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Mifepristone

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https://www.readbyqxmd.com/read/29688061/molecular-activities-and-ligand-binding-specificities-of-star-related-lipid-transfer-domains-exploring-integrated-in-silico-methods-and-ensemble-docking-approaches
#1
K Kranthi Kumar, B Uma Devi, P Neeraja
In this study, cholesterol biotransformation gene-set of human steroidogenic acute regulatory protein-related lipid transfer (START) domains were evaluated from high-throughput gene screening approaches. It was shown that STARD1, STARD3 and STARD4 proteins are better effective transporters of cholesterol than STARD5 and STARD6 domains. Docking studies show a strong agreement with gene ontology enrichment data. According to both complementary strategies, it was found that only STARD1, STARD3 and STARD4 are potentially involved in cholesterol biotransformation in mitochondria through Ω1-loop of C-terminal α4-helical domain...
April 24, 2018: SAR and QSAR in Environmental Research
https://www.readbyqxmd.com/read/29680774/targeting-hypothalamic-pituitary-adrenal-axis-hormones-and-sex-steroids-for-improving-cognition-in-major-mood-disorders-and-schizophrenia-a-systematic-review-and-narrative-synthesis
#2
REVIEW
Virginia Soria, Alexandre González-Rodríguez, Elena Huerta-Ramos, Judith Usall, Jesús Cobo, Miquel Bioque, Juan David Barbero, Clemente García-Rizo, Meritxell Tost, José Antonio Monreal, Javier Labad
Cognitive deficits are a core feature of serious mental illnesses such as schizophrenia, major depressive disorder (MDD) and bipolar disorder (BD) and are a common cause of functional disability. There is limited efficacy of pharmacological interventions for improving the cognitive deficits in these disorders. As pro-cognitive pharmacological treatments are lacking, hormones or drugs that target the endocrine system may become potential candidates for 'repurposing' trials aiming to improve cognition. We aimed to study whether treatment with drugs targeting the hypothalamic-pituitary-adrenal (HPA) axis and sex steroids can improve cognition in patients with schizophrenia, MDD or BD...
April 14, 2018: Psychoneuroendocrinology
https://www.readbyqxmd.com/read/29657247/protective-effect-of-taohong-siwu-decoction-on-abnormal-uterine-bleeding-induced-by-incomplete-medical-abortion-in-rats-during-early-pregnancy
#3
Yanyan Zhang, Jichen Wang, Chijing Zuo, Weidong Chen, Qian Zhu, Dongdong Guo, Huanru Wu, Huizhuo Wang, Daiyin Peng, Lan Han
Abnormal uterine bleeding (AUB) induced by incomplete abortion is a common gynecological disease. Taohong Siwu decoction (TSD) is a traditional Chinese medicine (TCM) formula, which has been developed to treat AUB for hundreds of years. In this study, rats had incomplete abortion induced in early pregnancy using mifepristone and misoprostol. The duration and quantity of uterine bleeding were recorded and measured. The pathologic histologic grade was evaluated by hematoxylin-eosin staining (HE). Estradiol (E2 ) and progesterone (P) levels were measured by enzyme linked immunosorbent assays (ELISA)...
April 14, 2018: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/29621762/mifepristone-inhibits-the-migration-of-cervical-cancer-cells-by-inhibiting-exocrine-secretion
#4
Lin Sang, Xiaoyan Wang, Xingbo Zhao
Cervical cancer (CC) is one of the most common gynecological malignancies, and metastasis limits the use of surgical resection. Metapristone (MIF) was reported to suppress the proliferation and migration of several cancer cells. Exosomes play a variety of roles in cellular biological processes. The relation of exosomes and CC is less studied. Cell viability, apoptosis assay and migration assay was conducted in HeLa cells treated by MIF by CCK-8 kit, staining by Annexin V-fluorescein isothiocyanate and propidium iodide, and wound test respectively...
April 5, 2018: Pharmacology
https://www.readbyqxmd.com/read/29615643/computational-repositioning-and-preclinical-validation-of-mifepristone-for-human-vestibular-schwannoma
#5
Jessica E Sagers, Adam S Brown, Sasa Vasilijic, Rebecca M Lewis, Mehmet I Sahin, Lukas D Landegger, Roy H Perlis, Isaac S Kohane, D Bradley Welling, Chirag J Patel, Konstantina M Stankovic
The computational repositioning of existing drugs represents an appealing avenue for identifying effective compounds to treat diseases with no FDA-approved pharmacotherapies. Here we present the largest meta-analysis to date of differential gene expression in human vestibular schwannoma (VS), a debilitating intracranial tumor, and use these data to inform the first application of algorithm-based drug repositioning for this tumor class. We apply an open-source computational drug repositioning platform to gene expression data from 80 patient tumors and identify eight promising FDA-approved drugs with potential for repurposing in VS...
April 3, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29603139/a-direct-to-patient-telemedicine-abortion-service-in-australia-retrospective-analysis-of-the-first-18-months
#6
Paul Hyland, Elizabeth G Raymond, Erica Chong
BACKGROUND: In 2015, the Tabbot Foundation launched a nationwide direct-to-patient telemedicine service to enable women to obtain medical abortion without visiting an abortion provider. AIMS: We aimed to describe results from the first 18 months of this service. MATERIALS AND METHODS: To have an abortion through the Foundation, a woman obtained screening tests locally and had a telephone consultation with a Foundation doctor. If she was eligible, mifepristone, misoprostol and other medications were sent to her by mail...
March 30, 2018: Australian & New Zealand Journal of Obstetrics & Gynaecology
https://www.readbyqxmd.com/read/29580890/mifepristone-attenuates-depression-like-changes-induced-by-chronic-central-administration-of-interleukin-1%C3%AE-in-rats
#7
Yong-Ping Zhang, Hao-Yin Wang, Cai Zhang, Bai-Ping Liu, Zhi-Lan Peng, Yu-Yu Li, Cai Song
Increased proinflammatory cytokines, such as interleukin (IL)-1β, may play an important role in the etiology of depression because they cause the hypothalamic-pituitary-adrenal axis to release glucocorticoids (GC) and induce dysfunction of serotonin and norepinephrine neurotransmission. Sustained increase in GC may activate microglia to induce neuroinflammation, and suppress astrocytes to produce neurotrophins, which lead to neuronal apoptosis. Here, we tested the hypothesis that glucocorticoid receptor (GR) antagonist mifepristone (RU486) may attenuate IL-1β-induced depression-like behavior by regulating the neuroinflammation and neurotrophin functions of microglia and astrocytes...
March 23, 2018: Behavioural Brain Research
https://www.readbyqxmd.com/read/29579710/bu-shen-zhu-yun-decoction-promotes-synthesis-and-secretion-of-fsh%C3%AE-and-lh%C3%AE-in-anterior-pituitary-cells-in-vitro
#8
Xiaofei Jiang, Huifang Zhou, Mingqing Shi, Boru Zhou, Bei Liu, Yizhen Yuan, Jinjun Shan, Jianya Xu, Tong Xie
Luteal phase defects (LPD) are an important etiology of infertility which has increased in recent years. Studies have shown that bu-shen-zhu-yun decoction (BSZY-D) can lower the expression of estrogen receptor and progesterone receptor, in rats endometrium of embryonic implantation period, which upregulated by mifepristone, and improve uterine receptivity. The aim of present study was to determine the effect of BSZY-D on the synthesis and secretion of gonadotropic hormones in the anterior pituitary cells of rats...
March 23, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29566059/the-immunological-effect-of-galectin-9-tim-3-pathway-after-low-dose-mifepristone-treatment-in-mice-at-14-5-day-of-pregnancy
#9
Adrienn Lajko, Matyas Meggyes, Beata Polgar, Laszlo Szereday
The abortifacient Mifepristone (RU486) has proven to be a safe, effective, acceptable option for millions of women seeking abortion during the first and second trimester of pregnancy although its precise mechanism of action is not well understood. The main objective of this study was to investigate the impact of low dose Mifepristone administration on placental Galectin-9 (Gal-9) expression, as well as its effect on the cell surface expression of Gal-9, TIM-3 and CD107a molecules by different T and NK cell subsets...
2018: PloS One
https://www.readbyqxmd.com/read/29558845/histopathologic-characterization-of-mifepristone-induced-ovarian-toxicity-in-cynomolgus-monkeys
#10
Yoshikazu Taketa, Kanta Horie, Tetsuya Goto, Etsuko Ohta, Kyoko Nakano-Ito, Kazuhiro Hayakawa, Yuki Seki, Aya Goto, Satoru Hosokawa
Mifepristone, which is an orally active synthetic steroid with antiprogesterone activity, is known as an ovarian toxicant. Because the available data regarding the histopathologic characteristics of ovarian toxicity in nonhuman primates are limited, the present study was undertaken in order to investigate detailed histopathologic changes accompanying mifepristone-induced ovarian toxicity and its relationship to changes in menstrual cycle and circulating sex steroid hormone. Twenty mg/kg of mifepristone was orally administered daily to 4 cynomolgus monkeys for 2 months...
January 1, 2018: Toxicologic Pathology
https://www.readbyqxmd.com/read/29544204/two-synthetic-progestins-and-natural-progesterone-are-responsible-for-most-of-the-progestagenic-activities-in-municipal-wastewater-treatment-plant-effluents-in-the-czech-and-slovak-republics
#11
Pavel Šauer, Alžběta Stará, Oksana Golovko, Olga Valentová, Adam Bořík, Roman Grabic, Hana Kocour Kroupová
Vast numbers of xenobiotics are known still to be present in treated municipal wastewater treatment plant (WWTP) effluents. Some of these possess endocrine-disrupting potency and pose risks for exposed aquatic animals. We searched for 17 potential environmental contaminants having affinity to the progesterone receptor. Relative potency values of these progesterone receptor-active chemicals were obtained. On the basis of relative potencies and measured environmental concentrations, the contribution of progestins to measured progestagenic activities was evaluated...
March 2, 2018: Water Research
https://www.readbyqxmd.com/read/29544105/pharmacokinetic-differences-of-mifepristone-between-sexes-in-animals
#12
Wenge Chen, Yunlong Cheng, Jianzhong Chen, Jiahang Chen, Kai Jiang, Yuyang Zhou, Lee Jia
Mifepristone (RU486) is developed originally as a contraceptive used by hundreds of millions of women world-wide, and also reported as a safe and long-term psychotic depressant, or as a cancer chemotherapeutic agent used by both sexes. In our preliminary study aimed at developing mifepristone as a cancer metastatic chemopreventive, we coincidentally observed that blood mifepristone concentrations in female rats seem to be higher than those in male ones post administration. To substantiate if the pharmacokinetic differences between sexes exist, we established a fast UPLC-MS/MS method to determine mifepristone concentrations in plasma, and analyzed blood concentrations of mifepristone over time in rats and dogs of both sexes...
March 8, 2018: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/29540178/hypothalamus-pituitary-adrenal-axis-involves-in-anti-viral-ability-through-regulation-of-immune-response-in-piglets-infected-by-highly-pathogenic-porcine-reproductive-and-respiratory-syndrome-virus
#13
Jie Tong, Ying Yu, Linlin Zheng, Chong Zhang, Yabin Tu, Yonggang Liu, Jianan Wu, Hai Li, Shujie Wang, Chenggang Jiang, En-Min Zhou, Gang Wang, Xuehui Cai
BACKGROUND: The highly pathogenic porcine reproductive and respiratory syndrome virus (HP-PRRSV) has been responsible for several viral attacks in the Asian porcine industry, since the first outbreak in China in 2006. During the early stages of the HP-PRRSV infection, high levels of proinflammatory cytokines are noted in the host peripheral blood, which are accompanied by severe lesions in the lungs and immune system organs; these are considered as the greatest contributors to the overall disease burden...
March 14, 2018: BMC Veterinary Research
https://www.readbyqxmd.com/read/29534996/low-sensitivity-urine-pregnancy-testing-to-assess-medical-abortion-outcome-a-systematic-review
#14
REVIEW
Elizabeth G Raymond, Tara Shochet, Hillary Bracken
OBJECTIVES: To summarize data on the accuracy and acceptability of a strategy for identifying ongoing pregnancy after medical abortion treatment using a low-sensitivity pregnancy test (LSPT). STUDY DESIGN: We searched PubMed to identify studies that evaluated the use of a single post-treatment LSPT for detection of ongoing pregnancy after treatment with mifepristone and misoprostol. We extracted, assessed, and summarized data from each study. RESULTS: We found 10 studies that evaluated 6 LSPTs with human chorionic gonadotropin detection thresholds of 1000, 1500, or 2000 mIU/ml...
March 10, 2018: Contraception
https://www.readbyqxmd.com/read/29530549/glucocorticoid-receptor-selectively-mediates-stress-induced-suppression-of-innate-immunity-in-the-house-sparrow-passer-domesticus
#15
Sisi Gao, Pierre J Deviche
Stress-induced inhibition of innate immune activity is widespread in free-ranging birds, but the mechanisms that are responsible for this inhibition are poorly understood. We previously demonstrated that an increase in plasma corticosterone (CORT), the primary avian glucocorticoid, is necessary for the inhibition of natural antibody- and complement-mediated as well as bactericidal activities to occur during stress. Here we investigated the role of glucocorticoid receptors in stress-induced inhibition of natural antibody- and complement-mediated activities and bactericidal activity within non-genomic (<10 min) and genomic (<120 min) time frames in male House Sparrows, Passer domesticus...
March 9, 2018: Developmental and Comparative Immunology
https://www.readbyqxmd.com/read/29528933/simultaneous-compared-with-interval-medical-abortion-regimens-where-home-use-is-restricted
#16
Patricia A Lohr, Jennifer E Starling, James G Scott, Abigail R A Aiken
OBJECTIVE: To evaluate outcomes with simultaneous administration of mifepristone and misoprostol for medical abortion at 63 days of gestation or less in the year after its implementation in a British clinic system. METHODS: We conducted a retrospective cohort study using deidentified data from the electronic booking and complications databases and medical records of women who underwent medical abortion at British Pregnancy Advisory Service. Our primary outcome was treatment success with simultaneous dosing compared with a regimen with a 24- to 48-hour interval between medications...
April 2018: Obstetrics and Gynecology
https://www.readbyqxmd.com/read/29523415/combined-analysis-of-mifepristone-for-psychotic-depression-plasma-levels-associated-with-clinical-response
#17
Thaddeus S Block, Harvey Kushner, Ned Kalin, Craig Nelson, Joseph Belanoff, Alan Schatzberg
BACKGROUND: Patients with psychotic depression exhibit elevated cortisol levels. Competitively antagonizing cortisol at the glucocorticoid receptor with mifepristone demonstrated therapeutic benefit in early studies of patients with psychotic depression. We present a combined analysis of all controlled phase 2 and 3 studies to report antipsychotic differences between treatment with mifepristone or placebo and to evaluate the relative contributions to response of attaining an a priori-defined, high mifepristone plasma level and markers of glucocorticoid receptor antagonism (increases in adrenocorticotropin hormone and cortisol) with treatment...
January 31, 2018: Biological Psychiatry
https://www.readbyqxmd.com/read/29510151/comparative-transcriptomeprofiling-and-characterization-of-gene-expression-for-ovarian-differentiation-under-ru486-treatment
#18
Shaohua Sun, Jing Cai, Wenjing Tao, Limin Wu, Chakraborty Tapas, Linyan Zhou, Deshou Wang
17α, 20β-dihydroxypregn-4-en-3-one (17α, 20β-DP, DHP), a teleost specific biologically active progestin, has been proved to play a critical role in oocytes maturation, ovulation and spermiation. RU486 (Mifepristone, an antagonist of progestin receptor) has been applied in contraceptives, abortion and hormone therapy in clinical medicine. To get further insights into the molecular mechanisms of nuclear progestin receptor (Pgr) activated ovarian differentiation and maintenance, we conducted comparative gonadal transcriptome analysis, and investigated histological and transcriptional differences using 4 mah (month after hatching) RU486-treated XX and control XX/XY Nile tilapia (Oreochromis niloticus)...
March 3, 2018: General and Comparative Endocrinology
https://www.readbyqxmd.com/read/29457742/response-to-progesterone-for-preventing-pregnancy-termination-after-initiation-of-medical-abortion-with-mifepristone-what-s-the-real-point-here
#19
Marge Berer
No abstract text is available yet for this article.
February 19, 2018: European Journal of Contraception & Reproductive Health Care
https://www.readbyqxmd.com/read/29453736/reproductive-epidemiology-of-glial-tumors-may-reveal-novel-treatments-high-dose-progestins-or-progesterone-antagonists-as-endocrino-immune-modifiers-against-glioma
#20
REVIEW
Meric A Altinoz, Aysel Ozpinar, Ilhan Elmaci
Female gender, contraceptives, and menopausal hormone replacement treatments containing progesterone analogues associate with higher risk of meningiomas yet with lower risk of gliomas. Progesterone receptor (PR) expression and mifepristone treatment was highly discussed for meningiomas. However, much less is known in regard to progesterone actions in gliomas despite PR expression strongly correlates with their grade. Meningiomas and gliomas may grow faster during gestation; but paradoxically, parousity reduces lifetime risk of gliomas which can be explained with dichotomous cell growth-stimulating and inhibitory actions of progesterone at low versus high levels...
February 17, 2018: Neurosurgical Review
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