Inhibitory Effects of Phytochemicals on Metabolic Capabilities of CYP2D6*1 and CYP2D6*10 Using Cell-Based Models in Vitro
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(12) United States Patent (10) Patent No.: US 9,498,481 B2 Rao Et Al
USOO9498481 B2 (12) United States Patent (10) Patent No.: US 9,498,481 B2 Rao et al. (45) Date of Patent: *Nov. 22, 2016 (54) CYCLOPROPYL MODULATORS OF P2Y12 WO WO95/26325 10, 1995 RECEPTOR WO WO99/O5142 2, 1999 WO WOOO/34283 6, 2000 WO WO O1/92262 12/2001 (71) Applicant: Apharaceuticals. Inc., La WO WO O1/922.63 12/2001 olla, CA (US) WO WO 2011/O17108 2, 2011 (72) Inventors: Tadimeti Rao, San Diego, CA (US); Chengzhi Zhang, San Diego, CA (US) OTHER PUBLICATIONS Drugs of the Future 32(10), 845-853 (2007).* (73) Assignee: Auspex Pharmaceuticals, Inc., LaJolla, Tantry et al. in Expert Opin. Invest. Drugs (2007) 16(2):225-229.* CA (US) Wallentin et al. in the New England Journal of Medicine, 361 (11), 1045-1057 (2009).* (*) Notice: Subject to any disclaimer, the term of this Husted et al. in The European Heart Journal 27, 1038-1047 (2006).* patent is extended or adjusted under 35 Auspex in www.businesswire.com/news/home/20081023005201/ U.S.C. 154(b) by Od en/Auspex-Pharmaceuticals-Announces-Positive-Results-Clinical M YW- (b) by ayS. Study (published: Oct. 23, 2008).* This patent is Subject to a terminal dis- Concert In www.concertpharma. com/news/ claimer ConcertPresentsPreclinicalResultsNAMS.htm (published: Sep. 25. 2008).* Concert2 in Expert Rev. Anti Infect. Ther. 6(6), 782 (2008).* (21) Appl. No.: 14/977,056 Springthorpe et al. in Bioorganic & Medicinal Chemistry Letters 17. 6013-6018 (2007).* (22) Filed: Dec. 21, 2015 Leis et al. in Current Organic Chemistry 2, 131-144 (1998).* Angiolillo et al., Pharmacology of emerging novel platelet inhibi (65) Prior Publication Data tors, American Heart Journal, 2008, 156(2) Supp. -
Investigation of Key Genes and Pathways in Inhibition of Oxycodone on Vincristine-Induced Microglia Activation by Using Bioinformatics Analysis
Hindawi Disease Markers Volume 2019, Article ID 3521746, 10 pages https://doi.org/10.1155/2019/3521746 Research Article Investigation of Key Genes and Pathways in Inhibition of Oxycodone on Vincristine-Induced Microglia Activation by Using Bioinformatics Analysis Wei Liu,1 Jishi Ye,2 and Hong Yan 1 1Department of Anesthesiology, the Central Hospital of Wuhan, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430014, China 2Department of Anesthesiology, Renmin Hospital of Wuhan University, Wuhan, 430060 Hubei, China Correspondence should be addressed to Hong Yan; [email protected] Received 2 November 2018; Accepted 31 December 2018; Published 10 February 2019 Academic Editor: Hubertus Himmerich Copyright © 2019 Wei Liu et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. Introduction. The neurobiological mechanisms underlying the chemotherapy-induced neuropathic pain are only partially understood. Among them, microglia activation was identified as the key component of neuropathic pain. The aim of this study was to identify differentially expressed genes (DEGs) and pathways associated with vincristine-induced neuropathic pain by using bioinformatics analysis and observe the effects of oxycodone on these DEG expressions in a vincristine-induced microglia activation model. Methods. Based on microarray profile GSE53897, we identified DEGs between vincristine-induced neuropathic pain rats and the control group. Using the ToppGene database, the prioritization DEGs were screened and performed by gene ontology (GO) and signaling pathway enrichment. A protein-protein interaction (PPI) network was used to explore the relationship among DEGs. -
2D6 Substrates 2D6 Inhibitors 2D6 Inducers
Physician Guidelines: Drugs Metabolized by Cytochrome P450’s 1 2D6 Substrates Acetaminophen Captopril Dextroamphetamine Fluphenazine Methoxyphenamine Paroxetine Tacrine Ajmaline Carteolol Dextromethorphan Fluvoxamine Metoclopramide Perhexiline Tamoxifen Alprenolol Carvedilol Diazinon Galantamine Metoprolol Perphenazine Tamsulosin Amiflamine Cevimeline Dihydrocodeine Guanoxan Mexiletine Phenacetin Thioridazine Amitriptyline Chloropromazine Diltiazem Haloperidol Mianserin Phenformin Timolol Amphetamine Chlorpheniramine Diprafenone Hydrocodone Minaprine Procainamide Tolterodine Amprenavir Chlorpyrifos Dolasetron Ibogaine Mirtazapine Promethazine Tradodone Aprindine Cinnarizine Donepezil Iloperidone Nefazodone Propafenone Tramadol Aripiprazole Citalopram Doxepin Imipramine Nifedipine Propranolol Trimipramine Atomoxetine Clomipramine Encainide Indoramin Nisoldipine Quanoxan Tropisetron Benztropine Clozapine Ethylmorphine Lidocaine Norcodeine Quetiapine Venlafaxine Bisoprolol Codeine Ezlopitant Loratidine Nortriptyline Ranitidine Verapamil Brofaramine Debrisoquine Flecainide Maprotline olanzapine Remoxipride Zotepine Bufuralol Delavirdine Flunarizine Mequitazine Ondansetron Risperidone Zuclopenthixol Bunitrolol Desipramine Fluoxetine Methadone Oxycodone Sertraline Butylamphetamine Dexfenfluramine Fluperlapine Methamphetamine Parathion Sparteine 2D6 Inhibitors Ajmaline Chlorpromazine Diphenhydramine Indinavir Mibefradil Pimozide Terfenadine Amiodarone Cimetidine Doxorubicin Lasoprazole Moclobemide Quinidine Thioridazine Amitriptyline Cisapride -
Comparative Pharmacokinetic Study of Luteolin After Oral Administration Of
Vol. 8(16), pp. 422-428, 29 April, 2014 DOI 10.5897/AJPP2013.3835 ISSN 1996-0816 African Journal of Pharmacy and Copyright © 2014 Author(s) retain the copyright of this article Pharmacology http://www.academicjournals.org/AJPP Full Length Research Paper Comparative pharmacokinetic study of luteolin after oral administration of Chinese herb compound prescription JiMaiTong in spontaneous hypertensive rats (SHR) and Sprague Dawley (SD) rats Zhao-Huan Lou1, Su-Hong Chen2, Gui-Yuan Lv1*,Bo-Hou Xia1, Mei-Qiu Yan1, Zhi-Ru Zhang1 and Jian-Li Gao1 1Institute of Material Medica, Zhejiang Chinese Medical University, 548 Binwen Road, Hangzhou, 310053, China. 2Academy of Tradition Chinese Medicine, Wenzhou Medical University, Wenzhou 325035, China. Received 7 August, 2013; Accepted 15 April, 2014 JiMaiTong (JMT), a Chinese herb compound prescription consisted of Flos chrysanthemi Indici, Spica prunellae and Semen cassiae for anti-hypertension. Luteolin is one of the major bioactivity compositions in F. chrysanthemi Indici in JMT. There are some reports about pharmacokinetics of luteolin in extract of F. chrysanthemi and husks of peanut in normal rats, but it lacked pharmacokinetic information of luteolin residing in a Chinese herb compound prescription in hypertensive animal models. The present study aimed to develop a high-performance liquid chromatography with photodiode array detection (HPLC-DAD) method for determination of luteolin in rat plasma and for pharmacokinetic study after oral administration of JMT to spontaneous hypertensive rats (SHR) and normal Sprague Dawley (SD) rats. After oral administration of JMT to SHR and SD rats, respectively the content of luteolin in blood samples at different time points were determined by a reversed-phase high- performance liquid chromatography (RP-HPLC) coupled with liquid-liquid phase extraction. -
NTP-CERHR Expert Panel Report on the Reproductive and Developmental Toxicity of Amphetamine and Methamphetamine
Published 2005 Wiley-Liss, Inc.w Birth Defects Research (Part B) 74:471–584 (2005) NTP-CERHR Expert Panel Report on the Reproductive and Developmental Toxicity Of Amphetamine and Methamphetamine Mari Golub,1 Lucio Costa,2 Kevin Crofton,3 Deborah Frank,4 Peter Fried,5 Beth Gladen6 Rogene Henderson,7 Erica Liebelt,8 Shari Lusskin,9 Sue Marty,10 Andrew Rowland11 John Scialli12 and Mary Vore13 1California Environment Protection Agency, Sacramento, California 2University of Washington, Seattle, Washington 3U.S. Environmental Protection Agency, Research Triangle Park, North Carolina 4Boston Medical Center, Boston, Massachusetts 5Carleton University, Ottawa, Ontario 6National Institute of Environmental Health Sciences, Research Triangle Park, North Carolina 7Lovelace Respiratory Research Institute, Albuquerque, New Mexico 8University of Alabama at Birmingham School of Medicine, Birmingham, Alabama 9New York University School of Medicine, New York, New York 10The Dow Chemical Company, Midland, Michigan 11University of New Mexico, Albuquerque, New Mexico 12Phoenix, Arizona 13University of Kentucky, Lexington, Kentucky PREFACE studies indexed before December 31, 2004. References were also identified from databases such as REPRO- The National Toxicology Program (NTP) and the TOXs, HSDB, IRIS, and DART and from report National Institute of Environmental Health Sciences bibliographies. (NIEHS) established the NTP Center for the Evaluation This evaluation resulted from the efforts of a 13- of Risks to Human Reproduction (CERHR) in June 1998. member panel of government and non-government The purpose of the Center is to provide timely, unbiased, scientists that culminated in a public expert panel scientifically sound evaluations of human and experi- meeting held January 10–12, 2005. This report is a mental evidence for adverse effects on reproduction and product of the Expert Panel and is intended to (1) development caused by agents to which humans may be interpret the strength of scientific evidence that exposed. -
Antidepressant-Like Behavioral and Neurochemical Effects of the Citrus
Available online at www.sciencedirect.com Life Sciences 82 (2008) 741–751 www.elsevier.com/locate/lifescie Antidepressant-like behavioral and neurochemical effects of the citrus-associated chemical apigenin ⁎ Li-Tao Yi, Jian-Mei Li, Yu-Cheng Li, Ying Pan, Qun Xu, Ling-Dong Kong State Key Laboratory of Pharmaceutical Biotechnology, School of Life Sciences, Nanjing University, Nanjing 210093, PR China Received 14 July 2007; accepted 16 January 2008 Abstract Apigenin is one type of bioflavonoid widely found in citrus fruits, which possesses a variety of pharmacological actions on the central nervous system. A previous study showed that acute intraperitoneal administration of apigenin had antidepressant-like effects in the forced swimming test (FST) in ddY mice. To better understand its pharmacological activity, we investigated the behavioral effects of chronic oral apigenin treatment in the FST in male ICR mice and male Wistar rats exposed to chronic mild stress (CMS). The effects of apigenin on central monoaminergic neurotransmitter systems, the hypothalamic–pituitary–adrenal (HPA) axis and platelet adenylyl cyclase activity were simultaneously examined in the CMS rats. Apigenin reduced immobility time in the mouse FST and reversed CMS-induced decrease in sucrose intake of rats. Apigenin also attenuated CMS-induced alterations in serotonin (5-HT), its metabolite 5-hydroxyindoleacetic acid (5-HIAA), dopamine (DA) levels and 5-HIAA/ 5-HT ratio in distinct rat brain regions. Moreover, apigenin reversed CMS-induced elevation in serum corticosterone concentrations and reduction in platelet adenylyl cyclase activity in rats. These results suggest that the antidepressant-like actions of oral apigenin treatment could be related to a combination of multiple biochemical effects, and might help to elucidate its mechanisms of action that are involved in normalization of stress- induced changes in brain monoamine levels, the HPA axis, and the platelet adenylyl cyclase activity. -
Chrysoeriol Prevents TNF-Induced CYP19 Gene Expression Via EGR-1
International Journal of Molecular Sciences Article Chrysoeriol Prevents TNFα-Induced CYP19 Gene Expression via EGR-1 Downregulation in MCF7 Breast Cancer Cells Dong Yeong Min 1, Euitaek Jung 1, Sung Shin Ahn 1, Young Han Lee 1,2 , Yoongho Lim 3 and Soon Young Shin 1,2,* 1 Department of Biological Sciences, Sanghuh College of Lifesciences, Konkuk University, Seoul 05029, Korea; [email protected] (D.Y.M.); [email protected] (E.J.); [email protected] (S.S.A.); [email protected] (Y.H.L.) 2 Cancer and Metabolism Institute, Konkuk University, Seoul 05029, Korea 3 Division of Bioscience and Biotechnology, BMIC, Konkuk University, Seoul 05029, Korea; [email protected] * Correspondence: [email protected]; Tel.: +82-2-2030-7946 Received: 27 August 2020; Accepted: 9 October 2020; Published: 12 October 2020 Abstract: Estrogen overproduction is closely associated with the development of estrogen receptor-positive breast cancer. Aromatase, encoded by the cytochrome P450 19 (CYP19) gene, regulates estrogen biosynthesis. This study aimed to identify active flavones that inhibit CYP19 expression and to explore the underlying mechanisms. CYP19 expression was evaluated using reverse transcription PCR, quantitative real-time PCR, and immunoblot analysis. The role of transcription factor early growth response gene 1 (EGR-1) in CYP19 expression was assessed using the short-hairpin RNA (shRNA)-mediated knockdown of EGR-1 expression in estrogen receptor-positive MCF-7 breast cancer cells. We screened 39 flavonoids containing 26 flavones and 13 flavanones using the EGR1 promoter reporter activity assay and observed that chrysoeriol exerted the highest inhibitory activity on tumor necrosis factor alpha (TNFα)-induced EGR-1 expression. -
Wogonin Attenuates Liver Fibrosis Via Regulating Hepatic Stellate Cell
International Immunopharmacology 75 (2019) 105671 Contents lists available at ScienceDirect International Immunopharmacology journal homepage: www.elsevier.com/locate/intimp Wogonin attenuates liver fibrosis via regulating hepatic stellate cell T activation and apoptosis Xiao-Sa Du, Hai-Di Li, Xiao-Juan Yang, Juan-Juan Li, Jie-Jie Xu, Yu Chen, Qing-Qing Xu, ⁎ Lei Yang, Chang-Sheng He, Cheng Huang, Xiao-Ming Meng, Jun Li The Key Laboratory of Major Autoimmune Diseases, Anhui Province, Anhui Institute of Innovative Drugs, School of Pharmacy, Anhui Medical University, China The Key Laboratory of Anti-inflammatory of Immune Medicines, Ministry of Education, Institute for Liver Diseases of Anhui Medical University, China School of Pharmacy, Anhui Key Laboratory of Bioactivity of Natural Products, Anhui Medical University, Hefei 230032, China ARTICLE INFO ABSTRACT Keywords: Liver fibrosis is the representative features of liver chronic inflammation and the characteristic of early cirrhosis. Wogonin To date, effective therapy for liver fibrosis is lacking. Recently, Traditional Chinese Medicine (TCM)hasat- Liver fibrosis tracted increasing attention due to its wide pharmacological effects and more uses in clinical. Wogonin, asone Hepatic stellate cells (HSCs) major active constituent of Scutellaria radix, has been reported it plays an important role in anti-inflammatory, Apoptosis anti-cancer, anti-viral, anti-angiogenesis, anti-oxidant and neuro-protective effects. However, the anti-fibrotic effect of wogonin is never covered in liver. In this study, we evaluated the protect effect of wogonininliver fibrosis. Wogonin significantly attenuated liver fibrosis both4 inCCl -induced mice and TGF-β1 activated HSCs. Meanwhile, wogonin can enhances apoptosis of TGF-β1 activated HSC-T6 cell from rat and LX-2 cell from human detected by flow cytometry. -
Cardiovascular Disease Dyslipidemia | Non-Pharmacologic Treatment |
Cardiovascular Disease Dyslipidemia: Non-Pharmacologic Treatment Mark C. Houston, M.D., M.S. ABAARM, FACP, FACN, FAHA, FASH INTRODUCTION Cardiovascular disease (CVD) is the number one cause of morbidity and mortality in the United States,1 coronary heart disease (CHD) and myocardial infarction being the leading causes of death.1 The five major risk factors for CHD – hypertension, dyslipidemia, diabetes mellitus, smoking, and obesity – account for 80% of the risk for CHD.1,2 Interventions, both pharmacologic and nonpharmacologic, can improve all of these risk factors and decrease the incidence of CVD and its consequences, such as 3-6 myocardial infarction, angina, congestive heart failure and stroke. Recent guidelines by the National Cholesterol Education Program (NCEP) recommend more aggressive control of serum lipids to reduce the incidence of CHD.7 Nutritional and dietary therapy, weight loss, exercise, and scientifically-proven nutritional supplementation should be used initially in appropriately selected patients to manage dyslipidemia. Hypertriglyceridemia, which is frequently due to obesity, insulin resistance, metabolic syndrome and diabetes mellitus, deserves special attention.7 Pharmacologic therapy should be administered in those cases that are at high or very high-risk for CHD and those who do not respond to non-drug therapy. Many patients prefer non-drug therapies for many reasons including adverse effects of anti-lipid drugs, contraindications or allergic reactions to drugs, perceptions of adverse effects of drugs, or personal preference for natural or alternative therapies. A more aggressive integrative approach to the management of dyslipidemia is recommended to improve CHD outcomes, minimize adverse effects, and reduce health-care costs. NUTRITION AND EXERCISE Optimal nutrition and proper aerobic and resistance exercise form the cornerstone for the management of dyslipidemia. -
In Vivo Effect of PC-SPES on Prostate Growth and Hepatic CYP3A Expression in Rats
JPET Fast Forward. Published on April 3, 2003 as DOI: 10.1124/jpet.102.048645 JPETThis Fast article Forward. has not been Published copyedited and on formatted. April 3, The 2003 final asversion DOI:10.1124/jpet.102.048645 may differ from this version. JPET #48645 In Vivo Effect of PC-SPES on Prostate Growth and Hepatic CYP3A Expression in Rats Teri Wadsworth, Hataya Poonyagariyagorn, Elinore Sullivan, Dennis Koop and Charles E. Roselli. Downloaded from Department of Physiology and Pharmacology Oregon Health & Science University, Portland, OR. jpet.aspetjournals.org at ASPET Journals on September 26, 2021 1 Copyright 2003 by the American Society for Pharmacology and Experimental Therapeutics. JPET Fast Forward. Published on April 3, 2003 as DOI: 10.1124/jpet.102.048645 This article has not been copyedited and formatted. The final version may differ from this version. JPET #48645 Running Title: In vivo effects of PC-SPES Correspondence: Dr. Charles E. Roselli, Department of Physiology and Pharmacology L334, Oregon Health Sciences University, 3181 SW Sam Jackson Park Road, Portland, OR 97201-3098, Tel (503) 494-5837, FAX (503) 494-4352, email: [email protected] Number of text pages: 20 number of tables: 4 Downloaded from number of figures: 4 number of references: 40 jpet.aspetjournals.org number of words in the Abstract: 250 number of words the Introduction: 748 number of words in the Discussion: 1478 at ASPET Journals on September 26, 2021 nonstandard abbreviations: National Institute of Diabetes and Digestive and Kidney Disease (NIDDK); -
Current Perspectives in Herbal and Conventional Drug Interactions
Surana et al. Future Journal of Pharmaceutical Sciences (2021) 7:103 Future Journal of https://doi.org/10.1186/s43094-021-00256-w Pharmaceutical Sciences REVIEW Open Access Current perspectives in herbal and conventional drug interactions based on clinical manifestations Ajaykumar Rikhabchand Surana* , Shivam Puranmal Agrawal, Manoj Ramesh Kumbhare and Snehal Balu Gaikwad Abstract Background: Herbs are an important source of pharmaceuticals. Herbs are traditionally used by millions of peoples for medicine, food and drink in developed and developing nations considering that they are safe. But, interaction of herbs with other medicines may cause serious adverse effects or reduces their efficacy. The demand for “alternative” medicines has been increased significantly, which include medicine derived from plant or herbal origin. The objective of this review article mainly focuses on drug interactions of commonly used herbs along with possible mechanisms. The method adopted for this review is searching of herb-drug interactions in online database. Main text: Herb-drug interaction leads to pharmacological modification. The drug use along with herbs may show pharmacodynamic and pharmacokinetic interactions. Pharmacokinetic interaction causes alteration in absorption, distribution, metabolism and elimination. Similarly, pharmacodynamic interaction causes additive or synergistic or antagonist effect on the drugs or vice versa. Researchers had demonstrated that herbs show the toxicities and drug interactions like other pharmacologically active compounds. There is lack of knowledge amongst physician, pharmacist and consumers related to pharmacological action and mechanism of herb-drug interaction. This review article focuses on the herb-drug interaction of danshen (Salvia miltiorrhiza), Echinacea (Echinacea purpurea), garlic (Allium sativum), ginkgo (Ginkgo biloba), goldenseal (Hydrastis canadensis), green tea (Camellia sinensis), kava (Piper methysticum), liquorice (Glycyrrhiza glabra), milk thistle (Silybum marianum) and St. -
List of European Pharmacopoeia Reference Standards Effective From
List of European Pharmacopoeia Reference Standards Effective from 2021/10/6 Order Reference Standard Batch Quantity Sale Information Monograph Storage Shipping Shipment Price Code n° per vial Unit group with DGD Y0001552 Abacavir for peak identification CRS 1 10 mg 1 2589 +5°C+/-3°C A1A 79 € Y0001551 Abacavir for system suitability CRS 1 10 mg 1 2589 +5°C+/-3°C A1A 79 € Y0001561 Abacavir sulfate CRS 1 20 mg 1 2589 +5°C+/-3°C A1A 79 € Y0002199 Acamprosate calcium CRS 1 80 mg 1 See leaflet 1585 +5°C+/-3°C A1A 79 € Y0000055 Acamprosate calcium - reference spectrum 1 n/a 1 This reference standard was officially withdrawn from monograph 1585 L 79 € 01/2017:1585 on 01/01/2021 and replaced by Y0002199 Acamprosate calcium. The reference will however remain available for sale for a further 6 months (subject to stock availability), i.e. until 01/07/2021. The reference will remain visible in the catalogue until 01/01/2022. ; Batch 1 is valid until 1 January 2022 Y0000116 Acamprosate impurity A CRS 2 110 mg 1 3-aminopropane-1-sulfonic acid (homotaurine) 1585 +5°C+/-3°C A1A 79 € Y0000500 Acarbose CRS 3 100 mg 1 See leaflet 2089 +5°C+/-3°C A1A 79 € Y0000354 Acarbose for identification CRS 1 10 mg 1 2089 +5°C+/-3°C A1A 79 € Y0000427 Acarbose for peak identification CRS 4 20 mg 1 2089 +5°C+/-3°C A1A 79 € A0040000 Acebutolol hydrochloride CRS 1 50 mg 1 0871 +5°C+/-3°C A1A 79 € Y0000359 Acebutolol impurity B CRS 2 10 mg 1 N-[3-acetyl-4-[(2RS)-2-hydroxy-3-[(1-methylethyl)amino] 0871 +5°C+/-3°C A1A 79 € propoxy]phenyl]acetamide (diacetolol) Y0000127 Acebutolol