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https://www.readbyqxmd.com/read/28646880/6-shogaol-a-neuroactive-compound-of-ginger-jahe-gajah-induced-neuritogenic-activity-via-ngf-responsive-pathways-in-pc-12-cells
#1
Syntyche Ling Sing Seow, Sok Lai Hong, Guan Serm Lee, Sri Nurestri Abd Malek, Vikineswary Sabaratnam
BACKGROUND: Ginger is a popular spice and food preservative. The rhizomes of the common ginger have been used as traditional medicine to treat various ailments. 6-Shogaol, a pungent compound isolated from the rhizomes of jahe gajah (Zingiber officinale var officinale) has shown numerous pharmacological activities, including neuroprotective and anti-neuroinflammatory activities. The aim of this study was to investigate the potential of 6-shogaol to mimic the neuritogenic activity of nerve growth factor (NGF) in rat pheochromocytoma (PC-12) cells...
June 24, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28642035/improving-the-efficacy-of-hormone-therapy-in-breast-cancer-the-role-ofcholesterol-metabolism-in-serm-mediated-autophagy-cell-differentiation-and-death
#2
REVIEW
Julie Leignadier, Florence Dalenc, Marc Poirot, Sandrine Silvente-Poirot
Breast cancer (BC) is one of the most common female cancers in the world, with estrogen receptor (ER)-positive BC the most frequent subtype. Tamoxifen (Tam) is an effective drug that competitively binds to the ER and is routinely used for the treatment of ER-positive BC. However, a number of ER-positive BC do not respond to Tam treatment and acquired resistance is often observed, constituting a major challenge for extending patient life expectancy. The mechanisms responsible for these treatment failures remain unclear, indicating the requirement for other targets and better predictors for patient response to Tam...
June 19, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28615284/tcl1a-snps-and-estrogen-mediated-toll-like-receptor-myd88-dependent-nf-%C3%AE%C2%BAb-activation-snp-and-serm-dependent-modification-of-inflammation-and-immune-response
#3
Ming-Fen Ho, James N Ingle, Tim Bongartz, Krishna R Kalari, Paul E Goss, Lois E Shepherd, Taisei Mushiroda, Michiaki Kubo, Liewei Wang, Richard M Weinshilboum
In a previous genome-wide association study (GWAS) for musculoskeletal adverse events during aromatase inhibitor therapy of breast cancer, we reported that single nucleotide polymorphisms (SNPs) near the TCL1A gene were associated with this adverse drug reaction. Functional genomic studies showed that TCL1A expression was induced by estradiol (E2), but only in cells with the variant sequence for the top GWAS SNP (rs11849538), a SNP that created a functional estrogen response element. In addition, TCL1A genotype influenced the "downstream" expression of a series of cytokines and chemokines and had a striking effect on NF-κB transcriptional activity...
June 14, 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/28591668/the-selective-estrogen-receptor-modulators-serms-raloxifene-and-tamoxifen-improve-anp-levels-and-decrease-nuclear-translocation-of-nf-kb-in-estrogen-deficient-rats
#4
Aline Z Lamas, Andrews M Nascimento, Ana Raquel S Medeiros, Izabela F Caliman, Polyana L M Dalpiaz, Luciana B Firmes, Glauciene J Sousa, Phablo Wendell C Oliveira, Tadeu U Andrade, Adelina M Reis, Sônia A Gouvea, Nazaré S Bissoli
BACKGROUND: The selective estrogen receptor modulators (SERMs) raloxifene and tamoxifen are used for the treatment of osteoporosis and cancer, respectively, in women. The impairment of both the Atrial Natriuretic Peptide (ANP) cell signaling system and the translocation of nuclear factor-kappa B (NF-kB) to the cell nucleus are associated with detrimental cardiovascular effects and inflammation. The effects of SERMs on these parameters in the cardiac tissue of estrogen-deficient rats has not been reported...
March 16, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28583434/27-hydroxycholesterol-a-novel-player-in-molecular-carcinogenesis-of-breast-and-prostate-cancer
#5
REVIEW
Gurdeep Marwarha, Shaneabbas Raza, Kimberly Hammer, Othman Ghribi
Several studies have suggested an etiological role for hypercholesterolemia in the pathogenesis of breast cancer and prostate cancer (PCa). However, the molecular mechanisms that underlie and mediate the hypercholesterolemia-fostered increased risk for breast cancer and PCa are yet to be determined. The discovery that the most abundant cholesterol oxidized metabolite in the plasma, 27 hydroxycholesterol (27-OHC), is a selective estrogen receptor modulator (SERM) and an agonist of Liver X receptors (LXR) partially fills the void in our understanding and knowledge of the mechanisms that may link hypercholesterolemia to development and progression of breast cancer and PCa...
June 2, 2017: Chemistry and Physics of Lipids
https://www.readbyqxmd.com/read/28570956/worry-and-risk-perception-of-breast-cancer-in-a-prevention-trial-of-low-dose-tamoxifen-in-midlife-postmenopausal-hormone-users
#6
Gabriella Rondanina, Matteo Puntoni, Aliana Guerrieri-Gonzaga, Domenico Marra, Bernardo Bonanni, Andrea DeCensi
OBJECTIVE: There is increasing interest in combining postmenopausal hormone therapy (HT) and SERMs in midlife women. We previously showed that refusal to participate in a prevention trial of low dose tamoxifen in HT users was associated with higher worry about breast cancer. Given this counterintuitive finding, we studied which factors influenced worry and risk perception of breast cancer. METHODS: We assessed the relationships of breast cancer worry and risk perception with age, age at menopause, Gail risk, education, adherence to mammographic screening, BMI, smoking, physical activity, alcohol use, anxiety and depression in 457 midlife HT users who were eligible to participate in the trial...
May 29, 2017: Breast: Official Journal of the European Society of Mastology
https://www.readbyqxmd.com/read/28551078/effects-of-a-tissue-selective-estrogen-complex-on-b-lymphopoiesis-and-b-cell-function
#7
Jauquline Nordqvist, Angelina Bernardi, Ulrika Islander, Hans Carlsten
BACKGROUND/OBJECTIVE: 17β-estradiol (E2) has major effects on the immune system. It induces thymic atrophy, inhibits both T and B lymphopoiesis and stimulates antibody production treatment with E2 has protective effects on the skeleton but is associated with negative side effects in reproductive organs. A tissue-selective estrogen complex (TSEC) comprise of estrogens combined with a selective estrogen receptor modulator (SERM). TSEC therapy displays the bone-protective effects of estrogen, while the negative side effects on reproductive organs are blocked by the SERM...
August 2017: Immunobiology
https://www.readbyqxmd.com/read/28535794/mutation-site-and-context-dependent-effects-of-esr1-mutation-in-genome-edited-breast-cancer-cell-models
#8
Amir Bahreini, Zheqi Li, Peilu Wang, Kevin M Levine, Nilgun Tasdemir, Lan Cao, Hazel M Weir, Shannon L Puhalla, Nancy E Davidson, Andrew M Stern, David Chu, Ben Ho Park, Adrian V Lee, Steffi Oesterreich
BACKGROUND: Mutations in the estrogen receptor alpha (ERα) 1 gene (ESR1) are frequently detected in ER+ metastatic breast cancer, and there is increasing evidence that these mutations confer endocrine resistance in breast cancer patients with advanced disease. However, their functional role is not well-understood, at least in part due to a lack of ESR1 mutant models. Here, we describe the generation and characterization of genome-edited T47D and MCF7 breast cancer cell lines with the two most common ESR1 mutations, Y537S and D538G...
May 23, 2017: Breast Cancer Research: BCR
https://www.readbyqxmd.com/read/28503095/the-cholesterol-metabolite-27-hydroxycholesterol-stimulates-cell-proliferation-via-er%C3%AE-in-prostate-cancer-cells
#9
Shaneabbas Raza, Megan Meyer, Casey Goodyear, Kimberly D P Hammer, Bin Guo, Othman Ghribi
BACKGROUND: For every six men, one will be diagnosed with prostate cancer (PCa) in their lifetime. Estrogen receptors (ERs) are known to play a role in prostate carcinogenesis. However, it is unclear whether the estrogenic effects are mediated by estrogen receptor α (ERα) or estrogen receptor β (ERβ). Although it is speculated that ERα is associated with harmful effects on PCa, the role of ERβ in PCa is still ill-defined. The cholesterol oxidized metabolite 27-hydroxycholesterol (27-OHC) has been found to bind to ERs and act as a selective ER modulator (SERM)...
2017: Cancer Cell International
https://www.readbyqxmd.com/read/28460819/design-synthesis-biological-evaluation-and-molecular-docking-studies-of-novel-3-aryl-4-anilino-2h-chromen-2-one-derivatives-targeting-er%C3%AE-as-anti-breast-cancer-agents
#10
Guoshun Luo, Mingqi Chen, Weiting Lyu, Ruheng Zhao, Qian Xu, Qidong You, Hua Xiang
The estrogen receptor (ER) has played an important role in breast cancer development and progression and is a central target for anticancer drug discovery. In order to develop novel selective ERα modulators (SERMs), we designed and synthesized 18 novel 3-aryl-4-anilino-2H-chromen-2-one derivatives based on previously reported lead compounds. The biological results indicated that most of the compounds presented potent ERα binding affinity and possessed better anti-proliferative activities against MCF-7 and Ishikawa cell lines than the positive control tamoxifen...
June 15, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28449918/better-knowledge-and-regular-vaccination-practices-correlate-well-with-higher-seasonal-influenza-vaccine-uptake-in-people-at-risk-promising-survey-results-from-a-university-outpatient-clinic
#11
Işıl Adadan Güvenç, Hülya Parıldar, Mustafa Kürşat Şahin, Selim Sermed Erbek
BACKGROUND: The knowledge, beliefs, opinions, and attitudes of patients and their relatives regarding seasonal influenza vaccination were evaluated. METHODS: This descriptive study was undertaken in the outpatient clinics of Baskent University Hospital. There were 566 responders who completed a self-administered questionnaire. RESULTS: The mean age of participants was 48.35 years, and 16.8% were ≥65 years. Of the responders, 21.7% were vaccinated this year, whereas 57...
April 24, 2017: American Journal of Infection Control
https://www.readbyqxmd.com/read/28439061/-calcium-and-bone-metabolism-across-women-s-life-stages-bone-quality-and-treatment-of-osteoporosis-by-serm
#12
Mitsuru Saito, Keishi Marumo
Estrogen deficiency induces bone resorption and bone collagen crosslink abnormalities such as reductions in enzymatic cross-links and accumulation of Advanced glycation end products(AGEs). In this review, we described that the mechanism of poor bone quality in estrogen deficiency and how selective estrogen receptor modulators such as raloxifene and bazedoxifene improve bone structural and material properties.
2017: Clinical Calcium
https://www.readbyqxmd.com/read/28412809/selective-estrogen-receptor-modulator-serm-like-activities-of-diarylheptanoid-a-phytoestrogen-from-curcuma-comosa-in-breast-cancer-cells-pre-osteoblast-cells-and-rat-uterine-tissues
#13
Natthakan Thongon, Nittaya Boonmuen, Kanoknetr Suksen, Patsorn Wichit, Arthit Chairoungdua, Patoomratana Tuchinda, Apichart Suksamrarn, Wipawee Winuthayanon, Pawinee Piyachaturawat
Diarylheptanoids from Curcuma comosa, of the Zingiberaceae family, exhibit diverse estrogenic activities. In this study we investigated the estrogenic activity of a major hydroxyl diarylheptanoid, 7-(3,4 -dihydroxyphenyl)-5-hydroxy-1-phenyl-(1E)-1-heptene (compound 092) isolated from C. comosa. The compound elicited different transcriptional activities of estrogen agonist at low concentrations (0.1-1 μM) and antagonist at high concentrations (10-50 μM) using luciferase reporter gene assay in HEK-293T cells...
May 3, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28401437/estrogens-regulate-life-and-death-in-mitochondria
#14
Carolyn M Klinge
Estrogens coordinate and integrate cellular metabolism and mitochondrial activities by direct and indirect mechanisms mediated by differential expression and localization of estrogen receptors (ER) in a cell-specific manner. Estrogens regulate transcription and cell signaling pathways that converge to stimulate mitochondrial function- including mitochondrial bioenergetics, mitochondrial fusion and fission, calcium homeostasis, and antioxidant defense against free radicals. Estrogens regulate nuclear gene transcription by binding and activating the classical genomic estrogen receptors α and β (ERα and ERβ) and by activating plasma membrane-associated mERα, mERβ, and G-protein coupled ER (GPER, GPER1)...
April 11, 2017: Journal of Bioenergetics and Biomembranes
https://www.readbyqxmd.com/read/28396978/a-novel-strategy-to-co-target-estrogen-receptor-and-nuclear-factor-%C3%AE%C2%BAb-pathways-with-hybrid-drugs-for-breast-cancer-therapy
#15
Irida Kastrati, Marton I Siklos, Svitlana D Brovkovych, Gregory R J Thatcher, Jonna Frasor
Nearly 75% of breast tumors express estrogen receptor (ER), and will be treated with endocrine therapy, such as selective estrogen receptor modulator (SERM), tamoxifen, or aromatase inhibitors. Despite their proven success, as many as 40-50% of ER+ tumors fail to respond to endocrine therapy and eventually recur as aggressive, metastatic cancers. Therefore, preventing and/or overcoming endocrine resistance in ER+ tumors remains a major clinical challenge. Deregulation or activation of the nuclear factor κB (NFκB) pathway has been implicated in endocrine resistance and poor patient outcome in ER+ tumors...
April 10, 2017: Hormones & Cancer
https://www.readbyqxmd.com/read/28396216/assessment-of-the-potential-activity-of-major-dietary-compounds-as-selective-estrogen-receptor-modulators-in-two-distinct-cell-models-for-proliferation-and-differentiation
#16
COMPARATIVE STUDY
Sylvain Lecomte, Marie Lelong, Gaëlle Bourgine, Theo Efstathiou, Christian Saligaut, Farzad Pakdel
Estrogen receptors (ERs) α and β are distributed in most tissues of women and men. ERs are bound by estradiol (E2), a natural hormone, and mediate the pleiotropic and tissue-specific effects of E2, such as proliferation of breast epithelial cells or protection and differentiation of neuronal cells. Numerous environmental molecules, called endocrine disrupting compounds, also interact with ERs. Phytoestrogens belong to this large family and are considered potent therapeutic molecules that act through their selective estrogen receptor modulator (SERM) activity...
June 15, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28374135/oxabicycloheptene-sulfonate-protects-against-%C3%AE-amyloid-induced-toxicity-by-activation-of-pi3k-akt-and-erk-signaling-pathways-via-gper1-in-c6-cells
#17
Li-Juan Deng, Chen Cheng, Jun Wu, Cai-Hua Wang, Hai-Bing Zhou, Jian Huang
Oxabicycloheptene sulfonate (OBHS) is a novel bicyclic core selective estrogen receptor modulator (SERM) with estrogen receptor (ER) antagonistic-activity and anti-inflammatory activity. However, little is known about protective action of OBHS on neurodegenerative disorders. In the present study, OBHS demonstrated a remarkably protective effect against amyloid beta (Aβ) induced cytotoxicity via G-protein-coupled estrogen receptor 1 (GPER1) in rat astroglial cell line (C6). The C6 cell death induced by Aβ was decreased by OBHS (1 μM) treatment for 45 min...
April 4, 2017: Neurochemical Research
https://www.readbyqxmd.com/read/28372959/-cherchez-la-femme-modulation-of-estrogen-receptor-function-with-selective-modulators-clinical-implications-in-the-field-of-urology
#18
REVIEW
Sevann Helo, Blake Wynia, Andrew McCullough
INTRODUCTION: Selective estrogen receptor modulators (SERMs) have been used off-label in men for more than 50 years. SERMs exert their action on the estrogen receptor agonistically or antagonistically. A fundamental knowledge of the complex molecular action and physiology of SERMs is important in understanding their use and future directions of study in men. AIM: To review the basic science and mechanism of the action of estrogens, the estrogen receptor, and SERMs, and the existing clinical publications on the use of SERMs in men for infertility and hypogonadism with their strengths and weaknesses and to identify the need for future studies...
March 31, 2017: Sexual Medicine Reviews
https://www.readbyqxmd.com/read/28364860/regulatory-effects-of-estetrol-on-the-endothelial-plasminogen-pathway-and-endothelial-cell-migration
#19
Maria Magdalena Montt-Guevara, Giulia Palla, Stefania Spina, Guja Bernacchi, Elena Cecchi, Adrian Esteban Campelo, Jorge Eduardo Shortrede, Alessio Canu, Tommaso Simoncini
BACKGROUND: Estetrol (E4) is a natural estrogen produced solely during human pregnancy. E4 is suitable for clinical use since it acts as a selective estrogen receptor modulator. In clinical trials E4 has been seen to have little or no effect on coagulation. Hence, it is interesting to investigate whether E4 alters endothelial-dependent fibrinolysis. OBJECTIVES: We studied the effects of E4 on the fibrinolytic system and whether this could influence the ability of endothelial cells to migrate...
May 2017: Maturitas
https://www.readbyqxmd.com/read/28349511/risk-of-endometrial-cancer-in-women-treated-with-ovary-stimulating-drugs-for-subfertility
#20
REVIEW
Alkistis Skalkidou, Theodoros N Sergentanis, Spyros P Gialamas, Marios K Georgakis, Theodora Psaltopoulou, Marialena Trivella, Charalampos S Siristatidis, Evangelos Evangelou, Eleni Petridou
BACKGROUND: Medical treatment for subfertility principally involves the use of ovary-stimulating agents, including selective oestrogen receptor modulators (SERMs), such as clomiphene citrate, gonadotropins, gonadotropin-releasing hormone (GnRH) agonists and antagonists, as well as human chorionic gonadotropin. Ovary-stimulating drugs may act directly or indirectly upon the endometrium (lining of the womb). Nulliparity and some causes of subfertility are recognized as risk factors for endometrial cancer...
March 25, 2017: Cochrane Database of Systematic Reviews
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