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Stratégies innovantes pour une valorisation d’extraits de plantes en cosmétique : Mise en oeuvre d’un outil de profilage métabolique et recherche de nouvelles activités biologiques / Innovative strategies for a valorization of plant extracts in cosmetic : development of a tool for metabolic profiling and search for new biological activitiesJouravel, Glorianne 11 June 2018 (has links)
La cosmétique valorise des extraits de plantes en les intégrant dans des produits de soin. Ces extraits constituent les ingrédients actifs de la formule cosmétique. Les plantes sont diverses, riches et contiennent de nombreux composés d’intérêt biologique. La phytochimie s’intéresse à décrire le contenu métabolique d’extraits de plantes. Mais la caractérisation moléculaire de ces matrices complexes reste un défi majeur aujourd’hui. En effet, les étapes de traitements de données sont longues et laborieuses. Un outil de profilage métabolique, GAINS, a ainsi été développé afin de traiter de façon automatisée les données issues d’analyses en chromatographie liquide couplée à la spectrométrie de masse haute résolution. Il constitue un support au phytochimiste car le traitement automatisé des données permet de gagner du temps par rapport à un traitement manuel. Cet outil associé à une vaste base de données de produits naturels permet d’attribuer des candidats potentiels aux pics détectés. GAINS fait aussi appel à un module de fragmentation in silico afin d’étayer les propositions de candidats. Cela permet de comparer le spectre de fragmentation modélisé des candidats avec le spectre de fragmentation expérimental.L’ensemble des études phytochimiques réalisées pour identifier ou isoler des composés va de pair avec l’étude du potentiel d’effet biologique des extraits sur la peau, organe ciblé par les cosmétiques. Cela sert à découvrir les actions bénéfiques que peut avoir l’extrait. En connaissant le contenu phytochimique, on peut expliquer et rationaliser les tests d’activités biologiques. Le développement d’un actif anti-âge à partir de la salicaire, une plante de la région Centre-Val de Loire, en est l’exemple. / The cosmetic field valorizes plant extracts by integrating them in care products. These extracts constitute the active ingredients of the cosmetic formulation. Plants are diverse, rich and contain numerous compounds of biological interest. Phytochemistry is a way to describe the metabolic content of plant extracts. But molecular characterization of these complex matrices remains a major challenge nowadays. Indeed,steps of data treatment are time-consuming and laborious. In this way, a tool of metabolic profiling, GAINS, has been developed in order to treat in an automatized way data from analyses performed in liquid chromatography coupled with high-resolution mass spectrometry. It constitutes a real support for phytochemists because automatized data treatment allows gaining time compared to manual treatment. This tool, associated with a large database of natural compounds make possible to assign potential candidates to detected peaks. GAINS appeals a module of in silico fragmentation for holding candidates assignments up.This permits to compare modeled spectrum of fragmentation of candidates with experimental spectrum off ragmentation.The whole set of phytochemical studies realized to identify or isolate compounds goes hand in hand with the study of potential biological effects of extracts to the skin, targeted organ by skin-care products. This allows the discovery of beneficial actions that the extract could have. By knowing the phytochemical content, it is possible to explain and rationalize assays about biological activities. The development of an anti-aging ingredient from purple loosestrife, a plant occurring in the region Centre-Val de Loire, is an example of it.
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Quimiometria aplicada à metabolômica de Aldama La Llave: contribuições quimiotaxonômicas e fitoquímica direcionada baseada em inibição de cicloxigease-1 e 5-lipoxigease / Chemometrics applied to metabolomics of Aldama La Llave: chemotaxonomic contributions and targeted phytochemistry based on cyclooxygenase-1 and 5-lipoxygenase inhibitionSantos, Felipe Antunes dos 26 January 2015 (has links)
As espécies do gênero Viguiera Kunth, recentemente transferidas para Aldama La Llave (Asteraceae, Heliantheae), ainda possuem problemas de delimitação taxonômica. Tal gênero possui 35 espécies distribuídas por todo o território brasileiro, principalmente no cerrado. Análises químicas têm demonstrado seu potencial em auxiliar na resolução de problemas em vários níveis taxonômicos com base em grupos químicos de metabólitos secundários. Além disso, análises fitoquímicas tem revelado que determinadas substâncias de Aldama possuem potencial para serem estudadas tendo vista a investigação de mecanismos moleculares anti-inflamatórios. Desta forma, foi proposto neste trabalho realizar a abordagem da metabolômica não-direcionada auxiliada por quimiometria, visando-se fornecer dados químicos tanto para contribuições quimiotaxonômicas quanto para encontrar substâncias bioativas. Por meio de tal abordagem, análises multivariadas não supervisionadas (PCA e HCA), bem como supervisionadas (OPLS-DA), com dados provenientes de UHPLC-DAD-Orbitrap, demonstraram que o gênero Aldama é quimioconsistente e, deste modo, determinadas substâncias químicas discriminantes foram sugeridas. Além disso, espécies que apresentam problemas taxonômicos tiveram os seus posicionamentos infragenéricos explicado do ponto de vista quimiotaxonômico. Quanto às análises para encontrar substâncias bioativas (fitoquímica direcionada), os alvos inflamatórios pesquisados foram as enzimas pró-inflamatórias COX-1 e 5-LOX, com as quais se realizou ensaios in vitro verificando-se a atividade positiva de extratos de espécies de Aldama. A. trichophylla foi a espécie selecionada para realizar a fitoquímica direcionada, uma vez que apresentou inibição dupla contra as enzimas e por se tratar de uma espécie muito pouco estudada do ponto de vista fitoquímico. Os melhores modelos de inibição de COX-1 e 5-LOX criados com dados químicos de Aldama foram selecionados a partir de diversas combinações de algoritmos, softwares de processamento (MZmine, MetAlign e MSClust) e técnicas-hifenadas, tais como UHPLC-Orbitrap e HPLC-TOF. Deste modo, determinados picos de íons foram apontados pela quimiometria como sendo discriminantes para a atividade de inibição dupla. Tais picos foram desreplicados com base em seus perfis de UV e padrões de fragmentação via HCD-Orbitrap e Ion-Trap. Deste modo, foi possível desreplicar três prováveis substâncias químicas inibidoras de COX-1 e 5-LOX: kaempferol-3-O-glucuronideo, quercetina-3-O-metil-7-glucuronideo e kaempferol-3-O-(6\"-malonil-glucosideo). Por fim, foi realizada a fitoquímica direcionada. O fracionamento cromatográfico permitiu isolar tais substâncias e uma análise preliminar de RMN 1H foi realizada com o intuito de realizar a identificação estrutural. Tais substâncias terão a suas atividades confirmadas na inibição das duas enzimas em um futuro próximo. / The species of the genus Viguiera Kunth, recently transferred to the genus Aldama La Llave (Asteraceae, Heliantheae), still show problems of taxonomic boundaries. This genus has 35 species distributed throughout the Brazilian territory, mostly in the cerrado. Chemical analyses has demonstrated its potential to help in the solution of problems at various taxonomic levels based on chemical groups of secondary metabolites. Furthermore, phytochemical analyses have shown that certain compounds from Aldama have the potential to be studied aiming to investigate anti-inflammatory molecular mechanisms. Thus, in this work it was proposed to carry out the untargeted metabolomic approach aided by chemometrics, aiming to provide chemical data either for chemotaxonomic contributions and to find bioactive compounds. Through this approach, both unsupervised (PCA and HCA) and supervised multivariate analysis (OPLS-DA) combined with data from UHPLC-DAD-Orbitrap analyses showed that the genus Aldama is \"chemoconsistent\" and thus certain discriminant compounds were suggested. Additionally, some species with taxonomic problems had their infrageneric positioning explained from the chemotaxonomic point of view of. With regards to the analyses carried out to find bioactive compounds (targeted phytochemistry), the inflammatory targets investigated in this study were the COX-1 and LOX-5 pro-inflammatory enzymes with which in vitro assays were made and positive activity of extracts from species of Aldama was observed. A. trichophylla was the selected species for the targeted phytochemistry because it showed dual inhibition activity against both enzymes and it is still little investigated from the chemical point of view. The best models for inhibition of COX-1 and 5-LOX obtained with chemical data of Aldama were selected by means of various combinations of algorithms, processing software (MZmine, MetAlign and MSClust) and hyphenated techniques, such as HPLC-TOF and UHPLC-Orbitrap. Thus, certain peak ions were appointed by chemometrics as discriminant for the dual inhibition activity. These peaks were dereplicated based on their UV profiles and fragmentation patterns via HCD-Orbitrap and Ion-Trap. Thus, it was possible to dereplicate three probable chemical inhibitors of COX-1 and 5-LOX: kaempferol-3-O-glucuronide, quercetin-3-O-methyl-7-glucuronide and kaempferol-3-O-(6\"-malonyl-glucoside). Finally, the targeted phytochemistry was carried out. The chromatographic fractionation allowed us to isolate these three compounds and a preliminary 1H NMR analysis was performed in order to conclude their structural identification. In the near future, these substances will have their activity evaluated by the inhibition of the two enzymes.
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Anatomia, germinação de sementes e análise do óleo essencial de Viguiera arenaria Baker in Martius e Viguiera robusta Gardner in Hook (Asteraceae - Heliantheae) / Anatomy, seed germination and analysis of essential oil of Viguiera arenaria Baker in Martius and Viguiera robusta Gardner in Hook (Asteraceae - Heliantheae)Oliveira, Tuane Santos de 16 December 2011 (has links)
A família Asteraceae possui cerca de 1.600 gêneros e 20.000 espécies, representando cerca de 10% da flora mundial. No Cerrado é a segunda maior família dentre as fanerógamas em número de espécies, com grande importância no estrato herbáceo e arbustivo. Dentre as tribos da família Asteraceae, Heliantheae é considerada um grupo monofilético, com 189 gêneros e aproximadamente 2.500 espécies de ervas, arbustos e árvores. É importante economicamente com utilização alimentícia (girassol), ornamental (dália) e medicinal (camomila). Dentre os maiores gêneros de Heliantheae estão Bidens, Viguiera e Wedelia. Viguiera Kunth é um gênero exclusivamente americano com 180 espécies, das quais 27 são exclusivamente brasileiras. Seus representantes ocorrem principalmente em regiões de inverno seco com eventos periódicos de queimada como o Cerrado. A adaptação a esses ambientes pode estar ligada ao comportamento sazonal destas espécies, o qual consiste na senescência dos ramos aéreos nos períodos de baixas temperaturas e seca (fase de dormência) e na formação de novos ramos nos períodos de disponibilidade hídrica e temperaturas favoráveis (fase de floração). As espécies Viguiera arenaria Baker in Martius e Viguiera robusta Gardner in Hook estão incluídas na seção Paradosa na classificação das espécies do gênero Viguiera e são confundidas em materiais herborizados, sendo distinguidas atualmente apenas por caracteres polínicos. O estudo anatômico de V. arenaria e V. robusta visa contribuir para o levantamento de caracteres diagnósticos que auxiliem no reconhecimento destas em materiais herborizados ou não. Ambas as espécies são aromáticas em campo, devido à presença de compostos voláteis. Estudos fitoquímicos têm destacado o potencial farmacológico destas espécies, com base na atividade de terpenos de alto peso molecular como lactonas sesquiterpênicas e diterpenos. A literatura carece, porém, de dados sobre a composição química dos óleos essenciais motivo pelo qual os mesmos são apresentados no presente estudo. Tais informações auxiliam, através da quimiotaxonomia, na distinção entre as espécies, além de identificar compostos possivelmente fitoterápicos. O estudo da germinação de espécies de Viguiera arenaria e V. robusta aqui apresentado visa contribuir para o conhecimento sobre a propagação destas espécies visando uma possível exploração de seus princípios ativos, já que atualmente, elas ocorrem apenas em ambientes naturais de Cerrado. / Asteraceae family has about 1,600 genera and 20,000 species, representing about 10% of the world flora. In the Cerrado is the second largest family among the phanerogams in number of species with a great importance in the herbaceous and shrubby layers. In the family Asteraceae, Heliantheae is considered a monophyletic group, with 189 genera and approximately 2,500 species of herbs, shrubs and trees. It is a tribe of economical importance, with different uses: food (sunflower), ornamental (dahlia) and medicinal (chamomile). The most important genera of Heliantheae are Bidens, Viguiera and Wedelia. Viguiera Kunth is an exclusively American genus with 180 species, and 27 are exclusively Brazilian. Its representatives occur mainly in Cerrado regions with dry winters and periodic fire events. The adaptation to these environments can be linked to the seasonal behavior of these species, which is the senescence of the aerial organs during periods of low temperatures and dry (dormant phase) and the formation of new aerial organs during periods of water availability and favorable temperatures (flowering phase). Viguiera arenaria Baker in Martius and Viguiera robusta Gardner in Hook are included in Paradosa section in the classification of the genus Viguiera and they are indistinguishable to herborized materials, being distinguished only by their pollen. The anatomical study of V. arenaria and V. robusta aims to contribute to gather of diagnostic characters that aid in the recognition of herborized materials or not. Both species are aromatic in the field, due to the presence of volatile compounds. Phytochemical studies have highlighted the pharmacological potential of these species, based on the activity of terpenes of high molecular weight such as sesquiterpene lactones and diterpenes. The literature lacks, however, data about the chemical composition of the essential oils. This is the reason why their chemical composition is presented in this study. Such information helps, by chemotaxonomy, the distinction among species and besides that, could contribute to identify possible phytotherapics compounds. The study of the seed germination of Viguiera arenaria and V. robusta presented here aims to contribute to the knowledge about the spread of these species towards a possible exploitation of their active compounds, because nowadays they occur only in natural areas of Cerrado.
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Estudo fitoqu?mico e avalia??o da atividade anticolinester?sica de extratos da casca da raiz da Mimosa tenuiflora (Willd.) PoiretNeves, Maiane dos Santos 30 June 2015 (has links)
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Previous issue date: 2015-06-30 / Coordena??o de Aperfei?oamento de Pessoal de N?vel Superior - CAPES / Mimosa tenuiflora (Willd.) Poiret (jurema preta) is a species in the Fabaceae family, native to the Caatinga, found throughout the Brazilian Northeast. In folk medicine, the shells of the stem and root of jurema preta are used in treatment of several diseases, as burns and inflammations, besides being maid traditionally as drink in indigenous rituals. Regarding to the root bark, there are few studies described in the literature about its phytochemical profile and biological properties. In this way, the present study has proposed perform a phytochemical study of the extracts from the root bark of Mimosa tenuiflora. For this, it was performed the fractionation of chloroformic extract from the column chromatography (CC), and the structural determinations of the isolated compounds were carried out by technique of nuclear magnetic resonance (NMR) of 1H and 13C, besides the identification and quantification of phenolic substances in the chloroformic extracts and the ethyl acetate from the high-efficiency liquid chromatography with diode arrangement detector (HPLC-DAD) and consequent validation of applied analytical method. Were also carried out assessment of anticholinesterasic activity of the extracts by the method of Ellman and quantification of the total flavonoid content of the crude extract through spectrophotometric method using as reactant aluminum chloride (AlCl3) and standard curve with quercetin. As a result, were obtained from the chloroformic extract a mixture of the ?-sitosterol and stigmasterol steroids and the betulinic acid triterpene. From of the HPLC-DAD were identified polyphenols such as catechin, epicatechin and procyanidin B2 beyond the gallic acid in the ethyl acetate extract and procyanidin B2, in the chloroformic extract of this species. With the validation of the analytical method, this proved to be reliable and suitable for the quantification of the substance catechin and epicatechin in the ethyl acetate extract, according to criteria recommended by the National Health Surveillance Agency ? NHSA. Regarding the anticholinesterasic activity, among the tested extracts of black jurema, the gross and the ethyl acetate were the ones who showed greater inhibition capacity on the enzyme acetylcholinesterase (AChE) in relation to other, presenting percentages of 89% + 0,31 and 93,8% + 0,4, respectively, what classifies this species as a potent inhibitor. The total flavonoids content quantified in the crude extract of Mimosa tenuiflora was of 1,386g/100g extract. Thus, this work indicates that the species Mimosa tenuiflora is a promising source of bioactive substances of chemical-medicinal interest, besides being a strong natural candidate that can aid in the treatment of Alzheimer's disease. It is important to mention that the present study provides an unprecedented contribution about the chemical composition of root bark of black jurema, since to date no records were found in the literature on phenolic constituents of this part of the plant. / Mimosa tenuiflora (Willd.) Poiret (jurema preta) ? uma esp?cie da fam?lia Fabaceae nativa da Caatinga, encontrada largamente em todo nordeste brasileiro. Na medicina popular, as cascas do caule e da raiz da jurema preta s?o utilizadas no tratamento de diversas enfermidades, como queimaduras e inflama??es, al?m de ser empregada tradicionalmente como bebida em rituais ind?genas. Com rela??o ? casca da raiz, h? poucos estudos descritos na literatura sobre seu perfil qu?mico e propriedades biol?gicas. Desta forma, o presente trabalho prop?s realizar um estudo fitoqu?mico dos extratos da casca da raiz da Mimosa tenuiflora. Para isso, foi realizado o fracionamento do extrato clorof?rmico a partir da cromatografia em coluna (CC), e as determina??es estruturais das subst?ncias isoladas foram realizadas atrav?s da t?cnica de resson?ncia magn?tica nuclear (RMN) de 1H e 13C, al?m da identifica??o e quantifica??o de subst?ncias fen?licas nos extratos clorof?rmico e acetato de etila a partir da cromatografia a l?quidos de alta efici?ncia com detector de arranjo de diodos (CLAE-DAD) e consequente valida??o do m?todo anal?tico aplicado. Tamb?m foram realizadas avalia??o da atividade anticolinester?sica dos extratos pelo m?todo de Ellman e quantifica??o do teor de flavonoides totais do extrato bruto atrav?s de m?todo espectrofotom?trico utilizando-se como reagente cloreto de alum?nio (AlCl3) e curva padr?o com quercetina. Como resultado, foram obtidos do extrato clorof?rmico uma mistura dos esteroides ?-sitosterol e estigmasterol e o triterpeno ?cido betul?nico. A partir da CLAE-DAD foram identificados polifen?is como a catequina, epicatequina e procianidina B2 al?m do ?cido g?lico no extrato acetato de etila e procianidina B2, no extrato clorof?rmico desta esp?cie. Com a valida??o do m?todo anal?tico, este se mostrou confi?vel e adequado para a quantifica??o das subst?ncias catequina e epicatequina no extrato acetato de etila, de acordo com crit?rios preconizados pela Ag?ncia Nacional de Vigil?ncia Sanit?ria - ANVISA. Com rela??o ? atividade anticolinester?sica, entre os extratos testados da jurema preta, o bruto e o de acetato de etila foram os que demonstraram maior capacidade de inibi??o sobre a enzima acetilcolinesterase (AChE) com rela??o aos demais, apresentando percentuais de 89% + 0,31 e 93,8% + 0,4, respectivamente, o que classifica esta esp?cie como potente inibidor. O teor de flavonoides totais quantificado no extrato bruto da Mimosa tenuiflora foi de 1,386g/100g extrato. Sendo assim, este trabalho indica que a esp?cie Mimosa tenuiflora ? uma fonte promissora de subst?ncias bioativas de interesse qu?mico-medicinal, al?m de ser uma forte candidata natural que pode auxiliar no tratamento do mal de Alzheimer. ? importante mencionar que o presente estudo fornece uma contribui??o in?dita acerca da composi??o qu?mica da casca da raiz da jurema preta, uma vez que at? o momento n?o foram encontrados registros na literatura sobre constituintes fen?licos desta parte da planta.
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Towards understanding the metabolism of in vitro Sutherlandia frutescens (L.)R.Br. culturesColling, Janine 12 1900 (has links)
Thesis (MSc (Plant Biotechnology))--University of Stellenbosch, 2009. / ENGLISH ABSTRACT: Sutherlandia frutescens (L.) R. Br., also regarded as Lessertia frutescens, is a leguminous, perennial shrub indigenous to South Africa. Extracts prepared from the leaves have
traditionally been used for the treatment of various diseases. Reports have also indicated that
S. frutescens provides certain health benefits to cancer and HIV/AIDS patients. Analysis of extracts indicated the presence of several compounds (bitter triterpenoid glycosides, several
flavonoids, amino acids, small amounts of saponins (no alkaloids though), asparagine, Larginine, canavanine, gamma-aminobutyric acid (GABA) and pinitol) which contribute to the
medicinal properties of this plant. The first part of this study involved testing the effect of six treatments (light, dark, soaking of
seeds, physical scarification, chemical scarification and flaming of seeds) on the in vitro germination of Sutherlandia seeds to elucidate the factors which control seed germination. Those treatments which removed the seed coat were most successful for germination with physical scarification being the most efficient method, resulting in 98.6% of the seeds
germinating after 21 days. Although the organogenesis of Sutherlandia explants (cotyledons
and hypocotyls) in vitro were investigated (results not included in this thesis), omitting plant growth regulators (PGR) in the cultivation medium was best for shoot multiplication. However,
this PGR-free system successfully provided a continuous supply of plant material for further
studies. It would be possible to successfully adopt it for commercial production of plants to
assist with cultivation of Sutherlandia as a field crop. Another advantage of this system is
spontaneous rooting with 85% of the in vitro microshoots rooting in PGR-free medium. These
rooted plants were acclimated in the glasshouse using vented lids to harden off the shoots and
this method resulted in 100% survival of plants. The second part of this study investigated the induction of hairy root cultures of S.
frutescens using Agrobacterium-mediated transformation. The efficiency of three
Agrobacterium strains (A4T, LBA9402 and C58C1) to transform different S. frutescens explants (cotyledons and hypocotyls) was analyzed. All three strains were equally efficient at
inducing hairy roots in both hypocotyls and cotyledons. However, transformation of S.
frutescens was dependent on the type of explant used with the hypocotyls being more
efficiently transformed than the cotyledons. Overall the transformation of both the hypocotyl
(93%) and cotyledon (47%) was highest when the strain A4T was used. Four hairy root clones
were selected and their cultivation in a liquid system was optimized by investigating their
growth in four different types of media (Gamborg B5 (Gamborg et al., 1968), White’s (White,
1934; White, 1954), MS (Murashige and Skoog, 1962) and half strength MS medium). All the
growth of hairy root clones was best in the B5 and MS medium, with White’s medium being the
least effective cultivation medium. Molecular analysis of hairy roots was used to prove the
transgenic status of these four putative transgenic clones. This was achieved using
polymerase chain reaction (PCR) amplification of rol A (320 bp), B (780 bp) and C (600 bp)
genes to determine the presence of the TL-DNA in the plant genome. During Southern
hybridization a radioactively labeled rol A probe was used to determine the copy number of the
rol A gene. The three rol genes were present in all four hairy root clones. The third part of this study focused on the effect of three abiotic stress factors (nitrogen availability, salinity and drought) on the synthesis of four metabolites (gamma-aminobutyric acid (GABA), asparagine, arginine and canavanine). The effect of nitrogen availability on metabolite synthesis and the morphology was determined using in vitro shoot cultures as well as the hairy root clone C58C1-g. Nitrogen availability studies were conducted by cultivating the microshoots or root tips on modified MS medium. The MS medium contained either the normal amount of nitrogen (1.9 g L-1 KNO3 and 1.65 g L-1 NH4NO3) in the MS medium (1x
nitrogen), half the normal nitrogen concentration in MS medium (0.5x nitrogen) or twice the
normal nitrogen concentration in MS medium (2x nitrogen). The arginine and asparagine
levels in the roots and shoots and the canavanine level in the shoots were directly correlated
with the amount of nitrogen in the medium (as the nitrogen level increased, the metabolite
levels increased). The GABA level in the shoots was inversely correlated with the amount of
nitrogen in the medium. Several reasons may explain these metabolic changes including the
assimilation of extra nitrogen into asparagine, canavanine and arginine in the shoots. The
reduced GABA levels may indicate the preferential flux of the free GABA into other nitrogen
assimilatory pathways such as protein synthesis as well as its rapid utilization to replenish the
tricarboxilic acid cycle intermediates.
The effect of water (induced by including 3% (w/v) PEG in the medium) and salt stress
(induced by including either 50 or 100 mM NaCl in the medium) was only investigated in the
shoot cultures as the root cultures lacked the synthesis of canavanine. Water stress did not
significantly alter the metabolite levels, but resulted in a significant decrease in the growth
(fresh weight and total shoot length) and the rooting response of these microshoots. Salt
stress only resulted in a significant increase in arginine levels with increasing salinity and also
caused a reduction in the rooting and growth response. Lowered plant vigour may be the first
visual sign of water stress. Addition of NaCl may lead to ion toxicity and requires osmotic
adjustment resulting in changes at the metabolic level concomitant to physiological growth
changes. Finally, the anti-bacterial activity and the phytochemistry of transgenic root cultures and untransformed in vitro and ex vitro plant material was examined. Only the extracts prepared from the wild harvested leaf material exhibited moderate anti-bacterial activity (1.25 mg ml-1) against all the bacteria (Escherichia coli, Klebsiella pneumoniae, Bacillus subtilis and
Staphylococcus aureus) tested. Changes to the secondary metabolism of hairy roots were
investigated using TLC and LC-MS analysis. Several of the compounds in the hairy root
extracts were present in higher levels than in the control root extracts. Transformation also
increased the complexity of the phytochemical pattern of the hairy roots, either due the
synthesis of novel compounds or upregulated synthesis of existing metabolic pathways. The
production of hairy roots and the establishment in a liquid system during this study was an
important step towards upscaling these cultures to a bioreactor. In future these roots can
assist in developing cultures which produce a high yield of the desired metabolites. / AFRIKAANSE OPSOMMING: Sutherlandia frutescens (L.) R. Br., ook bekend as Lessertia frutescens is ‘n peulagtige
meerjarige struik, inheems tot Suid Afrika. Ekstrakte wat van die blare voorberei word, is
tradisioneel gebruik vir die behandeling van verskeie siektes. Berigte het ook daarop gedui,
dat S. frutescens sekere gesondheidsvoordele vir kanker en HIV/VIGS pasiënte inhou. ‘n
Ontleding van die ekstrakte, dui op die teenwoordigheid van verskeie verbindings (bitter
triterpenoïed glikosiede, verskeie flavonoïede, aminosure, klein hoeveelhede saponiene
(alhoewel geen alkaloïede), asparagien, L-arginien, canavanien, gamma-aminobottersuur
(GABS) en pinitol) wat tot die medisinale eienskappe van hierdie plant bydrae.
Die eerste deel van die studie het die effek van ses behandelings (lig, donker, week van sade,
fisiese skarifikasie, chemiese skarifikasie en die vlam van sade) op die in vitro ontkieming van
Sutherlandia sade getoets met die doel om die faktore wat saadontkieming beheer, te
identifiseer. Die beste behandeling vir saadontkieming was dié behandelings wat die
saadhuid verwyder het. Die mees effektiewe metode van saadhuidverwydering was die
fisiese skarifikasie van sade, wat gelei het tot ‘n 98.6% ontkieming van sade na 21 dae.
Alhoewel in vitro organogenese van Sutherlandia eksplante (kotiel en hipokotiel) ondersoek
was (resultate nie ingesluit in die tesis nie), was plant groei reguleerders (PGR) uitgesluit in
die groeimedium om stingelvermeerdering te bevorder. Nie te min was die PGR-vrye sisteem
suksesvol om ‘n voortdurende bron van plant material vir verder studies te verskaf. Dit sou
egter moontlik wees om die PGR-vrye sisteem suksesvol te kon aanpas vir die kommersiële
produksie van plante met die doel om Sutherlandia as ‘n landbougewas te bevorder. ‘n
Verdere voordeel van dié sisteem, is die spontane wortelvorming, met 85% van die in vitro
mikrostingels wat wortels in die PGR-vrye medium produseer het. Hierdie bewortelde plante
was in die glashuis geakklimatiseer met behulp van geventileerde deksels (vir stingel
afharding) en het tot ‘n 100% oorlewing gelei.
Die tweede deel van die studie het die induksie van S. frutescens harige wortelkulture met
behulp van Agrobacterium-bemiddelde transformasie ondersoek. Die effektiwiteit van drie
Agrobacterium stamme (A4T, C58C1 en LBA9402) om verskillende S. frutescens eksplante
(kotiel en hipokotiele) te transformeer, was geanaliseer. Al drie stamme was ewe effektief om
harige wortels op beide hipokotiel en kotiele te induseer. S. frutescens transformasie blyk
egter tog van die tipe eksplant afhanklik te wees, aangesien die hipokotiele meer effektief as
die kotiele getransformeer kon word. Met inagneming van beide die hipokotiel (93%) en kotiel
vii
(47%), was transformasie optimaal met die gebruik van die A4T stam. Vier harige wortelklone
was geselekteer en hulle produksie in ‘n vloeibare sisteem was geoptimiseer deur hulle groei
in vier verskillende tipe media (Gamborg B5 (Gamborg et al., 1968), White’s (White, 1934;
White, 1954), MS (Murashige and Skoog, 1962) en half-sterkte MS medium) te ondersoek. B5
en MS medium was beskou as die beste vir alle die harige wortelklone se groei, terwyl White’s
medium die minste doeltreffende groeimedium was. Molekulêre analise van die harige wortels
was gebruik ten einde die transgeniese status van die vier vermoedelike transgeniese klone te
bewys. Dit was behaal deur polimerase kettingreaksie amplifisering (PKR) van die rol A, B en
C gene ten einde die teenwoordigheid van die TL-DNS in die plant genoom aan te toon.
Tydens Southern hibridisasie was ‘n radioaktief gemerkte peiler gebruik om die aantal rol A
geen kopieë te bepaal. Die drie rol gene was teenwoordig in al vier harige wortelklone.
Die derde deel van die studie het gefokus op die effek van drie abiotiese stress faktore
(stikstof beskikbaarheid, sout- en droogte stres) op die produksie van vier metaboliete (GABS,
asparagien, canavanien en arginien). Die effek van stikstof beskikbaarheid op die metaboliet
produksie asook die morfologie was bestudeer deur gebruik te maak van in vitro mikrostingels
asook die harige wortel kloon C58C1-g. Stikstof beskikbaarheidstudies was uitgevoer deur die
mikrostingels of wortelpunte in ‘n gewysigde MS medium te groei. Die MS medium was
aangepas om die normale hoeveelheid stikstof (1.9 g L-1 KNO3 en 1.65 g L-1 NH4NO3) in MS
medium (1x stikstof), of die helfte van die normale stikstof konsentrasie (0.5x stikstof) of twee
keer die normale stikstof konsentrasie in MS medium (2x stikstof) te bevat. Die arginien en
asparagien vlakke in die wortels en stingels, asook die canavanien vlak in die stingels was
positief gekorreleerd aan die stikstof konsentrasie in die medium. Die GABS vlak in die
stingels was egter omgekeerd eweredig aan die stikstof konsentrasie in die medium. Verskeie
redes kan aangevoer word om die metaboliet veranderinge te verduidelik, insluitende die
assimilasie van addisionele stikstof in asparagien, canavanien en arginien in die stingels. Die
verlaagde GABS vlakke kan dui op die voorkeur van vrye GABS vloei na ander stikstofassimilerende
metaboliese paaie soos proteïen sintese, asook die snelle benutting van GABS
ten einde die Trikarboksielsuursiklus intermediêre produkte aan te vul.
Die effek van droogte (geïnduseer deur die byvoeging van 3% (m/v) PEG tot die medium) en
sout stres (geïnduseer deur 50 of 100 mM NaCl byvoeging tot die medium) was slegs in die
stingel kulture ondersoek weens die afwesigheid van canavanien produksie in die wortel
kulture. Water stres het nie ‘n betekenisvolle verandering in die metaboliet vlakke meegebring
nie, maar dit het wel tot ‘n beduidende afname in groei (vars massa en totale stingel lengte) en
bewortelingsreaksie in die mikrostingels gelei. Sout stres het slegs tot ‘n betekenisvolle
viii
toename in arginien vlakke asook ‘n afname in die wortelvorming en groeireaksie tydens die
toenemende sout vlakke gelei. ‘n Verlaging in plant groeikragtigheid mag ‘n eerste visuele
teken van water stres wees. Die toevoeging van NaCl tot die medium kan tot ioontoksisiteit lei
en plante reageer deur middel van osmotiese aanpassing wat tot veranderinge in die
metaboliet vlakke asook veranderinge in fisiologiese groei, lei.
Die finale deel van die studie het die anti-bakteriële aktiwiteit en die fitochemie van die
transgeniese wortel kulture asook die ongetransformeerde in vitro en ex vitro plant materiaal
ondersoek. Slegs die ekstrakte verkry vanaf blaar materiaal geoes uit die natuur, het matige
anti-bakteriële aktiwiteit (1.25 mg ml-1) teen al die bakterië (Escherichia coli, Klebsiella
pneumoniae, Bacillus subtilis en Staphylococcus aureus) wat ondersoek is, getoon.
Aanpassings in die sekondêre metabolisme van die harige wortels is deur middel van dunlaag
chromatografie (DLC) en vloeibare chromatografie-massa spektroskopiese (VC-MS) analise
ondersoek. Verskeie verbindings was in hoër vlakke in die harige wortels teenwoordig, as in
die kontrole wortel ekstrakte. Transformasie het ook die kompleksiteit van die harige wortels
se fitochemiese patroon verhoog, moontlik weens die produksie van nuwe verbindings of
weens die opregulasie van bestaande metaboliese paaie. Die produksie van harige wortels
en die vestiging daarvan in ‘n vloeibare sisteem tydens hierdie studie word beskou as ‘n
belangrike stap na die opskalering van die kulture na bioreaktore. Hierdie wortels kan
toekomstig tot die ontwikkeling van kulture met ‘n hoë produksie van gewenste metaboliete lei.
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Etude phytochimique de trois espèces vénézuéliennes appartenant aux familles Burseraceae, Araliaceae, et Lamiaceae et de deux cultivars de la famille Pittosporaceae / Phytochemical study of three venezuelan species from Burseraceae, Araliaceae and Lamiaceae families and two cultivars of Pittosporaceae family / Estudio fitoquimico de tres especies venezolanas pertinecientes a las familias Burseraceae, Araliaceae y Lamiaceae y de dos cultivares de la familia PittosporaceaeRengifo Carrillo, Mayra Graciela 12 December 2017 (has links)
Cette thèse s'inscrit dans le cadre de la thématique du Laboratoire de Pharmacognosie de l'UFR des Sciences de santé, au sein de l'Université de Bourgogne Franche-Comté et du Laboratoire de Produits Naturels de la Faculté de Sciences, au sein de l'Universidad de Los Andes (Venezuela). Elle vise essentiellement l'isolement, purification et identification de molécules d'origine végétale avec activité biologique. Dans ce contexte, l'étude de plantes vénézuéliennes, Bursera inversa (Burseraceae), Lepechinia Bullata (Lamiaceae) et Hydrocotyle multifida (Araliaceae) avec des cultivars Pittosporum tenuifolium 'Variegatum' et Pittosporum tenuifolium 'Gold star' a conduit à l'obtention de treize glycosides naturels, un dérivé de l'acide caféique et diverses hydrocarbures à longue chaîne par les techniques de chromatographie de couche mince préparative, de chromatographie liquide à moyenne pression, chromatographie liquide haute performance, et de chromatographie liquide sous vide. Les structures ont été élucidées principalement par les techniques spectroscopiques de RMN-1 D et -2D, et de spectrométrie de masse. Il s'agit de treize saponines triterpéniques de type oléanane (parmi lesquelles neuf sont des nouveaux composés naturels) ainsi que de l'acide rosmarinique et des alcanes et esters d'acides gras à longue chaîne. / This thesis was carried out in the Laboratory of Pharmacognosy, on the Health Sciences section of Université de Bourgogne Franche-Comté (France) and also in the Laboratory of Natural Products of Sciences Faculty of Universidad de Los Andes (Venezuela). The aim of this thesis was the isolation, purification and identification of bioactive molecules from several plant species. ln this context, the study of Venezuelan species, Bursera inversa (Bùrseraceae), Lepechinia Bullata (Lamiaceae) and Hydrocotyle multifida (Araliaceae), together with the cultivars, Pittosporum tenuifolium 'Variegatum' and Pittosporum tenuifolium 'Gold star' was carried out. The study led to the isolation of thirteen natural glycosides, one caffeic acid derivative and several long chain hydrocarbons by column chromatography, preparative thin layer chromatography, medium pressure liquid chromatography, high performance chromatography and vacuum liquid chromatography. The structures were elucidate mainly by spectroscopie techniques, NMR-1 D and 2D, and mass spectrometry. The compounds were characterized as thirteen oleanane-type saponins (among them nine are new natural compounds), rosmarinic acid and several long chain alkanes and fattv acid esters / Este trabajo se presenta bajo la forma de secciones, donde en primer lugar se expone una breve introducción acerca de los géneros de interés para este estudio, como son Bursera (Burseraceae), Hydrocotyle (Araliaceae), Lepechinia (Lamiaceae) y Pittosporum (Pittosporaceae); así como los motivos que llevaron a la realización de este estudio fitoquímico. Cada género es tratado en un capítulo diferente, que abarca una revisión bibliográfica extensa (considerando los aspectos etnobotánicos, fitoquímicos y farmacológicos) del género, seguida por el procedimiento experimental llevado a cabo en cada especie analizada y por último el análisis de los resultados obtenidos.Los compuestos aislados de cultivares de Pittosporum tenuifolium estudiados: 'Variegatum' y 'Gold Star' se encuentran descritos en el primer capítulo entre los que se encuentran ocho nuevas saponinas triterpénicas tipo-oleanano: PT-PI y PT-P4 de los tallos deP. tenuifolium 'Variegatum', PT-P2 y PT-P3 de las hojas de este mismo cultivar, PT-P7 y PT-P8 de los tallos de P. tenuifolium 'Gold Star' y por último, PT-P5 y PT-P6 aisladas de los tallos de ambos cultivares. Además también se describe el compuesto ya conocido, udosaponinaF (PT-P9), identificado en los tallos de P. tenuifolium 'Variegatum' De las especie Hydrocotyle multifìda se aislaron cinco saponinas triterpénicas, descritas en el segundo capítulo, las cuales tienen al ácido oleanólico como genina. Dos de las cinco saponinas son productos naturales nuevos, HmE-P3 y HmE-P2 minoritario; las otras tres saponinas son compuestos ya conocidos, momordin I (HmE-P1), sandrosaponina X (HmE-P2 mayoritario) y hemslósido Mal (HmE-P4) En el tercer capítulo que abarca al género Bursera, incluye los resultados del estudio fitoquímico de las semillas de Bursera inversa, entre los que se puede mencionar la identificación de 45 compuestos en las semillas de esta planta. El último capítulo contiene la descripción del compuesto mayoritario, aislado de las mias de Lepechinia bullata e identificado como el ácido rosmarínico (LB-TI).
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Investigation Phytochimique de plantes utilisées en médecine traditionnelle au Mozambique : Ptaeroxylon obliquum Radlk - Pyrenacantha kaurabassana Baill - Monadenium lugardae N.EBr. / Phytochemical study of medicinal plants from Mozambique : Ptaeroxylan obliquum Radlk., Pyrenacantha kaurabassama Baill, Monadenium lugardiae N. Ebr.Agostinho, Daniel 24 June 2013 (has links)
Les travaux menés dans cette thèse s’inscrivent dans une démarche ethno-pharmacologique visant à valoriser des plantes utilisées traditionnellement en médecine au Mozambique. Cette étude a comme but principal d’apporter des éléments chimio taxonomiques concernant des espèces végétales peu décrites et de préciser la composition métabolique de parties de plante utilisées en médecine traditionnelle, pour aboutir potentiellement à de nouvelles molécules utilisables en thérapeutique. Le travail est ainsi découpé en trois parties distinctes, chacune portant sur une plante différente.La Partie 1présente l’étude phyto-chimique des racines sèches de Ptaeroxylon obliquum Radlk (Rutaceae). L’étude phyto-chimique de l’extrait chloroformique des racines de P.obliquum a permis l’isolement de cinq composés appartenant à la famille des coumarines ou de chromones dont un totalement original : un meroterpène de type chromone, le Ptaerobliquol. Les structures de ces composés ont été élucidées par différentes techniques analytiques de pointes (RMN, Spectrométrie de masse) et diffraction des rayons X.La Partie 2 porte sur l’étude phyto-chimique des écorces de tubercules de Pyrenacantha kaurabassana (Icacinaceae). Cette plante n’a été que très peu étudiée d’un point de vue phytochimique. Un criblage des métabolites présents a été réalisé, montrant la présence prépondérente de composés de la famille des quinones et des flavonoïdes. Le fractionnement de l’extrait acétate d’éthyle des écorces de tubercule a abouti à l’isolement et l’identification de 4 métabolites, dont 2 totalement originaux, appartenant à la famille des xanthones.Enfin la Partie 3 porte sur l’étude phytochimique des tiges de Monadenium lugardiae ou Euphorbia lugardiae (Euphorbiaceae). Le fractionnement de l’extrait chloroformique des tiges a permis l’isolement et l’identification de deux métabolites jamais décrits dans cette plante, le jolkinolide B, l’Hélioscopinolide F, conjointement avec la scopoletine. / This PhD work is part of an ethno-pharmacological approach to enhance plant used in traditional medicine in Mozambique. The aim of this work is to elucidate major metabolites through a chemo-taxonomic approach and clarify the phytochemical composition of plant used in traditional medicine, leading potentially to new molecules of therapeutical interest.The work is thus cut into three parts, each focusing on a different plant.The Part 1describes the phytochemical study of dry roots of Ptaeroxylon obliquum Radlk (Rutaceae). The phytochemical study of the chloroform extract of the roots of P. obliquum resulting in the isolation of five compounds belonging to coumarin or chromone. A totally original meroterpenoid chromone was then isolated and elucidated: the Ptaerobliquol. Structures of these metabolites were elucidated by various analytical techniques (NMR, mass spectrometry) and X-ray diffraction.Part 2 focuses on the phyto-chemical study of bark tubers of Pyrenacantha kaurabassana (Icacinaceae). Few phytochemical data were available about this plant in the litterature. Screening of metabolites was so carried out, showing the preponderant presence of compounds belonging to the family of quinones and flavonoids. The study of the ethyl acetate extract of the bark of tuber resulted in the isolation and identification of four metabolites, including two totally original, belonging to the family of xanthones.Finally, Part 3 focuses on the phytochemical study of stems of Monadenium lugardiae or Euphorbia lugardiae (Euphorbiaceae). Fractionnation of the chloroform extract of the stemshas led to the isolation and identification of two metabolites never described in this plant, jolkinolide B, the Hélioscopinolide F, together with scopoletin.
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Estudo químico e avaliação biológica do extrato das cascas das raízes de Caesalpinia pyramidalis Tul (Leguminosae)Oliveira, José Cândido Selva de January 2010 (has links)
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Previous issue date: 2010 / CAPES / O presente trabalho relata o estudo químico das cascas das raízes de Caesalpinia pyramidalis
Tul., uma árvore pertencente a família Leguminosae endêmica da região da caatinga baiana
cujas folhas são utilizadas na medicina popular como diurético e digestivo. O extrato
metanólico bruto foi submetido à extração liquido-liquido e sua atividade citotóxica e
antioxidante foram avaliadas. O extrato hexânico apresentou-se atóxico para o teste de
letalidade de Artemia salina e os demais extratos foram moderadamente tóxicos. Em relação à
atividade antioxidante, o extrato AcOEt foi o mais ativo, seguido do BuOH e MeOH. O
fracionamento cromatográfico da fase hexânica permitiu o isolamento do lupeol, acacetina,
um novo fenilpropanóide, ácido (E)-8-hidroxi-3,5-dimetoxicumarico, além de uma mistura de
sitosterol e estigmasterol. Da fase metanólica foram isolados o mesmo fenilpropanóide
encontrado na hexânica além de um novo biflavonóide, 7-hidroxi-4’-metoxiflavona-5α-2,4-
dihidroxi-4’-metoxidihidrochalcona. A estrutura deste novo biflavonóide bem como das
outras substâncias isoladas foram elucidadas a partir da análise dos dados de RMN 1H e 13C
(BB e APT) juntamente com a RMN de correlação (HMQC e HMBC). / Salvador
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Atividade antioxidante, cicatrizante e antiulcerogênica dos extratos e das frações das folhas de Oncidium flexuosum SIMS (Orchiaceae) / Antioxidant, cicatrizant and antiulcerogenic of extracts and fractions of Oncidium flexuosum Sims (Orchiaceae) leavesGaspi, Fernanda Oliveira de Gaspari 02 November 2011 (has links)
Orientadores: João Ernesto de Carvalho, Mary Ann Foglio / Tese (doutorado) - Universidade Estadual de Campinas, Faculdade de Ciências Médicas / Made available in DSpace on 2018-08-17T20:05:53Z (GMT). No. of bitstreams: 1
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Previous issue date: 2011 / Resumo: O conhecimento sobre as plantas, a descoberta de suas propriedades curativas têm sempre acompanhado a evolução do homem através dos tempos. A família Orchidaceae é a maior entre as angiospermas, são mais de 25 mil espécies já descritas. Entre elas está a Oncidium flexuosum Sims., uma importante espécie brasileira conhecida popularmente como bailarina e que possui grande valor ornamental. Porém, esta é a primeira pesquisa sobre as suas propriedades medicinais. Os objetivos deste trabalho foram avaliar as atividades antioxidante in vitro e in vivo, cicatrizante e antiulcerogênica dos extratos e das frações obtidas a partir das folhas de O. flexuosum e realizar as análises fitoquímicas e histoquímica preliminares. Para isto, foram utilizadas as análises da capacidade sequestradora do radical livre difenilhidrazil (DPPH), da atividade antiulcerogênica induzida por etanol, do reparo tecidual associado ou não a microcorrente, além das reações de caracterização e cromatografia de camada delgada. Também foram realizados testes histopatológicos para avaliar possíveis danos oxidativos. O extrato hidroalcoólico de O. flexuosum (EH) possui as atividades antioxidante in vitro diante do radical livre DPPH e in vivo, cicatrizante associado à microcorrente, estimulante da proliferação de fibroblastos in vitro e colágeno in vivo, e atividade antiulcerogênica. A fração terpeno (FrT) inibi o processo oxidativo causado pelo substâncias reativas do ácido tiobarbitúrico (TBARS). O extrato bruto enzimático (EBZ) e a FrT estimulam a proliferação de fibroblastos, porém com menor potência do que o EH. As análises fitoquímicas e histoquímica revelaram que as folhas de O. flexuosum possuem, entre os seus constituintes, as substâncias fenólicas, tais como flavonoides e taninos, e também cumarinas, triterpenos e esteróides. O EH não induziu danos renais nos animais, mas tem potencial hepatotóxico dose-tempo-dependente, causando inflamação e degeneração tecidual. Conclui-se que o EH possui atividade antioxidante, cicatrizante e antiulcerogênica, provavelmente devido à presença das substâncias fenólicas / Abstract: The knowledge about plants, the discovery of their healing properties has always followed the evolution of man through the ages. The Orchidaceae family is the largest among the angiosperms, they are more than 25,000 described species, among them is the Oncidium flexuosum Sims., an important Brazilian species popularly known as dancer and which has great ornamental value. However, this is the first survey of its medicinal properties. The objectives of this work were to investigate the antioxidant activity in vitro and in vivo, wound healing and antiulcerogenic activities of the extracts and fractions obtained from the leaves of Oncidium flexuosum and perform the preliminary phytochemical and histochemistry analysis. For this, analysis of free radical scavenging capacity with difenilhidrazil (DPPH) test, antiulcer activity induced by ethanol, tissue repair associated or not with microcurrent were made, other than the characterization reactions and thin layer chromatography. Histopathological tests were also performed to evaluate possible oxidative damage. The extract of Oncidium flexuosum (EH) has in vitro antioxidant activity against free radical DPPH and in vivo, cicatrizant associated with microcurrent, stimulating fibroblasts proliferation in vitro and collagen in vivo. The terpene fraction (FrT) inhibit the oxidative process caused by the thiobarbituric acid reactive substances (TBARS). The enzimatic crude extract (EBZ) and FrT stimulate proliferation of fibroblasts, but with less efficiency than the EH. The phytochemical and histochemistry analysis revealed that the leaves of Oncidium flexuosum plant species have among its constituents, the phenolic substances such as flavonoids and tannins, and also the coumarins, triterpenes and steroids. The EH was not induce kidney damage in animals, but has hepatotoxic potential dose-time-dependent, causing inflammation and tissue degeneration. It was concluded that the EH has antioxidant, cicatrizant and antiulcerogenic activities probably due to the presence of phenolic substances / Doutorado / Ciencias Basicas / Doutor em Clínica Médica
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Estudo Fitoquímico das Folhas da Espécie Psychotria prunifolia (Kunth) Steyerm (Rubiaceae) / Phytochemical study of leaves of Psychotria prunifolia (Kunth) Steyerm (Rubiaceae)FARIA, Emiret Otoni de 31 July 2009 (has links)
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Previous issue date: 2009-07-31 / Psychotria prunifolia is a Rubiaceae family specimen found in the Goiás cerrado , which is a huge ecosystem in the Brazilian Mid-West Mainland. The NCI (National Cancer Institute) highly referred to Psychotria as a hot genera with a cytotoxic potential from its extracts and fractions. Several related chemical studies have mostly indicated findings of indole alkaloid, which are keys to various biological activities. Current ongoing studies are focusing on phytochemical investigation of P. prunifolia, and its cytotoxic, antibacterial, antioxidant, and antifungal findings from its
leaves extracts and fractions. It was feasible to isolate four new indole-monoterpene alkaloids and estrictosamida upon fractioning the leaves gross extracts. Estrictosamida has been found in and isolated from other specimens from the same genera. Recently-found alkaloids have been named prunifolina, prunifoliona, EPP26.2 e EPP28.1. Indole-monoterpene alkaloid is of greater chemotaxonomic
importance for the Rubiaceae family, and it may assist with better classifying heteropsychotria sub-genera specimens.
In vitro analysis of four cultures of cellular kinds, (S-180- Mice Sarcoma, A549- Human-Lung Carcinoma, K562 Chronic Human Myeloid Leukemia e HFF- 1-Regular Human Cells fibroblasts), has demonstrated successful cytotoxic
activity of the P. prunifolia specimen. As a result of the antibacterial analysis, the leaves extracts were deemed to be less active. Extracts of leaves have shown little efficacy with its antioxidant potential, and in vitro antifungal analysis has indicated mild or little response. / Psychotria prunifolia é uma planta da família Rubiaceae com ocorrência no cerrado goiano. O NCI (Instituto Nacional do Câncer dos Estados Unidos - EUA) apontou o gênero Psychotria como hot gênero referindo-se ao potencial citotóxico de seus extratos e frações. Em estudos químicos do gênero foram encontrados principalmente alcalóides indólicos responsáveis por diversas atividades biológicas.
O presente estudo tem por objetivo a investigação fitoquímica de P. prunifolia, a avaliação citotóxica, antibacteriana, antioxidante e antifúngica dos extratos brutos e frações das folhas. A partir do fracionamento ácido-base do extrato bruto das folhas foi possível o isolamento de quatro novos alcalóides indol-monoterpenos e a estrictosamida, já isolada em outras espécies do gênero. Os alcalóides inéditos foram chamados de prunifolina, prunifoliona, EPP26.2 e EPP28.1. Os alcalóides
indol-monoterpenos tem importância quimiotaxionômica na família Rubiaceae e podem auxiliar na melhor classificação das espécies do subgênero heteropsychotria. Os testes in vitro com quatro tipos de cultura de células (S-180-sarcoma de
camundongo, A549-carcinoma de pulmão humano, K562- leucemia mielóide crônica humana e HFF-1-células normais humanas-fibroblastos) mostraram promissora atividade citotóxica da espécie P. prunifolia. No teste de atividade
antibacteriana, os extratos das folhas foram considerados pouco ativos. O extrato bruto das folhas mostrou-se pouco promissor quanto ao potencial antioxidante. A atividade antifúngica in vitro mostrou-se razoável.
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