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The protein-protein interaction network combined these 53 temperature-sensitive genes and another group of 65 genes, which enriched the development pathway. These results suggested that temperature-sensitive genes may be involved in growth and development related pathways.A new austin-type meroterpene, namely, ustusaustin A (1), together with seven related known analogues (2-8), were isolated and identified from the culture extract of Aspergillus ustus TK-5, an endophytic fungus obtained from the marine ascidian Pyura momus. The structures of these compounds were established on the basis of detailed interpretation of their NMR and MS data, and the relative and absolute configurations of 1 was confirmed by X-ray crystallographic analysis. Among them, ustusaustin A (1) represents the first example of 1'-nor-austin analogues with an unique 7-benzoylation. Compounds 1-4, 6, and 7 exhibited potent neuraminidase inhibitory activity and this is the first report of neuraminidase inhibitory activity for austin-type meroterpenes.This study aimed to compare the total phenolic (TPC), flavonoid (TFC), radical scavenging and cytotoxic activities in the aqueous methanolic extracts of Angelica sinensis, Dioscorea polystachya, Ginkgo biloba, Glycyrrhiza uralensis and Lycium barbarum with two dietary plants Brassica oleracea and Zingiber officinale. The TPC and TFC in medicinal plant extracts were 12-93% lower than Z. officinale as follows L. barbarum > G. uralensis > A. sinensis > G. biloba > D. polystachya. The decreasing radical scavenging activity in medicinal plant extracts shared similar trend G. https://www.selleckchem.com/products/otx015.html uralensis > L. barbarum > A. sinensis > G. biloba > D. polystachya. Both TPC and TFC were positively correlated with radical scavenging and cytotoxic activities. All medicinal plants were considered inactive (LC50 > 0.2 mg/ml) and safe for consumption. The TPC, TFC, radical scavenging and cytotoxic activities in the medicinal plants were plant-part dependant, in particular L. barbarum and G. uralensis.Freshwater sponges can be considered a promising new source of bioactive compounds for the pharmaceutical industry; however, the research on their chemical composition is still in the incipient stage. We evaluated the most endemic Amazonian freshwater sponge species from the Drulia and Metania genera by untargeted metabolomic approaches, based on UHPCL-HRMS, in order to identify chemical markers and explore the diversity of specialized metabolites. The use of untargeted approaches allowed us to observe subsets of metabolites that enabled the characterization of, not only each genus, but also, of each species. Freshwater sponge species presented themselves as rich sources of fatty acids and sterols, which were putatively identified. These metabolites were suggested as chemical markers for further targeted metabolomic studies.Two new compounds, a new lactone, quercilactone A (1), and (17R)-hydroxynafuredin (5), as well as five known compounds, scytalone (2), 3S,4R-hydoxy-scytalone (3), nafuredin (4), (+)-(3R,5R)-3-hydroxy-5-decanolide (6) and 3-ethyl-4-hydroxy-6-methyl-2H-pyran-2-one (7), were isolated from Raffaelea quercivora, a fungus that causes Japanese oak wilt disease. The structures of these compounds were determined by 1D and 2D NMR spectroscopic analyses. The absolute configuration at C-17 of 5 was determined to be R by the modified Mosher's method. Compounds 1, 2, and 7 exhibited weak phytotoxic activity in lettuce seedlings at a concentration of 100 μg mL-1.The hydroethanolic extract obtained from the dry leaves of Fridericia chica (HEFc) underwent several fractionations by different chromatographic techniques. The ethyl acetate and dichloromethane fraction were subjected to phytochemical analysis, resulting in the identification and isolation of scutellarein (1) and in a fraction rich in carajurone (2). They were tested for cytotoxicity in CHO-K1 and the antibacterial activity and mode of action by in vitro assays. The HEFc and scutellarein (1) presented no cytotoxicity. The results showed good antibacterial effect of HEFc against Streptococcus pyogenes and Staphylococcus aureus and moderate activity for Staphylococcus epidermidis, Pseudomonas aeruginosa and Salmonella typhimurium. The fraction containing the compound carajurone (2) showed good activity against Staphylococcus aureus and Staphylococcus epidermidis and moderate activity against Streptococcus pyogenes. Scutellarein (1) showed no activity against the bacteria tested. HEFc antibacterial mode of action appeared to be associated with changes in the permeability of bacterial membranes and nucleotide leakage.In this work, twenty-eight novel 17a-aza-D-homo-androster-17-one derivatives, which divided into two categories, were synthesized with commercial available starting material (dehydroepiandrosterone) via oximation reaction, Beckmann rearrangement, hydroxyl protection, N-alkylation and deprotection. All compounds were characterized by 1H NMR, 13C NMR and HRMS. The structure of 14 g was also identified by X-ray single crystal diffraction. The bioactivities, brine shrimp toxicity and cytotoxicity, of all derivatives were tested. The results indicated that compounds 11 h, 11i, 11 m, 11 s, 14 b and 14 g exhibited excellent toxicity against brine shrimp with LC50 values ranging from 5.34 to 16.89 μg/mL, and compounds 11 s and 14 g displayed significant cytotoxicity against HT29 cells and A549 cells with IC50 values of 9.70 μM and 8.85 μM, respectively. Structure-activity relationships are discussed based on the results obtained from our research, and some important determinants for further modification of steroids towards the development of novel drug candidates are identified.A new α,β-unsaturated 7-ketone sterol, 5β,6β-epoxy-3β, 15α-dihydroxy-(22E,24R)-ergosta-8(14),22-dien-7-one (1), along with five known sterone derivatives, 5β,6β-epoxy-3β,7α-dihydroxy-(22E,24R)-ergosta-8(14),22-dien-15-one (2), 5β,6β-epoxy-3β,7α,9α-trihydroxy-(22E,24R)-ergosta-8(14),22-dien-15-one (3), 3β,9α,15α-trihydroxy-(22E,24R)-10(5→4)-abeo-ergosta-6,8(14),22-trien-5-one (4), 3,15-dihydroxyl-(22E,24R)-ergosta-5,8(14),22-trien-7-one (5) and (22E,24R)-ergosta-4,6,8(14),22-tetraen-3,15-dione (6) were isolated from the mangrove-derived fungus Phomopsis sp. MGF222. Their structures were established on the basis of extensive spectroscopic data and comparison with the data of literature. Compound 2 showed weak antibacterial activity against Micrococcus tenuis with the MIC value of 28.2 (±0.52) μM. Compound 5 exhibited moderate antibacterial activity against Staphylococcus aureus with the MIC value of 14.6 (±0.47) μM.
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