Chemical constituents from a marine medicinal brown alga-derived Xylaria acuta SC1019.

In this study, a marine medicinal brown alga Sargassum cristaefolium-derived fungal strain Xylaria acuta SC1019 was isolated and identified. Column chromatography of the extracts from liquid- and solid-fermented products of the fungal strain was carried out, and led to the isolation of twenty-one compounds. Their structures were characterized by spectroscopic analysis, and the absolute configurations were further established by single X-ray diffraction analysis or modified Mosher's method as nine previously undescribed compounds, namely xylarilactones A-C (1-3), ent-gedebic acid 8-O-α-D-glucopyranoside (4), 5R-hydroxylmethylmellein 11-O-α-D-glucopyranoside (5), ent-hymatoxin E 16-O-α-D-mannopyranoside (6), 19,20-epoxycytochalasin S (7), 19,20-epoxycytochalasin T (8), and (2R)-butylitaconic acid (9), along with twelve known compounds 10-21. All the isolates were subjected to anti-inflammatory and anti-angiogenic assays. Compounds 1, 5, 7, 10, and 17 showed moderate nitric oxide production inhibitory activities in lipopolysaccharide-activated BV-2 microglial cells with IC50 values of 19.55 ± 0.35, 16.10 ± 0.57, 15.20 ± 0.87, 11.76 ± 0.49, and 11.30 ± 0.32 µM, respectively, as compared to curcumin (IC50 = 2.69 ± 0.34 µM) without any significant cytotoxicity. Compounds 7, 8, and 21 displayed potent anti-angiogenic activities by suppressing the growth of human endothelial progenitor cells with IC50 values of 0.44 ± 0.01, 0.47 ± 0.03, and 0.53 ± 0.01 µM, respectively, as compared to sorafenib (IC50 = 5.50 ± 1.50 µM).

Chemical Constituents and Anti-Angiogenic Principles from a Marine Algicolous Penicillium sumatraense SC29.

In this study, a marine brown alga Sargassum cristaefolium-derived fungal strain, Penicillium sumatraense SC29, was isolated and identified. Column chromatography of the extracts from liquid fermented products of the fungal strain was carried out and led to the isolation of six compounds. Their structures were elucidated by spectroscopic analysis and supported by single-crystal X-ray diffraction as four previously undescribed (R)-3-hydroxybutyric acid and glycolic acid derivatives, namely penisterines A (1) and C-E (3-5) and penisterine A methyl ether (2), isolated for the first time from natural resources, along with (R)-3-hydroxybutyric acid (6). Of these compounds identified, penisterine E (5) was a unique 6/6/6-tricyclic ether with an acetal and two hemiketal functionalities. All the isolates were subjected to in vitro anti-angiogenic assays using a human endothelial progenitor cell (EPCs) platform. Among these, penisterine D (4) inhibited EPC growth, migration, and tube formation without any cytotoxic effect. Further, in in vivo bioassays, the percentages of angiogenesis of compound 3 on Tg (fli1:EGFP) transgenic zebrafish were 54% and 37% as the treated concentration increased from 10.2 to 20.4 µg/mL, respectively, and the percentages of angiogenesis of compound 4 were 52% and 41% as the treated concentration increased from 8.6 to 17.2 µg/mL, respectively. The anti-angiogenic activity of penisterine D (4) makes it an attractive candidate for further preclinical investigation.

Cereal-Based Solid-State Fermentation and Anti-Inflammatory Potential of Paecilomyces cicadae SH1 (Ascomycota) Isolated in China.

Jin-Chan-Hua, a traditional Chinese medicine with numerous pharmaceutical properties, is a biological complex of fungus and cicada larvae. In this study, the fungus Paecilomyces cicadae strain SH1 was obtained and cultivated to produce fruiting bodies in solid-state fermentation by using various cereals as base nutrients. The results indicated that 15 media (e.g., wheat, buckwheat, oatmeal, adzuki bean, black soybean, soybean, mung bean, speckled kidney bean, rice, millet, black glutinous rice, unpolished rice, peanut, pearl barley, and Job's tears) were favorable for high biomass or fruiting body production; thus, we conducted an anti-inflammatory assay in RAW 264.7 cells by using the fermented extracts of these substrates. Among the cereal substrates fermented with P. cicadae SH1, the alcohol extract of fermented oatmeal had the best anti-inflammatory ability with a dose-dependent effect, and it did not reduce the viability of RAW 264.7 cells at a concentration of 200 µg/mL. The results demonstrated that oatmeal solid-state fermented by P. cicadae SH1 has potential applications in the prevention or treatment of inflammation. To our knowledge, this study is the first to report on the development of functional foods and nutraceuticals through the solid-state fermentation of oatmeal by P. cicadae.