Two new α-pyrones, dothideopyrones E (1) and F (2), were isolated from a culture of the endolichenic fungus Dothideomycetes sp. EL003334. Their structures were elucidated by spectroscopic data analysis. Their absolute configurations were established by the modified Mosher's method. Compound 2 inhibited nitric oxide (NO) production with IC values of 15.0 ± 2.8 μM in lipopolysaccharide (LPS)-induced BV2 cells. Compound 2 diminished the protein expression levels of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2). Additionally, 2 decreased the mRNA expression levels of pro-inflammatory cytokines, such as tumor necrosis factor-α (TNF-α), interleukin (IL)-1β, and IL-6.
Ein zellbasiertes Screening mit Annexin V als Färbemittel identifizierte Apoptozol (Az; siehe Schema) als ein Imidazolderivat, das Apoptose auslöst. Az bindet an Hsc70 und Hsp70 (antiapoptotische Chaperonproteine) mit Dissoziationskonstanten von 0.21 bzw. 0.14 μM und inhibiert so deren Funktion. Somit zeigt Az Antitumoraktivität und ist daher ein potenzielles Krebstherapeutikum.
Four new compounds, phomalichenones A-D (1-4), and seven known compounds (5-11) were isolated from the cultures of an endolichenic fungus Phoma sp. EL002650. Their structures were determined by the analysis of their spectroscopic data (NMR and MS). Compounds 1 and 6 inhibited nitric oxide (NO) production in lipopolysaccharide (LPS)-stimulated RAW264.7 macrophages. In addition, compound 1 diminished the protein expression levels of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2), and decreased the mRNA expression levels of pro-inflammatory cytokines, such as tumor necrosis factor-α (TNF-α), interleukin(IL)-1β, and IL-6.
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