WO 2007/039262 Al

Total Page:16

File Type:pdf, Size:1020Kb

WO 2007/039262 Al (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date (10) International Publication Number 12 April 2007 (12.04.2007) PCT WO 2007/039262 Al (51) International Patent Classification: (81) Designated States (unless otherwise indicated, for every A23L 1/30 (2006.01) A23L 1/22 (2006.01) kind of national protection available): AE, AG, AL, AM, AT,AU, AZ, BA, BB, BG, BR, BW, BY, BZ, CA, CH, CN, (21) International Application Number: CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, PCT/EP2006/009527 GB, GD, GE, GH, GM, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, (22) International Filing Date: 2 October 2006 (02.10.2006) LU, LV,LY,MA, MD, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RS, RU, (25) Filing Language: English SC, SD, SE, SG, SK, SL, SM, SV, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW (26) Publication Language: English (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, (30) Priority Data: GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, 60/721,993 30 September 2005 (30.09.2005) US ZW), Eurasian (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM), European (AT,BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, (71) Applicant (for all designated States except US): DSM IP FR, GB, GR, HU, IE, IS, IT, LT, LU, LV,MC, NL, PL, PT, ASSETS B.V. [NL/NL]; Het Overloon 1, NL-6411 TE RO, SE, SI, SK, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, Heerlen (NL). GN, GQ, GW, ML, MR, NE, SN, TD, TG). (72) Inventors; and Published: — with international search report (75) Inventors/Applicants (for US only): SCHWEIKERT, — before the expiration of the time limit for amending the Loni [DE/CH]; Kohliberg 5, CH-4315 Zuzgen (CH). claims and to be republished in the event of receipt of STEINKE, Peter [DE/DE]; Schlossweg 14d, 79639 amendments Grenzach-Wyhlen (DE). For two-letter codes and other abbreviations, refer to the "G uid (74) Agents: STECK, Melanie et al.; DSM Nutritional Prod ance Notes on Codes and Abbreviations" appearing at the beg in ucts Ltd, Wurmisweg 576, CH-4303 Kaiseraugst (CH). ning of each regular issue of the PCT Gazette. (54) Title: NOVEL COMPOSITIONS CONTAINING POLYPHENOLS (57) Abstract: The present invention is directed to compositions containing at least a polyphenol and polyethylenglycol, to prod- ucts such as food, beverages, dietary supplements, feed, pharmaceuticals and personal care products containing such a composition as well as to the use of polyethylenglycol for masking the bitter taste of such polyphenols. The polyphenols are preferably selected from the group consisting of epigallocatechin gallate, resveratrol, hydroxytyrosol, oleuropein, polyphenols present in green tea ex- tracts, catechins, polyphenols present in extracts of red grape skin, polyphenols present in olives and/or olive waste water, and their mixtures. Novel compositions containing polyphenols Field of the Invention The present invention is directed to compositions containing at least a polyphenol and polyethylenglycol, to products such as food, beverages, dietary supplements, feed, pharmaceuticals and personal care products containing such a composition as well as to the use of polyethylenglycol for masking the bitter taste of such polyphenols, especially in dry applications like powders, chewable tablets and lozenges. Background and Summary of the Invention Polyphenols often have a bitter taste which is not accepted by customers. The object of the present invention is therefore to provide a substance which can be added to a composition containing such a bitter tasting polyphenol whereby the bitter taste can be masked. The object is solved by adding polyethylenglycol to a composition containing at least a polyphenol, especially at least a bitter tasting polyphenol. Preferably, the polyethylenglycol will be present in an amount to achieve a weight ratio of the polyphenol to the polyethylenglycol of from 10 : 90 to 70 : 30. The polyethylenglycol may advantageously be one of the following formula HO-(CH 2-CH 2-O-) nH with n being an integer, so that the average molecular weight of the polyethylenglycol is in the range from 1000 to 20000 g/mol. In some embodiments of the invention, the polyphenol is selected from the group consisting of epigallocatechin gallate, resveratrol, hydroxytyrosol, oleuropein, polyphenols present in green tea extracts, catechins, polyphenols present in extracts of red grape skin, polyphenols present in olives and/or olive waste water, and their mixtures. The green tea extract that may be used satisfactorily in accordance with the invention may be one containing epigallocatechin gallate in an amount of at least 30 weight-%, preferably of at MST/02. 10.2006 Case 251 13WO least 50 weight-%, based on the total amount of the green tea extract. The extract of red grape skin that may be used satisfactorily in accordance with the invention may be one containing resveratrol in an amount of at least 30 weight-%, preferably of at least 50 weight-%, based on the total amount of the extract of red grape skin. The compositions of the invention may comprise vitamin C and/or vitamin E. The compositions of the invention may be forumulated into a product selected from the group consisting of dietary compositions, pharmaceuticals and personal care products. In some embodiments of the invention, the compositions of the invention may be in the form of a chewable tablet or a lozenge. Detailed Description of the Preferred Exemplary Embodiments The polyphenols are preferably selected from the group consisting of polyphenols present in green tea extracts like catechins, polyphenols present in extracts of red grape skin like resveratrol, polyphenols present in olives, olive waste water etc. like hydroxytyrosol and oleuropein, and their mixtures. Suitable green tea extracts are e.g. those containing epigallocatechin gallate (EGCG) in an amount of at least 30 weight-%, preferably in an amount in the range of from 30 weight-% to 100 weight-% (preferably in an amount in the range of from 35 weight-% to 60 weight- %), more preferably in an amount of at least 50 weight-%, most preferably in an amount in the range of from 50 weight-% to 99 weight-%, based on the total amount of the green tea extract. Those green tea extracts may also contain caffeine in an amount up to 15 weight- %, preferably in an amount in the range of from 0.1 to 12 weight-%, more preferably in an amount of from 0.1 to 3 weight-%, based on the total weight of the green tea extract. The total amount of tea polyphenols in such green tea extracts may be preferable in the range of from 85 to 98 weight-% (preferably in the range of from 90 to 98 weight-%), whereas the total amount of catechins may be preferably in the range of from 65 to 90 weight-% (preferably in the range of from 65 to 80 weight-%), based on the total weight of the green tea extract. Case 251 13WO The term "(-)-epigallocatechin gallate" (EGCG) encompasses also (-)-EGCG derivatives such as pharmaceutically acceptable salts. Catechins are especially found in green tea extracts such as epicatechin gallate (ECG), epigallocatechin (EGC), gallocatechin gallate (ECG) and epigallocatechin gallate (EGCG), whereby EGCG is the most preferred one. EGCG can also be used in a formulated product form such as a Teavigo® tablet grade (= a green tea extract containing ca. 88% of EGCG admixed with ca. 3% of pectin), which is a directly compressible form granulated with pectin and is commercially available from DSM Nutritional Products Ltd, Kaiseraugst, Switzerland. Another suitable (—)-EGCG is e.g. Teavigo (a green tea extract containing > 94% of EGCG), commercially available from DSM Nutritional Products Ltd, Kaiseraugst, Switzerland. Another preferred embodiment for (-)-epigallocatechin gallate is a green tea fraction comprising at least 90 weight-% of (-)-epigallocatechin gallate (EGCG) and at most 2 weight-% of caffeine, especially a green tea fraction comprising at least 90 weight-% of EGCG, at most 1 weight-% of caffeine and at most 10 weight-% of epicatechin gallate (ECG), more especially a green tea fraction comprising at least 90 weight-% of EGCG, at most 0.5 weight-% (preferably at most 0.1 weight-%) of caffeine, at most 5.0 weight-% of epicatechin gallate (ECG) (preferably in the range of from 0.1 to 2.5 weight-%) and at most 3.5 weight-% (preferably at most 1.0 weight-%) of a total amount of epicatechin (EC), catechin (CAT), catechin gallate (CG), epigallocatechin (EGC), gallocatechin gallate (GCG), gallocatechin (GC) and gallic acid (GA) together, based on the total weight of the green tea extract. Resveratrol can be used in its essentially pure form derived from natural sources or from chemical synthesis, in a product form containing resveratrol and further additives, e.g. as a directly compressible form or as an extract. The extracts of red grape skin are especially those containing resveratrol in an amount of at least 30 weight-%, preferably in an amount in the range of from 30 weight-% to 100 Case 251 13WO weight-%, more preferably in an amount of at least 50 weight-%, most preferably in an amount in the range of from 50 weight-% to 99 weight-%, based on the total amount of the red wine extract. The term "resveratrol" as used herein comprises a derivative, metabolite or analogue thereof. The carbon-carbon double bond may be trans or cis and includes cis/trans mixtures. Etherified or esterified hydroxy groups may be derived from non-substituted or substituted, straight or branched chain alkyl groups having 1 to 26 carbon atoms or from non-substituted or substituted, straight or branched chain aliphatic, araliphatic or aromatic carboxylic acids having 1 to 26 carbon atoms.
Recommended publications
  • Current Awareness in Clinical Toxicology Editors: Damian Ballam Msc and Allister Vale MD
    Current Awareness in Clinical Toxicology Editors: Damian Ballam MSc and Allister Vale MD April 2015 CONTENTS General Toxicology 9 Metals 44 Management 22 Pesticides 49 Drugs 23 Chemical Warfare 51 Chemical Incidents & 36 Plants 52 Pollution Chemicals 37 Animals 52 CURRENT AWARENESS PAPERS OF THE MONTH Acute toxicity profile of tolperisone in overdose: observational poison centre-based study Martos V, Hofer KE, Rauber-Lüthy C, Schenk-Jaeger KM, Kupferschmidt H, Ceschi A. Clin Toxicol 2015; online early: doi: 10.3109/15563650.2015.1022896: Introduction Tolperisone is a centrally acting muscle relaxant that acts by blocking voltage-gated sodium and calcium channels. There is a lack of information on the clinical features of tolperisone poisoning in the literature. The aim of this study was to investigate the demographics, circumstances and clinical features of acute overdoses with tolperisone. Methods An observational study of acute overdoses of tolperisone, either alone or in combination with one non-steroidal anti-inflammatory drug in a dose range not expected to cause central nervous system effects, in adults and children (< 16 years), reported to our poison centre between 1995 and 2013. Current Awareness in Clinical Toxicology is produced monthly for the American Academy of Clinical Toxicology by the Birmingham Unit of the UK National Poisons Information Service, with contributions from the Cardiff, Edinburgh, and Newcastle Units. The NPIS is commissioned by Public Health England Results 75 cases were included: 51 females (68%) and 24 males (32%); 45 adults (60%) and 30 children (40%). Six adults (13%) and 17 children (57%) remained asymptomatic, and mild symptoms were seen in 25 adults (56%) and 10 children (33%).
    [Show full text]
  • Pureweigh®-FM
    Manufacturers of Hypo-al ler gen ic Nutritional Sup ple ments PureWeigh®-FM INTRODUCED 2000 What Is It? than DHEA in stimulating the thermogenic enzymes of the liver, helping to support a leaner BMI (Body Mass PureWeigh®-FM is an encapsulated supplement companion Index) and healthy weight control. In a double blind to PureWeigh® PREMEAL Beverage containing banaba study involving 30 overweight adults, 7-KETO supported (Lagerstroemia speciosa L.) extract, green tea extract, healthy body composition and BMI when combined with taurine, 7-KETO™ DHEA, biotin, magnesium citrate and exercise.* chromium polynicotinate. PureWeigh®-FM may also be used independently of PureWeigh® PREMEAL Beverage to support • Biotin, facilitating protein, fat and carbohydrate healthy glucose metabolism and promote weight loss.* metabolism by acting as a coenzyme for numerous metabolic reactions. A clinical study reported that high Features Include dose administration of biotin helped promote healthy glucose metabolism. A number of animal studies support • Banaba extract, containing a triterpenoid compound this claim. Biotin may also act to promote transcription called corosolic acid, reported in studies to support and translation of glucokinase, an enzyme found in the healthy glucose function and absorption. A recent liver and pancreas that participates in the metabolism phase II, double-blind, placebo-controlled multi-center of glucose to form glycogen. In addition, a double-blind trial in Japan suggested that banaba extract maintained study reported that biotin supplementation may promote healthy glucose function and was well tolerated by healthy lipid metabolism, citing an inverse relationship volunteers. Furthermore, an independent U.S. between plasma biotin and total lipids.* preliminary clinical study reported statistically significant weight loss in human volunteers • Magnesium citrate, providing a highly bioavailable supplementing with a 1% corosolic acid banaba extract.
    [Show full text]
  • Redalyc.Identification and Characterisation of Phenolic
    Ciência e Tecnologia de Alimentos ISSN: 0101-2061 [email protected] Sociedade Brasileira de Ciência e Tecnologia de Alimentos Brasil LEOUIFOUDI, Inass; ZYAD, Abdelmajid; AMECHROUQ, Ali; OUKERROU, Moulay Ali; MOUSE, Hassan Ait; MBARKI, Mohamed Identification and characterisation of phenolic compounds extracted from Moroccan olive mill wastewater Ciência e Tecnologia de Alimentos, vol. 34, núm. 2, abril-junio, 2014, pp. 249-257 Sociedade Brasileira de Ciência e Tecnologia de Alimentos Campinas, Brasil Available in: http://www.redalyc.org/articulo.oa?id=395940095005 How to cite Complete issue Scientific Information System More information about this article Network of Scientific Journals from Latin America, the Caribbean, Spain and Portugal Journal's homepage in redalyc.org Non-profit academic project, developed under the open access initiative Food Science and Technology ISSN 0101-2061 DDOI http://dx.doi.org/10.1590/fst.2014.0051 Identification and characterisation of phenolic compounds extracted from Moroccan olive mill wastewater Inass LEOUIFOUDI1,2*, Abdelmajid ZYAD2, Ali AMECHROUQ3, Moulay Ali OUKERROU2, Hassan Ait MOUSE2, Mohamed MBARKI1 Abstract Olive mill wastewater, hereafter noted as OMWW was tested for its composition in phenolic compounds according to geographical areas of olive tree, i.e. the plain and the mountainous areas of Tadla-Azilal region (central Morocco). Biophenols extraction with ethyl acetate was efficient and the phenolic extract from the mountainous areas had the highest concentration of total phenols’ content. Fourier-Transform-Middle Infrared (FT-MIR) spectroscopy of the extracts revealed vibration bands corresponding to acid, alcohol and ketone functions. Additionally, HPLC-ESI-MS analyses showed that phenolic alcohols, phenolic acids, flavonoids, secoiridoids and derivatives and lignans represent the most abundant phenolic compounds.
    [Show full text]
  • Applications of in Silico Methods to Analyze the Toxicity and Estrogen T Receptor-Mediated Properties of Plant-Derived Phytochemicals ∗ K
    Food and Chemical Toxicology 125 (2019) 361–369 Contents lists available at ScienceDirect Food and Chemical Toxicology journal homepage: www.elsevier.com/locate/foodchemtox Applications of in silico methods to analyze the toxicity and estrogen T receptor-mediated properties of plant-derived phytochemicals ∗ K. Kranthi Kumara, P. Yugandharb, B. Uma Devia, T. Siva Kumara, N. Savithrammab, P. Neerajaa, a Department of Zoology, Sri Venkateswara University, Tirupati, 517502, India b Department of Botany, Sri Venkateswara University, Tirupati, 517502, India ARTICLE INFO ABSTRACT Keywords: A myriad of phytochemicals may have potential to lead toxicity and endocrine disruption effects by interfering Phytochemicals with nuclear hormone receptors. In this examination, the toxicity and estrogen receptor−binding abilities of a QSAR modeling set of 2826 phytochemicals were evaluated. The endpoints mutagenicity, carcinogenicity (both CAESAR and ISS Toxicity models), developmental toxicity, skin sensitization and estrogen receptor relative binding affinity (ER_RBA) Nuclear hormone receptor binding were studied using the VEGA QSAR modeling package. Alongside the predictions, models were providing pos- Self−Organizing maps sible information for applicability domains and most similar compounds as similarity sets from their training Clustering and classification schemes sets. This information was subjected to perform the clustering and classification of chemicals using Self−Organizing Maps. The identified clusters and their respective indicators were considered as potential hotspot structures for the specified data set analysis. Molecular screening interpretations of models wereex- hibited accurate predictions. Moreover, the indication sets were defined significant clusters and cluster in- dicators with probable prediction labels (precision). Accordingly, developed QSAR models showed good pre- dictive abilities and robustness, which observed from applicability domains, representation spaces, clustering and classification schemes.
    [Show full text]
  • Download Product Insert (PDF)
    PRODUCT INFORMATION (−)-Epigallocatechin Gallate Item No. 70935 CAS Registry No.: 989-51-5 Formal Name: 3,4-dihydro-5,7-dihydroxy-2R-(3,4,5- OH trihydroxyphenyl)-2H-1-benzopyran-3R- OH yl-3,4,5-trihydroxy-benzoate H HO O Synonym: EGCG OH MF: C22H18O11 O FW: 458.4 H OH OH Purity: ≥96% O UV/Vis.: λmax: 276 nm Supplied as: A crystalline solid OH Storage: -20°C OH Stability: ≥2 years Item Origin: Plant/Folium camelliae Information represents the product specifications. Batch specific analytical results are provided on each certificate of analysis. Laboratory Procedures (−)-Epigallocatechin gallate (EGCG) is supplied as a crystalline solid. A stock solution may be made by dissolving the EGCG in an organic solvent purged with an inert gas. EGCG is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide. The solubility of EGCG in these solvents is approximately 20, 25, and 30 mg/ml, respectively. Further dilutions of the stock solution into aqueous buffers or isotonic saline should be made prior to performing biological experiments. Ensure that the residual amount of organic solvent is insignificant, since organic solvents may have physiological effects at low concentrations. Organic solvent-free aqueous solutions of EGCG can be prepared by directly dissolving the crystalline compound in aqueous buffers. The solubility of EGCG in PBS (pH 7.2) is approximately 25 mg/ml. We do not recommend storing the aqueous solution for more than one day. Description EGCG is a phenol that has been found in green and black tea plants and has diverse biological activities.1-7 1 It is lytic against T.
    [Show full text]
  • Polyphenols in Cancer Prevention: New Insights (Review)
    INTERNATIONAL JOURNAL OF FUNCTIONAL NUTRITION 1: 9, 2020 Polyphenols in cancer prevention: New insights (Review) GIUSI BRIGUGLIO1, CHIARA COSTA2, MANUELA POLLICINO1, FEDERICA GIAMBÒ1, STEFANIA CATANIA1 and CONCETTINA FENGA1 1Department of Biomedical and Dental Sciences and Morpho‑functional Imaging, Occupational Medicine Section, and 2Department of Clinical and Experimental Medicine, University of Messina, I‑98125 Messina, Italy Received July 30, 2020; Accepted September 21, 2020 DOI:10.3892/ijfn.2020.9 Abstract. A huge volume of literature data suggests that a diet Contents rich in fruits and vegetables, mostly due to the contribution of natural polyphenols, could reduce the incidence of specific 1. Introduction cancers. Resveratrol, epigallocatechin gallate and curcumin 2. Literature search are among the most extensively studied polyphenols: The 3. Classification of polyphenols majority of the effects attributed to these compounds are 4. Prostate cancer linked to their antioxidant and anti‑inflammatory properties. 5. Colon cancer The multiple mechanisms involved include the modulation 6. Breast cancer of molecular events and signaling pathways associated with 7. Lung cancer cell survival, proliferation, differentiation, migration, angio‑ 8. Bladder cancer genesis, hormonal activities, detoxification enzymes and 9. Skin cancer immune responses. Notwithstanding their promising role in 10. Pancreatic cancer cancer prevention and treatment, polyphenols often have a 11. Leukemia poor bioavailability when administered as pure active prin‑
    [Show full text]
  • Chemical Oxidation Applications for Industrial Wastewaters
    ©2019 The Author(s) This is an Open Access book distributed under the terms of the Creative Commons Attribution Licence (CC BY 4.0), which permits copying and redistribution for non- commercial purposes, provided the original work is properly cited and that any new works are made available on the same conditions (http://creativecommons.org/licenses/by/4.0/). This does not affect the rights licensed or assigned from any third party in this book. This title was made available Open Access through a partnership with Knowledge Unlatched. IWA Publishing would like to thank all of the libraries for pledging to support the transition of this title to Open Access through the KU Select 2018 program. Downloaded from http://iwaponline.com/ebooks/book-pdf/521267/wio9781780401416.pdf by guest on 24 September 2021 Chemical Oxidation Applications for Industrial Wastewaters Chemical Oxidation Applications for Industrial This book covers the most recent scientific and technological developments (state-of-the-art) in the field of chemical oxidation processes applicable for the Chemical Oxidation efficient treatment of biologically-difficult-to-degrade, toxic and/or recalcitrant effluents originating from different manufacturing processes. It is a comprehensive Applications for review of process and pollution profiles as well as conventional, advanced and emerging treatment processes & technologies developed for the most relevant and pollution (wet processing)-intensive industrial sectors. Industrial Wastewaters It addresses chemical/photochemical oxidative treatment processes, case- Olcay Tünay, Işık Kabdaşlı, Idil Arslan-Alaton and Tuğba Ölmez-Hancı specific treatability problems of major industrial sectors, emerging (novel) as well as pilot/full-scale applications, process integration, treatment system design & sizing criteria (figure-of merits), cost evaluation and success stories in the application of chemical oxidative treatment processes.
    [Show full text]
  • Thyroid-Modulating Activities of Olive and Its Polyphenols: a Systematic Review
    nutrients Review Thyroid-Modulating Activities of Olive and Its Polyphenols: A Systematic Review Kok-Lun Pang 1,† , Johanna Nathania Lumintang 2,† and Kok-Yong Chin 1,* 1 Department of Pharmacology, Faculty of Medicine, Universiti Kebangsaan Malaysia, Jalan Yaacob Latif, Bandar Tun Razak, Cheras 56000, Kuala Lumpur, Malaysia; [email protected] 2 Faculty of Applied Sciences, UCSI University Kuala Lumpur Campus, Jalan Menara Gading, Taman Connaught, Cheras 56000, Kuala Lumpur, Malaysia; [email protected] * Correspondence: [email protected]; Tel.: +60-3-91459573 † These authors contributed equally to this work. Abstract: Olive oil, which is commonly used in the Mediterranean diet, is known for its health benefits related to the reduction of the risks of cancer, coronary heart disease, hypertension, and neurodegenerative disease. These unique properties are attributed to the phytochemicals with potent antioxidant activities in olive oil. Olive leaf also harbours similar bioactive compounds. Several studies have reported the effects of olive phenolics, olive oil, and leaf extract in the modulation of thyroid activities. A systematic review of the literature was conducted to identify relevant studies on the effects of olive derivatives on thyroid function. A comprehensive search was conducted in October 2020 using the PubMed, Scopus, and Web of Science databases. Cellular, animal, and human studies reporting the effects of olive derivatives, including olive phenolics, olive oil, and leaf extracts on thyroid function were considered. The literature search found 445 articles on this topic, but only nine articles were included based on the inclusion and exclusion criteria. All included articles were animal studies involving the administration of olive oil, olive leaf extract, or olive pomace residues orally.
    [Show full text]
  • Effect of Epigallocatechin-3-Gallate, Major Ingredient of Green Tea, on the Pharmacokinetics of Rosuvastatin in Healthy Volunteers
    Journal name: Drug Design, Development and Therapy Article Designation: Original Research Year: 2017 Volume: 11 Drug Design, Development and Therapy Dovepress Running head verso: Kim et al Running head recto: Effect of green tea on the pharmacokinetics of rosuvastatin open access to scientific and medical research DOI: http://dx.doi.org/10.2147/DDDT.S130050 Open Access Full Text Article ORIGINAL RESEARCH Effect of epigallocatechin-3-gallate, major ingredient of green tea, on the pharmacokinetics of rosuvastatin in healthy volunteers Tae-Eun Kim1 Abstract: Previous in vitro studies have demonstrated the inhibitory effect of green tea on Na Ha2 drug transporters. Because rosuvastatin, a lipid-lowering drug widely used for the prevention of Yunjeong Kim2 cardiovascular events, is a substrate for many drug transporters, there is a possibility that there Hyunsook Kim1 is interaction between green tea and rosuvastatin. The aim of this study was to investigate the Jae Wook Lee3 effect of green tea on the pharmacokinetics of rosuvastatin in healthy volunteers. An open-label, Ji-Young Jeon2 three-treatment, fixed-sequence study was conducted. On Day 1, 20 mg of rosuvastatin was given to all subjects. After a 3-day washout period, the subjects received 20 mg of rosuvastatin Min-Gul Kim2,4 plus 300 mg of epigallocatechin-3-gallate (EGCG), a major ingredient of green tea (Day 4). 1 Department of Clinical After a 10-day pretreatment of EGCG up to Day 14, they received rosuvastatin (20 mg) plus Pharmacology, Konkuk University Medical Center, Seoul, 2Center for EGCG (300 mg) once again (Day 15). Blood samples for the pharmacokinetic assessments Clinical Pharmacology, Biomedical were collected up to 8 hours after each dose of rosuvastatin.
    [Show full text]
  • Oleuropein Or Rutin Consumption Decreases the Spontaneous Development of Osteoarthritis in the Hartley Guinea Pig
    Osteoarthritis and Cartilage 23 (2015) 94e102 Oleuropein or rutin consumption decreases the spontaneous development of osteoarthritis in the Hartley guinea pig M.-N. Horcajada y a, C. Sanchez z a, F. Membrez Scalfo y, P. Drion x, F. Comblain z, * S. Taralla k, A.-F. Donneau ¶, E.A. Offord y, Y. Henrotin z # y Nestle Research Center, Nutrition and Health Research, Vers-Chez-les-Blanc, Lausanne 26 1000, Switzerland z Bone and Cartilage Research Unit, Arthropole,^ University of Liege, Institute of Pathology, CHU Sart-Tilman, 4000 Liege, Belgium x GIGA CHU Animal Facility, University of Liege, 4000 Liege, Belgium k Artialis SA, 4000 Liege Belgium ¶ Public Health Department, University of Liege, 4000 Liege, Belgium # Department of Physical Therapy and Rehabilitation, Princess Paola Hospital, Marche-en-famenne, Belgium article info summary Article history: Objective: To assess the potential protective effects of three polyphenols oleuropein, rutin and curcumin, Received 10 February 2014 on joint ageing and osteoarthritis (OA) development. Accepted 28 August 2014 Design: Sixty 4-week-old DunkineHartley guinea pigs were randomized into four groups and received daily during 31 weeks either standard guinea pig diet (control group) or a standard guinea pig diet Keywords: enriched with oleuropein (0.025%), rutin (0.5%) or rutin/curcumin (0.5%/0.25%) association. Biomarkers Osteoarthritis of OA (Coll2-1, Coll2-1NO2, Fib3-1, Fib3-2, ARGS), as well as inflammation prostaglandin E2 (PGE2) were Phytonutrients quantified in the serum. Histological assessments of knee cartilage and synovial membrane were per- Oleuropein fi Rutin formed at week 4 ( ve young reference guinea pigs) and week 35.
    [Show full text]
  • Hydroxytyrosol but Not Resveratrol Ingestion Induced an Acute Increment of Post Exercise Blood Flow in Brachial Artery
    Health, 2016, 8, 1766-1777 http://www.scirp.org/journal/health ISSN Online: 1949-5005 ISSN Print: 1949-4998 Hydroxytyrosol But Not Resveratrol Ingestion Induced an Acute Increment of Post Exercise Blood Flow in Brachial Artery Giorgia Sarais1, Antonio Crisafulli2, Daniele Concu3, Andrea Fois4, Abdallah Raweh5, Alberto Concu3,5 1Department of Life and Environmental Sciences, University of Cagliari, Cagliari, Italy 2Laboratory of Sports Physiology, University of Cagliari, Cagliari, Italy 3IIC Technologies Ltd., Cagliari, Italy 4EventFeel Ltd., Cagliari, Italy 5Medical Sciences Faculty, The LUdeS Foundation Higher Education Institution, Kalkara, Malta How to cite this paper: Sarais, G., Crisaful- Abstract li, A., Concu, D., Fois, A., Raweh, A. and Concu, A. (2016) Hydroxytyrosol But Not The aim of this study was to test if previous ingestion of compounds containing res- Resveratrol Ingestion Induced an Acute veratrol or hydroxytyrosol, followed by an exhausting hand grip exercise, could in- Increment of Post Exercise Blood Flow in duce an acute post-exercise increase in brachial blood flow. Six healthy subjects Brachial Artery. Health, 8, 1766-1777. http://dx.doi.org/10.4236/health.2016.815170 (three males and three females, 35 ± 7 years), 60 minutes after ingestion of a capsule containing 200 mg of resveratrol or 30 ml of extra virgin olive oil enriched with ty- Received: August 19, 2016 rosol, oleuropein and hydroxytyrosol, performed a hand grip exercise equal to half of Accepted: December 11, 2016 their maximum strength until they were no longer able to express the same force Published: December 14, 2016 (2-day interval between tests). The nonparametric Wilcoxon signed rank test was Copyright © 2016 by authors and used for statistical evaluations.
    [Show full text]
  • Reducing Toxic Reactive Carbonyl Species in E-Cigarette Emissions
    RSC Advances View Article Online PAPER View Journal | View Issue Reducing toxic reactive carbonyl species in e- cigarette emissions: testing a harm-reduction Cite this: RSC Adv., 2020, 10,21535 strategy based on dicarbonyl trapping Bruna de Falco, †af Antonios Petridis,†ac Poornima Paramasivan,b Antonio Dario Troise, de Andrea Scaloni,e Yusuf Deeni,b W. Edryd Stephens*c and Alberto Fiore *a Reducing the concentration of reactive carbonyl species (RCS) in e-cigarette emissions represents a major goal to control their potentially harmful effects. Here, we adopted a novel strategy of trapping carbonyls present in e-cigarette emissions by adding polyphenols in e-liquid formulations. Our work showed that the addition of gallic acid, hydroxytyrosol and epigallocatechin gallate reduced the levels of carbonyls formed in the aerosols of vaped e-cigarettes, including formaldehyde, methylglyoxal and glyoxal. Liquid chromatography mass spectrometry analysis highlighted the formation of covalent adducts between Creative Commons Attribution 3.0 Unported Licence. aromatic rings and dicarbonyls in both e-liquids and vaped samples, suggesting that dicarbonyls were formed in the e-liquids as degradation products of propylene glycol and glycerol before vaping. Short- Received 6th March 2020 term cytotoxic analysis on two lung cellular models showed that dicarbonyl-polyphenol adducts are not Accepted 29th May 2020 cytotoxic, even though carbonyl trapping did not improve cell viability. Our work sheds lights on the DOI: 10.1039/d0ra02138e ability of polyphenols to trap RCS in high carbonyl e-cigarette emissions, suggesting their potential value rsc.li/rsc-advances in commercial e-liquid formulations. Introduction smoking-related symptoms and conditions to become manifest, This article is licensed under a it is too early to evaluate the long-term clinical effects of vaping The use of e-cigarettes is a major issue in public health.
    [Show full text]