Acute Exposure Guideline Levels for Selected Airborne Chemicals: Volume 15
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Transient Receptor Potential Channel Promiscuity Frustrates Constellation
the sole sensor responsible for noxious cold responses in M+A+ LETTER neurons (1). However, TRPA1 is also activated by cooling and underlies at least part of the noxious cold responsiveness of Transient receptor potential channel AITC-sensitive neurons (3). Third, the authors used nicardipine 2+ promiscuity frustrates to selectively inhibit CaV1-type voltage-gated Ca channels (1). However, several dihydropyridines, including nicardipine, also constellation pharmacology act as TRPA1 agonists (4). These considerations led us to propose an alternative Sensory neurons from the trigeminal and dorsal root ganglia molecular interpretation of the difference between M+A− (DRG) have nerve endings in the skin and mucosa, where they and M+A+ neurons, which is in much better agreement with detect environmental stimuli and convey this information to published work. In accord with the authors, we conclude that the central nervous system. Several members of the transient M+A− neurons express TRPM8 but lack expression of receptor potential (TRP) superfamily of ion channels act as TRPA1. In contrast to the authors, we propose that M+A+ prime molecular sensors for thermal and chemical stimuli in neurons express TRPA1 as the prime cold and menthol these sensory neurons. However, it is incompletely understood sensor (2, 3). This interpretation is consistent with published how TRP channel expression and modulation affect the stimulus observations that menthol responses in M+A− but not in sensitivities of distinct neuronal subtypes. M+A+ neurons are inhibited by TRPM8 antagonists (5) In a recent article, Teichert et al. (1) described a “constellation and that TRPA1-mediated responses to cold in neurons are pharmacology approach” to identify and characterize subtypes characterized by a higher (colder) threshold (3). -
Chapter Four – TRPA1 Channels: Chemical and Temperature Sensitivity
CHAPTER FOUR TRPA1 Channels: Chemical and Temperature Sensitivity Willem J. Laursen1,2, Sviatoslav N. Bagriantsev1,* and Elena O. Gracheva1,2,* 1Department of Cellular and Molecular Physiology, Yale University School of Medicine, New Haven, CT, USA 2Program in Cellular Neuroscience, Neurodegeneration and Repair, Yale University School of Medicine, New Haven, CT, USA *Corresponding author: E-mail: [email protected], [email protected] Contents 1. Introduction 90 2. Activation and Regulation of TRPA1 by Chemical Compounds 91 2.1 Chemical activation of TRPA1 by covalent modification 91 2.2 Noncovalent activation of TRPA1 97 2.3 Receptor-operated activation of TRPA1 99 3. Temperature Sensitivity of TRPA1 101 3.1 TRPA1 in mammals 101 3.2 TRPA1 in insects and worms 103 3.3 TRPA1 in fish, birds, reptiles, and amphibians 103 3.4 TRPA1: Molecular mechanism of temperature sensitivity 104 Acknowledgments 107 References 107 Abstract Transient receptor potential ankyrin 1 (TRPA1) is a polymodal excitatory ion channel found in sensory neurons of different organisms, ranging from worms to humans. Since its discovery as an uncharacterized transmembrane protein in human fibroblasts, TRPA1 has become one of the most intensively studied ion channels. Its function has been linked to regulation of heat and cold perception, mechanosensitivity, hearing, inflam- mation, pain, circadian rhythms, chemoreception, and other processes. Some of these proposed functions remain controversial, while others have gathered considerable experimental support. A truly polymodal ion channel, TRPA1 is activated by various stimuli, including electrophilic chemicals, oxygen, temperature, and mechanical force, yet the molecular mechanism of TRPA1 gating remains obscure. In this review, we discuss recent advances in the understanding of TRPA1 physiology, pharmacology, and molecular function. -
Effect of Capsaicin and Other Thermo-TRP Agonists on Thermoregulatory Processes in the American Cockroach
Article Effect of Capsaicin and Other Thermo-TRP Agonists on Thermoregulatory Processes in the American Cockroach Justyna Maliszewska 1,*, Milena Jankowska 2, Hanna Kletkiewicz 1, Maria Stankiewicz 2 and Justyna Rogalska 1 1 Department of Animal Physiology, Faculty of Biology and Environmental Protection, Nicolaus Copernicus University, 87-100 Toruń, Poland; [email protected] (H.K.); [email protected] (J.R.) 2 Department of Biophysics, Faculty of Biology and Environmental Protection, Nicolaus Copernicus University, 87-100 Toruń, Poland; [email protected] (M.J.); [email protected] (M.S.) * Correspondence: [email protected]; Tel.: +48-56611-44-63 Academic Editor: Pin Ju Chueh Received: 5 November 2018; Accepted: 17 December 2018; Published: 18 December 2018 Abstract: Capsaicin is known to activate heat receptor TRPV1 and induce changes in thermoregulatory processes of mammals. However, the mechanism by which capsaicin induces thermoregulatory responses in invertebrates is unknown. Insect thermoreceptors belong to the TRP receptors family, and are known to be activated not only by temperature, but also by other stimuli. In the following study, we evaluated the effects of different ligands that have been shown to activate (allyl isothiocyanate) or inhibit (camphor) heat receptors, as well as, activate (camphor) or inhibit (menthol and thymol) cold receptors in insects. Moreover, we decided to determine the effect of agonist (capsaicin) and antagonist (capsazepine) of mammalian heat receptor on the American cockroach’s thermoregulatory processes. We observed that capsaicin induced the decrease of the head temperature of immobilized cockroaches. Moreover, the examined ligands induced preference for colder environments, when insects were allowed to choose the ambient temperature. -
Selected Kefir Water from Malaysia Attenuates Hydrogen Peroxide
antioxidants Article Selected Kefir Water from Malaysia Attenuates Hydrogen Peroxide-Induced Oxidative Stress by Upregulating Endogenous Antioxidant Levels in SH-SY5Y Neuroblastoma Cells Muganti Rajah Kumar 1, Swee Keong Yeap 2, Han Chung Lee 2, Nurul Elyani Mohamad 1,3 , Muhammad Nazirul Mubin Aziz 1, Melati Khalid 4, Mas Jaffri Masarudin 1,5 , Adam Thean Chor Leow 1 , Janna Ong Abdullah 1 and Noorjahan Banu Alitheen 1,5,* 1 Department of Cell and Molecular Biology, Faculty of Biotechnology and Biomolecular Sciences, Universiti Putra Malaysia, Serdang 43400 UPM, Selangor Darul Ehsan, Malaysia; [email protected] (M.R.K.); [email protected] (N.E.M.); [email protected] (M.N.M.A.); [email protected] (M.J.M.); [email protected] (A.T.C.L.); [email protected] (J.O.A.) 2 China-ASEAN College of Marine Sciences, Xiamen University Malaysia, Sepang 43900, Selangor Darul Ehsan, Malaysia; [email protected] (S.K.Y.); [email protected] (H.C.L.) 3 Biotechnology Research Institute, Universiti Malaysia Sabah, Kota Kinabalu 88400, Sabah, Malaysia Citation: Kumar, M.R.; Yeap, S.K.; 4 Department of Biomedical Sciences, Faculty of Medicine and Health Sciences, Universiti Putra Malaysia, Lee, H.C.; Mohamad, N.E.; Nazirul Serdang 43400 UPM, Selangor Darul Ehsan, Malaysia; [email protected] Mubin Aziz, M.; Khalid, M.; 5 UPM-MAKNA Cancer Research Laboratory, Institute of Bioscience, Universiti Putra Malaysia, Masarudin, M.J.; Leow, A.T.C.; Serdang 43400 UPM, Selangor Darul Ehsan, Malaysia Abdullah, J.O.; Alitheen, N.B. * Correspondence: [email protected]; Tel.: +603-976-97471 Selected Kefir Water from Malaysia Attenuates Hydrogen Abstract: Kefir, a fermented probiotic drink was tested for its potential anti-oxidative, anti-apoptotic, Peroxide-Induced Oxidative Stress by and neuroprotective effects to attenuate cellular oxidative stress on human SH-SY5Y neuroblastoma Upregulating Endogenous cells. -
Soil Mobility of Allyl Isothiocyanate and Chloropicrin As Influenced By
HORTSCIENCE 54(4):706–714. 2019. https://doi.org/10.21273/HORTSCI13836-18 and some soil arthropods, but it provides little control of fungi and weeds, whereas Met-Na controls weeds, nematodes, and some fungi. CP Soil Mobility of Allyl Isothiocyanate controls insects and fungi, but it has less activity against nematodes and weeds (Ajwa and Trout, and Chloropicrin as Influenced by 2004). The most promising MeBr alternatives are chloropicrin and Met-Na (Gao et al., 2012; Surfactants and Soil Texture Jacoby, 2016; Klose et al., 2008; Yates et al., 2002); therefore, more than 7000 tons of chlo- Feras Almasri ropicrin were used in 2011 (Nelson et al., 2013) Department of Plant Sciences, University of California at Davis, Davis, CA in California. 95616 Although Met-Na is an effective fumigant (Nelson et al., 2002), the use of Met-Na is Husein A. Ajwa strongly regulated due to the excessive soil fu- Department of Plant Sciences, University of California at Davis, 1636 East migant release into the atmosphere (Goodhue et al., 2016; Saeed et al., 1997). Because of Alisal Street, Salinas, CA 93905 this excessive release into the atmosphere, Sanjai J. Parikh Met-Na, Met-K, and DMTT labels require wide buffer zones and specific measures to University of California at Davis, Department of Land, Air and Water protect people from off-target movement Resources, Davis, CA 95616 (Guthman and Brown, 2016). Furthermore, 1 Met-Na, Met-K, and DMTT degrade in soil Kassim Al-Khatib to MITC, which is classified as a toxicity I Department of Plant Sciences, University of California at Davis, Davis, CA category pesticide (Gao et al., 2012; Klose 95616 et al., 2008). -
Isothiocyanates; Sources, Physiological Functions and Food Applications
1 Plant Archives Vol. 20, Supplement 2, 2020 pp. 2758-2763 e-ISSN:2581-6063 (online), ISSN:0972-5210 ISOTHIOCYANATES; SOURCES, PHYSIOLOGICAL FUNCTIONS AND FOOD APPLICATIONS Mudasir Yaqoob* 1,2 , Poonam Aggarwal 2, Mukul Kumar 1, Neha Purandare 1 1Department of Food Technology and Nutrition, Lovely professional University Phagwara India 2Department of Food Science &Technology Punjab agriculture University Ludhiana Email: [email protected] Abstract Foods are complex mixture of major and minor nutrients. They also contain some non-nutrient mixtures which exert beneficial effects to the human body known as phytochemicals. Phytochemicals are the chemical compounds that are synthesised by the plant cells to fight any kind of stress conditions. Isothiocyanates (ITCs) are the secondary metabolites produced by the plant from the enzymatic hydrolysis of glucosinolates by myrosinase during the plant tissue injury. They are present in Cruciferous vegetables, such as cabbage, broccoli and kale and are sulphur rich compounds. Isothiocyanates have been found to play an important role for the plant against microbial and pest infections. ITCs have been found to have beneficial activities like antibacterial, antifungal, bioherbicidal, and antioxidant, biopesticidal, anticarcinogenic and antimutagenic. Due to these activities they are having applications in food preservation like fruit juices and as an additive in Mayonnaise. Their recent application has been in the food packing’s and in MAP. The present review gives the insight of these phytochemicals, their physiological functions and food applications Keywords : Isothiocyanates, glucosionolate, sources, biocidal, food applications. Introduction in the vapour phase (Isshiki et al., 1992) and due to this characteristic property, it has been able to be used as food Isothiocyanates are the type of phytochemicals that are preservative in a number of foods stuffs. -
Isothiocyanates from Cruciferous Vegetables
Isothiocyanates from Cruciferous Vegetables: Kinetics, Biomarkers and Effects Martijn Vermeulen Promotoren Prof. dr. Peter J. van Bladeren Hoogleraar Toxicokinetiek en Biotransformatie, leerstoelgroep Toxicologie, Wageningen Universiteit Prof. dr. ir. Ivonne M.C.M. Rietjens Hoogleraar Toxicologie, Wageningen Universiteit Copromotor Dr. Wouter H.J. Vaes Productmanager Nutriënten en Biomarker analyse, TNO Kwaliteit van Leven, Zeist Promotiecommissie Prof. dr. Aalt Bast Universiteit Maastricht Prof. dr. ir. M.A.J.S. (Tiny) van Boekel Wageningen Universiteit Prof. dr. Renger Witkamp Wageningen Universiteit Prof. dr. Ruud A. Woutersen Wageningen Universiteit / TNO, Zeist Dit onderzoek is uitgevoerd binnen de onderzoeksschool VLAG (Voeding, Levensmiddelen- technologie, Agrobiotechnologie en Gezondheid) Isothiocyanates from Cruciferous Vegetables: Kinetics, Biomarkers and Effects Martijn Vermeulen Proefschrift ter verkrijging van de graad van doctor op gezag van de rector magnificus van Wageningen Universiteit, prof. dr. M.J. Kropff, in het openbaar te verdedigen op vrijdag 13 februari 2009 des namiddags te half twee in de Aula. Title Isothiocyanates from cruciferous vegetables: kinetics, biomarkers and effects Author Martijn Vermeulen Thesis Wageningen University, Wageningen, The Netherlands (2009) with abstract-with references-with summary in Dutch ISBN 978-90-8585-312-1 ABSTRACT Cruciferous vegetables like cabbages, broccoli, mustard and cress, have been reported to be beneficial for human health. They contain glucosinolates, which are hydrolysed into isothiocyanates that have shown anticarcinogenic properties in animal experiments. To study the bioavailability, kinetics and effects of isothiocyanates from cruciferous vegetables, biomarkers of exposure and for selected beneficial effects were developed and validated. As a biomarker for intake and bioavailability, isothiocyanate mercapturic acids were chemically synthesised as reference compounds and a method for their quantification in urine was developed. -
Patent Application Publication ( 10 ) Pub . No . : US 2019 / 0192440 A1
US 20190192440A1 (19 ) United States (12 ) Patent Application Publication ( 10) Pub . No. : US 2019 /0192440 A1 LI (43 ) Pub . Date : Jun . 27 , 2019 ( 54 ) ORAL DRUG DOSAGE FORM COMPRISING Publication Classification DRUG IN THE FORM OF NANOPARTICLES (51 ) Int . CI. A61K 9 / 20 (2006 .01 ) ( 71 ) Applicant: Triastek , Inc. , Nanjing ( CN ) A61K 9 /00 ( 2006 . 01) A61K 31/ 192 ( 2006 .01 ) (72 ) Inventor : Xiaoling LI , Dublin , CA (US ) A61K 9 / 24 ( 2006 .01 ) ( 52 ) U . S . CI. ( 21 ) Appl. No. : 16 /289 ,499 CPC . .. .. A61K 9 /2031 (2013 . 01 ) ; A61K 9 /0065 ( 22 ) Filed : Feb . 28 , 2019 (2013 .01 ) ; A61K 9 / 209 ( 2013 .01 ) ; A61K 9 /2027 ( 2013 .01 ) ; A61K 31/ 192 ( 2013. 01 ) ; Related U . S . Application Data A61K 9 /2072 ( 2013 .01 ) (63 ) Continuation of application No. 16 /028 ,305 , filed on Jul. 5 , 2018 , now Pat . No . 10 , 258 ,575 , which is a (57 ) ABSTRACT continuation of application No . 15 / 173 ,596 , filed on The present disclosure provides a stable solid pharmaceuti Jun . 3 , 2016 . cal dosage form for oral administration . The dosage form (60 ) Provisional application No . 62 /313 ,092 , filed on Mar. includes a substrate that forms at least one compartment and 24 , 2016 , provisional application No . 62 / 296 , 087 , a drug content loaded into the compartment. The dosage filed on Feb . 17 , 2016 , provisional application No . form is so designed that the active pharmaceutical ingredient 62 / 170, 645 , filed on Jun . 3 , 2015 . of the drug content is released in a controlled manner. Patent Application Publication Jun . 27 , 2019 Sheet 1 of 20 US 2019 /0192440 A1 FIG . -
Expression and Distribution of the Transient Receptor Potential Cationic Channel Ankyrin 1 (TRPA1) in the Human Vagina
International Journal of Impotence Research (2014) 27, 16–19 & 2014 Macmillan Publishers Limited All rights reserved 0955-9930/14 www.nature.com/ijir ORIGINAL ARTICLE Expression and distribution of the transient receptor potential cationic channel ankyrin 1 (TRPA1) in the human vagina SU¨ ckert1, JE Sonnenberg2, K Albrecht1, MA Kuczyk1 and P Hedlund3,4 The transient receptor potential cationic channel type A1 (TRPA1), belonging to a superfamily of cationic membrane channels, has been suggested to act as mechano- and pain sensor and, thus, to play a role in neurotransmission in the human body, including the urogenital tract. While the expression of TRPA1 has been investigated in a variety of tissues, up until today, no study has addressed the expression and distribution in the female genital tract. The present study aimed to investigate the expression and distribution of TRPA1 protein in human vaginal tissue. Reverse transcriptase PCR (RT-PCR) was applied in order to identify messenger ribonuleic acid specifically encoding for TRPA/A1. The distribution of TRPA1 in relation to the neuronal nitric oxide synthase (nNOS) and the signaling peptide calcitonin gene-related peptide (CGRP) was examined by means of immunohistochemical methods (double- antibody technique, laser fluorescence microscopy). RT-PCR analysis revealed the expression of mRNA encoding sequences specific for TRPA in the vaginal wall and epithelium. Immunostaining related to TRPA1 was observed in the basal epithelium and in slender varicose nerve fibers transversing the subepithelial and stromal space of the vaginal sections. In addition, these fibers presented immunoreactivity specific for nNOS or CGRP. The smooth musculature of the vaginal wall and small vessels interspersing the tissue did not present signals related to TRPA1. -
Human Exposure to Acrolein: Time-Dependence and Individual
Environmental Toxicology and Pharmacology 45 (2016) 20–27 Contents lists available at ScienceDirect Environmental Toxicology and Pharmacology j ournal homepage: www.elsevier.com/locate/etap Human exposure to acrolein: Time-dependence and individual variation in eye irritation a,∗ b Anna-Sara Claeson , Nina Lind a Department of Psychology, Umeå University, Umeå, Sweden b Department of Economics, Swedish University of Agricultural Science, Uppsala, Sweden a r t a b i s c l e i n f o t r a c t Article history: The aim of the study was to examine the time dependence on sensory irritation detection following Received 14 December 2015 exposure to threshold levels of acrolein, in humans. The exposures occurred in an exposure chamber and Received in revised form 10 May 2016 the subjects were breathing fresh air through a mask that covered the nose and mouth. All participants Accepted 12 May 2016 participated in four exposure conditions, of which three consisted of a mixture of acrolein and heptane Available online 13 May 2016 and one of only heptane. Exposure to acrolein at a concentration half of the TLV-C lead to sensory irritation. The perceived sensory irritation resulted in both increased detectability and sensory irritation after about Keywords: 6.8 min of exposure in 58% of the participants. The study confirm the previously suggested LOAEL of about Human exposure 3 0.34 mg/m for eye irritation due to acrolein exposure. The sensory irritation was still significant 10 min Eye irritation after exposure. These results have implications for risk assessment and limit setting in occupational Sensory irritation detection threshold Time dependence hygiene. -
Federal Register/Vol. 84, No. 230/Friday, November 29, 2019
Federal Register / Vol. 84, No. 230 / Friday, November 29, 2019 / Proposed Rules 65739 are operated by a government LIBRARY OF CONGRESS 49966 (Sept. 24, 2019). The Office overseeing a population below 50,000. solicited public comments on a broad Of the impacts we estimate accruing U.S. Copyright Office range of subjects concerning the to grantees or eligible entities, all are administration of the new blanket voluntary and related mostly to an 37 CFR Part 210 compulsory license for digital uses of increase in the number of applications [Docket No. 2019–5] musical works that was created by the prepared and submitted annually for MMA, including regulations regarding competitive grant competitions. Music Modernization Act Implementing notices of license, notices of nonblanket Therefore, we do not believe that the Regulations for the Blanket License for activity, usage reports and adjustments, proposed priorities would significantly Digital Uses and Mechanical Licensing information to be included in the impact small entities beyond the Collective: Extension of Comment mechanical licensing collective’s potential for increasing the likelihood of Period database, database usability, their applying for, and receiving, interoperability, and usage restrictions, competitive grants from the Department. AGENCY: U.S. Copyright Office, Library and the handling of confidential of Congress. information. Paperwork Reduction Act ACTION: Notification of inquiry; To ensure that members of the public The proposed priorities do not extension of comment period. have sufficient time to respond, and to contain any information collection ensure that the Office has the benefit of SUMMARY: The U.S. Copyright Office is requirements. a complete record, the Office is extending the deadline for the extending the deadline for the Intergovernmental Review: This submission of written reply comments program is subject to Executive Order submission of written reply comments in response to its September 24, 2019 to no later than 5:00 p.m. -
Capsaicin: Current Understanding of Its Mechanisms and Therapy of Pain and Other Pre-Clinical and Clinical Uses
molecules Review Capsaicin: Current Understanding of Its Mechanisms and Therapy of Pain and Other Pre-Clinical and Clinical Uses Victor Fattori †, Miriam S. N. Hohmann †, Ana C. Rossaneis, Felipe A. Pinho-Ribeiro and Waldiceu A. Verri Jr. * Departamento de Ciências Patológicas, Centro de Ciências Biológicas, Universidade Estadual de Londrina, Rodovia Celso Garcia Cid KM480 PR445, Caixa Postal 10.011, 86057-970 Londrina, Paraná, Brazil; [email protected] (V.F.); [email protected] (M.S.N.H.); [email protected] (A.C.R.); [email protected] (F.A.P.-R.) * Correspondence: [email protected] or [email protected]; Tel.: +55-43-3371-4979 † These authors contributed equally to this paper. Academic Editor: Pin Ju Chueh Received: 27 April 2016; Accepted: 27 April 2016; Published: 28 June 2016 Abstract: In this review, we discuss the importance of capsaicin to the current understanding of neuronal modulation of pain and explore the mechanisms of capsaicin-induced pain. We will focus on the analgesic effects of capsaicin and its clinical applicability in treating pain. Furthermore, we will draw attention to the rationale for other clinical therapeutic uses and implications of capsaicin in diseases such as obesity, diabetes, cardiovascular conditions, cancer, airway diseases, itch, gastric, and urological disorders. Keywords: analgesia; capsaicinoids; chili peppers; desensitization; TRPV1 1. Introduction Capsaicin is a compound found in chili peppers and responsible for their burning and irritant effect. In addition to the sensation of heat, capsaicin produces pain and, for this reason, is an important tool in the study of pain. Although our understanding of pain mechanisms has evolved greatly through the development of new techniques, experimental tools are still extremely necessary and widely used.