Bioactive A-ring rearranged limonoids from the root barks of Walsura robusta

Abstract

Screening active natural products, rapid identification, and accurate isolation are of great important for modern natural lead compounds discovery 1 . We hereby reported the isolation of seven new neotecleanin-type limonoids ( 1 — 7 ), seven new limonoids with 5-oxatricyclo[5.4.0.1 1. , 4. ]hendecane ring system ( 8 — 14 ), and two new precursors ( 15 — 16 ) together with four known limonoids ( 17 — 20 ) from the root barks of Walsura robusta . Their structures, including their absolute configurations, were elucidated based on analyses of HR-ESI-MS, 1D/2D NMR, ECD spectrum calculations and single-crystal X-ray diffraction techniques. Compounds 2 , 8 , 9 , 11 , 13 , 14 , 18 showed significant anti-inflammatory activities in LPS-induced RAW 264.7 cell line, BV2 microglial cells, and Propionibacterium acnes -stimulated THP-1 human monocytic cells. Walrobsin M ( 11 ) exhibited anti-inflammatory activity with IC 50 value of 7.96±0.36 μmol/L, and down-regulated phosphorylation levels of ERK and p38 in a dose-dependent manner.

Role of mitochondrial quality control in the pathogenesis of nonalcoholic fatty liver disease

“…Antioxidant systems are the primary line of defense to maintain a functional mitochondrial redox environment and prevent oxidative damage [12,13]. Mitochondria are highly dynamic organelles that constantly undergo fusion and fission, which are critical for mitochondrial homeostasis, mtDNA inheritance and intracellular distribution of the mitochondria [14][15][16][17]. Tight regulation of mitochondrial fission and fusion is required to constantly adapt to altering physiological needs [18][19][20].…”

Bioactive Indole Diketopiperazine Alkaloids from the Marine Endophytic Fungus Aspergillus sp. YJ191021

“…Besides, antimicrobial assays were performed to exclude false anti-inflammatory activity of these compounds raised from their inhibition to P. acnes . The inhibitory activity of the test compounds on the secretion of inflammatory factor 1L-1β by THP-1 cells was assayed by ELISA experiment [ 24 , 25 ]. The experimental procedure is detailed in the SI .…”

Curdepsidones B–G, Six Depsidones with Anti-Inflammatory Activities from the Marine-Derived Fungus Curvularia sp. IFB-Z10

“…The THP-1 cells were cultured in 96-well plates (2 × 10 5 cells/well) in RPMI1640 medium without FBS, treated with different concentrations of compounds and incubation for 4 h. Subsequently, the live P. acnes bacteria were added to stimulate the cells for 24 h, and the cell culture supernatants were collected to analyze the levels of IL-1β with ELISA assays (Genetimes Technology Inc., Shanghai, China). Retinoic acid was used as the positive control [32,36].…”