DOCSLIB.ORG

(12) Patent Application Publication (10) Pub. No.: US 2003/0099756A1 GOW 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 2003/0099756A1 GOW Et Al US 2003.0099756A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2003/0099756A1 GOW et al. (43) Pub. Date: May 29, 2003 (54) METHOD OF PRODUCING A PROCESSED Publication Classification KAVA PRODUCT HAVING AN ALTERED KAVALACTONE DISTRIBUTION AND (51) Int. Cl." ....................................................... A23K 1100 PROCESSED KAVA PRODUCTS PRODUCED (52) U.S. Cl. .............................................................. 426/615 USING THE SAME (76) Inventors: Robert Gow, Naples, FL (US); John (57) ABSTRACT Pierce, Moreno Valley, CA (US); Brian A method of producing a processed kava product involves Pierce, Thousand Oaks, CA (US); using an extraction Solvent, Such as liquid CO, to prefer William Birdsall, Naples, FL (US) entially extract different kavalactones from the Source mate Correspondence Address: rial at different rates. By controlling the extraction param CLIFFORD CHANCE US LLP eters and Stopping the extraction before all of the kavalactones have been extracted or allowing the extracted 200 PARKAVENUE kavalactones to be preferentially precipitated in one or more NEW YORK, NY 10166 (US) collection environments, a processed kava product can be (21) Appl. No.: 10/263,579 produced that has a kavalactone distribution profile that can differ Substantially from that of the source material. As a (22) Filed: Oct. 3, 2002 result, roots from a leSS desirable kava cultivar can be used to produce a processed kava product which has a kavalac Related U.S. Application Data tone distribution profile that is similar to that of a highly desired cultivar. The kava paste can be further processed to (60) Provisional application No. 60/326,928, filed on Oct. produce a dry flowable powder Suitable for use in, e.g., a 3, 2001. Provisional application No. 60/369,889, filed tableting formula. A rapid dissolve tablet formulation for use on Apr. 3, 2002. in the delivery of kavalactones is also disclosed. Patent Application Publication May 29, 2003 Sheet 1 of 7 US 2003/0099756A1 JeA}|no emey nenue/Wyo edAL Patent Application Publication May 29, 2003 Sheet 2 of 7 US 2003/0099756A1 Suemino emey nenueAgo JedunN US 2003/0099756A1 (p) uemey I uemeyoupAuO Patent Application Publication May 29, 2003 Sheet 4 of 7 US 2003/0099756A1 -- „KeG-OWLeJeA?InO säsv=š0?dae.(WHG+W)º...……………………………………………………ººº!V.-?---- sasv=sQNI(»Hq.+x)GNv.»||W| --·1-·||-·}.|- 0 Patent Application Publication May 29, 2003 Sheet 5 of 7 US 2003/0099756A1 -#-,--v•- briti?benxazoo | "OIHS o O wr c S S v v effeueoued ufeW (A) uuofue + (ANC) uuofueMAXOueused Patent Application Publication May 29, 2003 Sheet 6 of 7 US 2003/0099756A1 080/ 9"OIH ºqNWHq.+x)sasväg?NI uo?oeulxezoopinbl-? (A+Awa)sasv?Hoad O O w e5eue3.edu.6éMY (A)vm uluofueve + (ANC) uuofueMAXOueused Patent Application Publication May 29, 2003 Sheet 7 of 7 US 2003/0099756A1 Z1021)XEZOOb?T– /'OIH US 2003/0099756 A1 May 29, 2003 METHOD OF PRODUCING A PROCESSED KAVA “two-day”, “medicinal', and “no drink”. “Daily kava cul PRODUCT HAVING AN ALTERED KAVALACTONE tivars are generally consumed daily and have relatively DISTRIBUTION AND PROCESSED KAVA short-term effects. “Custom kava cultivars tend to be used PRODUCTS PRODUCED USING THE SAME for ritual and ceremonial purposes. “Two-day kava culti vars tend to have pronounced physiological effects and are CROSS-REFERENCE TO RELATED known as “two day” because the drinker is usually affected APPLICATIONS: for two days. “Medicinal kava cultivars are specific for the treatment of ailments like rheumatism. "No Drink' kava 0001. This application is claims priority under 35 U.S.C. cultivars are not recommended for consumption because S 119 to U.S. Provisional Patent Application Serial No. they tend to induce nausea and other undesirable effects. 60/326,928 entitled “Methods For Processing Kava Root (Piper Methysticum) And Kava-Derived Products Generated 0007 More recently, there have been concerns associat By These Methods Having Controllable Kavalactone ing kava with occurrences of liver damage, although these Ratios', filed on Oct. 3, 2001, and U.S. Provisional Appli reports are primarily anecdotal. Studies done in the 1970s cation Serial No. 60/369,889 entitled “Dry Flowable Kava and 1980s have found that “two day” kava cultivars have Extract Powder And Fast-Dissolve Kava Extract Composi particularly high concentrations of methysticin and dihy tion For Oral Delivery”, filed on Apr. 3, 2002. The entire dromethysticin. These kavalactones contain a methylene contents of both of these applications are hereby expressly dioxyphenyl functional group which, when activated incorporated by reference. through metabolic activity, forms intermediary compounds that can inactivate multiple P450 enzymes. There are some FIELD OF THE INVENTION(S) suggestions that inhibition of P450 enzymes can interfere with the metabolism of many pharmaceuticals. The Solution 0002 This invention is related to methods for processing proposed in the prior art is the development of new kava kava to produce a kava extract with particular kavalactone cultivars with reduced amounts of methysticin and dihy concentration profile, a processed kava product, Such as a dromethysticin and increased kavain content. dry flowable kava extract powder, and the use of Such a powder in a rapid-dissolve tablet for oral delivery. 0008 One of the most highly prized kava cultivars is a one-day cultivar that grows in Vanuatu. Relative to other cultivars, this cultivar is naturally low in methysticin and BACKGROUND dihydromethysticin and has a proportionally higher concen 0.003 Kava plants, a type of pepper plant also known as tration of kavain. However, this cultivar is not widely grown Piper methysticum, arc generally found in Polynesia, or available and most commercially available cultivars have Melanesia, and Micronesia. The kava plant contains high increased levels of methysticin and dihydromethysticin and concentrations of kavalactones (sometimes referred to as lower concentrations of kavain. Although breeding of new kavapyrones), including kavain, methysticin, yangonin, cultivars that can be widely grown and which have lower dihydromethysticin, desmethoxyyangonin, and dihy concentrations of methysticin and dihydromethysticin and drokavain, and has been used as an herbal medicine. The increased concentrations of kavain is possible, this can be a prized part of the kava plant is the root System because it time consuming proceSS and is not assured of Success. In contains the highest concentrations of the active kavalac addition, the kavalactones Suspected of producing toxic tones. Kavalactones are also found in other parts of the plant. effects when consumed by humans are also toxic to various General information about kava plants can be found in insects and microorganisms, Such as fungi. Thus, the hardi Vincent Lebot, et al., “Kava The Pacific Elixir; The Defini est cultivars are generally those which are least Suitable for tive Guide to its Ethnobotany, History, and Chemistry', human consumption. Inner Traditions Intl. Ltd. (March 1997). 0009. In a kava extraction process, the rate at which 0004. After a kava plant is harvested, the root is conven various kavalactone components are extracted varies tionally processed to generate a consumable product. In according to the extraction Solvent and extraction conditions conventional and historical methods, the root is dried and used. However, kava root extracts are conventionally Sold ground to a powder. This powder contains not only the based upon total kavalactone content. Thus, the focus of kavalactones but also plant oils, resins, and other Substances. conventional commercial extraction techniques has been to The powder can be mixed with water to form a beverage. extract as much of the kavalactone content from the root The resinous ground dried root can also be packaged into Source as possible and knowledge regarding different rates capsules or other forms of delivery. of extraction for different kavalactones is used to adjust the 0005 The effects of ingesting kava root extract will vary extraction proceSS or Select appropriate extraction Steps to from person to perSon. Common effects include a State of provide for the greatest total kavalactone extraction. relaxation and a reduction in muscle tenseneSS. Kava root 0010 Various extraction techniques have been used to has also been used to help Sufferers of insomnia. It can also process kava root. Such techniques include the use of produce a mild State of euphoria. The ratioS of the various Supercritical carbon dioxide (CO2) extraction, fluorocarbon kavalactones in the consumed product has a large impact on extraction, and the use of various other organic and non the effect experienced by the user. organic Solvents to remove the kavalactones from the dried 0006 There are a large number of different kava culti root. The resulting bulk extract is in the form of a paste. vars, each of which has differing ratios of the different 0011 Supercritical CO processes have been found to kavalactones. Through historical knowledge and experimen extract the largest quantity of kavalactones from the root and tation, various kava cultivars have been classified according thus conventional practice has been to focus on the use of to their effect, such as “daily” or “one-day”, “custom', Supercritical CO2 to extract all of the kavalactones from the US 2003/0099756 A1 May 29, 2003 root in the production of kava extracts. AS will be appreci use in a fast dissolve tablet and other applications, and which ated, bulk extracts of Substantially all of the kavalactones in as a kavalactone profile that is altered from the profile of the the root will generally contain kavalactones in the same or kava feedstock. The present methodologies also allow the nearly the Same proportions as present in the Source root. distribution of kavalactones to be altered or adjusted to Because of the differing effects produced by variations in the achieve a particular kavalactone profile wherein the effec kavalactone ratioS of different cultivars, producers of Such tiveness of the kava can be enhanced or the negative effects kava products are limited to specific kava cultivars as Source reduced.
Load more

Recommended publications
  • (12) Patent Application Publication (10) Pub. No.: US 2003/0105159 A1 Mccleary Et Al
    US 200301 05159A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2003/0105159 A1 McCleary et al. (43) Pub. Date: Jun. 5, 2003 (54) KAVALACTONE COMPOSITIONS AND Publication Classification METHODS OF USE (51) Int. Cl." ....................... A61K 31/35; A61K 31/366; (76) Inventors: Joel McCleary, The Plains, VA (US); A61K 35/78; A61K 31/16 Peter S. Staats, Towson, MD (US) (52) U.S. Cl. ........................... 514/460; 514/625; 424/760 Correspondence Address: FISH & RICHARDSON PC 225 FRANKLIN ST BOSTON, MA 02110 (US) (57) ABSTRACT (21) Appl. No.: 10/214,624 (22) Filed: Aug. 8, 2002 This invention relates tO kavalactone-containing composi tions, and more particularly to compositions having com Related U.S. Application Data pounds derived from kavalactones and from capsaicinoids. The compositions are useful in modulating pain, and thus (60) Provisional application No. 60/311,437, filed on Aug. can be used to mediate, or eliminate, Sensations of pain, 10, 2001. thereby providing pain relief and reduction. US 2003/0105159 A1 Jun. 5, 2003 KAVALACTONE COMPOSITIONS AND METHODS 0006. In one embodiment, the invention relates to an OF USE analgesic topical composition having: (a) a kavalactone; (b) capsaicinoid or Synthetic derivatives thereof; and (c) a CROSS-REFERENCE TO RELATED pharmaceutically acceptable carrier; wherein the weight APPLICATIONS ratio of(a):(b) is from 5000:1 to 1:2 (e.g., 800:1 to 1:1; 500:1 to 5:1). In other aspects, the composition includes an effec 0001. This application claims benefit of U.S. application tive amount of kavalactones, active kavalactones, or capsai Ser.
    [Show full text]
  • (12) United States Patent (10) Patent No.: US 9.421,180 B2 Zielinski Et Al
    USOO9421 180B2 (12) United States Patent (10) Patent No.: US 9.421,180 B2 Zielinski et al. (45) Date of Patent: Aug. 23, 2016 (54) ANTIOXIDANT COMPOSITIONS FOR 6,203,817 B1 3/2001 Cormier et al. .............. 424/464 TREATMENT OF INFLAMMATION OR 6,323,232 B1 1 1/2001 Keet al. ............ ... 514,408 6,521,668 B2 2/2003 Anderson et al. ..... 514f679 OXIDATIVE DAMAGE 6,572,882 B1 6/2003 Vercauteren et al. ........ 424/451 6,805,873 B2 10/2004 Gaudout et al. ....... ... 424/401 (71) Applicant: Perio Sciences, LLC, Dallas, TX (US) 7,041,322 B2 5/2006 Gaudout et al. .............. 424/765 7,179,841 B2 2/2007 Zielinski et al. .. ... 514,474 (72) Inventors: Jan Zielinski, Vista, CA (US); Thomas 2003/0069302 A1 4/2003 Zielinski ........ ... 514,452 Russell Moon, Dallas, TX (US); 2004/0037860 A1 2/2004 Maillon ...... ... 424/401 Edward P. Allen, Dallas, TX (US) 2004/0091589 A1 5, 2004 Roy et al. ... 426,265 s s 2004/0224004 A1 1 1/2004 Zielinski ..... ... 424/442 2005/0032882 A1 2/2005 Chen ............................. 514,456 (73) Assignee: Perio Sciences, LLC, Dallas, TX (US) 2005, 0137205 A1 6, 2005 Van Breen ..... 514,252.12 2005. O154054 A1 7/2005 Zielinski et al. ............. 514,474 (*) Notice: Subject to any disclaimer, the term of this 2005/0271692 Al 12/2005 Gervasio-Nugent patent is extended or adjusted under 35 et al. ............................. 424/401 2006/0173065 A1 8/2006 BeZwada ...................... 514,419 U.S.C. 154(b) by 19 days. 2006/O193790 A1 8/2006 Doyle et al.
    [Show full text]
  • Herbal Insomnia Medications That Target Gabaergic Systems: a Review of the Psychopharmacological Evidence
    Send Orders for Reprints to [email protected] Current Neuropharmacology, 2014, 12, 000-000 1 Herbal Insomnia Medications that Target GABAergic Systems: A Review of the Psychopharmacological Evidence Yuan Shia, Jing-Wen Donga, Jiang-He Zhaob, Li-Na Tanga and Jian-Jun Zhanga,* aState Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, P.R. China; bDepartment of Pharmacology, School of Marine, Shandong University, Weihai, P.R. China Abstract: Insomnia is a common sleep disorder which is prevalent in women and the elderly. Current insomnia drugs mainly target the -aminobutyric acid (GABA) receptor, melatonin receptor, histamine receptor, orexin, and serotonin receptor. GABAA receptor modulators are ordinarily used to manage insomnia, but they are known to affect sleep maintenance, including residual effects, tolerance, and dependence. In an effort to discover new drugs that relieve insomnia symptoms while avoiding side effects, numerous studies focusing on the neurotransmitter GABA and herbal medicines have been conducted. Traditional herbal medicines, such as Piper methysticum and the seed of Zizyphus jujuba Mill var. spinosa, have been widely reported to improve sleep and other mental disorders. These herbal medicines have been applied for many years in folk medicine, and extracts of these medicines have been used to study their pharmacological actions and mechanisms. Although effective and relatively safe, natural plant products have some side effects, such as hepatotoxicity and skin reactions effects of Piper methysticum. In addition, there are insufficient evidences to certify the safety of most traditional herbal medicine. In this review, we provide an overview of the current state of knowledge regarding a variety of natural plant products that are commonly used to treat insomnia to facilitate future studies.
    [Show full text]
  • Plant-Based Medicines for Anxiety Disorders, Part 2: a Review of Clinical Studies with Supporting Preclinical Evidence
    CNS Drugs 2013; 24 (5) Review Article Running Header: Plant-Based Anxiolytic Psychopharmacology Plant-Based Medicines for Anxiety Disorders, Part 2: A Review of Clinical Studies with Supporting Preclinical Evidence Jerome Sarris,1,2 Erica McIntyre3 and David A. Camfield2 1 Department of Psychiatry, Faculty of Medicine, University of Melbourne, Richmond, VIC, Australia 2 The Centre for Human Psychopharmacology, Swinburne University of Technology, Melbourne, VIC, Australia 3 School of Psychology, Charles Sturt University, Wagga Wagga, NSW, Australia Correspondence: Jerome Sarris, Department of Psychiatry and The Melbourne Clinic, University of Melbourne, 2 Salisbury Street, Richmond, VIC 3121, Australia. Email: [email protected], Acknowledgements Dr Jerome Sarris is funded by an Australian National Health & Medical Research Council fellowship (NHMRC funding ID 628875), in a strategic partnership with The University of Melbourne, The Centre for Human Psychopharmacology at the Swinburne University of Technology. Jerome Sarris, Erica McIntyre and David A. Camfield have no conflicts of interest that are directly relevant to the content of this article. 1 Abstract Research in the area of herbal psychopharmacology has revealed a variety of promising medicines that may provide benefit in the treatment of general anxiety and specific anxiety disorders. However, a comprehensive review of plant-based anxiolytics has been absent to date. Thus, our aim was to provide a comprehensive narrative review of plant-based medicines that have clinical and/or preclinical evidence of anxiolytic activity. We present the article in two parts. In part one, we reviewed herbal medicines for which only preclinical investigations for anxiolytic activity have been performed. In this current article (part two), we review herbal medicines for which there have been both preclinical and clinical investigations for anxiolytic activity.
    [Show full text]
  • Kava Kava Extract Is Available from Ashland Chemical Co., Mini Star International, Inc., and QBI (Quality Botanical Ingredients, Inc.)
    SUMMARY OF DATA FOR CHEMICAL SELECTION Kava Kava 9000-38-8; 84696-40-2 November 1998 TABLE OF CONTENTS Basis for Nomination Chemical Identification Production Information Use Pattern Human Exposure Regulatory Status Evidence for Possible Carcinogenic Activity Human Data Animal Data Metabolism Other Biological Effects Structure-Activity Relationships References BASIS OF NOMINATION TO THE CSWG Kava kava is brought to the attention of the CSWG because it is a rapidly growing, highly used dietary supplement introduced into the mainstream U.S. market relatively recently. Through this use, millions of consumers using antianxiety preparations are potentially exposed to kava kava. A traditional beverage of various Pacific Basin countries, kava clearly has psychoactive properties. The effects of its long-term consumption have not been documented adequately; preliminary studies suggest possibly serious organ system effects. The potential carcinogenicity of kava and its principal constituents are unknown. INPUT FROM GOVERNMENT AGENCIES/INDUSTRY The U.S. Pharmacopeia is in the process of reviewing kava kava. No decision on preparation of a monograph has been made. SELECTION STATUS ACTION BY CSWG: 12/14/98 Studies requested: - Toxicological evaluation, to include studies of reproductive toxicity and neurotoxicity - Genotoxicity Priority: High Rationale/Remarks: - Significant human exposure - Leading dietary supplement with rapidly growing use - Concern that kava has been promoted as a substitute for ritilin in children - Test extract standardized to 30 percent kavalactones - NCI is conducting studies in Salmonella typhimurium CHEMICAL IDENTIFICATION CAS Registry Number: 9000-38-8 Kava-kava resin (8CI) Chemical Abstract Service Name: 84696-40-2 CAS Registry Number: Pepper (Piper), P. methysticum, ext. Chemical Abstract Service Name: Extract of kava; kava extract; Piper Synonyms and Trade Names: methisticum extract Description: The tropical shrub Piper methysticum is widely cultivated in the South Pacific.
    [Show full text]
  • Article – – = = = = C7-C8 – – – – Is Known to = = C5-C6
    J. Braz. Chem. Soc., Vol. 20, No. 9, 1687-1697, 2009. Printed in Brazil - ©2009 Sociedade Brasileira de Química 0103 - 5053 $6.00+0.00 Article Synthesis of Novel Kavain-like Derivatives and Evaluation of their Cytotoxic Activity Patricia de A. Amaral,a,b Julien Petrignet,c Nicolas Gouault,b Taciane Agustini,a Françoise Lohézic-Ledévéhat,b Alexandre Cariou,b René Grée,c Vera L. Eifler-Lima*,a and Michèle Davidb aLaboratório de Síntese Orgânica Medicinal, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, 90610-000 Porto Alegre-RS, Brazil bLaboratoire de Chimie Therapeutique, UPRES 4090, Université de Rennes 1, Rennes, France cLaboratoire de Chimie et Photonique Moléculaires, CNRS UMR 6510, Université de Rennes 1, Rennes, France Reações de acoplamento do tipo Heck, Sonogashira-Hagihara, Suzuki-Miyaura e reação de aldolisação catalizadas por metal foram utilizadas para a obtenção de três séries de d-valerolactonas substituídas em posições 3, 4, 5 e 6 do anel lactônico. As 26 d-valerolactonas sintetizadas foram testadas contra três linhagens celulares e cinco delas exibiram uma moderada atividade citotóxica. Palladium-catalyzed cross coupling reactions (Sonogashira-Hagihara, Suzuki-Miyaura, and Heck) coupling and nickel hydride-mediated tandem isomerization aldolisation have been used for the synthesis of three series of d-valerolactones substituted in positions 3, 4, 5 and 6 of the lactone ring. The 26 kavaïn-like derivatives were tested against three cell lines and five of them exhibited a weak cytotoxic activity. Keywords:
    [Show full text]
  • Phytochem Referenzsubstanzen
    High pure reference substances Phytochem Hochreine Standardsubstanzen for research and quality für Forschung und management Referenzsubstanzen Qualitätssicherung Nummer Name Synonym CAS FW Formel Literatur 01.286. ABIETIC ACID Sylvic acid [514-10-3] 302.46 C20H30O2 01.030. L-ABRINE N-a-Methyl-L-tryptophan [526-31-8] 218.26 C12H14N2O2 Merck Index 11,5 01.031. (+)-ABSCISIC ACID [21293-29-8] 264.33 C15H20O4 Merck Index 11,6 01.032. (+/-)-ABSCISIC ACID ABA; Dormin [14375-45-2] 264.33 C15H20O4 Merck Index 11,6 01.002. ABSINTHIN Absinthiin, Absynthin [1362-42-1] 496,64 C30H40O6 Merck Index 12,8 01.033. ACACETIN 5,7-Dihydroxy-4'-methoxyflavone; Linarigenin [480-44-4] 284.28 C16H12O5 Merck Index 11,9 01.287. ACACETIN Apigenin-4´methylester [480-44-4] 284.28 C16H12O5 01.034. ACACETIN-7-NEOHESPERIDOSIDE Fortunellin [20633-93-6] 610.60 C28H32O14 01.035. ACACETIN-7-RUTINOSIDE Linarin [480-36-4] 592.57 C28H32O14 Merck Index 11,5376 01.036. 2-ACETAMIDO-2-DEOXY-1,3,4,6-TETRA-O- a-D-Glucosamine pentaacetate 389.37 C16H23NO10 ACETYL-a-D-GLUCOPYRANOSE 01.037. 2-ACETAMIDO-2-DEOXY-1,3,4,6-TETRA-O- b-D-Glucosamine pentaacetate [7772-79-4] 389.37 C16H23NO10 ACETYL-b-D-GLUCOPYRANOSE> 01.038. 2-ACETAMIDO-2-DEOXY-3,4,6-TRI-O-ACETYL- Acetochloro-a-D-glucosamine [3068-34-6] 365.77 C14H20ClNO8 a-D-GLUCOPYRANOSYLCHLORIDE - 1 - High pure reference substances Phytochem Hochreine Standardsubstanzen for research and quality für Forschung und management Referenzsubstanzen Qualitätssicherung Nummer Name Synonym CAS FW Formel Literatur 01.039.
    [Show full text]
  • (12) United States Patent (10) Patent No.: US 6,746,695 B1 Martin Et Al
    USOO6746695B1 (12) United States Patent (10) Patent No.: US 6,746,695 B1 Martin et al. (45) Date of Patent: Jun. 8, 2004 (54) PHARMACEUTICAL PREPARATIONS OF Abad, MJ et al., Anti-inflammatory activity of some medici BOACTIVE SUBSTANCES EXTRACTED nal plant extracts from Venezuela. J. Ethnopharmacol1996 FROM NATURAL SOURCES Dec;55(1):63–8. Alarcon-Aguilara, FJ, et al., Study of the anti-hyperglyce (75) Inventors: Michael Z. Martin, Laupahoehoe, HI mic effect of plants used as antidiabetics. J. Ethnopharmacol (US); Mehdi Ashraf-Khorassani, Blacksburg, VA (US); Larry Taylor, 612:101-110 (1998). Blacksburg, VA (US) Almeida CE et al., Analysis of anti-diarrheic effect of plants used in popular medicine. Rev Saude Publica 1995 (73) Assignees: Armadillo Pharmaceuticals, Inc., Dec;29(6):428-33. Armocas, CA (US); Virginia Tech. Alves KB, et al., Inhibition of aminopeptidase activity by Intellectual Properties, Inc., aromatic and other cyclic compounds. Braz, J Med Biol Res. Blackburg, VA (US) 1992:25(11):1103–6. (*) Notice: Subject to any disclaimer, the term of this Anesini C, et al., Screening of plants used in Argentine folk patent is extended or adjusted under 35 medicine for anti-microbial activity. J Ethnopharmacol. U.S.C. 154(b) by 0 days. 1993 Jun;39(2):119–28. Arletti, R, et al., Stimulating property of Turnera diffusa and Pfafia paniculata eXtracts on the Sexual behavior of male (21) Appl. No.: 09/578,849 rats, Psychopharmacology (Berl). 1999 Mar;143(1): 15-9. (22) Filed: May 26, 2000 Auterhoff, Het al., Constituents of the drug Damiana. Arch Related U.S.
    [Show full text]
  • Dr. Duke's Phytochemical and Ethnobotanical Databases List of Chemicals for Sedative
    Dr. Duke's Phytochemical and Ethnobotanical Databases List of Chemicals for Sedative Chemical Dosage (+)-BORNYL-ISOVALERATE -- (-)-DICENTRINE LD50=187 1,8-CINEOLE -- 2-METHYLBUT-3-ENE-2-OL -- 6-GINGEROL -- 6-SHOGAOL -- ACYLSPINOSIN -- ADENOSINE -- AKUAMMIDINE -- ALPHA-PINENE -- ALPHA-TERPINEOL -- AMYL-BUTYRATE -- AMYLASE -- ANEMONIN -- ANGELIC-ACID -- ANGELICIN ED=20-80 ANISATIN 0.03 mg/kg ANNOMONTINE -- APIGENIN 30-100 mg/kg ARECOLINE 1 mg/kg ASARONE -- ASCARIDOLE -- ATHEROSPERMINE -- BAICALIN -- BALDRINAL -- BENZALDEHYDE -- BENZYL-ALCOHOL -- Chemical Dosage BERBERASTINE -- BERBERINE -- BERGENIN -- BETA-AMYRIN-PALMITATE -- BETA-EUDESMOL -- BETA-PHENYLETHANOL -- BETA-RESERCYCLIC-ACID -- BORNEOL -- BORNYL-ACETATE -- BOSWELLIC-ACID 20-55 mg/kg ipr rat BRAHMINOSIDE -- BRAHMOSIDE -- BULBOCAPNINE -- BUTYL-PHTHALIDE -- CAFFEIC-ACID 500 mg CANNABIDIOLIC-ACID -- CANNABINOL ED=200 CARPACIN -- CARVONE -- CARYOPHYLLENE -- CHELIDONINE -- CHIKUSETSUSAPONIN -- CINNAMALDEHYDE -- CITRAL ED 1-32 mg/kg CITRAL 1 mg/kg CITRONELLAL ED=1 mg/kg CITRONELLOL -- 2 Chemical Dosage CODEINE -- COLUBRIN -- COLUBRINOSIDE -- CORYDINE -- CORYNANTHEINE -- COUMARIN -- CRYOGENINE -- CRYPTOCARYALACTONE 250 mg/kg CUMINALDEHYDE -- CUSSONOSIDE-A -- CYCLOSTACHINE-A -- DAIGREMONTIANIN -- DELTA-9-THC 10 mg/orl/man/day DESERPIDINE -- DESMETHOXYANGONIN 200 mg/kg ipr DIAZEPAM 40-200 ug/lg/3-4x/day DICENTRINE LD50=187 DIDROVALTRATUM -- DIHYDROKAWAIN -- DIHYDROMETHYSTICIN 60 mg/kg ipr DIHYDROVALTRATE -- DILLAPIOL ED50=1.57 DIMETHOXYALLYLBENZENE -- DIMETHYLVINYLCARBINOL -- DIPENTENE
    [Show full text]
  • Microbial Metabolism of Yangonin, a Styryl Lactone from Piper Methysticum(Kava)
    Natural Product Sciences 16(3) : 148-152 (2010) Microbial Metabolism of Yangonin, a Styryl Lactone from Piper methysticum (Kava) Ji Hye Kim1, Hyun Jung Kim2, and Ik-Soo Lee* College of Pharmacy and Research Institute of Drug Development, Chonnam National University, Gwangju 500-757, Republic of Korea 1Marine Natural Products Chemistry Laboratory, Korea Ocean Research & Development Institute, Ansan 426-744, Republic of Korea 2Medical Research Center for Gene Regulation and the Brain Korea 21 Project, Chonnam National University Medical School, Gwangju 501-746, Republic of Korea Abstract − Microbial metabolism studies of yangonin (1), a major styryl lactone from Piper methysticum, have resulted in the production of three hydroxylated metabolites (2-4). The chemical structures of these compounds were elucidated to be 4-methoxy-6-(12-hydroxystyryl)-2-pyrone (2), 4-methoxy-6-(11,12-dihydroxystyryl)-2-pyrone (3), and 4,12-dimethoxy-6-(7,8-dihydroxy-7,8-dihydrostyryl)-2-pyrone (4) on the basis of the chemical and spectroscopic analyses. The compounds 3 and 4 are reported herein as microbial metabolites of yangonin for the first time. Keywords − Microbial metabolism, Yangonin, Styryl lactone, Piper methysticum, Kava Introduction et al., 2003) studies provided several derivatives or metabolites including glucuronylated, hydroxylated, deme- The roots of the kava shrub (Piper methysticum G. thylated, and dehydrated metabolites. Microbial metabolism Forst, Piperaceae) have been used to prepare an intoxicating studies on kavalactones have been reported for kawain, beverage for South Pacific Islanders’ social occasions methysticin (Abourashed and Khan, 2000), and dihydro- (Whitton, et al., 2003). In Western countries, kava extracts kawain (Herath, et al., 2004).
    [Show full text]
  • Influência De Chalconas Análogas, Xantonas E Monossacarídeos Na Glicemia Em Modelo Experimental Animal
    ELGA HELOISA ALBERTON INFLUÊNCIA DE CHALCONAS ANÁLOGAS, XANTONAS E MONOSSACARÍDEOS NA GLICEMIA EM MODELO EXPERIMENTAL ANIMAL FLORIANÓPOLIS 2007 Elga Heloisa Alberton INFLUÊNCIA DE CHALCONAS ANÁLOGAS, XANTONAS E MONOSSACARÍDEOS NA GLICEMIA EM MODELO EXPERIMENTAL ANIMAL Dissertação apresentada ao curso de Pós-graduação em Farmácia da Universidade Federal de Santa Catarina, como requisito parcial para o título de Mestre em Farmácia. Área de concentração: Análises Clínicas . Orientadora: Profa. Dra. Fátima Regina Mena Barreto Silva Florianópolis 2007 ALBERTON, Elga Heloisa Influência de chalconas análogas, xantonas e monossacarídeos na glicemia em modelo experimental animal/Elga Heloisa Alberton. Flrianópolis, 2006. //p. Dissertação (Mestrado) – Universidade Federal de Santa Catarina. Programa de pós Graduação em Farmácia 1. Diabetes. 2. Ácido glicônico. 3. Ácido tatárico. 4. Polygala paniculata. 5. Polygala cyparissias. 6. Xantonas. 7. Chalconas. “INFLUÊNCIA DE CHALCONAS ANÁLOGAS, XANTONAS E MONOSSACARÍDEOS NA GLICEMIA EM MODELO EXPERIMENTAL ANIMAL” POR ELGA HELOISA ALBERTON Dissertação julgada e aprovada em sua forma final pelo Orientador e membros da Banca Examinadora, composta pelos Professores Doutores: Banca Examinadora: ____________________________________ Adair Roberto Soares dos Santos (UFSC) ____________________________________ Danilo Wilhelm Filho (UFSC) ____________________________________ Maria Rosa Chitolina Schetinger (UFSM-RS) Florianópolis, 12 de fevereiro de 2007. Dedico este trabalho aos meus pais, Hercílio C. Alberton e Alba R. Lopes Minatto, pela oportunidade recebida e, que por vezes tão longe fisicamente, estiveram sempre, através de seu carinho e apoio, presentes em todos os momentos da minha vida. AGRADECIMETOS A DEUS por me conceder a oportunidade de realizar mais um sonho. Agradecimento especial à minha orientadora Profa. Dra. Fátima Regina Mena Barreto Silva, pela confiança em mim depositada.
    [Show full text]
  • Piper Methysticum)
    Journal of Student Research (2015) Volume 4, Issue 2: pp. 69-72 Research Article A Closer Look at the Risks vs. Benefits of Kava (Piper methysticum) Anan A. Husseina If you took a trip to Fiji, the locals would probably welcome you with a drink of Kava. For centuries, the indigenous people of the South Pacific Islands have used the roots of a plant known as Kava. Beyond the use of Kava as a psychoactive substance, it has been incorporated as a cultural drink that is used in many ceremonies. In the late 1990’s Kava use spread quickly in Western countries including Europe, North America, and Australia. It was used as a treatment for anxiety. But just as quickly as it spread, the enthusiasm for it faded, because it was banned or restricted in many Western countries following reports of liver toxicity. In the United States, the Food and Drug Administration’s (FDA) concern for safety prompted a request for more research on the substance. The issues of safety and efficacy remain more specifically whether the benefits of using Kava outweigh the risks. History Kava is a beverage made from the roots of the plant included alcohol, cocaine, tobacco, and heroin. The findings Piper methysticum, and has been used historically in the suggest that kava may reduce the craving associated with the South Pacific Islands as a ceremonial drink. Kava was aforementioned substances, which may make kava a great introduced in Europe around the 1700s by Captain James future candidate to help with addiction. 13 Cook and has since spread widely to Australia, Europe, and Although the mechanism of action is not clear, it is the United States.
    [Show full text]