Journal of Food Bioactives
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INVESTIGATION of NATURAL PRODUCT SCAFFOLDS for the DEVELOPMENT of OPIOID RECEPTOR LIGANDS by Katherine M
INVESTIGATION OF NATURAL PRODUCT SCAFFOLDS FOR THE DEVELOPMENT OF OPIOID RECEPTOR LIGANDS By Katherine M. Prevatt-Smith Submitted to the graduate degree program in Medicinal Chemistry and the Graduate Faculty of the University of Kansas in partial fulfillment of the requirements for the degree of Doctor of Philosophy. _________________________________ Chairperson: Dr. Thomas E. Prisinzano _________________________________ Dr. Brian S. J. Blagg _________________________________ Dr. Michael F. Rafferty _________________________________ Dr. Paul R. Hanson _________________________________ Dr. Susan M. Lunte Date Defended: July 18, 2012 The Dissertation Committee for Katherine M. Prevatt-Smith certifies that this is the approved version of the following dissertation: INVESTIGATION OF NATURAL PRODUCT SCAFFOLDS FOR THE DEVELOPMENT OF OPIOID RECEPTOR LIGANDS _________________________________ Chairperson: Dr. Thomas E. Prisinzano Date approved: July 18, 2012 ii ABSTRACT Kappa opioid (KOP) receptors have been suggested as an alternative target to the mu opioid (MOP) receptor for the treatment of pain because KOP activation is associated with fewer negative side-effects (respiratory depression, constipation, tolerance, and dependence). The KOP receptor has also been implicated in several abuse-related effects in the central nervous system (CNS). KOP ligands have been investigated as pharmacotherapies for drug abuse; KOP agonists have been shown to modulate dopamine concentrations in the CNS as well as attenuate the self-administration of cocaine in a variety of species, and KOP antagonists have potential in the treatment of relapse. One drawback of current opioid ligand investigation is that many compounds are based on the morphine scaffold and thus have similar properties, both positive and negative, to the parent molecule. Thus there is increasing need to discover new chemical scaffolds with opioid receptor activity. -
Opportunities and Pharmacotherapeutic Perspectives
biomolecules Review Anticoronavirus and Immunomodulatory Phenolic Compounds: Opportunities and Pharmacotherapeutic Perspectives Naiara Naiana Dejani 1 , Hatem A. Elshabrawy 2 , Carlos da Silva Maia Bezerra Filho 3,4 and Damião Pergentino de Sousa 3,4,* 1 Department of Physiology and Pathology, Federal University of Paraíba, João Pessoa 58051-900, Brazil; [email protected] 2 Department of Molecular and Cellular Biology, College of Osteopathic Medicine, Sam Houston State University, Conroe, TX 77304, USA; [email protected] 3 Department of Pharmaceutical Sciences, Federal University of Paraíba, João Pessoa 58051-900, Brazil; [email protected] 4 Postgraduate Program in Bioactive Natural and Synthetic Products, Federal University of Paraíba, João Pessoa 58051-900, Brazil * Correspondence: [email protected]; Tel.: +55-83-3216-7347 Abstract: In 2019, COVID-19 emerged as a severe respiratory disease that is caused by the novel coronavirus, Severe Acute Respiratory Syndrome Coronavirus-2 (SARS-CoV-2). The disease has been associated with high mortality rate, especially in patients with comorbidities such as diabetes, cardiovascular and kidney diseases. This could be attributed to dysregulated immune responses and severe systemic inflammation in COVID-19 patients. The use of effective antiviral drugs against SARS-CoV-2 and modulation of the immune responses could be a potential therapeutic strategy for Citation: Dejani, N.N.; Elshabrawy, COVID-19. Studies have shown that natural phenolic compounds have several pharmacological H.A.; Bezerra Filho, C.d.S.M.; properties, including anticoronavirus and immunomodulatory activities. Therefore, this review de Sousa, D.P. Anticoronavirus and discusses the dual action of these natural products from the perspective of applicability at COVID-19. -
A Review on Amentoflavone
Indo American Journal of Pharmaceutical Research, 2017 ISSN NO: 2231-6876 A REVIEW ON AMENTOFLAVONE * Aroosa Siddique , Madiha Jabeen, Osman Ahmed Department of Pharmaceutical Chemistry, Deccan School of Pharmacy, Hyderabad, T.S. ARTICLE INFO ABSTRACT Article history Amentoflavone, is a bioflavonoid constituent of some of flora which includes ginkgo biloba, Received 06/02/2017 hypericum perforatum. It can have interaction with many medicinal drugs by using being a Available online potent inhibitor of CYP3A4 and CYP2C9 which are enzymes chargeable for the metabolism 28/02/2017 of some drugs in the body. Flavonoids exhibit a extensive variety of activities including antioxidant, antiviral, Antibacterial and anticancer pastime. As formerly we showed that Keywords amentoflavone is an activator of hPPARγ. Human PPARγ (hPPARγ) regulates the Amentoflavone, proliferation, apoptosis, and various human most cancers cells. Activated hPPARγ has both Flavonoid, tumor suppressor and tumor promoter. To affirm the mechanism of motion of amentoflavone Synthetic, in most cancers cells, we analyzed whether or not amentoflavone remedy affects the RSV, Hpparγ, appearance of hPPARy the use of opposite transcription polymerase chain response and CYP3A4 & CYP2C9. actual time quantitive PCR. Amentoflavone is synthesized with the aid of way of three techniques i.e natural, semi synthetic and synthetic methods. Among this synthetic method is widely used industrially. Application of the Suzuki-Miyaura response within the synthesis of flavonoids, is of vital magnificence of natural merchandise, is studied. Amentoflavone and three different flavonoids were separated from the ethanol extract of Selaginella sinensis. Amentoflavone show strong antiviral pastime in opposition to respiratory syncytial virus (RSV). The cytotoxic interest of amentoflavone is examined against 5 human most cancers cell strains (MCF-7, A549, HeLa, MDA-MB231, and PC3) treating with tetrazolium- primarily based colorimetric MTT assay. -
Effect of Sourdough Fermentation on Lunasin-Like Polypeptides
Rizzello et al. Microb Cell Fact (2015) 14:168 DOI 10.1186/s12934-015-0358-6 RESEARCH Open Access Italian legumes: effect of sourdough fermentation on lunasin‑like polypeptides Carlo Giuseppe Rizzello1*, Blanca Hernández‑Ledesma2, Samuel Fernández‑Tomé2, José Antonio Curiel1, Daniela Pinto3, Barbara Marzani3, Rossana Coda4 and Marco Gobbetti1 Abstract Background: There is an increasing interest toward the use of legumes in food industry, mainly due to the qual‑ ity of their protein fraction. Many legumes are cultivated and consumed around the world, but few data is available regarding the chemical or technological characteristics, and especially on their suitability to be fermented. Never‑ theless, sourdough fermentation with selected lactic acid bacteria has been recognized as the most efficient tool to improve some nutritional and functional properties. This study investigated the presence of lunasin-like polypeptides in nineteen traditional Italian legumes, exploiting the potential of the fermentation with selected lactic acid bacteria to increase the native concentration. An integrated approach based on chemical, immunological and ex vivo (human adenocarcinoma Caco-2 cell cultures) analyses was used to show the physiological potential of the lunasin-like polypeptides. Results: Italian legume varieties, belonging to Phaseulus vulgaris, Cicer arietinum, Lathyrus sativus, Lens culinaris and Pisum sativum species, were milled and flours were chemically characterized and subjected to sourdough fermenta‑ tion with selected Lactobacillus plantarum C48 and Lactobacillus brevis AM7, expressing different peptidase activities. Extracts from legume doughs (unfermented) and sourdoughs were subjected to western blot analysis, using an anti- lunasin primary antibody. Despite the absence of lunasin, different immunoreactive polypeptide bands were found. -
Medicinal Plants As Sources of Active Molecules Against COVID-19
REVIEW published: 07 August 2020 doi: 10.3389/fphar.2020.01189 Medicinal Plants as Sources of Active Molecules Against COVID-19 Bachir Benarba 1* and Atanasio Pandiella 2 1 Laboratory Research on Biological Systems and Geomatics, Faculty of Nature and Life Sciences, University of Mascara, Mascara, Algeria, 2 Instituto de Biolog´ıa Molecular y Celular del Ca´ ncer, CSIC-IBSAL-Universidad de Salamanca, Salamanca, Spain The Severe Acute Respiratory Syndrome-related Coronavirus 2 (SARS-CoV-2) or novel coronavirus (COVID-19) infection has been declared world pandemic causing a worrisome number of deaths, especially among vulnerable citizens, in 209 countries around the world. Although several therapeutic molecules are being tested, no effective vaccines or specific treatments have been developed. Since the COVID-19 outbreak, different traditional herbal medicines with promising results have been used alone or in combination with conventional drugs to treat infected patients. Here, we review the recent findings regarding the use of natural products to prevent or treat COVID-19 infection. Furthermore, the mechanisms responsible for this preventive or therapeutic effect are discussed. We conducted literature research using PubMed, Google Scholar, Scopus, and WHO website. Dissertations and theses were not considered. Only the situation Edited by: Michael Heinrich, reports edited by the WHO were included. The different herbal products (extracts) and UCL School of Pharmacy, purified molecules may exert their anti-SARS-CoV-2 actions by direct inhibition of the virus United Kingdom replication or entry. Interestingly, some products may block the ACE-2 receptor or the Reviewed by: Ulrike Grienke, serine protease TMPRRS2 required by SARS-CoV-2 to infect human cells. -
Soybean Bioactive Peptides and Their Functional Properties
nutrients Review Soybean Bioactive Peptides and Their Functional Properties Cynthia Chatterjee 1,2, Stephen Gleddie 2 and Chao-Wu Xiao 1,3,* 1 Nutrition Research Division, Food Directorate, Health Products and Food Branch, Health Canada, Banting Research Centre, 251 Sir Frederick Banting Drive, Ottawa, ON K1A 0K9, Canada; [email protected] 2 Ottawa Research & Development Centre, Central Experimental Farm, Agriculture and Agri-Food Canada, 960 Carling Avenue Building#21, Ottawa, ON K1A 0C6, Canada; [email protected] 3 Food and Nutrition Science Program, Department of Chemistry, Carleton University, 1125 Colonel By Drive, Ottawa, ON K1S 5B6, Canada * Correspondence: [email protected]; Tel.: +1-613-558-7865; Fax: +1-613-948-8470 Received: 26 July 2018; Accepted: 29 August 2018; Published: 1 September 2018 Abstract: Soy consumption has been associated with many potential health benefits in reducing chronic diseases such as obesity, cardiovascular disease, insulin-resistance/type II diabetes, certain type of cancers, and immune disorders. These physiological functions have been attributed to soy proteins either as intact soy protein or more commonly as functional or bioactive peptides derived from soybean processing. These findings have led to the approval of a health claim in the USA regarding the ability of soy proteins in reducing the risk for coronary heart disease and the acceptance of a health claim in Canada that soy protein can help lower cholesterol levels. Using different approaches, many soy bioactive peptides that have a variety of physiological functions such as hypolipidemic, anti-hypertensive, and anti-cancer properties, and anti-inflammatory, antioxidant, and immunomodulatory effects have been identified. -
Effect of Byrsonima Crassa and Phenolic Constituents on Helicobacter Pylori-Induced Neutrophils Oxidative Burst
Int. J. Mol. Sci. 2012, 13, 133-141; doi:10.3390/ijms13010133 OPEN ACCESS International Journal of Molecular Sciences ISSN 1422-0067 www.mdpi.com/journal/ijms Article Effect of Byrsonima crassa and Phenolic Constituents on Helicobacter pylori-Induced Neutrophils Oxidative Burst Cibele Bonacorsi 1, Maria Stella G. Raddi 1,*, Luiz Marcos da Fonseca 1,*, Miriam Sannomiya 2 and Wagner Vilegas 3 1 School of Pharmaceutical Sciences, São Paulo State University (UNESP), Araraquara, SP, 14801-902, Brazil; E-Mail: [email protected] 2 School of Arts, Sciences and Humanities, University of São Paulo (USP), São Paulo, SP, 03828-000, Brazil; E-Mail: [email protected] 3 Institute of Chemistry, São Paulo State University (UNESP), Araraquara, SP, 14800-900, Brazil; E-Mail: [email protected] * Authors to whom correspondence should be addressed; E-Mails: [email protected] (M.S.G.R.); [email protected] (L.M.F); Tel.:+55-16-3301-5720; Fax: +55-16-3322-0073. Received: 29 August 2011; in revised form: 28 November 2011 / Accepted: 13 December 2011 / Published: 23 December 2011 Abstract: Byrsonima crassa Niedenzu (Malpighiaceae) is used in Brazilian folk medicine for the treatment of diseases related mainly to gastric ulcers. In a previous study, our group described the gastric protective effect of the methanolic extract from the leaves of B. crassa. The present study was carried out to investigate the effects of methanolic extract and its phenolic compounds on the respiratory burst of neutrophils stimulated by H. pylori using a luminol-based chemiluminescence assay as well as their anti-H. pylori activity. -
Regulation of Intestinal Inflammation by Soybean and Soy-Derived Compounds
foods Review Regulation of Intestinal Inflammation by Soybean and Soy-Derived Compounds Abigail Raffner Basson 1,2,* , Saleh Ahmed 2, Rawan Almutairi 3, Brian Seo 2 and Fabio Cominelli 1,2 1 Division of Gastroenterology & Liver Diseases, School of Medicine, Case Western Reserve University, Cleveland, OH 44106, USA; [email protected] 2 Digestive Health Research Institute, University Hospitals Cleveland Medical Center, Cleveland, OH 44106, USA; [email protected] (S.A.); [email protected] (B.S.) 3 Department of Pathology, School of Medicine, Case Western Reserve University, Cleveland, OH 44106, USA; [email protected] * Correspondence: [email protected] Abstract: Environmental factors, particularly diet, are considered central to the pathogenesis of the inflammatory bowel diseases (IBD), Crohn’s disease and ulcerative colitis. In particular, the Westernization of diet, characterized by high intake of animal protein, saturated fat, and refined carbohydrates, has been shown to contribute to the development and progression of IBD. During the last decade, soybean, as well as soy-derived bioactive compounds (e.g., isoflavones, phytosterols, Bowman-Birk inhibitors) have been increasingly investigated because of their anti-inflammatory properties in animal models of IBD. Herein we provide a scoping review of the most studied disease mechanisms associated with disease induction and progression in IBD rodent models after feeding of either the whole food or a bioactive present in soybean. Keywords: inflammatory bowel disease; isoflavone; bioactive compound; isoflavones; inflammation; Crohn’s disease; western diet; plant-based Citation: Basson, A.R.; Ahmed, S.; Almutairi, R.; Seo, B.; Cominelli, F. Regulation of Intestinal Inflammation by Soybean and Soy-Derived Compounds. Foods 2021, 10, 774. -
Roth 04 Pharmther Plant Derived Psychoactive Compounds.Pdf
Pharmacology & Therapeutics 102 (2004) 99–110 www.elsevier.com/locate/pharmthera Screening the receptorome to discover the molecular targets for plant-derived psychoactive compounds: a novel approach for CNS drug discovery Bryan L. Rotha,b,c,d,*, Estela Lopezd, Scott Beischeld, Richard B. Westkaempere, Jon M. Evansd aDepartment of Biochemistry, Case Western Reserve University Medical School, Cleveland, OH, USA bDepartment of Neurosciences, Case Western Reserve University Medical School, Cleveland, OH, USA cDepartment of Psychiatry, Case Western Reserve University Medical School, Cleveland, OH, USA dNational Institute of Mental Health Psychoactive Drug Screening Program, Case Western Reserve University Medical School, Cleveland, OH, USA eDepartment of Medicinal Chemistry, Medical College of Virginia, Virginia Commonwealth University, Richmond, VA, USA Abstract Because psychoactive plants exert profound effects on human perception, emotion, and cognition, discovering the molecular mechanisms responsible for psychoactive plant actions will likely yield insights into the molecular underpinnings of human consciousness. Additionally, it is likely that elucidation of the molecular targets responsible for psychoactive drug actions will yield validated targets for CNS drug discovery. This review article focuses on an unbiased, discovery-based approach aimed at uncovering the molecular targets responsible for psychoactive drug actions wherein the main active ingredients of psychoactive plants are screened at the ‘‘receptorome’’ (that portion of the proteome encoding receptors). An overview of the receptorome is given and various in silico, public-domain resources are described. Newly developed tools for the in silico mining of data derived from the National Institute of Mental Health Psychoactive Drug Screening Program’s (NIMH-PDSP) Ki Database (Ki DB) are described in detail. -
Dr. Duke's Phytochemical and Ethnobotanical Databases List of Chemicals for Chronic Venous Insufficiency/CVI
Dr. Duke's Phytochemical and Ethnobotanical Databases List of Chemicals for Chronic Venous Insufficiency/CVI Chemical Activity Count (+)-AROMOLINE 1 (+)-CATECHIN 5 (+)-GALLOCATECHIN 1 (+)-HERNANDEZINE 1 (+)-PRAERUPTORUM-A 1 (+)-SYRINGARESINOL 1 (+)-SYRINGARESINOL-DI-O-BETA-D-GLUCOSIDE 1 (-)-ACETOXYCOLLININ 1 (-)-APOGLAZIOVINE 1 (-)-BISPARTHENOLIDINE 1 (-)-BORNYL-CAFFEATE 1 (-)-BORNYL-FERULATE 1 (-)-BORNYL-P-COUMARATE 1 (-)-CANADINE 1 (-)-EPICATECHIN 4 (-)-EPICATECHIN-3-O-GALLATE 1 (-)-EPIGALLOCATECHIN 1 (-)-EPIGALLOCATECHIN-3-O-GALLATE 2 (-)-EPIGALLOCATECHIN-GALLATE 3 (-)-HYDROXYJASMONIC-ACID 1 (-)-N-(1'-DEOXY-1'-D-FRUCTOPYRANOSYL)-S-ALLYL-L-CYSTEINE-SULFOXIDE 1 (1'S)-1'-ACETOXYCHAVICOL-ACETATE 1 (2R)-(12Z,15Z)-2-HYDROXY-4-OXOHENEICOSA-12,15-DIEN-1-YL-ACETATE 1 (7R,10R)-CAROTA-1,4-DIENALDEHYDE 1 (E)-4-(3',4'-DIMETHOXYPHENYL)-BUT-3-EN-OL 1 1,2,6-TRI-O-GALLOYL-BETA-D-GLUCOSE 1 1,7-BIS(3,4-DIHYDROXYPHENYL)HEPTA-4E,6E-DIEN-3-ONE 1 Chemical Activity Count 1,7-BIS(4-HYDROXY-3-METHOXYPHENYL)-1,6-HEPTADIEN-3,5-DIONE 1 1,8-CINEOLE 1 1-(METHYLSULFINYL)-PROPYL-METHYL-DISULFIDE 1 1-ETHYL-BETA-CARBOLINE 1 1-O-(2,3,4-TRIHYDROXY-3-METHYL)-BUTYL-6-O-FERULOYL-BETA-D-GLUCOPYRANOSIDE 1 10-ACETOXY-8-HYDROXY-9-ISOBUTYLOXY-6-METHOXYTHYMOL 1 10-GINGEROL 1 12-(4'-METHOXYPHENYL)-DAURICINE 1 12-METHOXYDIHYDROCOSTULONIDE 1 13',II8-BIAPIGENIN 1 13-HYDROXYLUPANINE 1 14-ACETOXYCEDROL 1 14-O-ACETYL-ACOVENIDOSE-C 1 16-HYDROXY-4,4,10,13-TETRAMETHYL-17-(4-METHYL-PENTYL)-HEXADECAHYDRO- 1 CYCLOPENTA[A]PHENANTHREN-3-ONE 2,3,7-TRIHYDROXY-5-(3,4-DIHYDROXY-E-STYRYL)-6,7,8,9-TETRAHYDRO-5H- -
The Effect of Lunasin from Indonesian Soybean Extract on Inducible Nitric Oxide Synthase and Β-Catenin Expression in Dextran Sodium Sulfate-Induced Mice Colon
Online - 2455-3891 Vol 11, Issue 1, 2018 Print - 0974-2441 Research Article THE EFFECT OF LUNASIN FROM INDONESIAN SOYBEAN EXTRACT ON INDUCIBLE NITRIC OXIDE SYNTHASE AND β-CATENIN EXPRESSION IN DEXTRAN SODIUM SULFATE-INDUCED MICE COLON KUSMARDI KUSMARDI1, NESSA NESSA2*, ARI ESTUNINGTYAS2, ARYO TEDJO3, PUSPITA EKA WUYUNG1 1Department of Anatomical Pathology, Faculty of Medicine, Universitas Indonesia, Indonesia. 2Department of Pharmacology and Therapeutic, Faculty of Medicine, Universitas Indonesia, Indonesia. 3Department of Chemical Medicine, Faculty of Medicine, Universitas Indonesia, Indonesia. Email: [email protected] Received: 04 August 2017, Received and Accepted: 23 September 2017 ABSTRACT Objective: Inflammatory bowel diseases are idiopathic inflammatory disorders of the gastrointestinal tract. Chronic inflammation that occurs in the colon can develop into colon cancer. Lunasin has been known to resist inflammatory reactions induced by lipopolysaccharide in vitro. The role of lunasin as anti-inflammatory in vivo is not widely known. In this study, we analyzed the effect of lunasin from Indonesian soybean to decrease the risk Methods:of inflammation A total by of analyzing 30 mice theare expressionsdivided into of six inducible groups. nitricNormal oxide group synthase was not (iNOS) induced and byβ-catenin. dextran sodium sulfate (DSS). The other groups were induced by DSS 2% through drinking water for 9 days. After 9 days, negative group did not receive any treatment, besides the other groups received treatment given lunasin dose 20 mg/kg BB and 40 mg/kg BB, commercial lunasin, and positive given aspirin. Treatment was performed for 5 weeks. Results:Immunohistochemistry scores of iNOS and β-catenin proteins were analyzed using statistical tests. -
Lunasin and Bowman-Birk Protease Inhibitor Concentrations of Protein Extracts from Enzyme- Assisted Aqueous Extraction of Soybeans Juliana Maria L
Food Science and Human Nutrition Publications Food Science and Human Nutrition 5-31-2011 Lunasin and Bowman-Birk Protease Inhibitor Concentrations of Protein Extracts from Enzyme- Assisted Aqueous Extraction of Soybeans Juliana Maria L. Nobrega de Moura Iowa State University Blanca Hernandez-Ledesma University of California - Berkeley Neiva M. de Almeida Universidade Federal da Paraiba Chia-Chien Hsieh University of California - Berkeley Ben O. de Lumen UFonilvloerwsit ythi of sC andlifor anddia - itBerionkealley works at: http://lib.dr.iastate.edu/fshn_ag_pubs Part of the Agricultural Science Commons, Food Chemistry Commons, and the Plant Biology See next page for additional authors Commons The ompc lete bibliographic information for this item can be found at http://lib.dr.iastate.edu/ fshn_ag_pubs/100. For information on how to cite this item, please visit http://lib.dr.iastate.edu/ howtocite.html. This Article is brought to you for free and open access by the Food Science and Human Nutrition at Iowa State University Digital Repository. It has been accepted for inclusion in Food Science and Human Nutrition Publications by an authorized administrator of Iowa State University Digital Repository. For more information, please contact [email protected]. Lunasin and Bowman-Birk Protease Inhibitor Concentrations of Protein Extracts from Enzyme-Assisted Aqueous Extraction of Soybeans Abstract Lunasin and Bowman-Birk protease inhibitor (BBI) are two soybean peptides to which health-promoting properties have been attributed. Concentrations of these peptides were determined in skim fractions produced by enzyme-assisted aqueous extraction processing (EAEP) of extruded full-fat soybean flakes (an alternative to extracting oil from soybeans with hexane) and compared with similar extracts from hexane- defatted soybean meal.