Dictionary of the Active Principles of Plants : Alkaloids, Bitter

Total Page:16

File Type:pdf, Size:1020Kb

Dictionary of the Active Principles of Plants : Alkaloids, Bitter PPP" DICTIONARY OF THE ACTIVE PRINCIPLES OF PLANTS SOHN i. [ir n ii>h^ -*' r < i^' : DIGTIOJSTAEY OF THE ACTIVE PRINCIPLES OF PLANTS: ALKALOIDS; BITTER PRINCIPLES; GLUCOSIDES: THEIR SOURCES, NATURE, AND CHE.UICAL CHARACTERISTICS, WITH TABULAR SUMMARY, CLASSIFICATION OF REACTIOSS, AND FULL BOTANICAL AND GENERAL INDEXES. CHARLES E. SOHN, F.LC, F.C.S. Member of the Society of Public Ana/y.tfs. LONDON BAILLIERE, TINDALL AND COX, 20 & 21, KING WILLIAM STREET, STRAND. 1894. PREFACE. bodies, has been The ceaseless flow of new facts into every branch of science is well The present work, which treats of nearly GOU of these illustrated in the particular section of organic chemistry embraced prepared with the hope that it may contribute to the attainment of the under the heading Alkaloids, Bitter Principles and (rlucosides. The above objects, and be found of service to those who have occasion to deal streamlet that started at the commencement of this century, when with these compounds or study them—particularly the analyst, professor, Derosne and Serti'irner made the discovery of Morphine, has swollen with research chemist, student, and manufacturer. ever-increasing rapidity, until at the present time the Hood of matter No efforts have been spared to render as full as possible the information reactions) wherever accumulated almost defies management. supplied (particularly as regards tests and chemical ; It becomes every day more desirable that something be done towards practicable, it has been drawn from the original sources, and embodies the classifying the substances so constantly being augmented in number, and results of the latest researches. that the details bearing upon them, now more or less scattered throughout Easy access to any fact contained in the book has been aimed at, intro- chemical literature, should be tabulated in a convenient form—one that and it is earnestly requested that the reader will peruse the will permit not only that a i/iven attribute of any substance shall be readily ductory and explanatory part, that he may the better acquire this found, but also will indicate wherein such substance differs from, or resembles, facility. another of its class. London, Uctobei; 18'J3. : ' : INTRODUCTORY AND EXPLANATORY. In addition to the Active Principles that are members of one or other of or chemically allied plants, whilst retaining as far as practicable an alpha- the three classes specially dealt with, I have included some substances betical order. Supplementary indexes being provided, that are liable to be met with in connection with the manifest these, or have bearino- on inconveniences which a purely the subjects under treatment. ° alphabetical method would occasion are by these means The term Alkaloid avoided. (or the letter A used for that word) has been employed ^- In order that no time may be lost in finding any statement con- to denote any naturally occurring vegetable base ; this covers a cerning wider a given substance, the following rotation has been adhered to in area than would the most modern application of the word which the enumeration of the properties restricts it to Pyridine and and tests : Quinoline derivatives, to the exclusion of such a body as Caffeine. Of course, Salts of Ammonia and albuminoid decom- Botanical Z»ctot7s.— position Plants furnishing the compound or compounds, with products cannot be comprised in this class (one or two of the technical as well as popular names and botanical order. latter receive notice, however). Parts of plant in which found. The Glucoshlet! embrace those substances Bibliographical (other than tannins) that reference (names of investigators and details of published yield sugar (with some other compound) when decomposed by the action researches). ot dilute acids or natural Each substance ferments. They are generally free from (when more than one) is then treated individually thus Nitrogen, exceptions being General, Physical Amygdalin, Solaniue, Indican, Linamarin, and Chemical Details.—^ame and synonyms, class (A = Myronic Acid, and Sinalbni, Alkaloid, B = Bitter Principle, = the last two of which contain Sulphur also G Glucoside). hemtter Pnndples Chemical formula. 1 are a very diverse group, as various in composition as in their chemical reactions. Crystalline form, etc. They contain no Nitrogen, and yield no Melting point and effects of heat sugar on treatment with dilute acids or otherwise. The generally. name Awaroid Rotatory power (action on IS suggested for such bodies polarized light). as these, in order to avoid confusion with Reaction glucosides and (alkaline, neutral, or acid). alkaloids, so many of which are also bitter. Being numerous verv Taste and odour (if any). and frequently of considerable importance, whilst Various generally : Character of salts, products of hydrolysis (action neglected in works upon organic of boiling dilute chemistry, it has been thought desirable acids), physiological effect. to describe them fully. Solubility in water, alcohol, ether, chloroform, benzene, petroleum ether, amyl In conformity with the system alcohol, carbon _ adopted by the Chemical Society in their bisulphide, and sundry other solvents. journal, all alkaloids are spelt Behaviour towards with the termination ine, whUst glucosides immiscible solvents. and Reactions amaroids end in in, without the final e. with precipitants, etc. (in this order) The book consists of three parts (besides two indexes and sub- 1. Alkaline indexes). hydrates and carbo- 4. Tannic acid. nates. '" Dictionary form, 5. Picric acid, * arranged upon a system which groups C,;Ho(NOo)3'OH together^'^'^'^xJ' 2. Ammonia. the constituents either of one plant or of a (Hager's reagent). number of botanically 3. Lead acetate, neutral and basic. 6. Ferric chloride. IN'TUODl'CTORY AND EXPLANATORY. 7. Platinum chloride, Phoapho-componiuh : GENERAL INDEX.—Special endeavours have been made to render 8. Palladious chloride. 22. Phosphomolybdio acid (.Sonnen- this comprehensive. 9. Gold chloride. schein's reagent). In the Tabular Sum.mary the order of insertion in Part I. has been 10. Silver nitrate. 23. Phospho-tungstio acid (Schei- preserved, because it permits a survey of all the active ])rinciples of a 11. Copper sulphate. bler's reagent). given plant at a glance —a manifest advantage over a purely alphabetical Fehling's solution (alkaline 12. 24. Phospho-antimonic acid. arrangement (which might upon a preliminary inspection have appeareil copper tartrate). Iodides, etc. : desirable), for in that case the reader, dealing, for instance, with Opium, 25. lodo-potassic iodide (Wagner's would have had nearly forty different positions to find, whilst here be has Cyanides, etc. : reagent). but one. 13. Potassium ferrocyanide. 26. Bismuth-potassic iodide ( Dragen- Synonyms and questions of identity cannot, for want of space, be 14. ferricyanide. dorff's reagent). ,, discussed in Part II. (the Tabular Summary), but receive full attention - potassic iodide Ih. ,, sulphocyanide. 27. Cadmium in Part I. ; for the same reason, many columns of precipitants have had 16. ,, cyanide. (Marme's reagent). is iodide. to be removed from Part II. ; but this curtailment amply compensated 17. ,, nitro-prusside. 28. Zinc-potassio 18. Silver potassium cyanide. 29. Mercuric-potassic iodide ( M ayer's for by the classified lists of reactions in Part IIL and the numerous solution). reference notes. Chromales, etc. : 30. Mercuric chloride. In the last section—Part III. —are classed, in a series of alphabetical 19. Potassium chromate. 31. Chlorine water. lists, sub.-itances having a common propertj-, or giving a similar reaction. 20. ,, bichromate. 32. Bromine water. 21. Chromic acid. 33. Iodine tincture. GENERAL RULES. Colour tests (in this order), time taken for development of colours and their 1^ 1. To facilitate reference, it is important to remember that the is invariably given durability ; series of details upon any substance in a particular Concentrated sulphuric acid alone and with various substances (sugar, potassioni rotation (see above). bichromate, manganese dio.\ide, nitric acid, etc.), Erdmann's reagent, sulphuric 2. Colour — Since the great majority of substances here dealt with are acid with a trace of nitric acid. colourless, colour is only mentioned when coloured compounds are spoken Concentrated nitric acid alone. of ; all others are to be understood to be white or colourlest. Acids in general. 3. Odour.—For analogous reasons, all bodies not described as h'triny Perchlorate of potash or perchloric acid. odour are odourless. Per-iodic acid. 4. Alkalinity.—When not otherwise stated, the reaction (alkaline, Frohde's solution (molybdic and sulphuric acids). neutral, or acid) has reference to litmus as indicator. PART II. A Tabular Su.m.mary designed for ready reference and — 5. Temper.\ture is always indicated in degrees Centigrade. as a means of contrasting one compound with another for analytical and G. Solubility'.—Figures in the solubility columns denote number of other purposes it gives the chief properties and tests of the substances ; parts of solvent required to dissolve one jjart of substance. that are more fully described in Part I. 7. Delicacy of Test. —Numbers in the columns of precipitants (or PART III. —A Cl.\ssification of Reactions for the special use of colour tests) signify degree of dilution at which the reaction is analysts, showing what compounds are known to respond to a given test. observable. BOTANICAL INDEX. —Each plant here appears in its alphabetical 8. Use of Re.a.gents. —Except where other indications are given, positions by popular and scientific names. Sub-lists of plants are also precipitants are to be applied to the substiitice dissolved in water, and in the inserted for those botanical orders which iuclude members containing alka- case of alkaloids to the salt, and not to the free base. loidal, bitter, or glucosidal principles. This facilitates comparison of the 9. Colour Tests. —The dry substance is to be employed when testing constituents of allied plants. with concentrated acids and colour tests generally. = INTRODUCTORY AND EXPLANATORY. AnnREvrATioNS have as far as possible been avoided, but in the (after = Tabular G name of [ substance) phos.-molyb.
Recommended publications
  • Potential Therapeutic Benefit of Low Dose Naltrexone in Myalgic Encephalomyelitis/Chronic Fatigue Syndrome
    Potential Therapeutic Benefit of Low Dose Naltrexone in Myalgic Encephalomyelitis/Chronic Fatigue Syndrome: Role of Transient Receptor Potential Melastatin 3 Ion Channels in Pathophysiology and Treatment. Author Cabanas, Helene, Muraki, Katsuhiko, Eaton-Fitch, Natalie, Staines, Donald Ross, Marshall- Gradisnik, Sonya Published 2021 Journal Title Frontiers in Immunology Version Version of Record (VoR) DOI https://doi.org/10.3389/fimmu.2021.687806 Copyright Statement © 2021 Cabanas, Muraki, Eaton-Fitch, Staines and Marshall-Gradisnik. This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms. Downloaded from http://hdl.handle.net/10072/406897 Griffith Research Online https://research-repository.griffith.edu.au ORIGINAL RESEARCH published: 13 July 2021 doi: 10.3389/fimmu.2021.687806 Potential Therapeutic Benefitof Low Dose Naltrexone in Myalgic Encephalomyelitis/Chronic Fatigue Syndrome: Role of Transient Receptor Potential Melastatin 3 Ion Channels in Pathophysiology and Treatment Edited by: Helene Cabanas 1,2*, Katsuhiko Muraki 2,3, Natalie Eaton-Fitch 1,2, Donald Ross Staines 1,2 Jorge Matias-Guiu, 1,2 Complutense University and Sonya Marshall-Gradisnik
    [Show full text]
  • Exploring the Activity of an Inhibitory Neurosteroid at GABAA Receptors
    1 Exploring the activity of an inhibitory neurosteroid at GABAA receptors Sandra Seljeset A thesis submitted to University College London for the Degree of Doctor of Philosophy November 2016 Department of Neuroscience, Physiology and Pharmacology University College London Gower Street WC1E 6BT 2 Declaration I, Sandra Seljeset, confirm that the work presented in this thesis is my own. Where information has been derived from other sources, I can confirm that this has been indicated in the thesis. 3 Abstract The GABAA receptor is the main mediator of inhibitory neurotransmission in the central nervous system. Its activity is regulated by various endogenous molecules that act either by directly modulating the receptor or by affecting the presynaptic release of GABA. Neurosteroids are an important class of endogenous modulators, and can either potentiate or inhibit GABAA receptor function. Whereas the binding site and physiological roles of the potentiating neurosteroids are well characterised, less is known about the role of inhibitory neurosteroids in modulating GABAA receptors. Using hippocampal cultures and recombinant GABAA receptors expressed in HEK cells, the binding and functional profile of the inhibitory neurosteroid pregnenolone sulphate (PS) were studied using whole-cell patch-clamp recordings. In HEK cells, PS inhibited steady-state GABA currents more than peak currents. Receptor subtype selectivity was minimal, except that the ρ1 receptor was largely insensitive. PS showed state-dependence but little voltage-sensitivity and did not compete with the open-channel blocker picrotoxinin for binding, suggesting that the channel pore is an unlikely binding site. By using ρ1-α1/β2/γ2L receptor chimeras and point mutations, the binding site for PS was probed.
    [Show full text]
  • Development and Application of a High-Throughput Luminescent Prophage Induction Assay for the Identification of Temperate Bacter
    Development and application of a high-throughput luminescent prophage induction assay for the identification of temperate bacteriophage-inducing food-grade compounds By Elizabeth Tompkins Food Science and Agricultural Chemistry, McGill University, Sainte-Anne-de-Bellevue, Quebec April 2019 A thesis submitted to McGill University in partial fulfillment of the requirements of the degree of Master of Science in Food Science © Elizabeth Tompkins 2019 Table of Contents Abstract ...........................................................................................................................vi Résumé ......................................................................................................................... viii Acknowledgements .........................................................................................................xi Contribution of authors .................................................................................................. xiii List of tables ...................................................................................................................xv List of figures ................................................................................................................. xvi List of abbreviations ..................................................................................................... xvii Chapter 1: Introduction .................................................................................................... 1 1.1 General introduction .............................................................................................
    [Show full text]
  • Deutsche Gesellschaft Für Experimentelle Und Klinische Pharmakologie Und Toxikologie E.V
    Naunyn-Schmiedeberg´s Arch Pharmacol (2013 ) 386 (Suppl 1):S1–S104 D OI 10.1007/s00210-013-0832-9 Deutsche Gesellschaft für Experimentelle und Klinische Pharmakologie und Toxikologie e.V. Abstracts of the 79 th Annual Meeting March 5 – 7, 2013 Halle/Saale, Germany This supplement was not sponsored by outside commercial interests. It was funded entirely by the publisher. 123 S2 S3 001 003 Multitarget approach in the treatment of gastroesophagel reflux disease – Nucleoside Diphosphate Kinase B is a Novel Receptor-independent Activator of comparison of a proton-pump inhibitor with STW 5 G-protein Signaling in Clinical and Experimental Atrial Fibrillation Abdel-Aziz H.1,2, Khayyal M. T.3, Kelber O.2, Weiser D.2, Ulrich-Merzenich G.4 Abu-Taha I.1, Voigt N.1, Nattel S.2, Wieland T.3, Dobrev D.1 1Inst. of Pharmaceutical & Medicinal Chemistry, University of Münster Pharmacology, 1Universität Duisburg-Essen Institut für Pharmakologie, Hufelandstr. 55, 45122 Essen, Hittorfstr 58-62, 48149 Münster, Germany Germany 2Steigerwald Arzneimittelwerk Wissenschaft, Havelstr 5, 64295 Darmstadt, Germany 2McGill University Montreal Heart Institute, 3655 Promenade Sir-William-Osler, Montréal 3Faculty of Pharmacy, Cairo University Pharmacology, Cairo Egypt Québec H3G 1Y6, Canada 4Medizinische Poliklinik, University of Bonn, Wilhelmstr. 35-37, 53111 Bonn, Germany 3Medizinische Fakultät Mannheim der Universität Heidelberg Institutes für Experimentelle und Klinische Pharmakologie und Toxikologie, Maybachstr. 14, 68169 Gastroesophageal reflux disease (GERD) was the most common GI-diagnosis (8.9 Mannheim, Germany million visits) in the US in 2012 (1). Proton pump inhibitors (PPI) are presently the mainstay of therapy, but in up to 40% of the patients complete symptom control fails.
    [Show full text]
  • Trace Organic Contaminant Removal by Fungal Membrane Bioreactors and Enzymatic Membrane Reactors
    University of Wollongong Research Online University of Wollongong Thesis Collection 1954-2016 University of Wollongong Thesis Collections 2015 Trace organic contaminant removal by fungal membrane bioreactors and enzymatic membrane reactors Luong Ngoc Nguyen University of Wollongong Follow this and additional works at: https://ro.uow.edu.au/theses University of Wollongong Copyright Warning You may print or download ONE copy of this document for the purpose of your own research or study. The University does not authorise you to copy, communicate or otherwise make available electronically to any other person any copyright material contained on this site. You are reminded of the following: This work is copyright. Apart from any use permitted under the Copyright Act 1968, no part of this work may be reproduced by any process, nor may any other exclusive right be exercised, without the permission of the author. Copyright owners are entitled to take legal action against persons who infringe their copyright. A reproduction of material that is protected by copyright may be a copyright infringement. A court may impose penalties and award damages in relation to offences and infringements relating to copyright material. Higher penalties may apply, and higher damages may be awarded, for offences and infringements involving the conversion of material into digital or electronic form. Unless otherwise indicated, the views expressed in this thesis are those of the author and do not necessarily represent the views of the University of Wollongong. Recommended Citation Nguyen, Luong Ngoc, Trace organic contaminant removal by fungal membrane bioreactors and enzymatic membrane reactors, Doctor of Philosophy thesis, School of Civil, Mining and Environmental Engineering, University of Wollongong, 2015.
    [Show full text]
  • RAC-GWVI: Research Alerts—Pubmed Citations for August 21 to 28, 2018 1
    RAC-GWVI: Research Alerts—PubMed Citations for August 21 to 28, 2018 1 GULF WAR ILLNESS Neurotoxicity in acute and repeated organophosphate exposure. Naughton SX1, Terry AV Jr2. Toxicology. 2018 Aug 22. pii: S0300-483X(18)30264-6. doi: 10.1016/j.tox.2018.08.011. PMID: 30144465. [Epub ahead of print] The term organophosphate (OP) refers to a diverse group of chemicals that are found in hundreds of products worldwide. As pesticides, their most common use, OPs are clearly beneficial for agricultural productivity and the control of deadly vector-borne illnesses. However, as a consequence of their widespread use, OPs are now among the most common synthetic chemicals detected in the environment as well as in animal and human tissues. This is an increasing environmental concern because many OPs are highly toxic and both accidental and intentional exposures to OPs resulting in deleterious health effects have been documented for decades. Some of these deleterious health effects include a variety of long-term neurological and psychiatric disturbances including impairments in attention, memory, and other domains of cognition. Moreover, some chronic illnesses that manifest these symptoms such as Gulf War Illness and Aerotoxic Syndrome have (at least in part) been attributed to OP exposure. In addition to acute acetylcholinesterase inhibition, OPs may affect a number of additional targets that lead to oxidative stress, axonal transport deficits, neuroinflammation, and autoimmunity. Some of these targets could be exploited for therapeutic purposes. The purpose of this review is thus to: 1) describe the important uses of organophosphate (OP)-based compounds worldwide, 2) provide an overview of the various risks and toxicology associated with OP exposure, particularly long-term neurologic and psychiatric symptoms, 3) discuss mechanisms of OP toxicity beyond cholinesterase inhibition, 4) review potential therapeutic strategies to reverse the acute toxicity and long term deleterious effects of OPs.
    [Show full text]
  • Promiscuous G-Protein-Coupled Receptor Inhibition of Transient Receptor Potential Melastatin 3 Ion Channels by Gβγ Subunits
    7840 • The Journal of Neuroscience, October 2, 2019 • 39(40):7840–7852 Cellular/Molecular Promiscuous G-Protein-Coupled Receptor Inhibition of Transient Receptor Potential Melastatin 3 Ion Channels by G␤␥ Subunits X Omar Alkhatib,1 XRobson da Costa,1,2 XClive Gentry,1 XTalisia Quallo,1 Stefanie Mannebach,3 Petra Weissgerber,3 Marc Freichel,4,5 Stephan E. Philipp,3 XStuart Bevan,1 and XDavid A. Andersson1 1Wolfson Centre for Age-Related Diseases, King’s College London, London SE1 1UL, United Kingdom, 2School of Pharmacy, Universidade Federal do Rio de Janeiro, 21941-908 Rio de Janeiro, Brazil, 3Experimental and Clinical Pharmacology and Toxicology/Center for Molecular Signaling (PZMS), Saarland University, 66421 Homburg, Germany, 4Pharmacological Institute, Ruprecht-Karls-University Heidelberg, 69120 Heidelberg, Germany, and 5German Centre for Cardiovascular Research (DZHK), partner site Heidelberg/Mannheim, 69120 Heidelberg, Germany Transient receptor potential melastatin 3 (TRPM3) is a nonselective cation channel that is inhibited by G␤␥ subunits liberated following ␣ ␤␥ ␣ activation of G i/o protein-coupled receptors. Here, we demonstrate that TRPM3 channels are also inhibited by G released from G s ␣ and G q. Activation of the Gs-coupled adenosine 2B receptor and the Gq-coupled muscarinic acetylcholine M1 receptor inhibited the activity of TRPM3 heterologously expressed in HEK293 cells. This inhibition was prevented when the G␤␥ sink ␤ARK1-ct (C terminus of ␤-adrenergic receptor kinase-1) was coexpressed with TRPM3. In neurons isolated from mouse dorsal root ganglion (DRG), native TRPM3 channels were inhibited by activating Gs-coupled prostaglandin-EP2 and Gq-coupled bradykinin B2 (BK2) receptors. The Gi/o inhibitor pertussis toxin and inhibitors of PKA and PKC had no effect on EP2- and BK2-mediated inhibition of TRPM3, demonstrating ␣ that the receptors did not act through G i/o or through the major protein kinases activated downstream of G-protein-coupled receptor (GPCR) activation.
    [Show full text]
  • Transient Receptor Potential Channels As Drug Targets: from the Science of Basic Research to the Art of Medicine
    1521-0081/66/3/676–814$25.00 http://dx.doi.org/10.1124/pr.113.008268 PHARMACOLOGICAL REVIEWS Pharmacol Rev 66:676–814, July 2014 Copyright © 2014 by The American Society for Pharmacology and Experimental Therapeutics ASSOCIATE EDITOR: DAVID R. SIBLEY Transient Receptor Potential Channels as Drug Targets: From the Science of Basic Research to the Art of Medicine Bernd Nilius and Arpad Szallasi KU Leuven, Department of Cellular and Molecular Medicine, Laboratory of Ion Channel Research, Campus Gasthuisberg, Leuven, Belgium (B.N.); and Department of Pathology, Monmouth Medical Center, Long Branch, New Jersey (A.S.) Abstract. ....................................................................................679 I. Transient Receptor Potential Channels: A Brief Introduction . ...............................679 A. Canonical Transient Receptor Potential Subfamily . .....................................682 B. Vanilloid Transient Receptor Potential Subfamily . .....................................686 C. Melastatin Transient Receptor Potential Subfamily . .....................................696 Downloaded from D. Ankyrin Transient Receptor Potential Subfamily .........................................700 E. Mucolipin Transient Receptor Potential Subfamily . .....................................702 F. Polycystic Transient Receptor Potential Subfamily . .....................................703 II. Transient Receptor Potential Channels: Hereditary Diseases (Transient Receptor Potential Channelopathies). ......................................................704
    [Show full text]
  • Natural Products As Chemopreventive Agents by Potential Inhibition of the Kinase Domain in Erbb Receptors
    Supplementary Materials: Natural Products as Chemopreventive Agents by Potential Inhibition of the Kinase Domain in ErBb Receptors Maria Olivero-Acosta, Wilson Maldonado-Rojas and Jesus Olivero-Verbel Table S1. Protein characterization of human HER Receptor structures downloaded from PDB database. Recept PDB resid Resolut Name Chain Ligand Method or Type Code ues ion Epidermal 1,2,3,4-tetrahydrogen X-ray HER 1 2ITW growth factor A 327 2.88 staurosporine diffraction receptor 2-{2-[4-({5-chloro-6-[3-(trifl Receptor uoromethyl)phenoxy]pyri tyrosine-prot X-ray HER 2 3PP0 A, B 338 din-3-yl}amino)-5h-pyrrolo 2.25 ein kinase diffraction [3,2-d]pyrimidin-5-yl]etho erbb-2 xy}ethanol Receptor tyrosine-prot Phosphoaminophosphonic X-ray HER 3 3LMG A, B 344 2.8 ein kinase acid-adenylate ester diffraction erbb-3 Receptor N-{3-chloro-4-[(3-fluoroben tyrosine-prot zyl)oxy]phenyl}-6-ethylthi X-ray HER 4 2R4B A, B 321 2.4 ein kinase eno[3,2-d]pyrimidin-4-ami diffraction erbb-4 ne Table S2. Results of Multiple Alignment of Sequence Identity (%ID) Performed by SYBYL X-2.0 for Four HER Receptors. Human Her PDB CODE 2ITW 2R4B 3LMG 3PP0 2ITW (HER1) 100.0 80.3 65.9 82.7 2R4B (HER4) 80.3 100 71.7 80.9 3LMG (HER3) 65.9 71.7 100 67.4 3PP0 (HER2) 82.7 80.9 67.4 100 Table S3. Multiple alignment of spatial coordinates for HER receptor pairs (by RMSD) using SYBYL X-2.0. Human Her PDB CODE 2ITW 2R4B 3LMG 3PP0 2ITW (HER1) 0 4.378 4.162 5.682 2R4B (HER4) 4.378 0 2.958 3.31 3LMG (HER3) 4.162 2.958 0 3.656 3PP0 (HER2) 5.682 3.31 3.656 0 Figure S1.
    [Show full text]
  • (12) United States Patent (10) Patent No.: US 9,333,192 B2 Tam Et Al
    USOO9333 192B2 (12) United States Patent (10) Patent No.: US 9,333,192 B2 Tam et al. (45) Date of Patent: May 10, 2016 (54) PHYTOESTROGEN PRODUCT OF RED WO OO64438 11, 2000 CLOVER AND PHARMACEUTICALUSES WO 2008/O16768 2, 2008 THEREOF WO 2008/057934 5, 2008 WO 2008/1201.05 10, 2008 WO 2013,050930 4/2013 (71) Applicant: Sinoveda Canada Inc., Edmonton, OTHER PUBLICATIONS Alberta (CA) Lee etal, Biol. Pharm. Bull. 28(10) 1948-1953 (2005).* (72) Inventors: Yun Kau Tam, Edmonton (CA); Moon et al. The AAPS Journal 2006; 8(3) Article 51.* Yi-Chan James Lin, Edmonton (CA); U.S. Office Action, May 1, 2013, for U.S. Appl. No. 13/251.267, filed Oct. 2, 2011. Brian Duff Sloley, Edmonton (CA); PCT International Search Report, Jan. 25, 2013, for Int' App'l No. Chih-Yuan Tseng, Edmonton (CA) PCT/IB2012/055277, filed Oct. 2, 2012. PCT Written Option, Jan. 25, 2013, for Int' App'l No. PCT/IB2012/ (73) Assignee: SINOVEDA CANADA, INCCA (US) 055277, filed Oct. 2, 2012. Abrams, S. A. I. J. Griffin, et al. (2002). “Using stable isotopes to (*) Notice: Subject to any disclaimer, the term of this assess the bioavailability of minerals in food fortification programs.” patent is extended or adjusted under 35 Food Nutr Bull 23(3 Suppl): 158-165. Allred, C. D. K. F. Allred, et al. (2004). “Dietary genistein results in U.S.C. 154(b) by 0 days. larger MNU-induced, estrogen-dependent mammary tumors follow ing ovariectomy of Sprague-Dawley rats.” Carcinogenesis 25(2): (21) Appl.
    [Show full text]
  • Identification and Application of Novel and Selective Blockers for the Heat-Activated Cation Channel TRPM3
    Identification and application of novel and selective blockers for the heat-activated cation channel TRPM3 Der Fakult¨atf¨urBiowissenschaften, Pharmazie und Psychologie der Universit¨atLeipzig eingereichte DISSERTATION zur Erlangung des akademischen Grades doctor rerum naturalium Dr. rer. nat. vorgelegt von Diplom Biologin Isabelle Straub geboren am 18.01.1980 in Neunkirchen Leipzig, den 23.05.2014 Bibliography Isabelle Straub Identification and application of novel and selective blockers for the heat-activated cation channel TRPM3 Fakult¨atf¨urBiowissenschaften, Pharmazie und Psychologie Universit¨atLeipzig Dissertation 86 Seiten, 165 Literaturangaben, 38 Abbildungen, 0 Tabellen TRPM3 (melastatin-related transient receptor potential 3) is a calcium-permeable nonselective cation channel that is expressed in various tissues, including insulin- secreting β-cells and a subset of sensory neurons from trigeminal and dorsal root ganglia (DRG). TRPM3 can be activated by the neurosteroid pregnenolone sul- phate (PregS) or heat. TRPM3−=− mice display an impaired sensation of nox- ious heat and inflammatory thermal hyperalgesia. A calcium-based screening of a compound library identified four natural compounds as TRPM3 blockers. Three of the natural compounds belong to the citrus fruit flavanones (hesperetin, erio- dictyol and naringenin), the forth compound is a deoxybenzoin that can be syn- thesized from an isoflavone of the root of Ononis spinosa (ononetin). The IC50 for the substances ranged from upper nanomolar to lower micromolar concentra- tions. Electrophysiological whole-cell measurements as well as calcium measure- ments confirmed the potency of the compounds to block TRPM3 in DRG neu- rones. To further improve the potency and the selectivity of TRPM3 block and to identify the pharmacophore within the flavanone structure, we conducted a hit optimisation procedure by re-screening a focussed library.
    [Show full text]
  • (12) Patent Application Publication (10) Pub. No.: US 2009/0269772 A1 Califano Et Al
    US 20090269772A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2009/0269772 A1 Califano et al. (43) Pub. Date: Oct. 29, 2009 (54) SYSTEMS AND METHODS FOR Publication Classification IDENTIFYING COMBINATIONS OF (51) Int. Cl. COMPOUNDS OF THERAPEUTIC INTEREST CI2O I/68 (2006.01) CI2O 1/02 (2006.01) (76) Inventors: Andrea Califano, New York, NY G06N 5/02 (2006.01) (US); Riccardo Dalla-Favera, New (52) U.S. Cl. ........... 435/6: 435/29: 706/54; 707/E17.014 York, NY (US); Owen A. (57) ABSTRACT O'Connor, New York, NY (US) Systems, methods, and apparatus for searching for a combi nation of compounds of therapeutic interest are provided. Correspondence Address: Cell-based assays are performed, each cell-based assay JONES DAY exposing a different sample of cells to a different compound 222 EAST 41ST ST in a plurality of compounds. From the cell-based assays, a NEW YORK, NY 10017 (US) Subset of the tested compounds is selected. For each respec tive compound in the Subset, a molecular abundance profile from cells exposed to the respective compound is measured. (21) Appl. No.: 12/432,579 Targets of transcription factors and post-translational modu lators of transcription factor activity are inferred from the (22) Filed: Apr. 29, 2009 molecular abundance profile data using information theoretic measures. This data is used to construct an interaction net Related U.S. Application Data work. Variances in edges in the interaction network are used to determine the drug activity profile of compounds in the (60) Provisional application No. 61/048.875, filed on Apr.
    [Show full text]