Bailleul, François

Hennebelle, Thierry

Mesquita, Adriana Spirotto Stein

Nunez, Cecilia Veronica

Roumy, Vincent

Santos, Pierre Alexandre dos

Repositório do INPA

See discussions, stats, and author profiles for this publication at: https://www.researchgate.net/publication/247474347Raunitidine isolated from Duroia macrophylla (Rubiaceae)Article  in  Planta Medica · July 2009DOI: 10.1055/s-0029-1234835CITATIONS7READS1497 authors, including:Some of the authors of this publication are also working on these related projects:Melatonin assessment as a dietary supplement component in France View projectMedicina Tradicional na Amazônia Legal Brasileira: Potencial Etnofarmacobotânico de PFNM View projectCecilia Veronica NunezInstituto Nacional de Pesquisas da Amazônia78 PUBLICATIONS   575 CITATIONS   SEE PROFILEPierre SantosUniversidade Federal de Goiás25 PUBLICATIONS   219 CITATIONS   SEE PROFILEVincent RoumyUniversité de Lille45 PUBLICATIONS   491 CITATIONS   SEE PROFILEThierry HennebelleUniversité de Lille66 PUBLICATIONS   1,000 CITATIONS   SEE PROFILEAll content following this page was uploaded by Cecilia Veronica Nunez on 15 May 2015.The user has requested enhancement of the downloaded file.are the antiulcus/antiphlogistic, and the spasmolytic activity, which areattributed to triterpene saponins (glycyrrhicinic acid and derivatives)and flavonoids (liquiritin, isoliquiritin and their aglycones), respectively[1]. According to the purposed use, it would be useful to have to disposaldifferent licorice genotypes with a respective composition of the activecompounds. Although licorice is routinely cultivated, it is well knownthat propagation through conventional methods like e. g. cuttings isslow, when compared to in vitro-techniques. With the aim to developan in vitro protocol for the rapid multiplication of selected genotypes, inour study we chose the method of somatic embryogenesis, because of itspotential for scale-up [2]. Cotyledon explants of 7 day old seedlingsproved to be best suitable to establish callus cultures. As for the forma-tion of embryogenic callus, the growth regulator TDZ was superior to2,4-D or picloram, and resulted in vigorous growth of embryogenic cal-lus. For embryo maturation, subculture on nutrient medium withoutgrowth regulators gave best results of more than 80 embryos per gramof inoculated callus tissue. Within this study, the genotype did not sig-nificantly influence the embryogenic potential. Through this protocol,the large scale clonal propagation of selected genotypes of Glycyrrhizaglabra is feasible, allowing for the production of plantlets of definedquality for further field culture. References: [1] Wichtl, M. (2009) Tee-drogen und Phytopharmaka. 5th edition. Wissenschaftliche Verlagsge-sellschaft mbH. Stuttgart, Germany. [2] George, E.F. (2008) Plant Propa-gation by Tissue Culture. 3 rd edition. Springer. Dordrecht, The Nether-lands.PJ29Comparative effects of a valerian extract andsingle compounds on sleep and bodytemperature in mice evaluated by telemetryChow N1, Fretz M2, Hamburger M2, Butterweck V11Department of Pharmaceutics, College of Pharmacy,University of Florida, Gainesville, FL, POBOX 100494, USA;2Department of Pharmaceutical Sciences, Institute ofPharmaceutical Biology, University of Basel, CH-4056 Basel,SwitzerlandTraditional use of Valeriana officinalis L. suggests sleep promoting prop-erties, yet contemporary observations in clinical trials and rodent mod-els using the extract and isolated compounds are contradictory [1,2]. Weevaluated locomotor activity and body temperature of mice using tele-metry to obtain evidence of sleep promoting effects. This method pro-vides a reduced variable environment which improves upon previousmethodologies. A 70% ethanolic extract of Valeriana officinalis root(250, 500, and 1000 mg/kg) was administered orally and data recordedfor 180 minutes thereafter in male C 57BL/6 J mice. Oral administrationof valerian extract had no effect on locomotor activity and body tem-perature compared to vehicle. Zolpidem (5 mg/kg, positive control) sig-nificantly decreased locomotor activity by 57% (activity counts after30 min; control: 492.1 € 41.8, zolpidem: 212.6 € 44.2; p < 0.001) andbody temperature by 0.57 C (DTmax at 18 minutes, control:36.53 € 0.12 C, zolpidem: 35.96 € 0.13 C; p < 0.01) whereas caffeine(5 mg/kg, negative control) induced an increase in activity of 47% (activ-ity counts after 30 minutes; control: 492.1 € 41.8, caffeine: 725.1 € 76.4;p < 0.01) without affecting body temperature. In conclusion, telemetry isa simple, adequate method for the specific measurement of sleep pro-moting effects. The extract showed no significant difference to vehicle;yet, further studies on single compounds may help substantiate the useof Valeriana officinalis as insomnia treatment. References: [1]Hattel-stohl, M. et al. (2008) Phytomedicine 15:2 – 15. [2] Fernndez, S. et al.(2003) Pharmacol. Biochem. Behav. 77:399 – 404.PJ30Raunitidine isolated from Duroia macrophylla(Rubiaceae)Nunez CV1, Santos PA1, Roumy V2, Hennebelle T2, Sahpaz S2,Mesquita ASS1, Bailleul F21Laboratrio de Bioprospec¼o, Coordena¼o de Pesquisasem Produtos Naturais, Instituto Nacional de Pesquisas daAmaznia, Av. Andr Araffljo, 2936, Aleixo, Manaus,Amazonas, 69060 – 001, Brazil; 2Laboratoire dePharmacognosie, EA 1043, Facult des SciencesPharmaceutiques et Biologiques, Universit de Lille 2, BP 83,F-59006 Lille Cedex, FranceDuroia macrophylla Huber is a tropical tree, known as “puru”, whichoccurs in the Amazon region. Their fruits can be eaten and, as we know,no chemical study has been performed before. Leaves of D. macrophyllawere dried at room temperature, ground and extracted with dichloro-methane, methanol and later with water, by using ultra-sound for 20minutes, each twice repeated and concentrated with reduced-pressureevaporator or liophylizer. The methanolic extract was fractioned byusing chromatographic techniques and HPLC for further purification.The chemical identification of the indolic alkaloid raunitidine wasachieved by NMR and MS data analyses and literature comparison [1].Acknowledgements: PPBio/INPA/MCT; CNPq; FAPEAM. References: [1]Merlini, L. et al. (1976) Helv. Chim. Acta 59:2254 – 2260.PJ31Cannabinoid receptor Ga fusion proteins as ahighly sensitive model system forcharacterization of receptor ligandsGeiger S1, Seifert R2, Heilmann J11Department of Pharmaceutical Biology, University ofRegensburg, Universittsstraße 31, 93053 Regensburg,Germany; 2Institute of Pharmacology, Medical School ofHannover, Carl-Neuberg-Straße 1, 30625 Hannover,GermanySo far two human cannabinoid receptors (hCBRs) have been identified[1], both belonging to the family of G-protein coupled receptors(GPCRs): the hCB1R [2] is mainly located in the brain and the hCB2R[3] is predominantly located in the periphery on immune cells. Becauseof their involvement in many physiological functions, such as move-ment, metabolic regulation, host defense, analgesia and memory, thereis a great interest in targeting these receptors for therapeutic applica-tions. For the search for new CBR ligands, we refined an existing in vitroassay [4] that allows for the differentiation of the pharmacological prop-erties of a compound. In the already established steady-state [g-32P]-GTPase assay Spodoptera frugiperda (SF9) cells were used for the co-expression of the CBR, the Ga-subunit and the Gbg-heterodimer. Becausethe expression levels and the density of these proteins in the cell mem-brane influence the efficiency of the interaction between the receptorand the G proteins, we improved this assay using CBR-Ga fusion pro-teins. With these fusion proteins we can ensure a close proximity anddefined stoichiometry of the signalling partners, resulting in higher cou-pling efficiency than the conventional co-expressing system. This verysensitive test system enabled us to detect an agonist at the CBRs in amatrix of other compounds. Therefore we added D9-THC to a D9-THC-free Cannabis sativa extract and found the expected increase of potency(e. g. extract logEC50 -6,08 vs. extract enriched with D9-THC logEC50 -6,86 at the CB1R and extract logEC50 -5,86 vs. extract enriched with D9-THC logEC50 -6,38 at the CB2R). References: [1] Howlett, A.C. et al.(2002) Pharmacol. Rev. 54:161 – 202. [2] Matsuda, L.A. et al. (1990) Nat-ure 346:561 – 564. [3] Munro, S. et al. (1993) Nature 365:61 – 65. [4]Egger, M. et al. (2008) Chem. Eur. J. 14:10978 – 10984.PJ32Catechin-derivates affinity for humancannabinoid receptorsKorte G1, Geiger S2, Heilmann J2, Sand PG11Department of Psychiatry, University of Regensburg, Franz-Josef-Strauss-Allee 11, 93053 Regensburg, Germany;2Department of Pharmaceutical Biology, University ofRegensburg, Universittsstrasse 31, 93053 Regensburg,GermanyFlavonoids are common secondary plant metabolites and possess mani-fold health-enhancing effects. In addition to neuroprotective and anti-inflammatory activities, growing evidence suggests that flavonoids may& Korrekturexemplar: Verffentlichung (auch online), Vervielfltigung oder Weitergabe nicht erlaubt! &Planta Med 2009; 75: 877–1095 Georg Thieme Verlag KG Stuttgart · New York · ISSN 0032-0943103757th International Congress and Annual Meeting of the GA | August 16 – 20, 2009, Geneva, SwitzerlandView publication stats

Raunitidine isolated from Duroia macrophylla (Rubiaceae).

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Raunitidine isolated from Duroia macrophylla (Rubiaceae).

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