The known chalcone (±)-sanjuanolide (1) can be isolated from Dalea frutescens. This study presents a convergent strategy for the first total synthesis of ( R)-, ( S)-, and (±)-sanjuanolide (1). The key step for synthesizing ( R)- and ( S)-1 was a Corey-Bakshi-Shibata enantioselective carbonyl reduction to construct the C-2″ configuration. ( R)-1 efficiently inhibited the lipopolysaccharides (LPS)-induced expression of tumor necrosis factor alpha (TNF-α) and interleukin-6 (IL-6), while ( S)-1 produced no significant anti-inflammatory effect. ( R)-1 also effectively inhibited the mRNA expression of several inflammatory cytokines after the LPS challenge in vitro. The synthesis and biological properties of these compounds have confirmed ( R)-sanjuanolide and (±)-sanjuanolide as promising new leads for developing anti-inflammatory agents.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1021/acs.jnatprod.8b00596 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
"I'm not sad anymore, I'm proud to have such a child": The experiences of caregivers of dependents with cerebral palsy living in Greece.
J Pediatr Nurs
January 2025
Department of Nursing, School of Health Rehabilitation Sciences, University of Patras, Nikolaou Gizi 4, Patras, Greece.
Background: People with cerebral palsy are largely dependent on their caregivers, who are most often members of their family. Caring for people with disabilities can be challenging as both dependents and caregivers face problems of social isolation and stigmatization.
Aim: The aim of this study was to understand the experiences of caregivers of dependents with cerebral palsy in Greece.
Differential effects of warming on carbon budget, photosynthetic yield and biochemical composition of cold-temperate and Arctic isolates of Laminaria digitata (Phaeophyceae).
J Plant Physiol
January 2025
Department of Ecology, Faculty of Sciences, University of Málaga, Málaga, Spain.
Cold-temperate and Arctic hard bottom coastal ecosystems are dominated by kelp forests, which have a high biomass production and provide important ecosystem services, but are subject to change due to ocean warming. However, the photophysiological response to increasing temperature of ecologically relevant species, such as Laminaria digitata, might depend on the local thermal environment where the population has developed. Therefore, the effects of temperature on growth rate, biochemical composition, maximum quantum yield, photosynthetic quotient and carbon budget of young cultured sporophytes of Laminaria digitata from the Arctic at Spitsbergen (SPT; cultured at 4, 10 and 16 °C) and from the cold-temperate North Sea island of Helgoland (HLG; cultured at 10, 16 and 22 °C) were comparatively analyzed.
View Article and Find Full Text PDFNear-Native Imaging of Metal Ion-Initiated Cell State Transition.
ACS Nano
January 2025
National Synchrotron Radiation Laboratory, University of Science and Technology of China, Hefei 230026, China.
Metal ions are indispensable to life, as they can serve as essential enzyme cofactors to drive fundamental biochemical reactions, yet paradoxically, excess is highly toxic. Higher-order cells have evolved functionally distinct organelles that separate and coordinate sophisticated biochemical processes to maintain cellular homeostasis upon metal ion stimuli. Here, we uncover the remodeling of subcellular architecture and organellar interactome in yeast initiated by several metal ion stimulations, relying on near-native three-dimensional imaging, cryo-soft X-ray tomography.
View Article and Find Full Text PDFEndothelial-specific knockout of the scramblase TMEM16F impairs in vivo clot formation.
Shock
January 2025
Pharmacology, University of Vermont, Burlington, VT.
Objective: Loss of function of the phospholipid scramblase (PLS) TMEM16F results in Scott Syndrome, a hereditary bleeding disorder generally attributed to intrinsic platelet dysfunction. The role of TMEM16F in endothelial cells, however, is not well understood. We sought to test the hypothesis that endothelial TMEM16F contributes to hemostasis by measuring bleeding time and venous clotting in endothelial-specific knockout (ECKO) mice.
View Article and Find Full Text PDFAculeapyridones A-Q, Pyranopyridone Alkaloids with Protective Effects against Acetaminophen-Induced Acute Liver Injury Discovered from a Coculture of WHUF0198 and a sp.
J Nat Prod
January 2025
Department of Nephrology, Zhongnan Hospital of Wuhan University, School of Pharmaceutical Sciences, Wuhan University, Wuhan 430071, People's Republic of China.
In the search for novel natural products with hepatoprotective effects against acetaminophen-induced acute liver injury, the marine-derived fungus WHUF0198 was investigated. Seventeen undescribed pyranopyridone alkaloids, aculeapyridones A-Q (-), were isolated by bioactivity-guided fractionation of an extract obtained by coculture of the WHUF0198 with the mangrove-associated fungus sp. DM27.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!