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Highly Potent Visnagin Derivatives Inhibit Cyp1 and Prevent Doxorubicin Cardiotoxicity
Highly potent visnagin derivatives inhibit Cyp1 and prevent doxorubicin cardiotoxicity Aarti Asnani, … , David E. Sosnovik, Randall T. Peterson JCI Insight. 2018;3(1):e96753. https://doi.org/10.1172/jci.insight.96753. Research Article Cardiology Oncology Anthracyclines such as doxorubicin are highly effective chemotherapy agents used to treat many common malignancies. However, their use is limited by cardiotoxicity. We previously identified visnagin as protecting against doxorubicin toxicity in cardiac but not tumor cells. In this study, we sought to develop more potent visnagin analogs in order to use these analogs as tools to clarify the mechanisms of visnagin-mediated cardioprotection. Structure-activity relationship studies were performed in a zebrafish model of doxorubicin cardiomyopathy. Movement of the 5-carbonyl to the 7 position and addition of short ester side chains led to development of visnagin analogs with 1,000-fold increased potency in zebrafish and 250-fold increased potency in mice. Using proteomics, we discovered that doxorubicin caused robust induction of Cytochrome P450 family 1 (CYP1) that was mitigated by visnagin and its potent analog 23. Treatment with structurally divergent CYP1 inhibitors, as well as knockdown of CYP1A, prevented doxorubicin cardiomyopathy in zebrafish. The identification of potent cardioprotective agents may facilitate the development of new therapeutic strategies for patients receiving cardiotoxic chemotherapy. Moreover, these studies support the idea that CYP1 is an important contributor to doxorubicin cardiotoxicity and suggest that modulation of this pathway could be beneficial in the clinical setting. Find the latest version: https://jci.me/96753/pdf RESEARCH ARTICLE Highly potent visnagin derivatives inhibit Cyp1 and prevent doxorubicin cardiotoxicity Aarti Asnani,1,2 Bahoui Zheng,1 Yan Liu,1 You Wang,1 Howard H. -
Synthesis and Biological Activities Of5h-Furo [3,2-G] [1] Benzopyran-5-One Derivatives
IndianJournalof Chemistry Vol. 37B, January1998, pp. 68 - 72 Synthesis and biological activities of5H-furo [3,2-g] [1] benzopyran-5-one derivatives JehanA A Miky& HammoudaH Sharar ChemistryDepartment,Facultyof Science(Girls) 'PharmacologyDepartment,Facultyof Medicine,Al-AzharUniversity,NasrCity,Cairo,Egypt Received30 September1996; accepted(revised)31 May 1997 The acetylation of 4-methoxy and 4,9-dimethoxy-7-methyl-5H-furo-[3,2-g] [1] benzopyran-c-one (visnagin and khellin) 1 a-b with acetic anhydride gives 3-acetyl-visnagin and khellin 2a-b which on reaction with cyanoacetamide, a-cyanothioacetamide, malononitriles or ethyl cyanoacetate yield furobenzopyranyl pyridone derivatives 3 a-h or the possible isomer 4 a-h. When 3-acetyl-visnagin or khellin is treated with bromine 6-(ro-bromoacetyl) visnagin or khellin 5 a-b is obtained. The latter compound on treatment with thiourea and amines forms the 2-substituted-4-(3-furobenzopyranyl) thiazole 6 a-b and 6-(ro-aminoacetyl) furochromone derivatives 8 a-g respectively. The 2-amino-4-(3- furobenzopyranyl) thiazole on condensation with aldehyde yields the iminosubstituted thiazole derivatives 7 a-e. Results of the biological effect of compounds la, 6b, 3a, 8a and 3d on blood pressure in experimental animals have been reported. Benzopyran derivatives are known to have wide were condensed with the appropriate aldehyde (i.e. variety of pharmacological activities!". This benzaldehyde, 4-chlorobenzaldehyde or p-N,N- prompted us to modify this ring and to explore new dimethylaminobenzaldehyde) iminosubstituted thi- activities associated with this nucleus. Herein we azole derivatives 7a-e were obtained (cf. Table I). report the synthesis and biological activity of Analytical and spectroscopic results for all the hitherto unknown derivatives of 3-acetyl-visnagin compounds were in conformity with the assigned and khellin. -
Visnagin—A New Protectant Against Doxorubicin Cardiotoxicity? Inhibition of Mitochondrial Malate Dehydrogenase 2 (MDH2) and Beyond
Editorial Page 1 of 5 Visnagin—a new protectant against doxorubicin cardiotoxicity? Inhibition of mitochondrial malate dehydrogenase 2 (MDH2) and beyond Lei Xi Pauley Heart Center, Division of Cardiology, Virginia Commonwealth University, Richmond, VA 23298-0204, USA Correspondence to: Lei Xi, MD, FAHA. Associate Professor, Division of Cardiology, Box 980204, Virginia Commonwealth University, 1101 East Marshall Street, Room 7-020C, Richmond, VA 23298-0204, USA. Email: [email protected]. Submitted Oct 08, 2015. Accepted for publication Oct 13, 2015. doi: 10.3978/j.issn.2305-5839.2015.10.43 View this article at: http://dx.doi.org/10.3978/j.issn.2305-5839.2015.10.43 Doxorubicin (DOX) is a broad-spectrum and potent with excessive ROS generation in mitochondria (12,13). anthracycline antibiotic that has been widely used since Due to the complex multi-factorial cellular and 1960s as a chemotherapeutic agent to treat a variety of molecular drivers underlying DOX cardiotoxicity, the human cancers (1). Despite its superior anti-cancer efficacy, optimal therapeutic approaches for protection against the clinical use of DOX is often limited by dose-dependent DOX cardiotoxicity have not yet been identified, despite cardiotoxicity, which may lead to irreversible dilated over 40 years of extensive research. Notably Herman et al. cardiomyopathy and congestive heart failure (2,3). Currently in 1972 first introduced bisdioxopiperazine compound as predominant theories for explaining DOX cardiotoxicity a cardioprotective agent against DOX cardiotoxicity (14). include the DOX-induced increase of oxidative stress in The subsequent research in this area led to identification cardiomyocytes (4), alteration of mitochondrial energetics of dexrazoxane, the only drug currently approved by the (5,6), and direct effect on DNA. -
University of Bradford Ethesis
Effect of nanoparticles on human cells from healthy individuals and patients with respiratory diseases. Item Type Thesis Authors Osman, Ilham F. Rights <a rel="license" href="http://creativecommons.org/licenses/ by-nc-nd/3.0/"><img alt="Creative Commons License" style="border-width:0" src="http://i.creativecommons.org/l/by- nc-nd/3.0/88x31.png" /></a><br />The University of Bradford theses are licenced under a <a rel="license" href="http:// creativecommons.org/licenses/by-nc-nd/3.0/">Creative Commons Licence</a>. Download date 23/09/2021 14:42:50 Link to Item http://hdl.handle.net/10454/4864 University of Bradford eThesis This thesis is hosted in Bradford Scholars – The University of Bradford Open Access repository. Visit the repository for full metadata or to contact the repository team © University of Bradford. This work is licenced for reuse under a Creative Commons Licence. EFFECT OF NANOPARTICLES ON HUMAN CELLS FROM HEALTHY INDIVIDUALS AND PATIENTS WITH RESPIRATORY DISEASES ILHAM F. OSMAN MBBS, Khartoum University (Sudan) MSC, Manchester University (UK) PhD UNIVERSITY OF BRADFORD 2010 i Abstract Ever increasing applications of nanomaterials (materials with one or more dimension less than 100 nm) has raised awareness of their potential genotoxicity. They have unique physico–chemical properties and so could have unpredictable effects. Zinc oxide (ZnO) and titanium dioxide (TiO 2) are widely used in a number of commercial products. There are published studies indicating that some forms of these compounds may be photo-clastogenic in mammalian cells. What has not been investigated before is the effect of nanoparticles from these compounds in human germ cells. -
Dietary Plants for the Prevention and Management of Kidney Stones: Preclinical and Clinical Evidence and Molecular Mechanisms
International Journal of Molecular Sciences Review Dietary Plants for the Prevention and Management of Kidney Stones: Preclinical and Clinical Evidence and Molecular Mechanisms Mina Cheraghi Nirumand 1, Marziyeh Hajialyani 2, Roja Rahimi 3, Mohammad Hosein Farzaei 2,*, Stéphane Zingue 4,5 ID , Seyed Mohammad Nabavi 6 and Anupam Bishayee 7,* ID 1 Office of Persian Medicine, Ministry of Health and Medical Education, Tehran 1467664961, Iran; [email protected] 2 Pharmaceutical Sciences Research Center, Kermanshah University of Medical Sciences, Kermanshah 6734667149, Iran; [email protected] 3 Department of Traditional Pharmacy, School of Traditional Medicine, Tehran University of Medical Sciences, Tehran 1416663361, Iran; [email protected] 4 Department of Life and Earth Sciences, Higher Teachers’ Training College, University of Maroua, Maroua 55, Cameroon; [email protected] 5 Department of Animal Biology and Physiology, Faculty of Science, University of Yaoundé 1, Yaounde 812, Cameroon 6 Applied Biotechnology Research Center, Baqiyatallah University of Medical Sciences, Tehran 1435916471, Iran; [email protected] 7 Department of Pharmaceutical Sciences, College of Pharmacy, Larkin University, Miami, FL 33169, USA * Correspondence: [email protected] (M.H.F.); [email protected] or [email protected] (A.B.); Tel.: +98-831-427-6493 (M.H.F.); +1-305-760-7511 (A.B.) Received: 21 January 2018; Accepted: 25 February 2018; Published: 7 March 2018 Abstract: Kidney stones are one of the oldest known and common diseases in the urinary tract system. Various human studies have suggested that diets with a higher intake of vegetables and fruits play a role in the prevention of kidney stones. In this review, we have provided an overview of these dietary plants, their main chemical constituents, and their possible mechanisms of action. -
Chris Olukayode Adedire Fesn " 2·
..,.. CHRIS OLUKAYODE ADEDIRE FESN B.Sc., M.Sc (Ilorin), Ph.D. (lfe) Professor- of Etitomology' " 2· _ place between individuals, between collectivities, or between individuals and collectivities. Intergroup as well as intragroup conflicts are perennial features of social life". In the present context, conflict may be conceptualised as competition for the same resources; notably food, water, nutrients etc - except mating partners and it is interspecific. The Bible attests to the fact that there was ecological equilibrium at the dawn of creation because God said that all the things He created were good (Genesis 1:3 I). However, a significant step in the cultural evolution of man is the development oflarge scale cu Itivation or crops or monoculture and the capacity to store the excess crops so produced. This step, ' significant as it is, also led to the creation of artificial environment for insects; thus resulting in ecological imbalances. The built-up environment, road constructions, impoundment of inland waterways and various other activities associated with human development have all created breeding sites for some insects and intermediate hosts of the causative organisms of diseases at the expense of their natural enem ies. It is apparent, therefore, that either overtly or covertly, many human activities result into conflict either with fellow humans or with other components ofhis other biotic or abiotic environment. Consequently, cdriflicts in this context may be perceived as an integral part of human existence and may not necessarily result in the destruction of human society even though they start and terminate with or without human intervention. Sandole (1993) suggested that nothing.was inherently wrong with conflict but, instead, it.is seen as a catalyst for promoting social development, higher degree social order and new awareness in cooperative living. -
Microlepidoptera.Hu Redigit: Fazekas Imre
Microlepidoptera.hu Redigit: Fazekas Imre 5 2012 Microlepidoptera.hu A magyar Microlepidoptera kutatások hírei Hungarian Microlepidoptera News A journal focussed on Hungarian Microlepidopterology Kiadó—Publisher: Regiograf Intézet – Regiograf Institute Szerkesztő – Editor: Fazekas Imre, e‐mail: [email protected] Társszerkesztők – Co‐editors: Pastorális Gábor, e‐mail: [email protected]; Szeőke Kálmán, e‐mail: [email protected] HU ISSN 2062–6738 Microlepidoptera.hu 5: 1–146. http://www.microlepidoptera.hu 2012.12.20. Tartalom – Contents Elterjedés, biológia, Magyarország – Distribution, biology, Hungary Buschmann F.: Kiegészítő adatok Magyarország Zygaenidae faunájához – Additional data Zygaenidae fauna of Hungary (Lepidoptera: Zygaenidae) ............................... 3–7 Buschmann F.: Két új Tineidae faj Magyarországról – Two new Tineidae from Hungary (Lepidoptera: Tineidae) ......................................................... 9–12 Buschmann F.: Új adatok az Asalebria geminella (Eversmann, 1844) magyarországi előfordulásához – New data Asalebria geminella (Eversmann, 1844) the occurrence of Hungary (Lepidoptera: Pyralidae, Phycitinae) .................................................................................................. 13–18 Fazekas I.: Adatok Magyarország Pterophoridae faunájának ismeretéhez (12.) Capperia, Gillmeria és Stenoptila fajok új adatai – Data to knowledge of Hungary Pterophoridae Fauna, No. 12. New occurrence of Capperia, Gillmeria and Stenoptilia species (Lepidoptera: Pterophoridae) ………………………. -
EU Project Number 613678
EU project number 613678 Strategies to develop effective, innovative and practical approaches to protect major European fruit crops from pests and pathogens Work package 1. Pathways of introduction of fruit pests and pathogens Deliverable 1.3. PART 7 - REPORT on Oranges and Mandarins – Fruit pathway and Alert List Partners involved: EPPO (Grousset F, Petter F, Suffert M) and JKI (Steffen K, Wilstermann A, Schrader G). This document should be cited as ‘Grousset F, Wistermann A, Steffen K, Petter F, Schrader G, Suffert M (2016) DROPSA Deliverable 1.3 Report for Oranges and Mandarins – Fruit pathway and Alert List’. An Excel file containing supporting information is available at https://upload.eppo.int/download/112o3f5b0c014 DROPSA is funded by the European Union’s Seventh Framework Programme for research, technological development and demonstration (grant agreement no. 613678). www.dropsaproject.eu [email protected] DROPSA DELIVERABLE REPORT on ORANGES AND MANDARINS – Fruit pathway and Alert List 1. Introduction ............................................................................................................................................... 2 1.1 Background on oranges and mandarins ..................................................................................................... 2 1.2 Data on production and trade of orange and mandarin fruit ........................................................................ 5 1.3 Characteristics of the pathway ‘orange and mandarin fruit’ ....................................................................... -
Analytical Technology in Nutrition Analysis • Jose M
Analytical Technology in Nutrition in Analytical Analysis Technology • Jose M. Miranda Analytical Technology in Nutrition Analysis Edited by Jose M. Miranda Printed Edition of the Special Issue Published in Molecules www.mdpi.com/journal/molecules Analytical Technology in Nutrition Analysis Analytical Technology in Nutrition Analysis Special Issue Editor Jose M. Miranda MDPI • Basel • Beijing • Wuhan • Barcelona • Belgrade • Manchester • Tokyo • Cluj • Tianjin Special Issue Editor Jose M. Miranda Universidade de Santiago de Compostela Spain Editorial Office MDPI St. Alban-Anlage 66 4052 Basel, Switzerland This is a reprint of articles from the Special Issue published online in the open access journal Molecules (ISSN 1420-3049) (available at: https://www.mdpi.com/si/molecules/Nutrition analysis). For citation purposes, cite each article independently as indicated on the article page online and as indicated below: LastName, A.A.; LastName, B.B.; LastName, C.C. Article Title. Journal Name Year, Article Number, Page Range. ISBN 978-3-03928-764-2 (Hbk) ISBN 978-3-03928-765-9 (PDF) c 2020 by the authors. Articles in this book are Open Access and distributed under the Creative Commons Attribution (CC BY) license, which allows users to download, copy and build upon published articles, as long as the author and publisher are properly credited, which ensures maximum dissemination and a wider impact of our publications. The book as a whole is distributed by MDPI under the terms and conditions of the Creative Commons license CC BY-NC-ND. Contents About the Special Issue Editor ...................................... vii Jose M. Miranda Analytical Technology in Nutrition Analysis Reprinted from: Molecules 2020, 25, 1362, doi:10.3390/molecules25061362 ............ -
Highly Potent Visnagin Derivatives Inhibit Cyp1 and Prevent Doxorubicin Cardiotoxicity
Highly potent visnagin derivatives inhibit Cyp1 and prevent doxorubicin cardiotoxicity Aarti Asnani, … , David E. Sosnovik, Randall T. Peterson JCI Insight. 2018;3(1):e96753. https://doi.org/10.1172/jci.insight.96753. Research Article Cardiology Oncology Anthracyclines such as doxorubicin are highly effective chemotherapy agents used to treat many common malignancies. However, their use is limited by cardiotoxicity. We previously identified visnagin as protecting against doxorubicin toxicity in cardiac but not tumor cells. In this study, we sought to develop more potent visnagin analogs in order to use these analogs as tools to clarify the mechanisms of visnagin-mediated cardioprotection. Structure-activity relationship studies were performed in a zebrafish model of doxorubicin cardiomyopathy. Movement of the 5-carbonyl to the 7 position and addition of short ester side chains led to development of visnagin analogs with 1,000-fold increased potency in zebrafish and 250-fold increased potency in mice. Using proteomics, we discovered that doxorubicin caused robust induction of Cytochrome P450 family 1 (CYP1) that was mitigated by visnagin and its potent analog 23. Treatment with structurally divergent CYP1 inhibitors, as well as knockdown of CYP1A, prevented doxorubicin cardiomyopathy in zebrafish. The identification of potent cardioprotective agents may facilitate the development of new therapeutic strategies for patients receiving cardiotoxic chemotherapy. Moreover, these studies support the idea that CYP1 is an important contributor to doxorubicin cardiotoxicity and suggest that modulation of this pathway could be beneficial in the clinical setting. Find the latest version: https://jci.me/96753/pdf RESEARCH ARTICLE Highly potent visnagin derivatives inhibit Cyp1 and prevent doxorubicin cardiotoxicity Aarti Asnani,1,2 Baohui Zheng,1 Yan Liu,1 You Wang,1 Howard H. -
Lepidoptera: Pyralidae]
Pak. J. Sci. Ind. Res. 2009 52 (6) 322-327 Effects of Delayed Mating on Reproductive Performance of Ephestia cautella [Walker] [Lepidoptera: Pyralidae] J. O. Akinneye* and M. O. Ashamo Storage Research Laboratory, Department of Biology, Federal University of Technology, Akure, Nigeria (received January 26, 2009; revised September 30, 2009; accepted October 10, 2009) Abstract. The effect of age at mating of male and female warehouse moth, Ephestia cautella (Walker), soon after the emergence or delayed for 1-5 days was studied on the number of eggs laid (fecundity), egg viability, longevity and adult emergence. It was found that with the delay in mating after emergence of male, female or both, the number of eggs laid decreased proportionately. Egg viability decreased when female or both male and female were delayed from mating for more than 4 days. Male insects, that were delayed from mating, lived longer than the females delayed from mating. Average male and female longevity in all the treatments was 10 and 7 days, respectively. Delayed mating had significant effect on females than on males. Unmated males lived longer than the mated males. Thus methods that can delay and disrupt mating may be effective behavioural strategies for managing E. cautella. Keywords: Ephestia cautella, mating delay, longevity, adult emergence, eggs Introduction history traits including the number of eggs laid (fecundity), The stored product moths are cosmopolitan, infesting a wide egg viability, pre-oviposition success and longevity (Jiao variety of harvest and food products such as cereals, dried et al., 2006; Fangneng and Bhadriraju, 2003; Peralta et al., fruits, cocoa beans, chocolates, candies and confectionery. -
A Provisional Checklist and Bibliography of the Pyraloidea of the Balkan Peninsula (Lepidoptera: Pyralidae & Crambidae) by Colin W
Atalanta 49 (1-4): 219-263, Marktleuthen (1. September 2018), ISSN 0171-0079 A provisional checklist and bibliography of the Pyraloidea of the Balkan Peninsula (Lepidoptera: Pyralidae & Crambidae) by COLIN W. PLANT & PREDRAG JAKšIć received 28.V.2018 Abstract: A literature search was undertaken by us to locate all published data on the Pyraloidea (Lepidoptera: Crambidae & Pyralidae) of the Balkan Peninsula of south-east Europe. All known paper publications to the end of June 2018 were researched. All publications apparently containing relevant data were read and scrutinised by us and valid data extracted to a database. With the exception of the Fauna Europaea and Lepiforum websites, electronic sources were not searched, because initial examination suggested that these were likely to include non-corroborated data. From the results of this exercise, a checklist of 569 species of Py- raloidea recorded in the Balkans (310 Crambidae and 259 Pyralidae) was created along with a bibliography of the 426 works con- sulted. Forty-four of the species in the checklist (~8%) were not included for the same area in a 1996 European checklist; this may reflect a genuine change in the fauna over the last quarter century. Some updating of nomenclature and related matters has been undertaken, but we have done only minimal checking of the data itself to eliminate any incorrect records. It should be noted that no attempt has been made to determine if the listed species remain extant within each country at year 2018 nor is any comment made concerning present-day status of any species. Both the checklist and the bibliography are regarded as provisional; a database will be maintained by the authors and will be updated from time to time.