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Neuroprotective Effect of Fisetin Through Suppression of IL-1R/TLR Axis and Apoptosis in Pentylenetetrazole-Induced Kindling in Mice
ORIGINAL RESEARCH published: 21 July 2021 doi: 10.3389/fneur.2021.689069 Neuroprotective Effect of Fisetin Through Suppression of IL-1R/TLR Axis and Apoptosis in Pentylenetetrazole-Induced Kindling in Mice Saima Khatoon 1, Nidhi Bharal Agarwal 2*, Mohammed Samim 3 and Ozair Alam 4 1 Department of Medical Elementology and Toxicology, School of Chemical and Life Sciences, Jamia Hamdard, New Delhi, India, 2 Centre for Translational and Clinical Research, School of Chemical and Life Sciences, Jamia Hamdard, New Delhi, India, 3 Department of Chemistry, School of Chemical and Life Sciences, Jamia Hamdard, New Delhi, India, 4 Department of Pharmaceutical Chemistry, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi, India Epilepsy is a complex neurological disorder, characterized by frequent electrical activity in brain regions. Inflammation and apoptosis cascade activation are serious neurological sequelae during seizures. Fisetin (3, 3′,4′,7-tetrahydroxyflavone), a flavonoid molecule, is considered for its effective anti-inflammatory and anti-apoptotic properties. This study Edited by: investigated the neuroprotective effect of fisetin on experimental epilepsy. For acute Mohd Farooq Shaikh, studies, increasing current electroshock (ICES) and pentylenetetrazole (PTZ)-induced Monash University, Malaysia seizure tests were performed to evaluate the antiseizure activity of fisetin. For the chronic Reviewed by: Shuai Guo, study, the kindling model was established by the administration of PTZ in subconvulsive Huazhong Agricultural dose (25 mg/kg, i.p.). Mice were treated with fisetin (5, 10, and 20 mg/kg, p.o.) to study University, China Syed Shadab Raza, its probable antiseizure mechanism. The kindled mice were evaluated for seizure scores. ERA’s Lucknow Medical College, India Their hippocampus and cortex were assessed for neuronal damage, inflammation, and *Correspondence: apoptosis. -
Anti-Inflammatory Effects of Kaempferol, Myricetin, Fisetin and Ibuprofen in Neonatal Rats
Guo & Feng Tropical Journal of Pharmaceutical Research August 2017; 16 (8): 1819-1826 ISSN: 1596-5996 (print); 1596-9827 (electronic) © Pharmacotherapy Group, Faculty of Pharmacy, University of Benin, Benin City, 300001 Nigeria. All rights reserved. Available online at http://www.tjpr.org http://dx.doi.org/10.4314/tjpr.v16i8.10 Original Research Article Anti-inflammatory effects of kaempferol, myricetin, fisetin and ibuprofen in neonatal rats Peng Guo and Yun-Yun Feng* The Second Pediatric Department of Internal Medicine, Zhumadian Central Hospital, Zhumadian, No. 747 Zhonghua Road, Zhumadian, Henan Province 463000, China *For correspondence: Email: [email protected]; Tel/Fax: 0086-0396-2726840 Sent for review: 9 September 2016 Revised accepted: 14 July 2017 Abstract Purpose: To investigate the anti-inflammatory effects of kaempferol, myricetin, fisetin and ibuprofen in rat pups. Methods: The expression levels of cyclooxygenase (COX)-1, COX-2 and tumour necrosis factor-α (TNF-α) were determined by western blotting; the inhibition of these proteins by plant compounds was evaluated. In addition, a computational simulation of the molecular interactions of the compounds at the active sites of the proteins was performed using a molecular docking approach. Absorption, distribution, metabolism and excretion (ADME) and toxicity analysis of the plant compounds was also performed. Results: Kaempferol, myricetin and fisetin inhibited the activities of COX-1, COX-2 and TNF-α by 70–88 %. The computational simulation revealed the molecular interactions of these compounds at the active sites of COX-1, COX-2 and TNF-α. ADME and toxicity analysis demonstrated that the three plant compounds were safe. Conclusion: The data obtained indicate that myricetin, kaempferol and fisetin exert anti-inflammatory effects in neonatal rats, with fewer side effects than those of ibuprofen. -
Theoretical and Kinetic Tools for Selecting Effective Antioxidants: Application to the Protection of Omega-3 Oils with Natural and Synthetic Phenols
International Journal of Molecular Sciences Article Theoretical and Kinetic Tools for Selecting Effective Antioxidants: Application to the Protection of Omega-3 Oils with Natural and Synthetic Phenols Romain Guitard, Véronique Nardello-Rataj * and Jean-Marie Aubry * Univ. Lille, CNRS, Centrale Lille, ENSCL, Univ. Artois, UMR 8181–UCCS-Unité de Catalyse et Chimie du Solide, F-59000 Lille, France; [email protected] * Correspondence: [email protected] (V.N.-R.); [email protected] (J.-M.A.); Tel.: +33-3-2033-6369 (V.N.-R.); +33-3-2033-6364 (J.-M.A.) Academic Editor: Maria Laura Colombo Received: 3 June 2016; Accepted: 21 July 2016; Published: 29 July 2016 Abstract: Radical-scavenging antioxidants play crucial roles in the protection of unsaturated oils against autoxidation and, especially, edible oils rich in omega-3 because of their high sensitivity to oxygen. Two complementary tools are employed to select, among a large set of natural and synthetic phenols, the most promising antioxidants. On the one hand, density functional theory (DFT) calculations provide bond dissociation enthalpies (BDEs) of 70 natural (i.e., tocopherols, hydroxybenzoic and cinnamic acids, flavonoids, stilbenes, lignans, and coumarins) and synthetic (i.e., 2,6-di-tert-butyl-4-methylphenol (BHT), 3-tert-butyl-4-hydroxyanisol (BHA), and tert-butylhydroquinone (TBHQ)) phenols. These BDEs are discussed on the basis of structure–activity relationships with regard to their potential antioxidant activities. On the other hand, the kinetic rate constants and number of hydrogen atoms released per phenol molecule are measured by monitoring the reaction of phenols with 2,2-diphenyl-1-picrylhydrazyl (DPPH‚) radical. -
Suspect and Target Screening of Natural Toxins in the Ter River Catchment Area in NE Spain and Prioritisation by Their Toxicity
toxins Article Suspect and Target Screening of Natural Toxins in the Ter River Catchment Area in NE Spain and Prioritisation by Their Toxicity Massimo Picardo 1 , Oscar Núñez 2,3 and Marinella Farré 1,* 1 Department of Environmental Chemistry, IDAEA-CSIC, 08034 Barcelona, Spain; [email protected] 2 Department of Chemical Engineering and Analytical Chemistry, University of Barcelona, 08034 Barcelona, Spain; [email protected] 3 Serra Húnter Professor, Generalitat de Catalunya, 08034 Barcelona, Spain * Correspondence: [email protected] Received: 5 October 2020; Accepted: 26 November 2020; Published: 28 November 2020 Abstract: This study presents the application of a suspect screening approach to screen a wide range of natural toxins, including mycotoxins, bacterial toxins, and plant toxins, in surface waters. The method is based on a generic solid-phase extraction procedure, using three sorbent phases in two cartridges that are connected in series, hence covering a wide range of polarities, followed by liquid chromatography coupled to high-resolution mass spectrometry. The acquisition was performed in the full-scan and data-dependent modes while working under positive and negative ionisation conditions. This method was applied in order to assess the natural toxins in the Ter River water reservoirs, which are used to produce drinking water for Barcelona city (Spain). The study was carried out during a period of seven months, covering the expected prior, during, and post-peak blooming periods of the natural toxins. Fifty-three (53) compounds were tentatively identified, and nine of these were confirmed and quantified. Phytotoxins were identified as the most frequent group of natural toxins in the water, particularly the alkaloids group. -
The Metabolites of the Dietary Flavonoid Quercetin Possess Potent Antithrombotic Activity, and Interact with Aspirin to Enhance Antiplatelet Effects
The metabolites of the dietary flavonoid quercetin possess potent antithrombotic activity, and interact with aspirin to enhance antiplatelet effects Article Published Version Creative Commons: Attribution 4.0 (CC-BY) Open Access Stainer, A. R., Sasikumar, P., Bye, A. P., Unsworth, A. P., Holbrook, L. M., Tindall, M., Lovegrove, J. A. and Gibbins, J. M. (2019) The metabolites of the dietary flavonoid quercetin possess potent antithrombotic activity, and interact with aspirin to enhance antiplatelet effects. TH Open, 3 (3). e244- e258. ISSN 2512-9465 doi: https://doi.org/10.1055/s-0039- 1694028 Available at http://centaur.reading.ac.uk/85495/ It is advisable to refer to the publisher’s version if you intend to cite from the work. See Guidance on citing . To link to this article DOI: http://dx.doi.org/10.1055/s-0039-1694028 Publisher: Thieme All outputs in CentAUR are protected by Intellectual Property Rights law, including copyright law. Copyright and IPR is retained by the creators or other copyright holders. Terms and conditions for use of this material are defined in the End User Agreement . www.reading.ac.uk/centaur CentAUR Central Archive at the University of Reading Reading’s research outputs online Published online: 30.07.2019 THIEME e244 Original Article The Metabolites of the Dietary Flavonoid Quercetin Possess Potent Antithrombotic Activity, and Interact with Aspirin to Enhance Antiplatelet Effects Alexander R. Stainer1 Parvathy Sasikumar1,2 Alexander P. Bye1 Amanda J. Unsworth1,3 Lisa M. Holbrook1,4 Marcus Tindall5 Julie A. Lovegrove6 Jonathan M. Gibbins1 1 Institute for Cardiovascular and Metabolic Research, School of Address for correspondence Jonathan M. -
Astragalin: a Bioactive Phytochemical with Potential Therapeutic Activities
Hindawi Advances in Pharmacological Sciences Volume 2018, Article ID 9794625, 15 pages https://doi.org/10.1155/2018/9794625 Review Article Astragalin: A Bioactive Phytochemical with Potential Therapeutic Activities Ammara Riaz,1 Azhar Rasul ,1 Ghulam Hussain,2 Muhammad Kashif Zahoor ,1 Farhat Jabeen,1 Zinayyera Subhani,3 Tahira Younis,1 Muhammad Ali,1 Iqra Sarfraz,1 and Zeliha Selamoglu4 1Department of Zoology, Faculty of Life Sciences, Government College University, Faisalabad 38000, Pakistan 2Department of Physiology, Faculty of Life Sciences, Government College University, Faisalabad 38000, Pakistan 3Department of Biochemistry, University of Agriculture, Faisalabad 38000, Pakistan 4Department of Medical Biology, Faculty of Medicine, Nigde O¨ mer Halisdemir University, Nigde 51240, Turkey Correspondence should be addressed to Azhar Rasul; [email protected] Received 8 January 2018; Revised 5 April 2018; Accepted 12 April 2018; Published 2 May 2018 Academic Editor: Paola Patrignani Copyright © 2018 Ammara Riaz et al. %is 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. Natural products, an infinite treasure of bioactive chemical entities, persist as an inexhaustible resource for discovery of drugs. %is review article intends to emphasize on one of the naturally occurring flavonoids, astragalin (kaempferol 3-glucoside), which is a bioactive constituent of various traditional -
Sephadex® LH-20, Isolation, and Purification of Flavonoids from Plant
molecules Review Sephadex® LH-20, Isolation, and Purification of Flavonoids from Plant Species: A Comprehensive Review Javad Mottaghipisheh 1,* and Marcello Iriti 2,* 1 Department of Pharmacognosy, Faculty of Pharmacy, University of Szeged, Eötvös u. 6, 6720 Szeged, Hungary 2 Department of Agricultural and Environmental Sciences, Milan State University, via G. Celoria 2, 20133 Milan, Italy * Correspondence: [email protected] (J.M.); [email protected] (M.I.); Tel.: +36-60702756066 (J.M.); +39-0250316766 (M.I.) Academic Editor: Francesco Cacciola Received: 20 August 2020; Accepted: 8 September 2020; Published: 10 September 2020 Abstract: Flavonoids are considered one of the most diverse phenolic compounds possessing several valuable health benefits. The present study aimed at gathering all correlated reports, in which Sephadex® LH-20 (SLH) has been utilized as the final step to isolate or purify of flavonoid derivatives among all plant families. Overall, 189 flavonoids have been documented, while the majority were identified from the Asteraceae, Moraceae, and Poaceae families. Application of SLH has led to isolate 79 flavonols, 63 flavones, and 18 flavanones. Homoisoflavanoids, and proanthocyanidins have only been isolated from the Asparagaceae and Lauraceae families, respectively, while the Asteraceae was the richest in flavones possessing 22 derivatives. Six flavones, four flavonols, three homoisoflavonoids, one flavanone, a flavanol, and an isoflavanol have been isolated as the new secondary metabolites. This technique has been able to isolate quercetin from 19 plant species, along with its 31 derivatives. Pure methanol and in combination with water, chloroform, and dichloromethane have generally been used as eluents. This comprehensive review provides significant information regarding to remarkably use of SLH in isolation and purification of flavonoids from all the plant families; thus, it might be considered an appreciable guideline for further phytochemical investigation of these compounds. -
Guava (Psidium Guajava L.) Leaves: Nutritional Composition, Phytochemical Profile, and Health-Promoting Bioactivities
foods Review Guava (Psidium guajava L.) Leaves: Nutritional Composition, Phytochemical Profile, and Health-Promoting Bioactivities Manoj Kumar 1 , Maharishi Tomar 2, Ryszard Amarowicz 3,* , Vivek Saurabh 4 , M. Sneha Nair 5, Chirag Maheshwari 6, Minnu Sasi 7, Uma Prajapati 4, Muzaffar Hasan 8, Surinder Singh 9, Sushil Changan 10 , Rakesh Kumar Prajapat 11, Mukesh K. Berwal 12 and Varsha Satankar 13 1 Chemical and Biochemical Processing Division, ICAR—Central Institute for Research on Cotton Technology, Mumbai 400019, India; [email protected] 2 ICAR—Indian Grassland and Fodder Research Institute, Jhansi 284003, India; [email protected] 3 Institute of Animal Reproduction and Food Research, Polish Academy of Sciences, Tuwima 10 Str., 10-748 Olsztyn, Poland 4 Division of Food Science and Postharvest Technology, ICAR—Indian Agricultural Research Institute, New Delhi 110012, India; [email protected] (V.S.); [email protected] (U.P.) 5 Department of Nutrition and Dietetics, Faculty of Allied Health Sciences, Manav Rachna International Institute of Research and Studies, Faridabad 121004, Haryana, India; [email protected] 6 Department of Agriculture Energy and Power, ICAR—Central Institute of Agricultural Engineering, Bhopal 462038, India; [email protected] 7 Division of Biochemistry, ICAR—Indian Agricultural Research Institute, New Delhi 110012, India; [email protected] 8 Agro Produce Processing Division, ICAR—Central Institute of Agricultural Engineering, Citation: Kumar, M.; Tomar, M.; Bhopal 462038, India; [email protected] 9 Amarowicz, R.; Saurabh, V.; Nair, Dr. S.S. Bhatnagar University Institute of Chemical Engineering and Technology, Panjab University, Chandigarh 160014, India; [email protected] M.S.; Maheshwari, C.; Sasi, M.; 10 Division of Crop Physiology, Biochemistry and Post-Harvest Technology, ICAR—Central Potato Research Prajapati, U.; Hasan, M.; Singh, S.; Institute, Shimla 171001, India; [email protected] et al. -
Flavonoid Glucodiversification with Engineered Sucrose-Active Enzymes Yannick Malbert
Flavonoid glucodiversification with engineered sucrose-active enzymes Yannick Malbert To cite this version: Yannick Malbert. Flavonoid glucodiversification with engineered sucrose-active enzymes. Biotechnol- ogy. INSA de Toulouse, 2014. English. NNT : 2014ISAT0038. tel-01219406 HAL Id: tel-01219406 https://tel.archives-ouvertes.fr/tel-01219406 Submitted on 22 Oct 2015 HAL is a multi-disciplinary open access L’archive ouverte pluridisciplinaire HAL, est archive for the deposit and dissemination of sci- destinée au dépôt et à la diffusion de documents entific research documents, whether they are pub- scientifiques de niveau recherche, publiés ou non, lished or not. The documents may come from émanant des établissements d’enseignement et de teaching and research institutions in France or recherche français ou étrangers, des laboratoires abroad, or from public or private research centers. publics ou privés. Last name: MALBERT First name: Yannick Title: Flavonoid glucodiversification with engineered sucrose-active enzymes Speciality: Ecological, Veterinary, Agronomic Sciences and Bioengineering, Field: Enzymatic and microbial engineering. Year: 2014 Number of pages: 257 Flavonoid glycosides are natural plant secondary metabolites exhibiting many physicochemical and biological properties. Glycosylation usually improves flavonoid solubility but access to flavonoid glycosides is limited by their low production levels in plants. In this thesis work, the focus was placed on the development of new glucodiversification routes of natural flavonoids by taking advantage of protein engineering. Two biochemically and structurally characterized recombinant transglucosylases, the amylosucrase from Neisseria polysaccharea and the α-(1→2) branching sucrase, a truncated form of the dextransucrase from L. Mesenteroides NRRL B-1299, were selected to attempt glucosylation of different flavonoids, synthesize new α-glucoside derivatives with original patterns of glucosylation and hopefully improved their water-solubility. -
Shilin Yang Doctor of Philosophy
PHYTOCHEMICAL STUDIES OF ARTEMISIA ANNUA L. THESIS Presented by SHILIN YANG For the Degree of DOCTOR OF PHILOSOPHY of the UNIVERSITY OF LONDON DEPARTMENT OF PHARMACOGNOSY THE SCHOOL OF PHARMACY THE UNIVERSITY OF LONDON BRUNSWICK SQUARE, LONDON WC1N 1AX ProQuest Number: U063742 All rights reserved INFORMATION TO ALL USERS The quality of this reproduction is dependent upon the quality of the copy submitted. In the unlikely event that the author did not send a com plete manuscript and there are missing pages, these will be noted. Also, if material had to be removed, a note will indicate the deletion. uest ProQuest U063742 Published by ProQuest LLC(2017). Copyright of the Dissertation is held by the Author. All rights reserved. This work is protected against unauthorized copying under Title 17, United States C ode Microform Edition © ProQuest LLC. ProQuest LLC. 789 East Eisenhower Parkway P.O. Box 1346 Ann Arbor, Ml 48106- 1346 ACKNOWLEDGEMENT I wish to express my sincere gratitude to Professor J.D. Phillipson and Dr. M.J.O’Neill for their supervision throughout the course of studies. I would especially like to thank Dr. M.F.Roberts for her great help. I like to thank Dr. K.C.S.C.Liu and B.C.Homeyer for their great help. My sincere thanks to Mrs.J.B.Hallsworth for her help. I am very grateful to the staff of the MS Spectroscopy Unit and NMR Unit of the School of Pharmacy, and the staff of the NMR Unit, King’s College, University of London, for running the MS and NMR spectra. -
Research Article Simultaneous Extraction Optimization And
Hindawi Publishing Corporation ISRN Biotechnology Volume 2013, Article ID 450948, 10 pages http://dx.doi.org/10.5402/2013/450948 Research Article Simultaneous Extraction Optimization and Analysis of Flavonoids from the Flowers of Tabernaemontana heyneana by High Performance Liquid Chromatography Coupled to Diode Array Detector and Electron Spray Ionization/Mass Spectrometry Thiyagarajan Sathishkumar,1 Ramakrishnan Baskar,1 Mohan Aravind,1 Suryanarayanan Tilak,1 Sri Deepthi,1 and Vellalore Maruthachalam Bharathikumar2 1 Department of Biotechnology, Kumaraguru College of Technology, Coimbatore 641049, India 2 Department of Biochemistry, University of Saskatchewan, Saskatoon, SK, Canada S7N 5E5 Correspondence should be addressed to iyagarajan Sathishkumar; [email protected] Received 24 June 2012; Accepted 9 August 2012 Academic Editors: Y. H. Cheong, H. Kakeshita, W. A. Kues, and D. Pant Copyright © 2013 iyagarajan Sathishkumar et al. is 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. Flavonoids are exploited as antioxidants, antimicrobial, antithrombogenic, antiviral, and antihypercholesterolemic agents. Normally, conventional extraction techniques like soxhlet or shake �ask methods provide low yield of �avonoids with structural loss, and thereby, these techniques may be considered as inefficient. In this regard, an attempt was made to optimize the �avonoid extraction using orthogonal design of experiment and subsequent structural elucidation by high-performance liquid chromatography-diode array detector-electron spray ionization/mass spectrometry (HPLC-DAD-ESI/MS) techniques. e shake �ask method of �avonoid extraction was observed to provide a yield of (mg/g tissue). With the two different solvents, namely, ethanol and ethyl acetate, tried for the extraction optimization of �avonoid, ethanol (80.1 mg/g tissue) has been proved better than ethyl acetate (20.5 mg/g tissue). -
The Role of Selected Flavonols in Tumor Necrosis Factor-Related Apoptosis-Inducing Ligand Receptor–1 (TRAIL-R1) Expression on Activated RAW 264.7 Macrophages
Molecules 2015, 20, 900-912; doi:10.3390/molecules20010900 OPEN ACCESS molecules ISSN 1420-3049 www.mdpi.com/journal/molecules Article The Role of Selected Flavonols in Tumor Necrosis Factor-Related Apoptosis-Inducing Ligand Receptor–1 (TRAIL-R1) Expression on Activated RAW 264.7 Macrophages Monika Warat 1, Tadeusz Sadowski 2, Ewelina Szliszka 1, Wojciech Król 1 and Zenon P. Czuba 1,* 1 School of Medicine with the Division of Dentistry in Zabrze, Medical University of Silesia in Katowice, Chair and Department of Microbiology and Immunology, Jordana 19, 41-808 Zabrze, Poland; E-Mails: [email protected] (M.W.); [email protected] (E.S.); [email protected] (W.K.) 2 School of Public Health in Bytom, Medical University of Silesia in Katowice, Toxicology and Drug Addiction Division, Communal Department of Hygiene and Sanitary Supervision, Medyków 18, 40-752 Katowice, Poland; E-Mail: [email protected] * Author to whom correspondence should be addressed; E-Mail: [email protected]; Tel./Fax: +48-32-272-25-54. Academic Editor: Marcello Iriti Received: 24 November 2014 / Accepted: 5 January 2015 / Published: 8 January 2015 Abstract: Tumor Necrosis Factor-Related Apoptosis-Inducing Ligand Receptors (TRAIL-R) are an important factor of apoptosis in cancer cells. There are no data about the effect of flavonols on the receptor expression on a surface of macrophage like cells. In this study, the expression level of TRAIL-R1 on murine RAW264.7 macrophages in the presence of selected flavonols: galangin, kaempferol, kaempferide and quercetin, which differ from their phenyl ring substituents, were studied. The expression of TRAIL-R1 death receptors on non-stimulated and lipopolysaccharide (LPS)-stimulated macrophages was determined using flow cytometry.