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Design, Synthesis, and Evaluation of Selective PDE4 Inhibitors for the Therapy of Pulmonary Injury.
J Med Chem
January 2025
Guangdong Key Laboratory of Animal Conservation and Resource Utilization, Guangdong Public Laboratory of Wild Animal Conservation and Utilization, Institute of Zoology, Guangdong Academy of Sciences, Guangzhou, Guangdong 510260, China.
Pulmonary inflammation is the main cause of lung injury. Phosphodiesterase 4 (PDE4) is a promising anti-inflammatory target for the treatment of respiratory diseases. Herein, we designed and synthesized 43 compounds in two novel series of benzimidazole derivatives as PDE4 inhibitors.
View Article and Find Full Text PDFThe metabolic pathway of Deg-AZM and investigations into the contribution of drug metabolizing enzymes and drug transporters in the drug interactions of Deg-AZM, a clinical-stage new transgelin agonist.
Front Pharmacol
January 2025
State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin, China.
Introduction: Deglycosylated azithromycin (Deg-AZM), a new transgelin agonist with positive therapeutic effects on slow transit constipation, has been approved for clinical trials in 2024. This work investigated the drug metabolism and transport of Deg-AZM to provide research data for further development of Deg-AZM.
Methods: A combination of UPLC-QTOF-MS was used to obtain metabolite spectra of Deg-AZM in plasma, urine, feces and bile.
Evaluation of bioaccessibility, metabolic clearance and interaction with xenobiotic receptors (PXR and AhR) of cinnamaldehyde.
Food Chem (Oxf)
June 2025
National Center for Natural Products Research, School of Pharmacy, The University of Mississippi, MS 38677, United States.
Cinnamon is one of the oldest known spices used in various food delicacies and herbal formulations. Cinnamaldehyde is a primary active constituent of cinnamon and substantially contributes to the food additive and medicinal properties of cinnamon. This report deals with cinnamaldehyde bioaccessibility, metabolic clearance, and interaction with human xenobiotic receptors (PXR and AhR).
View Article and Find Full Text PDFTranscriptomic and enzymatic analysis of peroxidase families at the early growth stage of halophyte ice plant (Mesembryanthemum crystallinum L.) under salt stress.
Bot Stud
January 2025
Department of Life Sciences, National Chung Hsing University, Taichung, 40227, Taiwan.
Ice plant (Mesembryanthemum crystallinum L.) is a halophyte and an inducible CAM plant. Ice plant seedlings display moderate salt tolerance, with root growth unaffected by 200 mM NaCl treatments, though hypocotyl elongation is hindered in salt-stressed etiolated seedlings.
View Article and Find Full Text PDFActivation of the COX-2/mPGES-1/PGE-2 cascade through the NLRP3 inflammasome contributes to Angiostrongylus cantonensis-induced eosinophilic meningoencephalitis.
Parasitol Res
January 2025
Department of Parasitology, Chung Shan Medical University, Taichung, 402, Taiwan.
Prostaglandin E2 (PGE-2) is synthesised by cyclooxygenase-2 (COX-2) and microsomal prostaglandin E synthase 1 (mPGES-1). PGE-2 exhibits pro-inflammatory properties in inflammatory conditions. However, there remains limited understanding of the COX-2/mPGES-1/PGE-2 pathway in Angiostrongylus cantonensis-induced meningoencephalitis.
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