Immunomodulatory and anti-angiogenesis effects of excavatolide B and its derivatives in alleviating atopic dermatitis.

Atopic dermatitis (AD) is a chronic inflammatory skin condition primarily driven by T helper 2 (Th2) cytokines, resulting in skin barrier defects, angiogenesis, and inflammatory responses. The marine natural product excavatolide B (EXCB), isolated from the Formosan Gorgonian coral Briareum stechei, exhibits anti-inflammatory and analgesic properties. To enhance solubility, EXCB is chemically modified into the derivatives EXCB-61 salt and EXCB-79.

Marein Ameliorates Myocardial Fibrosis by Inhibiting HIF-1α and TGF-β1/Smad2/3 Signaling Pathway in Isoproterenol-stimulated Mice and TGF-β1-stimulated Cardiac Fibroblasts.

Background: Myocardial fibrosis significantly contributes to the pathogenesis and progression of heart failure.

Objective: We probe into the impact of marein, a key bioactive compound in functional food Coreopsis tinctoria, on isoproterenol-stimulated myocardial fibrotic mice and transforming growth factor β1 (TGF-β1)-stimulated cardiac fibroblasts (CFs).

Methods: Isoproterenol was administered to the experimental mice via subcutaneous injection, and simultaneous administration of marein (25-100 mg/kg) was performed via oral gavage.

FGF21 protects against doxorubicin-induced cardiotoxicity by inhibiting connexin 43 ubiquitination.

Background: Fibroblast growth factor 21 (FGF21) regulates glycolipid metabolism and insulin homeostasis and acts as a cardioprotective factor by protecting against myocardial ischemia/reperfusion injury, hypertension, and vascular dysfunction. FGF21 has been reported to prevent Doxorubicin (Dox)-induced cardiotoxicity, and the related signaling pathway is worthy of further study. Connexin43 (Cx43) protein was reduced by Dox treatment, especially low phosphorylated form of Cx43.

Marine diterpenoid targets STING palmitoylation in mammalian cells.

Natural products are important sources of therapeutic agents and useful drug discovery tools. The fused macrocycles and multiple stereocenters of briarane-type diterpenoids pose a major challenge to total synthesis and efforts to characterize their biological activities. Harnessing a scalable source of excavatolide B (excB) from cultured soft coral Briareum stechei, we generated analogs by late-stage diversification and performed structure-activity analysis, which was critical for the development of functional excB probes.

Inhibition of SARS-CoV-2 by Highly Potent Broad-Spectrum Anti-Coronaviral Tylophorine-Based Derivatives.

Tylophorine-based compounds and natural cardiotonic steroids (cardenolides and bufadienolides) are two classes of transmissible gastroenteritis coronavirus inhibitors, targeting viral RNA and host cell factors, respectively. We tested both types of compounds against two types of coronaviruses, to compare and contrast their antiviral properties, and with view to their further therapeutic development. Examples of both types of compounds potently inhibited the replication of both feline infectious peritonitis virus and human coronavirus OC43 with EC values of up to 8 and 16 nM, respectively.

Marein ameliorates Ang II/hypoxia-induced abnormal glucolipid metabolism by modulating the HIF-1α/PPARα/γ pathway in H9c2 cells.

The objectives of this study were to investigate the effects of marein, a major bioactive compound in functional food Coreopsis tinctoria, in hypertrophic H9c2 cells. Treating angiotensin II/hypoxia-stimulated H9c2 cells with marein led to decreasing cell surface area, intracellular total protein, atrial natriuretic peptide, and free fatty acids levels, but increasing glucose level. Marein treatment decreased hypoxia inducible factor-1α (HIF-1α), peroxisome proliferator activated receptor γ (PPARγ), medium chain acyl-coenzyme A dehydrogenase, glucose transporter-4, and glycerol-3-phosphate acyltransferase protein expressions, and increased PPARα, fatty acid transport protein-1, carnitine palmitoyltransferase-1, and pyruvate dehydrogenase kinase-4 protein expressions.

Visible Light Absorption and Long-Lived Excited States in Dinuclear Silver(I) Complexes with Redox-Active Ligands.

Well-defined dinuclear silver(I) complexes have been targeted for applications in catalysis and materials chemistry, and the effect of close silver-silver interactions on electronic structure remains an area of active inquiry. In this study, we describe the synthesis, structure, and photophysical properties of dimeric silver complexes featuring a redox-active naphthyridine diimine ligand. Unusually for silver(I), these complexes display absorption features in the visible region due to metal-metal to ligand charge transfer (MMLCT) transitions, which arise from the combination of close silver-silver interactions and low-lying ligand π* orbitals.

Formal Synthesis of (±)-Pentalenolactone A Methyl Ester.

We report the formal synthesis of (±)-pentalenolactone A methyl ester from simple 2-methoxyphenol. The key features of our route are as follows: a Diels-Alder reaction of masked -benzoquinone to assemble the functionalized bicyclo[2.2.