Activity of microsomal enzymes was studied using an indirect method for estimation of the rate of antipyrine secretion with saliva in 70 healthy persons at the age from 16 to 86 years. Distinct individual differences were observed in the activity of the enzymes: time of the antipyrine half-secretion varied from 6.4 hrs to 50.1 hrs. The time of antipyrine half-secretion was significantly higher in the older (60-86 years) than in younger persons (16-30 years), suggesting decreased activity of the microsomal enzymes in older people. The microsomal enzymes activity might be increased distinctly under effect of several drugs, especially of hypotensive drugs--reserpine and dibasole. The data obtained suggest that for effective medicinal therapy it is essential to control the initial activity of microsomal enzymes as well as its alterations in the course of medicamentous treatment; the activity of microsomal enzymes in a given person must be taken into consideration for correct individual selection of doses of the drugs.
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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.
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 PDFParasitol 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.
View Article and Find Full Text PDFSci Total Environ
January 2025
Department of Arctic and Marine Biology, UiT The Arctic University of Norway, N-9037 Tromsø, Norway.
Increased industrial offshore activities in northern waters raise the question of impact of polycyclic aromatic hydrocarbons (PAHs) on key Arctic marine species. One of these is the ecologically important polar cod (Boreogadus saida), which is the primary food source for Arctic marine mammals and seabirds. In the present work, we have conducted the first comprehensive proteomics study with this species by exploring the effects of dietary PAH exposure on the hepatic proteome, using benzo[a]pyrene (BaP) as a PAH model-compound.
View Article and Find Full Text PDFRSC Med Chem
January 2025
School of Chemical Sciences, University of Auckland Auckland 1010 New Zealand
Dysregulation of choline phospholipid metabolism and overexpression of phosphatidylcholine-specific phospholipase C (PC-PLC) is implicated in various cancers. Current known enzyme inhibitors include compounds based on a 2-morpholino-5--benzylamino benzoic acid, or hydroxamic acid, scaffold. In this work, 81 compounds were made by modifying this core structure to explore the pharmacophore.
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