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  • About
  • The Global ETD Search service is a free service for researchers to find electronic theses and dissertations. This service is provided by the Networked Digital Library of Theses and Dissertations.
    Our metadata is collected from universities around the world. If you manage a university/consortium/country archive and want to be added, details can be found on the NDLTD website.
1

Isolation, chemical characterisation and biological activity ofacylphloroglucinols from petroleum ether extract of Hypericum barbatumJacq. 1775 / Izolacija, hemijska karakterizacija i biološka aktivnost acilfloroglucinola izpetroletarskog ekstrakta Hypericum barbatum Jacq. 1775

Šibul Filip 19 February 2018 (has links)
<p>Within this doctoral thesis, eighteen new compounds, polycyclic polyprenylated<br />acylphloroglucinols, were isolated from petrol ether extract of <em>Hypericum barbatum</em><br />plant. The compounds are named hyperibarbins A&ndash;R. For hyperibarbins A&ndash;D,<br />cytotoxicity towards carcinogenic cells and antibacterial activity were evaluated. All<br />four compounds exhibited intermediate activity towards tumor cells in vitro. Although<br />inactive towards Gram negative bacteria, examined compounds have expressed<br />extraordinary bacteriostatic activity towards Gram positive bacterial strains.<br />Hyperibarbins C, E, N and K were, since having endoperoxide bridge in their structures,<br />tested for antiprotozoal activity, but shown intermediate activity towards the examined<br />parasite strains. All goals set for this doctoral thesis at the beginning have been fully<br />met, with isolation of new compounds, described andcompletely chemically<br />characterized for the first time.</p> / <p>U okviru ove doktorske disertacije izolovano je osamnaest novih jedinjenja, policikličnih&nbsp; poliprenilovanih acilfloroglucinola, iz petroletarskog ekstrakta biljke <em>Hypericum&nbsp; barbatum</em>. Imena jedinjenja su hiperibarbini A&ndash;R. Za hiperibarbine A&ndash;D, ispitana je&nbsp; citotoksičnost prema kancerogenim ćelijama i antibakterijska aktivnost. Sva četiri&nbsp; jedinjenja su ispoljila srednju aktivnost prema tumorskim ćelijama <em>in vitro</em>.&nbsp; Iako neaktivni&nbsp; prema Gram negativnim bakterijama, ispitana jedinjenja su ispoljila izuzetnu bakteriostatsku aktivnost prema sojevima Gram pozitivnih bakterija. Hiperibarbini C, E, N i K su, zbog posedovanja endoperoksidnog prstena u svojoj strukturi, testirana na antiprotozoalnu aktivnost, ali su pokazali srednju aktivnost prema ispitanim sojevima parazita. Svi ciljevi postavljeni na početku izrade ove doktorske disertacije su do kraja ispunjeni, sa izolacijom novih, prvi put opisanih i u potpunosti hemijski okarakterisanih jedinjenja.</p>
2

Pharmacochimie d'anthranoïdes issus du genre Psorospermum (Hypericaceae) : isolement, activités antiparasitaires et synthèse d'analogues structuraux / Pharmacochemistry of anthranoids from Psorospermum genus (Hypericaceae) : isolation, antiprotozoal activities and structural analogues synthesis

Gallé, Jean-Baptiste 06 November 2015 (has links)
L’étude de plantes utilisées en médecine traditionnelle camerounaise contre le paludisme a révélé des activités antiprotozoaires pour des espèces du genre Psorospermum conduisant à l’isolement d’anthranoïdes prénylés. De nouveaux fractionnements basés sur des techniques chromatographiques en polarité de phase inverse et de partage centrifuge ont permis d’isoler 9 vismiones de l’écorce de P. glaberrimum qui ont montré de fortes activités antileishmaniennes (30 nM < CI50 < 827 nM). Un protocole d’isolement à l’échelle du gramme de ces molécules, sensibles aux conditions classiques de purification, a été développé pour fournir les quantités nécessaires à une démarche d’hémisynthèse et pour comprendre leur mécanisme d’action. La répartition de ces molécules dans les organes de 10 espèces de Psorospermum a été étudiée. Une approche de synthèse organique a également été développée afin d’obtenir des analogues, déterminer leurs activités antiprotozoaires et leurs relations de structure-activité. / The screening of plants used in Cameroonian traditional medicine against malaria revealed significant antiprotozoal activities for species belonging to the Psorospermum genus and led to the isolation of prenylated anthranoids. Further fractionations based on reversed-phase and centrifugal partition chromatography allowed us to isolate 9 vismiones from the bark of P. glaberrimum. All these compounds exhibited strong antileishmanial activities (30 nM<IC50<827 nM).A gram-scale isolation protocol of these highly unstable compounds, when traditional ill-suited purification processes are used, has been developed to provide enough starting material for further hemisynthesis steps and to investigate their mechanism of action. The repartition of these metabolites in different parts of 10 Psorospermum species has been studied. A synthetic approach has also been developed to obtain anthranoid analogues to investigate their antiprotozoal activities and explore structure-activity relationships.

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