysis of caspase activation. The effect of SZ‐685C on the Akt/FOXO pathway was studied using Western blotting analysis, and the in vivo anti‐tumour efficacy was examined in an MDA‐MB‐435 breast cancer xenograft model.Key results: SZ‐685C suppressed the proliferation of six cancer cell lines derived from human breast cancer, prostate cancer, glioma and hepatoma (IC50 values ranged from 3.0 to 9.6 µM) and the growth of breast cancer xenografts in mice. SZ‐685C had a direct apoptosis‐inducing effect through both the extrinsic and intrinsic apoptotic pathways, as shown by activation of caspase‐8 and 9 as well as effector caspase‐3 and poly (ADP‐ribose) polymerase. Phosphorylation of Akt and its downstream effectors, forkhead box protein O1 and forkhead box protein O3a, was down‐regulated in SZ‐685C‐treated cancer cells. Furthermore, the pro‐apoptotic protein Bim was up‐regulated by SZ‐685C treatment consistent with FOXO dephosphorylation.Conclusions and implications: SZ‐685C could induce apoptosis through the Akt/FOXO pathway, which consequently leads to the observed anti‐tumour effect both in vitro and in vivo. Our data suggest that SZ‐685C may be a potentially promising Akt inhibitor and anti‐cancer drug candidate.
Six new isocoumarins, compounds 1–4 and 14–15, two new benzofurans, 16–17, along with nine known isocoumarin analogues, 5–13 were obtained from the mangrove endophytic fungus Talaromyces amestolkiae YX1. Their structures were elucidated by analysis of spectroscopic data. The absolute configuration of compounds 4, 14 and 15 were determined by the modified Mosher's method and comparison of their CD spectra with dihydroisocoumarins described in the literature. The structure of compound 5 was further confirmed by a single-crystal X-ray diffraction experiment using Cu Kα radiation. Compounds 2, 6, 8, and 10 showed α-glucosidase inhibitory activity with IC50 values of 89.4, 17.2, 36.4, and 38.1 μM, respectively. In the antibiotic assay, compounds 16 and 17 exhibited antibacterial activities with MIC values between 25–50 μg mL−1 against the Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli, and Bacillus subtilis.