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Conjugated oestrogen

Andrew Condappa, Maxine Gossell-Williams, William Aiken
Conjugated oestrogen is one of the more affordable secondary hormonal options available for castrate-resistant prostate cancer (CRPC) in Jamaica. The present study was conducted to examine the disease response in Jamaican men with CRPC treated with conjugated oestrogen. This study retrospectively reviewed the medical notes of patients who attended the urologic clinic of the University Hospital of the West Indies from 1 January 2009 to 31 December 2013 and a private urology clinic from 2 November 2005 to 3 June 2015 to identify patients diagnosed with CRPC treated with conjugated oestrogen (Premarin ®) as secondary therapy...
2018: Ecancermedicalscience
Sebastián Carranza-Lira, Miriam Elizabeth Cruz-Ramírez, Diana Sulvarán-Victoria
Introduction: Microscopic haematuria is common in adults and it has been reported in 13% of postmenopausal women. Objective: To evaluate the changes in urinary sediment after the use of vaginal conjugated oestrogens. Material and methods: Postmenopausal women with vaginal dryness were studied. In all them a urinalysis was done, looking for density, pH, and the presence of leukocytes and erythrocytes. In order to be included in the study, all of the women had to have microscopic haematuria, considered as the presence of 3 or more erythrocytes in the urinary sediment...
September 2017: Przeglad Menopauzalny, Menopause Review
M Ghadimi, S Dashti-Khavidaki, M Shahali, M Gohari, M-R Khatami, A Alamdari
WHAT IS KNOWN AND OBJECTIVE: Oestrogens could inhibit the metabolism of drugs, such as calcineurin inhibitors, that are substrates for cytochrome P-450 microsomal enzymes. This study assessed the potential tacrolimus interaction with oral conjugated oestrogen in kidney transplant recipients who received conjugated oestrogen as prophylaxis against bleeding, before kidney biopsy. METHODS: In this case-control study, 13 kidney transplant recipients who received oral conjugated oestrogen as prophylaxis against uraemic bleeding before allograft biopsy were considered as cases...
February 28, 2018: Journal of Clinical Pharmacy and Therapeutics
Cheng-Yuan Gu, Gao-Xiang Li, Yu Zhu, Hua Xu, Yao Zhu, Xiao-Jian Qin, Dai Bo, Ding-Wei Ye
BACKGROUND: Cytochrome P450 1B1 (CYP1B1) is a key enzyme in its oestrogen metabolism pathway, giving rise to hydroxylation and conjugation. Functionally relevant genetic variants within CYP1B1 may affect the telomere length and subsequently lead to prostate carcinogenesis. METHODS: We evaluated 8 CYP1B1 tag single nucleotide polymorphisms (SNPs) in 1015 men with prostate cancer (PCa) and 1052 cancer-free controls, and calculated odds ratios (ORs) and 95% confidence intervals (CIs) to estimate their association with risk of PCa...
2018: Journal of Cancer
Germán D Carrasquilla, Paolo Frumento, Anita Berglund, Christer Borgfeldt, Matteo Bottai, Chiara Chiavenna, Mats Eliasson, Gunnar Engström, Göran Hallmans, Jan-Håkan Jansson, Patrik K Magnusson, Peter M Nilsson, Nancy L Pedersen, Alicja Wolk, Karin Leander
BACKGROUND: Recent research indicates a favourable influence of postmenopausal hormone therapy (HT) if initiated early, but not late, on subclinical atherosclerosis. However, the clinical relevance of timing of HT initiation for hard end points such as stroke remains to be determined. Further, no previous research has considered the timing of initiation of HT in relation to haemorrhagic stroke risk. The importance of the route of administration, type, active ingredient, and duration of HT for stroke risk is also unclear...
November 2017: PLoS Medicine
(no author information available yet)
No abstract text is available yet for this article.
June 2017: Australian Prescriber
Qiang Hao, Guoxing Xu, Yue Yang, Yuxin Sun, Dengli Cong, Hongrui Li, Xin Liu, Zeng Wang, Zheng Zhang, Jinglin Chen, Yao Li, Xue Luan, Lin Wang, Lin Tian, Kun Liu, Yan Li, Qianru Jiao, Jin Pei
OBJECTIVES: Targeted delivery of mitoxantrone (MTO, an anthraquinone drug with high antitumour effect) may be achieved using a novel nanoparticulate delivery system via binding the oestrogen receptor (ER, highly expressed in a variety of human tumours). METHODS: A novel liposomal nanoparticle (NP) was developed using a conjugate derived from 1, 2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[amino (polyethylene glycol)-2000] (DSPE-PEG2000 -NH2 ) and oestrone (ES, is known to bind the ER) to produce an ES-targeted PEGylated liposome (ES-SSL)...
April 26, 2017: Journal of Pharmacy and Pharmacology
(no author information available yet)
Duavive (Pfizer) is a modified-release formulation of conjugated oestrogens plus bazedoxifene acetate (a selective oestrogen receptor modulator). It is licensed for treatment of oestrogen deficiency symptoms in postmenopausal women with a uterus for whom treatment with progestogen-containing therapy is not appropriate.(1,2) It was licensed by the European Medicines Agency (EMA) in 2014 and launched in the UK in July 2016.(1,3) Here, we review the evidence on efficacy and safety of conjugated oestrogens/bazedoxifene and consider its place in the management of symptoms associated with the menopause...
April 2017: Drug and Therapeutics Bulletin
Ashraf H Ahmed, Richard D Gordon, Gregory Ward, Martin Wolley, Brett C McWhinney, Jacobus P Ungerer, Michael Stowasser
Background: Plasma aldosterone/renin ratio (ARR) is the most popular screening test for primary aldosteronism (PA). Because both estrogen and progesterone (including in oral contraceptive agents) affect aldosterone and renin levels, we studied the effects of combined hormonal replacement therapy (HRT) on ARR; renin was measured as both direct renin concentration (DRC) and plasma renin activity (PRA). Methods: Fifteen normotensive, healthy postmenopausal women underwent measurement (seated, midmorning) of plasma aldosterone, DRC, PRA, electrolytes, and creatinine and urinary aldosterone, cortisol, electrolytes, and creatinine at baseline and after 2 weeks and 6 weeks of treatment with combined HRT (conjugated estrogens 0...
July 1, 2017: Journal of Clinical Endocrinology and Metabolism
Amanda Tivnan, Tatjana Heilinger, Joanne M Ramsey, Gemma O'Connor, Jenny L Pokorny, Jann N Sarkaria, Brett W Stringer, Bryan W Day, Andrew W Boyd, Ella L Kim, Holger N Lode, Sally-Ann Cryan, Jochen H M Prehn
Aromatase is a critical enzyme in the irreversible conversion of androgens to oestrogens, with inhibition used clinically in hormone-dependent malignancies. We tested the hypothesis that targeted aromatase inhibition in an aggressive brain cancer called glioblastoma (GBM) may represent a new treatment strategy. In this study, aromatase inhibition was achieved using third generation inhibitor, Letrozole, encapsulated within the core of biodegradable poly lactic-co-glycolic acid (PLGA) nanoparticles (NPs). PLGA-NPs were conjugated to human/mouse chimeric anti-GD2 antibody ch14...
March 7, 2017: Oncotarget
Natalia Sutiman, Joanne Siok Liu Lim, Thomas E Muerdter, Onkar Singh, Yin Bun Cheung, Raymond Chee Hui Ng, Yoon Sim Yap, Nan Soon Wong, Peter Cher Siang Ang, Rebecca Dent, Werner Schroth, Matthias Schwab, Chiea Chuen Khor, Balram Chowbay
Tamoxifen (TAM) is an established endocrine treatment for all stages of oestrogen receptor (ER)-positive breast cancer. Its complex metabolism leads to the formation of multiple active and inactive metabolites. One of the main detoxification and elimination pathways of tamoxifen and its active metabolites, 4-hydroxytamoxifen (4-OHT) and endoxifen, is via glucuronidation catalysed by uridine 5'-diphospho-glucuronosyltransferases (UGTs). However, few studies have comprehensively examined the impact of variations in the genes encoding the major hepatic UGTs on the disposition of tamoxifen and its metabolites...
October 2016: Clinical Pharmacokinetics
Antonella Borrelli, Antonietta Schiattarella, Roberto Mancini, Alessandra Pica, Maria Laura Pollio, Maria Grazia Ruggiero, Patrizia Bonelli, Viviana De Luca, Franca Maria Tuccillo, Clemente Capasso, Enrico Gori, Marina Sanseverino, Andrea Carpentieri, Leila Birolo, Piero Pucci, Jean Rommelaere, Aldo Mancini
A 24-amino acid leader peptide of a new human recombinant manganese superoxide dismutase can enter cells and carry molecules. Here, we demonstrated that six of the 24 amino acids penetrate cells through a particular gate represented by a specific amino acid sequence of the oestrogen receptor (ER). We analysed the internalization of the synthetic hexapeptide and the cytotoxic activity of the hexapeptide conjugated to cisplatin on a cell line panel. In most cell lines, the hexapeptide delivered an amount of cisplatin that was 2 to 8 times greater than that released by cisplatin when the drug was used alone...
January 4, 2016: Scientific Reports
S A Mitchell, A Paine, M Moffatt, T A Neale, M E Orme, C Hawes
No abstract text is available yet for this article.
November 2015: Value in Health: the Journal of the International Society for Pharmacoeconomics and Outcomes Research
Xiaojuan Chai, Yan Guo, Mengxi Jiang, Bingfang Hu, Zhigang Li, Jie Fan, Meihong Deng, Timothy R Billiar, Heidi R Kucera, Nilesh W Gaikwad, Meishu Xu, Peipei Lu, Jiong Yan, Haiyan Fu, Youhua Liu, Lushan Yu, Min Huang, Su Zeng, Wen Xie
Sepsis is the host's deleterious systemic inflammatory response to microbial infections. Here we report an essential role for the oestrogen sulfotransferase (EST or SULT1E1), a conjugating enzyme that sulfonates and deactivates estrogens, in sepsis response. Both the caecal ligation and puncture (CLP) and lipopolysaccharide models of sepsis induce the expression of EST and compromise the activity of oestrogen, an anti-inflammatory hormone. Surprisingly, EST ablation sensitizes mice to sepsis-induced death. Mechanistically, EST ablation attenuates sepsis-induced inflammatory responses due to compromised oestrogen deactivation, leading to increased sepsis lethality...
August 10, 2015: Nature Communications
Ting Qu, Shi-Mao Zhang, Lin-Lin Yu, Sheng Zhang, Dong-Zhi Yuan, Qian Xu, Jin-Hu Zhang, Ya-Ping He, Li-Min Yue
Integrins are the dominant and final adhesion molecules in the attachment process between the blastocysts and endometrium. It is necessary for oestrogen to rapidly activate mouse blastocysts so that they attach to the endometrial epithelium. Our previous study suggested that oestrogen can rapidly induce an increase in intracellular calcium in mouse blastocysts via G-protein-coupled receptor 30 (GPR30). Thus, we deduced that integrins may be involved in GPR30 mediation of the fast effect of oestrogen on mouse blastocysts in implantation...
May 8, 2015: Reproduction, Fertility, and Development
M Ghazanfarpour, R Latifnejad Roudsari, G Treglia, R Sadeghi
Current systematic review evaluated the efficacy of topical isoflavones to relieve vaginal symptoms in menopausal women. MEDLINE (1966 to January 2014), Scopus (1990 to January 2014), and the Cochrane Central Register of Controlled Trials (The Cochrane Library issue 1, 2013) were searched using keywords 'isoflavone and vagina'. Relevant studies were reviewed by two independent reviewers. Only randomised controlled trials (RCTs) were included in the systematic review. Out of 115 potentially relevant publications, four studies met the inclusion criteria...
2015: Journal of Obstetrics and Gynaecology: the Journal of the Institute of Obstetrics and Gynaecology
Robert W Schwenk, Christian Baumeier, Brian Finan, Oliver Kluth, Christine Brauer, Hans-Georg Joost, Richard D DiMarchi, Matthias H Tschöp, Annette Schürmann
AIMS/HYPOTHESIS: Oestrogens have previously been shown to exert beta cell protective, glucose-lowering effects in mouse models. Therefore, the recent development of a glucagon-like peptide-1 (GLP-1)-oestrogen conjugate, which targets oestrogen into cells expressing GLP-1 receptors, offers an opportunity for a cell-specific and enhanced beta cell protection by oestrogen. The purpose of this study was to compare the effects of GLP-1 and GLP-1-oestrogen during beta cell failure under glucolipotoxic conditions...
March 2015: Diabetologia
Young-Hoon Ko, Sook-Haeng Joe, Woong Cho, Jeong-Hyun Park, Jung-Jae Lee, In-Kwa Jung, Leen Kim, Seung-Hyun Kim
Objective. The purpose of this investigation was to assess the cognitive effects of adjuvant hormone replacement therapy (HRT) when used to treat premenopausal women with chronic schizophrenia using an 8-week, double-blind, placebo-controlled, randomized trial. Method. Women of childbearing age with chronic schizophrenia were recruited and randomized into placebo and HRT groups, the latter of which was administered 0.625 mg of conjugated oestrogen with 2.5 mg of medroxyprogesterone acetate daily. Each group contained 14 subjects...
2006: International Journal of Psychiatry in Clinical Practice
R Cao, J Chen, X Zhang, Y Zhai, X Qing, W Xing, L Zhang, Y S Malik, H Yu, X Zhu
BACKGROUND: Myosin X (MYO10) was recently reported to promote tumour invasion by transporting integrins to filopodial tips in breast cancer. However, the role of MYO10 in tumours remains poorly defined. Here, we report that MYO10 is required in invadopodia to mediate invasive growth and extracellular matrix degradation, which depends on the binding of MYO10's pleckstrin homology domain to PtdIns(3,4,5)P3. METHODS: The expression of MYO10 and its associations with clinicopathological and biological factors were examined in breast cancer cells and breast cancer specimens (n=120)...
July 29, 2014: British Journal of Cancer
Jiajia Wang, Yongfeng Wang, Ting Wang, Kai Cui, Lianhong Wang, Rong Ji
Steroid oestrogens are typical endocrine-disrupting compounds in the environment and are excreted from the human and animals mainly as conjugates, including sulfate and glucuronide salts. The oestrogen conjugates are largely biologically inactive, but they can be de-conjugated and release free oestrogens, which usually exhibit strong oestrogenicity. Therefore, it is important to study the fate of oestrogen conjugates in the environment. However, because of the complexity of environmental matrixes, time-consuming pre-treatments of samples are usually required to reduce the interference of the matrixes...
June 15, 2014: Journal of Labelled Compounds & Radiopharmaceuticals
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