Influence of Living in the Same Home on Biomonitored Levels of Consumer
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Characterization of an Abiraterone Ultraresponsive Phenotype in Castration-Resistant
Author Manuscript Published OnlineFirst on December 19, 2016; DOI: 10.1158/1078-0432.CCR-16-2054 Author manuscripts have been peer reviewed and accepted for publication but have not yet been edited. 1 Characterization of an Abiraterone Ultraresponsive Phenotype in Castration-Resistant 2 Prostate Cancer Patient-Derived Xenografts 3 4 Hung-Ming Lam1,2*, Ryan McMullin3*†, Holly M. Nguyen1, Ilsa Coleman4, Michael Gormley5, 5 Roman Gulati4, Lisha G. Brown1, Sarah K. Holt1, Weimin Li5, Deborah S. Ricci6, Karin 6 Verstraeten7, Shibu Thomas5, Elahe A. Mostaghel4, 8, Peter S. Nelson4, 8, Robert L. Vessella1, 7 9, and Eva Corey1 8 9 Affiliation of authors: 1Department of Urology, University of Washington School of 10 Medicine, Seattle, Washington; 2State Key Laboratory of Quality Research in Chinese 11 Medicine, Macau Institute for Applied Research in Medicine and Health, Macau University of 12 Science and Technology, Macau (SAR), China; 3LabConnect, Seattle, Washington; 4Fred 13 Hutchinson Cancer Research Center, Seattle, Washington; 5Janssen Research & 14 Development, Spring House, Pennsylvania; 6Janssen Research & Development, Raritan, 15 New Jersey; 7Janssen Research & Development, Beerse, Belgium; 8Department of 16 Medicine, University of Washington, Seattle, Washington; 9Department of Veterans Affairs 17 Medical Center, Seattle, Washington 18 19 *Co-primary lead authors 20 †Current affiliation: Janssen Research & Development, Spring House, Pennsylvania 21 22 23 Running title (60 characters max): Abiraterone Response and Resistance 24 25 Keywords: abiraterone acetate, prostate cancer, xenografts, biomarkers, androgen 26 receptor, glucocorticoid receptor, castration resistance 27 28 Grant/funding support: The work was supported by The Richard M. Lucas Foundation, the 29 Prostate Cancer Foundation, SU2C, a NIH PO1 CA085859, and the PNW Prostate Cancer 1 Downloaded from clincancerres.aacrjournals.org on September 23, 2021. -
Parabens Preservatives for Focused Protection
PARABENS Preservatives For Focused Protection Parabens are the most commonly used preservatives in personal care products. Parabens display a low irritation potential, have low toxicity levels, and are active against a wide spectrum of fungi and bacteria at low concentrations. They are stable and effective over a wide pH range, can withstand temperatures up to 100°C, and are biodegradable. Also, they are highly compatible with other compounds. When combining two or more Parabens, their antimicrobial performance is enhanced due to a synergistic effect. While this is not a complete listing of Paraben features, it is clear why they are such an effective preservative and so commonly used. MINIMUM INHIBITION CONCENTRATIONS (MIC) FOR PARABENS Microorganism Methyl Ethyl Propyl Butyl Aspergillus niger 600 300 300 200 Candida albicans 900 500 200 100 Pseudomonas aeruginosa 1600 1500 >900 - Bacillus cereus 1600 800 300 100 Burkholderia cepacia 600 350 200 200 Escherichia coli 1400 700 350 140 INCI CAS Staphylococcus epidermidis 2000 900 350 150 Methylparaben 99-76-3 Staphylococcus aureus 2000 1000 300 110 Ethylparaben 120-47-8 Propylparaben 94-13-3 All the Parabens have low aqueous solubility, but will dissolve in most systems Butylparaben 94-26-6 at temperatures above 60°C. When considering the solubility of Parabens, we recommend dissolving short-chained Parabens (such as Methylparaben) Appearance in the aqueous phase and longer-chained Parabens in the oil phase. If all the White, dry powder Parabens must be introduced to the water phase, pre-heating of the water is recommended. In the event that heating is undesirable, we recommend using Solubility Paraben sodium salts. -
01 Excipients Prelims 1..9
Ethylparaben 1 Nonproprietary Names BP: Ethyl Hydroxybenzoate SEM 1: Excipient: ethylparaben; magnification: 600Â. JP: Ethyl Parahydroxybenzoate PhEur: Ethyl Parahydroxybenzoate E USP-NF: Ethylparaben 2 Synonyms Aethylum hydrobenzoicum; CoSept E; E214; ethylis parahydroxy- benzoas; ethyl p-hydroxybenzoate; Ethyl parasept; 4-hydroxyben- zoic acid ethyl ester; Nipagin A; Solbrol A; Tegosept E; Uniphen P- 23. 3 Chemical Name and CAS Registry Number Ethyl-4-hydroxybenzoate [120-47-8] 4 Empirical Formula and Molecular Weight C9H10O3 166.18 5 Structural Formula SEM 2: Excipient: ethylparaben; magnification: 3000Â. 6 Functional Category Antimicrobial preservative. 7 Applications in Pharmaceutical Formulation or Technology Ethylparaben is widely used as an antimicrobial preservative in cosmetics,(1) food products, and pharmaceutical formulations. It may be used either alone or in combination with other paraben esters or with other antimicrobial agents. In cosmetics it is one of the most frequently used preservatives. The parabens are effective over a wide pH range and have a broad spectrum of antimicrobial activity, although they are most effective against yeasts and molds; see Section 10. Owing to the poor solubility of the parabens, paraben salts, particularly the sodium salt, are frequently used. However, this may cause the pH of poorly buffered formulations to become more alkaline. See Methylparaben for further information. 8 Description Ethylparaben occurs as a white, odorless or almost odorless, active against yeasts and molds than against bacteria. They crystalline powder. are also more active against Gram-positive than against Gram-negative bacteria. 9 Pharmacopeial Specifications The activity of the parabens increases with increasing chain See Table I. See also Section 18. length of the alkyl moiety, but solubility decreases. -
Pesticides Reduce Symbiotic Efficiency of Nitrogen-Fixing Rhizobia and Host Plants
Pesticides reduce symbiotic efficiency of nitrogen-fixing rhizobia and host plants Jennifer E. Fox*†, Jay Gulledge‡, Erika Engelhaupt§, Matthew E. Burow†¶, and John A. McLachlan†ʈ *Center for Ecology and Evolutionary Biology, University of Oregon, 335 Pacific Hall, Eugene, OR 97403; †Center for Bioenvironmental Research, Environmental Endocrinology Laboratory, Tulane University, 1430 Tulane Avenue, New Orleans, LA 70112-2699; ‡Department of Biology, University of Louisville, Louisville, KY 40292 ; §University of Colorado, Boulder, CO 80309; and ¶Department of Medicine and Surgery, Hematology and Medical Oncology Section, Tulane University Medical School, 1430 Tulane Avenue, New Orleans, LA 70112-2699 Edited by Christopher B. Field, Carnegie Institution of Washington, Stanford, CA, and approved May 8, 2007 (received for review January 8, 2007) Unprecedented agricultural intensification and increased crop by plants, in rotation with non-N-fixing crops (8, 15). The yield will be necessary to feed the burgeoning world population, effectiveness of this strategy relies on maximizing symbiotic N whose global food demand is projected to double in the next 50 fixation (SNF) and plant yield to resupply organic and inorganic years. Although grain production has doubled in the past four N and nutrients to the soil. The vast majority of biologically fixed decades, largely because of the widespread use of synthetic N is attributable to symbioses between leguminous plants (soy- nitrogenous fertilizers, pesticides, and irrigation promoted by the bean, alfalfa, etc.) and species of Rhizobium bacteria; replacing ‘‘Green Revolution,’’ this rate of increased agricultural output is this natural fertilizer source with synthetic N fertilizer would cost unsustainable because of declining crop yields and environmental Ϸ$10 billion annually (16, 17). -
Triclosan Disrupts Thyroid Hormones: Mode-Of-Action, Developmental Susceptibility, and Determination of Human Relevance
Triclosan Disrupts Thyroid Hormones: Mode-of-Action, Developmental Susceptibility, and Determination of Human Relevance Katie Beth Paul “A dissertation submitted to the faculty of the University of North Carolina at Chapel Hill in partial fulfillment of the requirements for the degree of Doctor of Philosophy in the Curriculum of Toxicology.” Chapel Hill 2011 Approved by: Kim L. R. Brouwer, Pharm.D., Ph.D. Kevin M. Crofton, Ph.D. Michael J. DeVito, Ph.D. Philip C. Smith, Ph.D James A. Swenberg, D.V.M., Ph.D. ©2011 Katie Beth Paul ALL RIGHTS RESERVED ii Abstract Katie Beth Paul Triclosan Disrupts Thyroid Hormones: Mode-of-Action, Developmental Susceptibility, and Determination of Human Relevance (Under the direction of Kevin M. Crofton, Ph.D.) Preliminary study demonstrated that triclosan (TCS), a bacteriostat in myriad consumer products, decreases serum thyroxine (T4) in rats. Adverse neurodevelopmental consequences result from thyroid hormone (TH) disruption; therefore determination of whether TCS disrupts THs during development, its mode-of-action (MOA), and the human relevance is critical. This research tested the hypothesis that TCS disrupts THs via activation of pregnane X and constitutive androstane receptors (PXR, CAR), mediating Phase I-II enzyme and hepatic transporter expression and protein changes, thereby increasing catabolism and elimination of THs, resulting in decreased TH concentrations. For Aim One, the hypothesized MOA was assessed using weanling female Long-Evans rats orally exposed to TCS (0-1000 mg/kg/day) for four days. Serum T4 decreased 35% at 300 mg/kg/day. Activity and expression of markers of Phase I (Cyp2b, Cyp3a1) and Phase II (Ugt1a1, Sult1c1) metabolism were moderately induced, consistent with PXR and/or CAR activation and increased hepatic catabolism. -
Pharmaceuticals and Endocrine Active Chemicals in Minnesota Lakes
Pharmaceuticals and Endocrine Active Chemicals in Minnesota Lakes May 2013 Authors Mark Ferrey Contributors/acknowledgements The MPCA is reducing printing and mailing costs This report contains the results of a study that by using the Internet to distribute reports and characterizes the presence of unregulated information to wider audience. Visit our website contaminants in Minnesota’s lakes. The study for more information. was made possible through funding by the MPCA reports are printed on 100 percent post- Minnesota Clean Water Fund and by funding by consumer recycled content paper manufactured the U.S. Environmental Protection Agency without chlorine or chlorine derivatives. (EPA), which facilitated the sampling of lakes for this study. The Minnesota Pollution Control Agency (MPCA) thanks the following for assistance and advice in designing and carrying out this study: Steve Heiskary, Pam Anderson, Dereck Richter, Lee Engel, Amy Garcia, Will Long, Jesse Anderson, Ben Larson, and Kelly O’Hara for the long hours of sampling for this study. Cynthia Tomey, Kirsten Anderson, and Richard Grace of Axys Analytical Labs for the expert help in developing the list of analytes for this study and logistics to make it a success. Minnesota Pollution Control Agency 520 Lafayette Road North | Saint Paul, MN 55155-4194 | www.pca.state.mn.us | 651-296-6300 Toll free 800-657-3864 | TTY 651-282-5332 This report is available in alternative formats upon request, and online at www.pca.state.mn.us. Document number: tdr-g1-16 Contents Contents ........................................................................................................................................... -
Polystyrene Microplastics Do Not Affect Juvenile Brown Trout (Salmo Trutta F
Schmieg et al. Environ Sci Eur (2020) 32:49 https://doi.org/10.1186/s12302-020-00327-4 RESEARCH Open Access Polystyrene microplastics do not afect juvenile brown trout (Salmo trutta f. fario) or modulate efects of the pesticide methiocarb Hannah Schmieg1*, Sven Huppertsberg2, Thomas P. Knepper2, Stefanie Krais1, Katharina Reitter1, Felizitas Rezbach1, Aki S. Ruhl3,4, Heinz‑R. Köhler1 and Rita Triebskorn1,5 Abstract Background: There has been a rising interest within the scientifc community and the public about the environmen‑ tal risk related to the abundance of microplastics in aquatic environments. Up to now, however, scientifc knowledge in this context has been scarce and insufcient for a reliable risk assessment. To remedy this scarcity of data, we inves‑ tigated possible adverse efects of polystyrene particles (10 4 particles/L) and the pesticide methiocarb (1 mg/L) in juvenile brown trout (Salmo trutta f. fario) both by themselves as well as in combination after a 96 h laboratory expo‑ sure. PS beads (density 1.05 g/mL) were cryogenically milled and fractionated resulting in irregular‑shaped particles (< 50 µm). Besides body weight of the animals, biomarkers for proteotoxicity (stress protein family Hsp70), oxidative stress (superoxide dismutase, lipid peroxidation), and neurotoxicity (acetylcholinesterase, carboxylesterases) were analyzed. As an indicator of overall health, histopathological efects were studied in liver and gills of exposed fsh. Results: Polystyrene particles by themselves did not infuence any of the investigated biomarkers. In contrast, the exposure to methiocarb led to a signifcant reduction of the activity of acetylcholinesterase and the two carboxy‑ lesterases. Moreover, the tissue integrity of liver and gills was impaired by the pesticide. -
Effect of Antimicrobial Triclosan on Reproductive System of Male
A tica nal eu yt c ic a a m A r a c t h a P Ibtisham et al., Pharm Anal Acta 2016, 7:11 Pharmaceutica Analytica Acta DOI: 10.4172/2153-2435.1000516 ISSN: 2153-2435 Review Article Open Access Effect of Antimicrobial Triclosan on Reproductive System of Male Rat Fahar Ibtisham, Aamir Nawab, Yi Zhao, Guanghui Li, Mei Xiao and Lilong An* Agricultural Collage, Guangdong Ocean University, Zhanjiang, Guangdong, China *Corresponding author; Lilong An, Agricultural Collage, Guangdong Ocean University, Haida Road, Mazhang District, Zhanjiang 524088, Guangdong, China, Tel: +86-759-2383247; E-mail: [email protected] Received date: October 31, 2016; Accepted date: November 26, 2016; Published date: November 28, 2016 Copyright: © 2016 Ibtisham F, et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited. Abstract Triclosan (5-chloro-2-(2,4-dichlorophenoxy)phenol: TCS) is a synthetic, broad-spectrum antibacterial agent used in broad range of household and personal care products including hand soap, toothpaste, and deodorants. Recently, concerns have been raised over TCS’s potential for endocrine and reproductive disruption. This review contains the information about deleterious toxic effects of TCS on reproductive system of male rat and the possible mechanism. The literature findings showed that TCS deadly affects the reproductive profile of male rats. According to literature TCS depress the testicular function of male rat including spermatogenesis and steroidogenesis by decreasing the androgen production. 3-hydroxysteroid dehydrogenase (3β-HSD) and 17β-hydroxysteroid dehydrogenase (17β- HSD) are two critical enzymes in the steroidogenesis pathway, while according to findings TCS treated rats had lowered concentration of androgen. -
Estrogen-Like Effect of Mitotane Explained by Its Agonist Activity on Estrogen Receptor-Α
biomedicines Article Estrogen-Like Effect of Mitotane Explained by Its Agonist Activity on Estrogen Receptor-α Elisa Rossini 1,†, Edoardo Giacopuzzi 2,3,† , Fabrizio Gangemi 4,† , Mariangela Tamburello 1, Deborah Cosentini 5, Andrea Abate 1, Marta Laganà 5, Alfredo Berruti 5 , Salvatore Grisanti 5,‡ and Sandra Sigala 1,*,‡ 1 Section of Pharmacology, Department of Molecular and Translational Medicine, University of Brescia, 25123 Brescia, Italy; [email protected] (E.R.); [email protected] (M.T.); [email protected] (A.A.) 2 Wellcome Centre for Human Genetics, University of Oxford, Oxford OX3 7BN, UK; [email protected] 3 National Institute for Health Research Oxford Biomedical Research Centre, Oxford OX4 2PG, UK 4 Unit of Physics, Department of Molecular and Translational Medicine, University of Brescia, 25123 Brescia, Italy; [email protected] 5 Medical Oncology Unit, Department of Medical and Surgical Specialties, Radiological Sciences, and Public Health, University of Brescia at A.S.S.T. Spedali Civili di Brescia, 25123 Brescia, Italy; [email protected] (D.C.); [email protected] (M.L.); [email protected] (A.B.); [email protected] (S.G.) * Correspondence: [email protected] † These Authors equally contributed to this paper. ‡ These authors are co-senior authors of this paper. Citation: Rossini, E.; Giacopuzzi, E.; Abstract: Mitotane is the cornerstone of medical treatment of adrenocortical carcinoma. Estrogenic- Gangemi, F.; Tamburello, M.; like side effects frequently occur in patients, and previous studies explored the chemical nature Cosentini, D.; Abate, A.; Laganà, M.; of the interaction between estrogen receptor-α (ER-α) and toxic compounds, including the DDD Berruti, A.; Grisanti, S.; Sigala, S. -
Identification of Methyl Triclosan and Halogenated Analogues
SCIENCE OF THE TOTAL ENVIRONMENT 407 (2009) 2102– 2114 available at www.sciencedirect.com www.elsevier.com/locate/scitotenv Identification of methyl triclosan and halogenated analogues in male common carp (Cyprinus carpio) from Las Vegas Bay and semipermeable membrane devices from Las Vegas Wash, Nevada Thomas J. Leikera,1, Sonja R. Abneya, Steven L. Goodbredb, Michael R. Rosenc,⁎ aUS Geological Survey, Box 25046, MS 407, Denver, CO 80225-0046, USA bUS Geological Survey, California State University, Modoc Hall, 3020 State University Drive East, Suite 3005, Sacramento, CA 95819-6129, USA cUS Geological Survey, 2730 North Deer Run Road, Carson City NV, 89701, USA ARTICLE DATA ABSTRACT Article history: Methyl triclosan and four halogenated analogues have been identified in extracts of individual Received 22 August 2008 whole-body male carp (Cyprinus carpio) tissue that were collected from Las Vegas Bay, Nevada, Received in revised form and Semipermeable Membrane Devices (SPMD) that were deployed in Las Vegas Wash, Nevada. 3 November 2008 Methyl triclosan is believed to be the microbially methylated product of the antibacterial agent Accepted 9 November 2008 triclosan (2, 4, 4'-trichloro-4-hydroxydiphenyl ether, Chemical Abstract Service Registry Number Available online 2 December 2008 3380-34-5, Irgasan DP300). The presence of methyl triclosan and four halogenated analogues was confirmed in SPMD extracts by comparing low- and high-resolution mass spectral data and Keywords: Kovats retention indices of methyl triclosan with commercially obtained triclosan that was Triclosan derivatized to the methyl ether with ethereal diazomethane. The four halogenated analogues of Methyl triclosan methyltriclosandetectedinbothwhole-body tissue and SPMD extracts were tentatively Common carp identified by high resolution mass spectrometry. -
Conjugate and Prodrug Strategies As Targeted Delivery Vectors for Antibiotics † † ‡ Ana V
Review Cite This: ACS Infect. Dis. XXXX, XXX, XXX−XXX pubs.acs.org/journal/aidcbc Signed, Sealed, Delivered: Conjugate and Prodrug Strategies as Targeted Delivery Vectors for Antibiotics † † ‡ Ana V. Cheng and William M. Wuest*, , † Department of Chemistry, Emory University, 1515 Dickey Drive, Atlanta, Georgia 30322, United States ‡ Emory Antibiotic Resistance Center, Emory School of Medicine, 201 Dowman Drive, Atlanta, Georgia 30322, United States ABSTRACT: Innate and developed resistance mechanisms of bacteria to antibiotics are obstacles in the design of novel drugs. However, antibacterial prodrugs and conjugates have shown promise in circumventing resistance and tolerance mechanisms via directed delivery of antibiotics to the site of infection or to specific species or strains of bacteria. The selective targeting and increased permeability and accumu- lation of these prodrugs not only improves efficacy over unmodified drugs but also reduces off-target effects, toxicity, and development of resistance. Herein, we discuss some of these methods, including sideromycins, antibody-directed prodrugs, cell penetrating peptide conjugates, and codrugs. KEYWORDS: oligopeptide, sideromycin, antibody−antibiotic conjugate, cell penetrating peptide, dendrimer, transferrin inding new and innovative methods to treat bacterial F infections comes with many inherent challenges in addition to those presented by the evolution of resistance mechanisms. The ideal antibiotic is nontoxic to host cells, permeates bacterial cells easily, and accumulates at the site of infection at high concentrations. Narrow spectrum drugs are also advantageous, as they can limit resistance development and leave the host commensal microbiome undisturbed.1 However, various resistance mechanisms make pathogenic infections difficult to eradicate: Many bacteria respond to antibiotic pressure by decreasing expression of active transporters and porins2 and 3,4 Downloaded via EMORY UNIV on April 18, 2019 at 12:34:17 (UTC). -
Abiraterone and MDV3100 Inhibits the Proliferation and Promotes The
Han et al. Cancer Cell Int (2019) 19:332 https://doi.org/10.1186/s12935-019-1021-9 Cancer Cell International PRIMARY RESEARCH Open Access Abiraterone and MDV3100 inhibits the proliferation and promotes the apoptosis of prostate cancer cells through mitophagy Jingli Han1† , Junhua Zhang1†, Wei Zhang2, Dalei Zhang3, Ying Li1, Jinsong Zhang2, Yaqun Zhang3, Tongxiang Diao3, Luwei Cui3, Wenqing Li1, Fei Xiao1,2,4, Ming Liu3* and Lihui Zou1* Abstract Background: Abiraterone and MDV3100 are two efective anticancer agents for prostate cancer, however, the mechanism of their downstream action remains undefned. Methods: A dual fuorescent biosensor plasmid was transfected in LNCaP cells to measure mitophagy. The DNA of LNCaP cells was extracted and performed with quantitative real-time PCR to detect mitochondrial DNA copy number. JC-1 staining was utilized to detect the mitochondrial membrane potential and electron microscope was performed to analyze mitochondrial morphology. Moreover, the protein levels of mitochondrial markers and apoptotic markers were detected by western blot. At last, the proliferation and apoptosis of LNCaP cells were analyzed with CCK-8 assay and fow cytometry after abiraterone or MDV3100 treatment. Results: Mitophagy was induced by abiraterone and MDV3100 in LNCaP cells. The low expression level of mito- chondrial DNA copy number and mitochondrial depolarization were further identifed in the abiraterone or MDV3100 treatment groups compared with the control group. Besides, severe mitochondria swelling and substantial autophagy-lysosomes were observed in abiraterone- and MDV3100-treated LNCaP cells. The expression of mito- chondria-related proteins, frataxin, ACO2 and Tom20 were signifcantly downregulated in abiraterone and MDV3100 treated LNCaP cells, whereas the expression level of inner membrane protein of mitochondria (Tim23) was signif- cantly upregulated in the same condition.