Eleven compounds were obtained from L., including two novel ketone alkaloids, (, ), 4-hydroxy-3-methoxybenzamide () (isolated for the first time), β-adenosine (), oleracrylimide A and B (, ), oleracein H, C, D, Q and A (-). The two novel ketone alkaloids were identified as 5-acetyl-5-methylcyclopent-2-ene-1-carboxamide (), named oleraciamide H, and (2 R,3S,4R,5R)-5-((R)-1,2-dihydroxyethyl)-3,4-dihydroxytetrahydrofuran-2-yl glycinate (), named oleracone Q by spectroscopic methods, including 1D, 2D NMR and compound fingerprints. Additionally, their anti-inflammatory activities were tested RAW 264.7 cells induced by LPS and found that they could significantly inhibit the release of IL-1 and TNF-.
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http://dx.doi.org/10.1080/14786419.2024.2325593 | DOI Listing |
J Immunother Cancer
January 2025
Qingdao Key Laboratory of Materials for Tissue Repair and Rehabilitation, School of Rehabilitation Sciences and Engineering, University of Health and Rehabilitation Sciences, Qingdao, Shandong, People's Republic of China
Background: Tumor cells can drive the senescence of effector T cells by unbalancing their lipid metabolism, thereby limiting adoptive T cell therapy and contributing to tumor immune evasion. Our objective is to provide a feasible strategy for enhancing T cell treatment efficacy against solid tumors.
Methods: In this study, liposomal arachidonyl trifluoromethyl ketone (ATK) was anchored onto the adoptive T cell surface via bioorthogonal reactions, aiming to specifically inhibit the group IVA cytosolic phospholipase Aα (cPLAα), a key enzyme facilitating phospholipid metabolism and senescent state of T cells.
J Am Chem Soc
January 2025
Department of Chemistry, University of Texas at Austin, Austin 78712, Texas, United States.
A novel mechanism for -heteroaryl C-H functionalization via dearomative addition-hydrogen autotransfer is described. Upon exposure to the catalyst derived from RuHCl(CO)(PPh) and Xantphos, dienes - suffer hydroruthenation to form allylruthenium nucleophiles that engage in -heteroaryl addition-β-hydride elimination to furnish branched products of C-C coupling - and -. Oxidative cleavage of isoprene adducts , , , and followed by ruthenium-catalyzed dynamic kinetic asymmetric ketone reduction provides enantiomerically enriched -heteroarylethyl alcohols - and, therefrom, -heteroarylethyl amines -.
View Article and Find Full Text PDFChemistry
January 2025
Universite Catholique de Louvain, IMCN / MOST, 1 Place Louis Pasteur, Batîment Lavoisier, b.172, 1348, Louvain-La-Neuve, BELGIUM.
We introduce mechanochemical deracemization (MCDR) as a novel strategy for obtaining enantiopure compounds. This study demonstrates the successful transposition of six archetypical deracemization reactions from a solvent-based to a solvent-minimized ball milling environment. The scope includes a ketone, isoindolinones, imines, an ester, and an inorganic compound, all of which deracemized successfully.
View Article and Find Full Text PDFFundam Clin Pharmacol
February 2025
Experimental Oncology and Hemopathies Laboratory, Clinical Analysis Department, Federal University of Santa Catarina, Florianópolis, 88040-900, Brazil.
Background: Chalcones have been described in the literature as promising antineoplastic compounds.
Objectives: Therefore, the objective of this study was to analyze the cytotoxic effect of 23 synthetic chalcones on human acute leukemia (AL) cell lines (Jurkat and K562).
Methods: Cytotoxicity assessment was performed using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method.
Cell Mol Life Sci
December 2024
Department of Life Science, Chung-Ang University, Seoul, 06974, Republic of Korea.
Over the past few decades, microtubules have been targeted by various anticancer drugs, including paclitaxel and eribulin. Despite their promising effects, the development of drug resistance remains a challenge. We aimed to define a novel cell death mechanism that targets microtubules using eribulin and to assess its potential in overcoming eribulin resistance.
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