DOCSLIB.ORG

(12) Patent Application Publication (10) Pub. No.: US 2017/0143667 A1 Rinsch Et Al

Total Page：16

File Type：pdf, Size：1020Kb

Download full-text PDF Read full-text
(12) Patent Application Publication (10) Pub. No.: US 2017/0143667 A1 Rinsch Et Al US 20170143667A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2017/0143667 A1 Rinsch et al. (43) Pub. Date: May 25, 2017 (54) COMPOSITIONS AND METHODS FOR (60) Provisional application No. 61/426,957, filed on Dec. IMPROVING MITOCHONORAL FUNCTION 23, 2010. AND TREATING NEURODEGENERATIVE DISEASES AND COGNITIVE DISORDERS Publication Classification (51) Int. Cl. (71) Applicant: Amazentis SA, Ecublens (CH) A63L/366 (2006.01) (72) Inventors: Christopher Rinsch, Morges (CH): A6IR 9/00 (2006.01) William Blanco-Bose, Lausanne (CH); (52) U.S. Cl. Bernard Schneider, Pully (CH): CPC .......... A61 K3I/366 (2013.01); A61K 9/0053 Charles Thomas, (2013.01); A61K 9/0014 (2013.01) Cheseaux-Sur-Lausanne (CH); Carmen (57) ABSTRACT Sandi, Bremblens (CH); Johan Auwerx, Buchillon (CH); Penelope Provided are compositions comprising compounds or pre Andreux, Lausanne (CH); Richardus cursors to compounds which may be used for a variety of Houtkooper, Lausanne (CH); Eija therapeutic applications including, for example, treating and/or preventing a disease or disorder related to reduced or Pirinen, Lausanne (CH); Laurent inadequate mitochondrial activity, including aging or stress, Mouchiroud, Lausanne (CH); David diabetes, obesity, and neurodegenerative diseases. The com Genoux, Lausanne (CH) pounds relate generally to urolithins and precursors thereof, including but not limited to ellagitannins and urolithin A. In (21) Appl. No.: 15/218,790 certain embodiments the compositions are presented in or as food products or nutritional Supplements. These same com (22) Filed: Jul. 25, 2016 pounds and compositions can also be used advantageously in generally healthy individuals to increase or maintain metabolic rate, decrease percent body fat, increase or main Related U.S. Application Data tain muscle mass, manage body weight, improve or maintain (62) Division of application No. 14/644.912, filed on Mar. mental performance (including memory), improve or main 11, 2015, which is a division of application No. tain muscle performance, improve or maintain mood, and 13/336,841, filed on Dec. 23, 2011. manage Stress. Patent Application Publication May 25, 2017. Sheet 1 of 46 US 2017/O143667 A1 Figure 1 Urolithin A (UA) Eliagic Acid (EA) Punicalagin (PA) Punicalin (PB) Patent Application Publication May 25, 2017. Sheet 2 of 46 US 2017/O143667 A1 Figure 2 O HO O HO-()-(y-OH O OH O EA O O HO. O. O OH OH UD UC O O O O UB UA Patent Application Publication May 25, 2017. Sheet 4 of 46 US 2017/O143667 A1 Figure 4 8 Control : ty e 0 ti 3: 50 it. ex e & 2x {} 3:30:3gia eiagic acii 8&isit A Patent Application Publication May 25, 2017. Sheet 5 of 46 US 2017/O143667 A1 Figure 5A B: P-AMPK B: AMPK Control RSV EA 50 M B : P-AMPK B : AMPK Control RSV UA 50 M Figure 5B k 3. 8. 83 S. : - EA 508 3. Patent Application Publication May 25, 2017. Sheet 6 of 46 US 2017/O143667 A1 Figure 6 x x88: i88 *** {383,333 x888 (3833 x to 3:fier8:3888 &c:::::::::::s Patent Application Publication May 25, 2017. Sheet 7 of 46 US 2017/O143667 A1 Figure 7 Patent Application Publication May 25, 2017. Sheet 8 of 46 US 2017/O143667 A1 Figure 8 * 3×3:83. ** <88: 8** 3:8,833. 8:8; ga::::::::::$8 xiiifesa:::::stax: g::::::::::::s Patent Application Publication May 25, 2017. Sheet 9 of 46 US 2017/O143667 A1 Figure 9 * ps. 0.05, * p-0.01, ** p30.001 when compared to differentiated control cells Patent Application Publication May 25, 2017. Sheet 10 of 46 US 2017/0143667 A1 Figure 10 ck k sk k is 2 s sk : k seas 3r:8: 1.38 4:3, 3.38 +8.8 ** p30.001 when compared to differentiated control cells Patent Application Publication May 25, 2017. Sheet 11 of 46 US 2017/0143667 A1 Figure 11 see : seek kk k :::: 838; i. --Sp3888 +&ips. & 8,388 +8, 8.3:38 4; 3.38: * p30.001 when compared to differentiated control cells Patent Application Publication May 25, 2017. Sheet 12 of 46 US 2017/0143667 A1 Figure 12 see & sks k k kit & 8. 3.: : 8.0 ic {: +3888: &88:8 -83.38 - a 3,8 - , is: * ps. 0.05, * p30.001 when compared to differentiated control cells Patent Application Publication May 25, 2017. Sheet 13 of 46 US 2017/0143667 A1 Figure 13 k.k. i8 :::::: sk sk se:: 8. 3 +388 4-cska883: 4:3,338 E 8.3: $33,88 *" p<0.001 when compared to differentiated control cells Patent Application Publication May 25, 2017. Sheet 14 of 46 US 2017/0143667 A1 Figure 14 3.38 : se: sk & K. 3.03 - S: 3 & x83888 --83.388 Sai i8 + .338 * ps. 0.05, * p30.01, p<0.001 when compared to differentiated control cells Patent Application Publication May 25, 2017. Sheet 15 of 46 US 2017/0143667 A1 Figure 15 ck sk 3.78 3.68 3.58 cr: -3; 33:8: \{xc388 1- 3.38 Y-SE& 3.38 -: ,388 * p40.01," p<0.001 when compared to differentiated control cells Patent Application Publication May 25, 2017. Sheet 16 of 46 US 2017/0143667 A1 Figure 16 k-k-k sks sk: . 3. --Sp3ig 88 - 8& 3:3 ** {3.38 a R. 33 * p-0.01.** p<0.001 when compared to differentiated control cells Patent Application Publication May 25, 2017. Sheet 17 of 46 US 2017/O143667 A1 08 s s": “s “s (%) Uesuffe M Apog {}{}{} VII,a.infi!-- (%) ues) ubie W. Apog Patent Application Publication 81),?unfilº Patent Application Publication US 2017/O143667 A1 VOZ?un61-I (16x11us) &OA Patent Application Publication May 25, 2017 Sheet 22 of 46 US 2017/O143667 A1 000Z009?.000}, S. GTZaan513 &B Patent Application Publication May 25, 2017 Sheet 23 of 46 US 2017/O143667 A1 (addad) ope afue 33 / Joe Edsel uee, s co N n N ed s es s (232) ope afueues AJOeidsey ueeW Ces es s N. a. N c ZATO (33) vzzeun61-B one e5ue to Ajoleidsed ueeA Patent Application Publication May 25, 2017 Sheet 26 of 46 US 2017/O143667 A1 gGZaun61+ ( 9 0 w wgzaun61-) (uomful upond) OO Patent Application Publication May 25, 2017. Sheet 27 of 46 US 2017/0143667 A1 Figure 26 DMSO 25 V UA 50uM C) S. 20 CD O 15 O O t g 1O ":CS 5 Patent Application Publication May 25, 2017. Sheet 28 of 46 US 2017/0143667 A1 Figure 27 60 en 50 k “ Stress + water 40 x Stress + Extract 101 low dose O 2 Stress -- Extract 101 medium dose E 30 x Stress + Extract 1011 high dose 8 20 SS 10 & O X : Water S W S low Smed Shigh One way ANOVA followed by Dunnett's test *"p<0.01 was water -non-stressed "p<0.05 vs water-chronic stress Figure 28 70 Stress + water 60 growows sex Stress + Extract 1011 low dose g 50 Stress + Extract 1011 medium dose 40 x Stress + Extract 1011 high dose sa 30 sesses & S. 20 1 O O E. x: SW Slow Smed One way ANOVA followed by Dunnett's test: * p-0.01 vs SW Patent Application Publication May 25, 2017. Sheet 29 of 46 US 2017/0143667 A1 Figure 29 I Stress + water E StreSS - Extract 011 OW dose StreSS - Extract 1011 medium dose X Stress + Extract 1011 high dose 4 SW Slow Smed S. high One way ANOVA followed by Dunnett's test: * p-0.5: * p-0.01 vs SW Figure 30 6 area Stress + Water o 5 E Stress + Extract 011 OW dose 4. Stress + Extract 101 medium dose 8 3 Stress + Extract 1011 high dose 5 3 s O 2 SS 1 O T. V. V. Patent Application Publication May 25, 2017. Sheet 30 of 46 US 2017/0143667 A1 Figure 31 150 -O- Chronic Stress Untreated -- Chronic Stress + Urolithin A ^x Non-Stressed Untreated 10 O 5 O Patent Application Publication May 25, 2017. Sheet 31 of 46 US 2017/0143667 A1 Figure 32 Average per day 50 0.50 950- -H Water 850- -8- Stress + water 3 750 2: 650 25 550 450 350 o 2 3 Day * p-0.05, *p-0.001 versus water Figure 33 Average di - d2 -d3 k 3000 900- -- Water Stress + water Stress h Extract 10 low dose x Stress + Extract 101 mediurn dose Stress + Extract 1011 high dose Slow Smed S high * p<0.05, "p-0.001 versus Stress + water, student's T-test Patent Application Publication May 25, 2017. Sheet 32 of 46 US 2017/0143667 A1 Figure 34 80,000 * Control stress H Urolithin A 6 0, O O O 40, OO O KN K. K. K. Ko KS K & K& S N & Trial number Patent Application Publication May 25, 2017. Sheet 33 of 46 US 2017/0143667 A1 Figure 35 8 sat 8 Figure 36 * p=0.0141 1 5 O O Patent Application Publication May 25, 2017. Sheet 34 of 46 US 2017/0143667 A1 Figure 37 80 one-way ANOVA ** p-0.01, * p-0.05 70 sk 60 50 40 Normal AD mouse Untreated Untreated PE Patent Application Publication May 25, 2017. Sheet 35 of 46 US 2017/O143667 A1 Figure 38 : Patent Application Publication May 25, 2017. Sheet 36 of 46 US 2017/0143667 A1 Figure 39 110 Normal Early-life Stress 8. Untreated Punicalagin Patent Application Publication May 25, 2017. Sheet 37 of 46 US 2017/0143667 A1 Figure 40 Normal Early-life Stress 8 Untreated Punicalagin Patent Application Publication May 25, 2017. Sheet 38 of 46 US 2017/0143667 A1 Figure 41 18O 160 140 120 100 80 Normal Early-life stress Untreated Punicalagin Patent Application Publication May 25, 2017 Sheet 39 of 46 US 2017/0143667 A1 Figure 42 80 60 4.
Load more

Recommended publications
  • Diabetic Neuropathy)
    A PROSPECTIVE OPEN LABELLED NON RANDOMIZED PHASE-II CLINICAL TRIAL OF “KADUKKAI CHOORANAM FOR “AKKINI SELATHUMAM” (DIABETIC NEUROPATHY) Dissertation submitted to THE TAMILNADU DR. MGR. MEDICAL UNIVERSITY CHENNAI-32 For the partial fulfillment of the requirements to the Degree of DOCTOR OF MEDICINE (SIDDHA) BRANCH-I DEPARTMENT OF POTHU MARUTHUVAM DEPARTMENT OF POTHU MARUTHUVAM GOVERNMENT SIDDHA MEDICAL COLLEGE PALAYAMKOTTAI - 627 002 TAMIL NADU, INDIA. OCTOBER 2019 GOVERNMENT SIDDHA MEDICAL COLLEGE PALAYAMKOTTAI - 627 002 TAMIL NADU, INDIA. BONAFIDE CERTIFICATE This is to certify that the dissertation entitled “A PROSPECTIVE OPEN LABELLED NON RANDOMIZED PHASE-II CLINICAL TRIAL OF “KADUKKAI CHOORANAM FOR AKKINI SELATHUMAM (DIABETIC NEUROPATHY)” is abonafide work done by Dr.RAJENDRAM AJANTHAN (Reg. No.321611008) Govt. Siddha Medical College, Palayamkottai - 627 002 in partial fulfilment of the university rules and regulations for award for MD (S) POTHU MARUTHUVAM (BRANCH-I) under my guidance and supervision during the academic year OCTOBER 2016-2019. Supervisor and Guide Prof. Dr.A.MANOHARAN, MD (S),( Ph.D). Head, Department of PothuMaruthuvam, Govt. Siddha Medical College, Palayamkottai. Name and signature of the HOD Name and signature of the Principal Prof. Dr. A.MANOHARAN, MD (S),( Ph.D). Prof. Dr.S.Victoria,MD(S) Dept. of PothuMaruthuvam, Govt. Siddha Medical College Govt. Siddha Medical College, Palayamkottai. Palayamkottai. GOVERNMENT SIDDHA MEDICAL COLLEGE PALAYAMKOTTAI - 627 002 TAMIL NADU, INDIA. CERTIFICATE Certified that I have gone through the dissertation entitled “A PROSPECTIVE OPEN LABELLED NON RANDOMIZED PHASE-II CLINICAL TRIAL OF “KADUKKAI CHOORANAM FOR AKKINI SELATHUMAM (DIABETIC NEUROPATHY)” submitted by Dr.RAJENDRAM AJANTHAN (Reg. No.321611008) a student of final year MD(S) Department of Pothu Maruthuvam (Branch-I)of this college and the dissertation work has been carried out by the individual only.
    [Show full text]
  • Advances in Distilled Beverages Authenticity and Quality Testing Teodora Emilia Coldea, Elena Mudura and Carmen Socaciu Teodora Emilia Coldea, Elena Mudura And
    Chapter 6 Advances in Distilled Beverages Authenticity and Quality Testing Teodora Emilia Coldea, Elena Mudura and Carmen Socaciu Teodora Emilia Coldea, Elena Mudura and CarmenAdditional information Socaciu is available at the end of the chapter Additional information is available at the end of the chapter http://dx.doi.org/10.5772/intechopen.72041 Abstract Given the advent of the consumers and producers demands, researches are focusing lately to develop innovative, cost-effective, progressively complex alcoholic beverages. As alco- hol consumption has a heavy impact on social environment and health, fast and safe solu- tions for industrial application are needed. In this chapter, the recent advances in the field of alcoholic beverages authenticity and quality testing are summarised. Solutions for the online monitoring of the process of distilled beverages are offered and the recent methods for identification of raw material and process formed biomarkers of distilled beverages are presented. Keywords: distilled beverages, authenticity, biomarkers 1. Introduction Distilled beverages are important for consumers, producers and agricultural sector. Last decades presented us continuously changed requirements and descriptive practices for high level of consumer’s protection with impact on the market transparency and fair competition. Both traditional methods and innovative technologies applied in distilled beverages production are focusing on their quality improvement. The principal requirement set for an alcoholic beverage can be summarised as: are intended for human consumption, have specific sensory properties, with a minimum ethyl alcohol content of 15% v/v produced either by distillation with addition of flavourings, of naturally fermented products, or by addition of plant ethanol macerates, or by blending of flavourings, sugars, other © 2016 The Author(s).
    [Show full text]
  • Intereferents in Condensed Tannins Quantification by the Vanillin Assay
    INTEREFERENTS IN CONDENSED TANNINS QUANTIFICATION BY THE VANILLIN ASSAY IOANNA MAVRIKOU Dissertação para obtenção do Grau de Mestre em Vinifera EuroMaster – European Master of Sciences of Viticulture and Oenology Orientador: Professor Jorge Ricardo da Silva Júri: Presidente: Olga Laureano, Investigadora Coordenadora, UTL/ISA Vogais: - Antonio Morata, Professor, Universidad Politecnica de Madrid - Jorge Ricardo da Silva, Professor, UTL/ISA Lisboa, 2012 Acknowledgments First and foremost, I would like to thank the Vinifera EuroMaster consortium for giving me the opportunity to participate in the M.Sc. of Viticulture and Enology. Moreover, I would like to express my appreciation to the leading universities and the professors from all around the world for sharing their scientific knowledge and experiences with us and improving day by day the program through mobility. Furthermore, I would like to thank the ISA/UTL University of Lisbon and the personnel working in the laboratory of Enology for providing me with tools, help and a great working environment during the experimental period of this thesis. Special acknowledge to my Professor Jorge Ricardo Da Silva for tutoring me throughout my experiment, but also for the chance to think freely and go deeper to the field of phenols. Last but most important, I would like to extend my special thanks to my family and friends for being a true support and inspiration in every doubt and decision. 1 UTL/ISA University of Lisbon “Vinifera Euromaster” European Master of Science in Viticulture&Oenology Ioanna Mavrikou: Inteferents in condensed tannins quantification with vanillin assay MSc Thesis: 67 pages Key Words: Proanthocyanidins; Interference substances; Phenols; Vanillin assay Abstract Different methods have been established in order to perform accurately the quantification of the condensed tannins in various plant products and beverages.
    [Show full text]
  • Glucosidase Inhibition and Antioxidant Activity of an Oenological Commercial Tannin
    Food Chemistry 215 (2017) 50–60 Contents lists available at ScienceDirect Food Chemistry journal homepage: www.elsevier.com/locate/foodchem a-Glucosidase inhibition and antioxidant activity of an oenological commercial tannin. Extraction, fractionation and analysis by HPLC/ESI-MS/MS and 1H NMR ⇑ ⇑ Vera Muccilli , Nunzio Cardullo, Carmela Spatafora , Vincenzo Cunsolo, Corrado Tringali Dipartimento di Scienze Chimiche, Università degli Studi di Catania, V.le A. Doria 6, 95125 Catania, Italy article info abstract Article history: Two batches of the oenological tannin Tan’Activ R, (toasted oak wood – Quercus robur), were extracted Received 6 November 2015 with ethanol. A fractionation on XAD-16 afforded four fractions for each extract. Extracts and fractions Received in revised form 27 May 2016 were evaluated for antioxidant activity (DPPH), polyphenol content (GAE) and yeast a-glucosidase inhi- Accepted 25 July 2016 bitory activity. Comparable results were obtained for both columns, fractions X1B and X2B showing the Available online 25 July 2016 highest antioxidant activity. Fractions X1C and X2C notably inhibited a-glucosidase, with IC50 = 9.89 and 8.05 lg/mL, respectively. Fractions were subjected to HPLC/ESI-MS/MS and 1H NMR analysis. The main Keywords: phenolic constituents of both X1B and X2B were a monogalloylglucose isomer (1), a HHDP-glucose Plant polyphenols isomer (2), castalin (3) gallic acid (4), vescalagin (5), and grandinin (or its isomer roburin E, 6). X1C Oenological tannins Quercus robur and X2C showed a complex composition, including non-phenolic constituents. Fractionation of X2C gave a l a-Glucosidase inhibition a subfraction, with enhanced -glucosidase inhibitory activity (IC50 = 6.15 g/mL), with castalagin (7)as HPLC/ESI-MS/MS the main constituent.
    [Show full text]
  • In Vitro Bioaccessibility, Human Gut Microbiota Metabolites and Hepatoprotective Potential of Chebulic Ellagitannins: a Case of Padma Hepatenr Formulation
    Article In Vitro Bioaccessibility, Human Gut Microbiota Metabolites and Hepatoprotective Potential of Chebulic Ellagitannins: A Case of Padma Hepatenr Formulation Daniil N. Olennikov 1,*, Nina I. Kashchenko 1,: and Nadezhda K. Chirikova 2,: Received: 28 August 2015 ; Accepted: 30 September 2015 ; Published: 13 October 2015 1 Laboratory of Medical and Biological Research, Institute of General and Experimental Biology, Siberian Division, Russian Academy of Science, Sakh’yanovoy Street 6, Ulan-Ude 670-047, Russia; [email protected] 2 Department of Biochemistry and Biotechnology, North-Eastern Federal University, 58 Belinsky Street, Yakutsk 677-027, Russian; [email protected] * Correspondence: [email protected]; Tel.: +7-9021-600-627; Fax: +7-3012-434-243 : These authors contributed equally to this work. Abstract: Chebulic ellagitannins (ChET) are plant-derived polyphenols containing chebulic acid subunits, possessing a wide spectrum of biological activities that might contribute to health benefits in humans. The herbal formulation Padma Hepaten containing ChETs as the main phenolics, is used as a hepatoprotective remedy. In the present study, an in vitro dynamic model simulating gastrointestinal digestion, including dialysability, was applied to estimate the bioaccessibility of the main phenolics of Padma Hepaten. Results indicated that phenolic release was mainly achieved during the gastric phase (recovery 59.38%–97.04%), with a slight further release during intestinal digestion. Dialysis experiments showed that dialysable phenolics were 64.11% and 22.93%–26.05% of their native concentrations, respectively, for gallic acid/simple gallate esters and ellagitanins/ellagic acid, in contrast to 20.67% and 28.37%–55.35% for the same groups in the non-dialyzed part of the intestinal media.
    [Show full text]
  • Wo 2009/114810 A2
    (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (10) International Publication Number (43) International Publication Date 17 September 2009 (17.09.2009) WO 2009/114810 A2 (51) International Patent Classification: Box#: 19 162, 701 South Nedderman Drive, Arlington, A61K 31/357 (2006.01) A61P 31/12 (2006.01) TX 76019 (US). (21) International Application Number: (74) Agents: BRASHEAR, Jeanne, M . et al; Marshall, Ger- PCT/US2009/037163 stein & Borun LLP, 233 S. Wacker Drive, Suite 6300, Sears Tower, Chicago, IL 60606-6357 (US). (22) International Filing Date: 13 March 2009 (13.03.2009) (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, (25) Filing Language: English AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, (26) Publication Language: English CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, (30) Priority Data: HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, 61/036,8 12 14 March 2008 (14.03.2008) US KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, (71) Applicant (for all designated States except US): THE MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, FLORIDA INTERNATIONAL UINVERSITY NZ, OM, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, BOARD OF TRUSTEES [US/US]; University Park, PC SK, SL, SM, ST, SV, SY, TJ, TM, TN, TR, TT, TZ, UA, 511, Miami, FL 33 199 (US).
    [Show full text]
  • Concentrations of Blood Serum and Urinal Ellagitannin Metabolites Depend Largely on the Post-Intake Time and Duration of Strawberry Phenolics Ingestion in Rats
    Pol. J. Food Nutr. Sci., 2019, Vol. 69, No. 4, pp. 379–386 DOI: 10.31883/pjfns/111866 http://journal.pan.olsztyn.pl Original article Section: Nutritional Research Concentrations of Blood Serum and Urinal Ellagitannin Metabolites Depend Largely on the Post-Intake Time and Duration of Strawberry Phenolics Ingestion in Rats Ewa Żary-Sikorska1*, Monika Kosmala2, Joanna Milala2, Bartosz Fotschki3, Katarzyna Ognik4, Jerzy Juśkiewicz3 1Department of Microbiology and Food Technology, Faculty of Agriculture and Biotechnology University of Science and Technology, Kaliskiego 7, 85–796 Bydgoszcz, Poland 2Institute of Food Technology and Analysis, Łódź University of Technology, Stefanowskiego 4/10, 90–924 Łódź, Poland 3Department of Biological Functions of Food, Institute of Animal Reproduction and Food Research of the Polish Academy of Sciences, Tuwima 10, 10–748 Olsztyn, Poland 4Department of Biochemistry and Toxicology, Faculty of Biology, Animal Sciences and Bioeconomy, University of Life Sciences, Akademicka 13, 20–950 Lublin, Poland Key words: strawberry, ellagitannins, metabolites, urine, serum, rat The different duration of a strawberry phenolic fraction intake and different post-intake time were experimental factors affecting the concentrations of ellagitannin metabolites in the urine and blood serum of rats. For four days, the animals were gavaged once a day as follows: group C (water, days 1–4), group F1–4 (fraction, days 1–4), group F1–3 (fraction, days 1–3; water, day 4), group F1–2 (fraction, days 1, 2; water, days 3, 4), group F3–4 (water, days 1, 2; fraction, days 3, 4), and group F4 (water, days 1–3; and fraction, day 4). The daily dosage of the fraction gavaged to one rat was 20 mg/kg of body weight.
    [Show full text]
  • Universidade Federal Do Rio De Janeiro Kim Ohanna
    UNIVERSIDADE FEDERAL DO RIO DE JANEIRO KIM OHANNA PIMENTA INADA EFFECT OF TECHNOLOGICAL PROCESSES ON PHENOLIC COMPOUNDS CONTENTS OF JABUTICABA (MYRCIARIA JABOTICABA) PEEL AND SEED AND INVESTIGATION OF THEIR ELLAGITANNINS METABOLISM IN HUMANS. RIO DE JANEIRO 2018 Kim Ohanna Pimenta Inada EFFECT OF TECHNOLOGICAL PROCESSES ON PHENOLIC COMPOUNDS CONTENTS OF JABUTICABA (MYRCIARIA JABOTICABA) PEEL AND SEED AND INVESTIGATION OF THEIR ELLAGITANNINS METABOLISM IN HUMANS. Tese de Doutorado apresentada ao Programa de Pós-Graduação em Ciências de Alimentos, Universidade Federal do Rio de Janeiro, como requisito parcial à obtenção do título de Doutor em Ciências de Alimentos Orientadores: Profa. Dra. Mariana Costa Monteiro Prof. Dr. Daniel Perrone Moreira RIO DE JANEIRO 2018 DEDICATION À minha família e às pessoas maravilhosas que apareceram na minha vida. ACKNOWLEDGMENTS Primeiramente, gostaria de agradecer a Deus por ter me dado forças para não desistir e por ter colocado na minha vida “pessoas-anjo”, que me ajudaram e me apoiaram até nos momentos em que eu achava que ia dar tudo errado. Aos meus pais Beth e Miti. Eles não mediram esforços para que eu pudesse receber uma boa educação e para que eu fosse feliz. Logo no início da graduação, a situação financeira ficou bem apertada, mas eles continuaram fazendo de tudo para me ajudar. Foram milhares de favores prestados, marmitas e caronas. Meu pai diz que fez anos de curso de inglês e espanhol, porque passou anos acordando cedo no sábado só para me levar no curso que eu fazia no Fundão. Tinha dia que eu saía do curso morta de fome e quando eu entrava no carro, tinha uma marmita com almoço, com direito até a garrafa de suco.
    [Show full text]
  • "Ellagic Acid, an Anticarcinogen in Fruits, Especially in Strawberries: a Review"
    FEATURE Ellagic Acid, an Anticarcinogen in Fruits, Especially in Strawberries: A Review John L. Maasl and Gene J. Galletta2 Fruit Laboratory, U.S. Department of Agriculture, Agricultural Research Service, Beltsville, MD 20705 Gary D. Stoner3 Department of Pathology, Medical College of Ohio, Toledo, OH 43699 The various roles of ellagic acid as an an- digestibility of natural forms of ellagic acid, Mode of inhibition ticarcinogenic plant phenol, including its in- and the distribution and organ accumulation The inhibition of cancer by ellagic acid hibitory effects on chemically induced cancer, or excretion in animal systems is in progress appears to occur through the following its effect on the body, occurrence in plants at several institutions. Recent interest in el- mechanisms: and biosynthesis, allelopathic properties, ac- lagic acid in plant systems has been largely a. Inhibition of the metabolic activation tivity in regulation of plant hormones, for- for fruit-juice processing and wine industry of carcinogens. For example, ellagic acid in- mation of metal complexes, function as an applications. However, new studies also hibits the conversion of polycyclic aromatic antioxidant, insect growth and feeding in- suggest that ellagic acid participates in plant hydrocarbons [e.g., benzo (a) pyrene, 7,12- hibitor, and inheritance are reviewed and hormone regulatory systems, allelopathic and dimethylbenz (a) anthracene, and 3-methyl- discussed in relation to current and future autopathic effects, insect deterrent princi- cholanthrene], nitroso compounds (e.g., N- research. ples, and insect growth inhibition, all of which nitrosobenzylmethylamine and N -methyl- N- Ellagic acid (C14H6O8) is a naturally oc- indicate the urgent need for further research nitrosourea), and aflatoxin B1 into forms that curring phenolic constituent of many species to understand the roles of ellagic acid in the induce genetic damage (Dixit et al., 1985; from a diversity of flowering plant families.
    [Show full text]
  • Formulation Strategies to Improve Oral Bioavailability of Ellagic Acid
    Preprints (www.preprints.org) | NOT PEER-REVIEWED | Posted: 7 April 2020 doi:10.20944/preprints202004.0100.v1 Peer-reviewed version available at Appl. Sci. 2020, 10, 3353; doi:10.3390/app10103353 Review Formulation strategies to improve oral bioavailability of ellagic acid Guendalina Zuccari 1,*, Sara Baldassari 1, Giorgia Ailuno 1, Federica Turrini 1, Silvana Alfei 1, and Gabriele Caviglioli 1 1 Department of Pharmacy, Università di Genova, 16147 Genova, Italy * Correspondence: [email protected]; Tel.: +39 010 3352627 Featured Application: An updated description of pursued approaches for efficiently resolving the low bioavailability issue of ellagic acid. Abstract: Ellagic acid, a polyphenolic compound present in fruits and berries, has recently been object of extensive research for its antioxidant activity, which might be useful for the prevention and treatment of cancer, cardiovascular pathologies, and neurodegenerative disorders. Its protective role justifies numerous attempts to include it in functional food preparations and in dietary supplements not only to limit the unpleasant collateral effects of chemotherapy. However, ellagic acid use as chemopreventive agent has been debated because of its poor bioavailability associated to low solubility, limited permeability, first pass effect, and interindividual variability in gut microbial transformations. To overcome these drawbacks, various strategies for oral administration including solid dispersions, micro-nanoparticles, inclusion complexes, self- emulsifying systems, polymorphs have been proposed. Here, we have listed an updated description of pursued micro/nanotechnological approaches focusing on the fabrication processes and the features of the obtained products, as well as on the positive results yielded by in vitro and in vivo studies in comparison to the raw material.
    [Show full text]
  • Bio-Guided Fractionation of Extracts of Geranium Robertianum L.: Relationship MARK Between Phenolic Profile and Biological Activity ⁎ V.C
    Industrial Crops & Products 108 (2017) 543–552 Contents lists available at ScienceDirect Industrial Crops & Products journal homepage: www.elsevier.com/locate/indcrop Bio-guided fractionation of extracts of Geranium robertianum L.: Relationship MARK between phenolic profile and biological activity ⁎ V.C. Graçaa,b,c, Lillian Barrosb, Ricardo C. Calhelhab, Maria Inês Diasb, Isabel C.F.R. Ferreirab, , ⁎ P.F. Santosc, a Centre for Research and Technology of Agro-Environmental and Biological Sciences (CITAB) – Vila Real, University of Trás-os-Montes and Alto Douro, 5001-801 Vila Real, Portugal b Centro de Investigação de Montanha (CIMO), ESA, Instituto Politécnico de Bragança, Campus de Santa Apolónia, 5300-253 Bragança, Portugal c Chemistry Center – Vila Real (CQVR), University of Trás-os-Montes and Alto Douro, 5001-801 Vila Real, Portugal ARTICLE INFO ABSTRACT Keywords: Geranium robertianum L. is used in folk medicine and herbalism practice for the treatment of a variety of ail- Geranium robertianum L ments. Recently, we studied the bioactivity of several aqueous and organic extracts of this plant. In this work, the Fractionation more active extracts were fractionated and the fractions evaluated for their antioxidant activity and cytotoxicity Antioxidant activity against several human tumor cell lines and non-tumor porcine liver primary cells. Some of the fractions from the Antiproliferative activity acetone extract consistently displayed low EC and GI values and presented the higher contents of total Phenolic compounds 50 50 phenolic compounds in comparison to other fractions. The phenolic compounds profile of the fractions was determined. The bio-guided fractionation of the extracts resulted in several fractions with improved bioactivity relative to the corresponding extracts.
    [Show full text]
  • Determination of Phytocompounds from Terminalia Chebula Retz by Hptlc Densitometric Method
    Innovare International Journal of Pharmacy and Pharmaceutical Sciences Academic Sciences ISSN- 0975-1491 Vol 6, Issue 7, 2014 Original Article DETERMINATION OF PHYTOCOMPOUNDS FROM TERMINALIA CHEBULA RETZ BY HPTLC DENSITOMETRIC METHOD SAVITHA T.1,3*, ARIVUKKARASU R.2 1PG & Research Department of Microbiology, KSR College of Arts & Science, Tiruchengode, Tamilnadu, India. 2Department of Pharmaceutical Analysis, KMCH College of Pharmacy, Coimbatore. Tamilnadu, India. 3Department of Microbiology, Tiruppur Kumaran College for Women, Tiruppur, Tamilnadu, India Email: [email protected] Received: 22 May 2014 Revised and Accepted: 03 Jul 2014 ABSTRACT Objective: The present investigation has been focused on the detection of antibacterial activity of methanolic extract by disc diffusion method and the quantitative estimation of phyto constituents from Terminalia chebula, (King of Medicine) by High Performance Thin Layer Chromatography (HPTLC) method. Methods: An in vitro study on the efficacy of methanol extract of T.chebula was carried out. For this analysis, Tannic acid (TA), Gallic acid (GA), Ellagic acid (EA) were as used as standard markers by using toluene: ethyl acetate: formic acid: methanol (4.3:4.3:1:1.2:0.3, V/V/V/V) was used as a mobile phase. Detection and quantification were performed densitometrically at Lambda 254 nm. Results: The methanol extract has shown best activity against test strains. The Rf values of standards were 0.78 for TA, 0.74 for GA and 0.63 for EA. The total peak areas of the standards and the corresponding peak areas of extracts were composed and the statistical analysis was carried out. Conclusions: Based on the present findings, there is a wide opportunity for the development of new drug formulations for the effective treatment against multiple drug resistant micro organisms with no side effects with lesser costs.
    [Show full text]