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Objective: To obtain structurally novel and bioactive secondary metabolites from the marine fungus Xylariaceae sp. SCSIO41212. Methods: Compounds were purified by comprehensive chromatography methods of silica gel column, Sephadex LH-20, Ostade-cylsilane (ODS) and semi-preparative HPLC, and their structures were elucidated by means of physical and chemical properties, magnefic resonance imaging, spectroscopic analysis, and comparison with the reported literatures. Results: Chemical investigation of the fungus Xylariaceae sp. SCSIO41212 has led to the isolation of two new compounds, xylaolide B (1) and xylaolide C (2), together with nine known compounds (3–11). Their structures were determined on the basis of detailed analysis of the 1D and 2D NMR as well as MS data. Compounds 1–6 were evaluated for their antiviral, and cytotoxic activities, respectively. Compound 1 showed weak cytotoxicities against K562, MCF-7 and SGC7901 respectively. Conclusion: This study enriches the diversity of secondary metabolites of marine-derived fungi and provides an important reference for novel promising drug leads research.

Psoriasis is reported to be a common chronic immune-mediated skin disease characterized by abnormal keratinocytes and cell proliferation. Perilla leaves are rich in essential oils, fatty acids, and flavonoids, which are recognized for their antioxidant and anti-inflammatory effects. In this study, the alleviating effect of essential oil (PO) extracted from Perilla frutescens stems and leaves on imiquimod (IMQ) -induced psoriasis-like lesions in BALB/c mice were investigated. Results showed that PO ameliorated psoriasis-like lesions in vivo, reduced the expression of lymphocyte antigen 6 complex locus G6D (Ly-6G), which is a marker of neutrophil activation, and inhibited the expression of inflammatory factors interleukin 1 (IL-1), interleukin 6 (IL-6), inducible nitric oxide synthase (iNOS), and cyclooxygenase 2 (COX2). In addition, PO significantly decreased the expression of cytokines such as IL-6, IL-1, interleukin 23 (IL-23), interleukin 17 (IL-17), and nuclear factor kappa-B (NF-κB). Furthermore, the down-regulation of mRNA levels of psoriasis-related pro-inflammatory cytokines, such as IL-17, interleukin 22 (IL-22), IL-23, interferon-α (IFN-α), and Interferon-γ (IFN-γ) was observed with the treatment of PO. All results show a concentration dependence of PO, with low concentrations showing the best results. These results suggest that PO effectively alleviated psoriasis-like skin lesions and down-regulated inflammatory responses, which indicates that PO could potentially be used for further studies on inflammation-related skin diseases such as psoriasis and for the treatment of psoriasis such as psoriasis natural plant essential oil resources.

A growing body of evidence indicates that glycosylated natural products have become vital platforms for the development of many existing first-line drugs. This review covers 205 new glycosides over the last 22 years (1997–2018), from marine microbes, including bacteria, cyanobacteria, and fungi. Herein, we discuss the structures and biological activities of these compounds, as well as the details of their source organisms.

Eight new compounds, sinulolides A–H (1–8), along with two known compounds, α-methoxy-2,3-dimethyl-butenolide (9) and sinularone D (10), were isolated from the soft coral Sinularia sp. The structures of these compounds were elucidated on the basis of extensive spectroscopic analysis. The absolute configurations were determined on the basis of electronic circular dichroism (ECD) data analysis. Compounds 5 and 10 exhibited moderate effects for the inhibition of NF-κB activation.

A new macrodiolide, mangrovlide A (1) and two new polycyclic chromones, penixanthones C (2) and D (3), as well as four other known compounds (4−7), have been isolated from the mangrove sediment derived fungus Penicillium sp. SCSIO041218, cultured in the 0.25% NaCl rice substrate. The structures of the new compounds were determined by analysis of the NMR and MS spectroscopic data. Compound 1 possesses a 10-membered macrodiolide unit, while 2 and 3 are chromones with an unprecedented 6/6/6/5 polycyclic skeleton. Compounds 1−7 were evaluated for their cytotoxicities, while all the compounds displayed weak or no activity.

Propofol has been shown to against intestinal reperfusion injury when treated either before or after ischemia, during which mast cell could be activated. The aim of this study was to evaluate the role of propofol in restoring the intestinal epithelial cells integrity disrupted by mast cell activation or the released tryptase after activation in vitro. We investigated the effect of: (1) tryptase on Caco-2 monolayers in the presence of PAR-2 inhibitor or propofol, (2) mast cell degranulation in a Caco-2/LAD-2 co-culture model in the presence of propofol, and (3) propofol on mast cell degranulation. Epithelial integrity was detected using transepithelial resistance (TER) and permeability to fluorescein isothiocyanate (FITC)-dextran (the apparent permeability coefficient, Papp). The expression of junctional proteins zonula occludens-1 (ZO-1/TJP1) and occludin were determined using western blot analysis and immunofluorescence microscopy. The intracellular levels of reactive oxidative species (ROS) and Ca2+ were measured using flow cytometry. Tryptase directly enhanced intestinal barrier permeability as demonstrated by significant reductions in TER, ZO-1, and occludin protein expression and concomitant increases in Papp. The intestinal barrier integrity was restored by PAR-2 inhibitor but not by propofol. Meanwhile, mast cell degranulation resulted in epithelial integrity disruption in the Caco-2/LAD-2 co-culture model, which was dramatically attenuated by propofol. Mast cell degranulation caused significant increases in intracellular ROS and Ca2+ levels, which were blocked by propofol and NAC. Propofol pretreatment can inhibit mast cell activation via ROS/Ca2+ and restore the intestinal barrier integrity induced by mast cell activation, instead of by tryptase. [ABSTRACT FROM AUTHOR]

Two new α-methoxy-γ-pyrone analogs, 2-methoxy-3-methyl-5,6-diethyl-γ-pyrone (2) and 2-methoxy-3,5-dimethyl-6-propyl-γpyrone (3), together with 2-methoxy-3,5-dimethyl-6-ethyl-γ-pyrone (1), firstly isolated from natural sources, were obtained from the EtOAc-solube extract of the mangrove sediment-derived actinomycete strain Streptomyces psammoticus SCSIO NS126, under the optimized fermentation conditions. Their structures were elucidated by detailed spectroscopic analysis and by comparison of their spectroscopic data with those reported in the literature. Those α-methoxy-γ-pyrones were evaluated for their acetylcholinesterase inhibitory activity; however, none of them exhibited obvious activity. Moreover, their biosynthetic relationship with piericidins was also discussed. [ABSTRACT FROM AUTHOR]

Chemical investigation of the sponge Callyspongia sp. from the South China Sea afforded one new diketopiperazine, cyclo-(R-Pro-6-hydroxyl-S-Ile) (1), along with six known diketopiperazines: staphyloamide A (2), cyclo- (S-Pro-S-Phe) (3), cyclo-(R-Pro-R-Phe) (4), cyclo-(S-Pro-R-Leu) (5), cyclo-(S-Pro-R-Ala) (6), cyclo- (R-Tyr-R-Phe) (7), and three known tryptophan-derived alkaloids: C²-α-D-mannosylpyranosyl-tryptophan (8), (1R, 3S)-1-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole-3-carboxylic acid (9), and (1R,3R)-1-methyl- 2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole-3-carboxylic acid (10). The structures were determined on the basis of NMR and MS analysis, and the absolute configuration was determined by comparison of the optical rotation with the known compounds. This is the first report of compounds 1, 2, 8-10 from the sponge Callyspongia. Cyclo-(S-Pro-R-Leu) (5), and cyclo-(S-Pro-R-Ala) (6) exhibited antifouling activity against cyprid larvae of the barnacle with the LC50 values of 3.5 μg/cm² and 6.0 μg/cm², respectively. [ABSTRACT FROM AUTHOR]