The plasma oestrone and oestradiol levels of 34 postmenopausal women were studied and related to various of their other characteristics. The plasma oestrone and oestradiol-17beta levels (Mean +/- SE) were, respectively, 32.09 +/- 4.6 pg/ml and 13.9 +/- 3.1 pg/ml. There was a highly significant negative linear association between the years elapsed since the menopause and oestrone levels (P less than 0.001) and oestradiol levels (P less than 0.02). Both plasma oestrone and oestradiol levels were directly related to weight, but the relation was only significant for oestradiol. A significant positive correlation was found between vaginal bleeding and excess weight. The degree of oestrogenicity of the vaginal smear was directly related to the levels of oestrone (P less than 0.08) and oestradiol (P less than 0.005) and to the degree of endometrial hyperplasia (P less than 0.02).
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Metabolites
September 2024
Proteomics Resource Unit, Obesity Research Center, College of Medicine, King Saud University, Riyadh 11461, Saudi Arabia.
Background: Liraglutide, a long-acting glucagon-like peptide-1 receptor agonist (GLP1RA), is a well-established anti-diabetic drug, has also been approved for the treatment of obesity at a dose of 3 mg. There are a limited number of studies in the literature that have looked at changes in metabolite levels before and after liraglutide treatment in patients with obesity. To this end, in the present study we aimed to explore the changes in the plasma metabolomic profile, using liquid chromatography-high resolution mass spectrometry (LC-HRMS) in patients with obesity.
View Article and Find Full Text PDFReprod Toxicol
December 2024
Environment and Health, Amsterdam Institute for Life and Environment, Vrije Universiteit Amsterdam, De Boelelaan 1085, Amsterdam 1081 HV, the Netherlands. Electronic address:
Cancer Res Commun
September 2024
Division of Pharmaceutics and Pharmacology, College of Pharmacy, Comprehensive Cancer Center, The Ohio State University, Columbus, Ohio.
Unlabelled: Although the primary elimination pathway for most tyrosine kinase inhibitors (TKI) involves CYP3A4-mediated metabolism, the mechanism by which these agents are brought into hepatocytes remains unclear. In this study, we optimized and validated a competitive counterflow (CCF) assay to examine TKIs as substrates of the hepatic uptake transporter OATP1B1. The CCF method was based on the stimulated efflux of radiolabeled estradiol-17β-glucuronide under steady-state conditions in HEK293 cells engineered to overexpress OATP1B1.
View Article and Find Full Text PDFCancer Epidemiol Biomarkers Prev
August 2024
Brigham and Women's Hospital, Boston, MA, United States.
Background: Estradiol and estrone are well-established risk factors for postmenopausal breast cancer (BC). Experimental evidence suggests that specific estrogen metabolites, produced via irreversible hydroxylation of estrone and estradiol at the 2- or 16-position may independently influence carcinogenesis.
Methods: We performed a nested case-control study of BC (328 BC cases; 639 controls) among postmenopausal women within the Nurses' Health Study (NHS)to examine the role of estrogens and estrogen metabolites (jointly referred to as EM).
Front Pharmacol
August 2024
Department of Pharmaceutics, School of Pharmacy, University of Washington, Seattle, WA, United States.
Introduction: Pregnancy results in significant changes in drug pharmacokinetics (PK). While previous studies have elucidated the impact of pregnancy-related hormones (PRH) on mRNA or protein expression and activity of major hepatic metabolizing enzymes, their effect on hepatic drug transporters remains largely unexplored. Therefore, we investigated the effect of a cocktail of PRH on the mRNA expression and activity of hepatic transporters.
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