Charles University in Prague, Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Botany Candidate: MSc. Latifah Al Shammari Supervisor: Prof. Ing. Lucie Cahlíková, Ph.D. Title of Doctoral Thesis: Alkaloids of the genus Hippeastrum (Amaryllidaceae): isolation, identification, biological activity. Hippeastrum x hybridum cv. Ferrari was chosen based on results of previous screening studies for detailed phytochemical study for the purpose of isolation of the widest range of AAs. From 25 kg of fresh bulbs was obtained 29,46 g of purified alkaloidal extract, which was processed using column chromatography. Finally, 18 pure alkaloids were isolated including one new homolycorine-type alkaloid (9-O-demethyllycorenine). All compounds were identified by spectrometric techniques (GC-MS, ESI-MS, NMR, optical rotation) and by comparison with literature data. All alkaloids, isolated in sufficient amount, were tested for their biological activities associated with Alzheimer's disease (inhibition of hAChE, hBuChE, and POP), and cytotoxic activity. The inhibitory activity against human cholinesterases was determined in vitro by a modified Ellmanʼs spectrophotometric method. In the hAChE/hBuChE assay, except for 1,2- O,O'-diacetyl-dihydrolycorine which demonstrated a mild hBuChE inhibition potency...

Resveratrol (RV) is a naturally occurring phytoalexin of the stilbenoid family produced by some plant species, and present in grape skin, peanuts, and red wine. It has been found to exhibit anti-cancer, anti-inflammatory, anti-viral, anti-aging, cardio protective, and anti-oxidant properties. Bioavailability is a huge setback that limits the potentials of RV. As a result, efforts have been made to design and synthesize RV esters and aliphatic acids in an attempt to increase its bioavailability, solubility in water, and possibly improving its biological activities. Resveratrol esters, 3,5,4'-triacetyloxystilbene (2) and Methyl 1,1',1''- (3,4',5-stilbenyl)-1,6-hexanedioate (3) have been synthesized. Compound 3 is a new compound, synthetic yield is 88%, and purity is above 95% based on NMR integration. Both 2 and 3 are good candidates for biological evaluation. 3 was used as a precursor in the synthesis of resveratrol aliphatic acid, 8-(3',5'-dihydroxylstilbene-4''-oxy)-3,6-dioxocotanoic acid (9). First, 2 was hydrolyzed to resveratrol diester, 3,5-diacetyloxystilbene (4). Mitsunobu reaction of 4 and methyl 8-hydroxy-3,6-dioxooctanoate (7) was then carried out to afford methyl 8-(3',5'-diacetyoxystilben-4''-oxy)-3.6-dioxooctanoate (/5), which was then hydrolyzed to afford 9 in total 43.6 % yield. Structures of all newly synthesized compounds were confirmed by 1H and 13C NMR spectroscopy.

В работе представлены результаты исследования влияния производных 1,2,4-триазинов на ранние этапы онтогенеза растений ячменя. Объект исследования – производные 1,2,4-триазины. Охарактеризовано влияние исследуемых веществ на всхожесть семян, параметры роста проростков и активность перекисного окисления липидов. Показано, что исследуемые вещества №2, 6, 10 и 11 проявляют гербицидную активность. Работа изложена на 43 страницах, содержит список использованной литературы из 62 источников, 21 рисунок и 1 таблицу. / The paper presents the results of a study of derivatives of 1,2,4-triazines at the early stages of ontogenesis of barley plants. The object of research is derivatives of 1,2,4-triazines. The influence of the studied substances on the germination of seeds, the parameters of the growth of seedlings and the activity of lipid peroxidation is characterized. It is shown that the investigated substances № 2, 6, 10 and 11 exhibit herbicidal activity. The work is presented on 43 pages, contains a list of used literature from 62 sources, 21 figures and 1 table.

<p> The objective of this study was to synthesize and biologically evaluate a series of novel nucleoside derivatives of the naturally occurring lignans, podophyllotoxin and 4'-demethylepipodophyllotoxin. Epipodophyllotoxin derivatives display two types of biological activity: while the naturally occurring compounds are potent inhibitors of microtubule polymerization, two semi-synthetic glycoside derivatives, viz VP16-213 (etoposide) and VM26 (teniposide), are specific inhibitors of mammalian DNA topoisomerase II. The latter two compounds have proven to be very useful in the treatment of many different types of cancer. In this study, the glycoside moiety of VP16-213/VM26 was replaced with either a thymidine or a 2'-deoxyadenosine group. The synthetic approach involved protective group chemistry, where functional groups on the nucleosides and DMEP were selectively blocked prior to their condensation in the presence of boron trifluoride etherate catalyst. These compounds are of interest because they involve substitution of the glucoside moiety with a nucleoside residue, whose effect on the biological activity of epipodophyllotoxin derivatives has not been examined. The biological activity of these compounds was assessed by examining their cross-resistance patterns towards a set of Chinese hamster ovary mutants resistant to podophyllotoxin VP16-213/VM26, mitotic index, and by a competition assay. From the cross resistance assay, all of the thymidine derivatives were found to be considerably less active than the parent podophyllotoxin and 4'-demethylepipodophyllotoxin molecules, while the 2'-deoxyadenosine derivatives were found to be completely inactive. The cross-resistance patterns of the thymidine derivatives suggests that these compounds display podophyllotoxin-like activity in vivo and show no VP16-213/VM26-like activity. Treatment of wild type cells with the active thymidine derivatives (compounds 1.2, 2.2, 2.3, and 2.4) increased the mitotic indices approximately ten-fold in a dose-dependent manner, which parallels the results of the dose-response curves in the initial cross-resistance assay. Furthermore, there was a marked increase in the levels of drug required to elevate the mitotic index in second-step mutants resistant to podophyllotoxin, again lending support to the initial results indicating that the cellular target of these compounds is tubulin. Only one compound (1.2), was found to out compete the binding of radiolabelled podophyllotoxin to purified calf brain tubulin. However, due to their low activity relative to podophyllotoxin, most of these compounds were insoluble at concentrations required to out compete the binding of radiolabelled podophyllotoxin. Molecular modelling studies have provided useful insights regarding the structure/activity relationships among the active and inactive nucleoside derivatives showing podophyllotoxin-like antimitotic activity. There appears to be steric limits for substituents attached at the C4 moiety that maintain the antimitotic activities of the parent molecules. The electrostatic potential and hydrophobic properties of these groups also seem to play a role in the degree of activity these compounds show, but remain unclear at this point. By simple comparison of the three-dimensional structures of these compounds there appears to be a very limited spacial and electrostatic requirement for the bulky glycosidic moiety attached to C4 which is essential for targeting VP16-213 and VM26 to DNA topoisomerase II. Thus, several important structural features which may distinguish the selectivity POD derivatives show for either tubulin or DNA topoisomerase II are described.</p> / Thesis / Master of Science (MSc)

No / The aim of the present study was to investigate an opioid receptor involvement in the adaptation response to motion sickness in Suncus murinus. Different groups of animals were treated intraperitoneally with either saline, morphine (0.1 and 1.0 mg/kg), naloxone (1.0, 10.0 and 5.0 mg/kg) or a combination of naloxone plus morphine in the absence or 30 min prior to a horizontal motion stimulus of I Hz and 40 mm amplitude. For the study of adaptation, different groups received saline on the first trial, and in subsequent trials (every 2 days) they received either saline, naloxone (1.0 and 10.0 mg/kg, ip) or morphine (0.1 mg/kg, ip) 30 min prior to the motion stimulus. Pretreatment with morphine caused a dose-related reduction in emesis induced by a single challenge to a motion stimulus. Pretreatment with naloxone alone did not induce emesis in its own right nor did it modify emesis induced by a single challenge to a motion stimulus. However, pretreatment with naloxone (5.0 mg/kg, ip) revealed an emetic response to morphine (P<.001) (1.0 mg/kg, ip) and antagonised the reduction of motion sickness induced by morphine. In animals that received saline or naloxone (1.0 mg/kg), a motion stimulus inducing emesis decreased the responsiveness of animals to a second and subsequent motion stimulus challenge when applied every 2 days for 11 trials. However, the animals receiving naloxone 10.0 mg/kg prior to the second and subsequent challenges showed no significant reduction in the intensity of emesis compared to the first trial. The data are revealing of an emetic potential of morphine when administered in the presence of a naloxone pretreatment. The administration of naloxone is also revealing of an additional inhibitory opioid system whose activation by endogenous opioid(s) may play a role in the adaptation to motion sickness on repeated challenge in S. murinus.

Darbo tikslas ‒ ištirti drėgnio įtaką susmulkinto gluosninio žilvičio savaiminiam kaitimui ir šilumos sklaidai pjaustinio sampile. Atlikti tyrimai ir literatūros analizė leidžia teigti, kad didelis drėgmės kiekis lemia pjaustinio biologinį aktyvumą, taip pat jo tankį, poringumą ir kitas savybes. Susidaro palankios sąlygos pjaustinio savaiminio kaitimo procesui, kuris siejamas su medienos audinių kvėpavimu, grybų ir bakterijų veikla, biodegradacijos proceso intensyvumu bei medienos pjaustinio savaiminio užsiliepsnojimo rizika. Atlikus tyrimus nustatyta, jog didžiausiu biologiniu aktyvumu (800 ÷ 340 W/(t•h)) pasižymi nuo 50 % iki 33 % drėgnio gluosninio žilvičio pjaustinys. Jam džiūstant toliau, išskiriamas šilumos srautas intensyviai mažėja ir išdžiūvus iki 12 % drėgnio, tampa visiškai biologiškai neaktyvus. Nustatyta, jog medienos pjaustinio temperatūrinis laidis nevienodas įvairuojant jo drėgniui. Temperatūrinio laidžio maksimali vertė 21,6 m2/s fiksuota, kai gluosnių pjaustinio drėgnis siekė 30 %. / The aim of this paper is to explore the influence of humidity to self‒heating and thermal dissipation pile chaff to cut Salicaceae osier. Performed research and analysis of literature suggests that high moisture content determines the biological activity of carving its density, porosity and other properties. It creates favourable conditions for self‒heating process of carving, which is associated with the wood tissue of breath, fungi and bacteria activity, biodegradation process, the intensity of wood carving and the risk of spontaneous ignition. The investigation revealed that the highest biological activity (800 ÷ 340 W/(t•h)) have between 50 % and 33 % of humidity Oyster osier chops. Further drying, heat flow decreases intensively and drying up to 12 % humidity, it is completely becoming biological inactive. It was found that the conductivity of wood carving temperature difference of unequal moisture. Thermal conductivity maximum value of 21,6 m2/s fixed, the willow carving moisture content was 30 %.

Les substances synthétisées par les bactéries du genre Bacillus présentent un grand intérêt en raison de leurs nombreuses activités antimicrobiennes. L’objectif de ce travail a consisté à mettre au point un protocole analytique fiable pour extraire ces substances, et les caractériser par spectrométrie de masse et par leurs activités biologiques. Une première approche par spectrométrie de masse MALDI-ToF ne nous a pas donné de résultats satisfaisants en raison d’un phénomène de suppression spectrale. Une seconde stratégie d’étude combinant deux techniques analytiques a alors été envisagée. Les composés et les familles lipopeptidiques ont d’abord été séparés par chromatographie liquide analytique et analysés en ligne en mode de couplage ESI-IT. Ensuite les fractions collectées ont été caractérisées par spectrométrie de masse MALDI-Q-ToF (et ESI-Q-ToF) pour déterminer les masses exactes et obtenir des spectres de fragmentation complémentaires des premiers. Ce procédé nous a permis d’établir des critères d’identification des composés et des familles de lipopeptides de structures connues. Cette caractérisation est basée sur des temps de rétention en chromatographie, des mesures de masses exactes et sur des schémas de fragmentations. Nous avons fait de même avec les composés non identifiés et ensuite évalué leur activité biologique en réalisant des tests de diffusion sur agar. Cette stratégie d’étude permet de faire un criblage de l’ensemble des biomolécules produites par des souches de Bacillus et de relier une structure à une activité biologique. Ce protocole, mis au point pour des cultures réalisées en milieu liquide, a ensuite été adapté aux cultures sur boîtes de Pétri pour pouvoir analyser les composés produits à l’échelle de la colonie bactérienne. / Compounds produced by Bacillus bacteria present a major interest because of their biological activities. The aim of this work was to develop a reliable analytical methodology to extract these compounds, and to characterize them by mass spectrometry and by their biological activities. A first approach by MALDI-ToF mass spectrometry doesn’t give satisfactory results because of strong spectral suppression effects. Therefore, we have designed a second strategy which combined two analytical technologies. First, compounds and lipopeptides families were separated by analytical liquid chromatography and analysed by ESI-IT. Then, collected fractions were characterized by MALDI-Q-ToF (and ESI-Q-ToF) in order to determine accurate mass measurements and obtain complementary product ion spectra. This process led us to establish identification criteria of compounds and lipopeptides families which have known structures. This characterization is based of retention times in chromatography, accrurate mass measurements and fragmentation schemes. We have achieved the same experiments with non identified compounds and then assessed their biological activity by agar well diffusion test.This strategy allows to obtain a screening of whole of the biomolecules produced by bacillus strains and establishes a link between structure and biological activity. This methodology, designed for cultures in liquid medium, was then adapted to cultures in Petri disches in order to analyse compounds producted at the bacterial colony scale.

Nesta dissertação são apresentadas a síntese e caracterização de duas novas substâncias, consideradas aqui como metalo-fármacos em potencial: o composto iônico (C17H19FN3O3)3[RuCl6].3H2O e o complexo [Ru(C17H17FN3O3)3].4H2O, obtidos através da reação entre RuIII e a fluoroquinona ciprofloxacina em diferentes condições de síntese (meio ácido ou neutro e refluxo, respectivamente). O espectro ESI MS em modo positivo de (C17H19FN3O3)3[RuCl6].3H2O exibiu um pico principal em m/z = 994,6 que foi atribuído ao aduto (ciprofloxacina)3.H+ em fase gasosa, enquanto [Ru(C17H17FN3O3)3].4H2O apresentou picos m/z em 1093,3 e 547,1, atribuídos aos íons [Ru(C17H17FN3O3)3].H+ e [Ru(C17H17FN3O3)3].2H+, respectivamente. Os resultados de análise térmica estão em concordância com os conteúdos de água propostos para as duas substâncias. Os espectros de absorção em meio aquoso são dominados pelas transições da ciprofloxacina na região UV. Não obstante, duas bandas foram observadas em 421 e 496 nm no caso de (C17H19FN3O3)3[RuCl6].3H2O, e atribuídas à transição de transferência de carga e à transição d-d, respectivamente; no caso de [Ru(C17H17FN3O3)3].4H2O, apenas um ombro largo em torno de 450 nm foi observado na região do Visível, tendo sido atribuído à uma transição d-d. O voltamograma cíclico deste complexo exibiu um processo quase-reversível em 0,25 V (versus EPH) enquanto o composto iônico apresentou o mesmo processo em 0,11 V, sugerindo que, neste caso, o íon central de rutênio é estabilizado no estado de oxidação III através da coordenação dos átomos de oxigênio das três unidades de ciprofloxacina. O complexo de coordenação é estável por mais de 48 horas em pH fisiológico, estomacal e intestinal. Ambos foram incubados nas condições estomacais (pH = 1,5 e temperatura = 370C) e não causaram diminuições significativas nos valores de pH. / This work presents the synthesis and characterization of two potential new metallodrugs, the ionic (C17H19FN3O3)3[RuCl6].3H2O and the coordination [Ru(C17H17FN3O3)3].4H2O compounds, by combining ruthenium (III) and the fluoroquinolone ciprofloxacin in different synthetic conditions (acid media or neutral and reflux conditions, respectively). The ESI MS (positive mode) spectrum of the ionic compound displayed a main peak at m/z = 994.6, which was assigned to the gaseous phase adduct (ciprofloxacin)3.H+, while the coordination compound featured peaks at m/z 1093.3 and 547.1 ascribed to the singly and doubly charged ions [Ru(C17H17FN3O3)3].H+ and [Ru(C17H17FN3O3)3].2H+, respectively. Thermal analysis corroborated the proposed water content for both complexes. The absorption spectra of the compounds in aqueous medium are dominated by the ciprofloxacin transitions in the UV region but two bands were observed at 421nm and 496nm for the ionic compound, assigned to a charge transfer and d-d transitions. In the case of the coordination compound only a broad shoulder around 450 nm was observed in the visible region, also assigned to a ligand field transition The cyclic voltammograms of the [Ru(C17H17FN3O3)3] complex exhibited a quasi-reversible process ascribed to the Ru(II) / (III) redox pair at -0.25 V (vs SHE) while compound (C17H19FN3O3)3[RuCl6] displayed this process at -0.11V, showing that the central ruthenium ion is stabilized in the (III) oxidation state by the coordination to the hard oxygen atoms of the ciprofloxacin ligand. The coordination compound is stable under physiological, stomachal and intestinal pH over 48 hours. Both compounds are stable incubated under stomachal conditions (pH=1.5 and 37oC) without significant pH lowering.

Lectinas são proteínas cuja principal característica é a de se ligar específica e reversivelmente a carboidratos. BanLec é a lectina presente na polpa de bananas, que se liga especificamente a manose e glicose, e é capaz de induzir a proliferação de células T, podendo estimular a resposta imune. Existem indícios de que o teor de BanLec pode variar dependendo do estádio de amadurecimento e do tipo de cultivar, o que pode afetar a quantidade de BanLec existente na fruta quando consumida in natura e a possível resposta imune frente ao consumo de banana. Por este motivo, um dos objetivos desse trabalho foi determinar os teores e a atividade hemaglutinante de BanLec em extratos de farinha de banana verde, além de bananas das cultivares Pacovan, Figo, Terra, Mysore e Nanicão, nos estádios de maturação verde e maduro, e submetidas a tratamento com 1-MCP e baixa temperatura (para cv. Nanicão). Com vista a atender ao objetivo de avaliar seus efeitos imunomoduladores in vivo, a BanLec foi purificada da cultivar Nanicão e administrada por via oral a camundongos BALB/c. Os ensaios de atividade hemaglutinante dos extratos de banana apontaram para maior quantidade de BanLec no fruto maduro, quando comparado ao verde, e ausência dessa proteína na cultivar Figo. Os parâmetros imunológicos analisados após administração de BanLec aos camundongos demonstram que a resposta imune gerada após ingestão de BanLec é dose dependente, além disso, a administração de 50 &#181;g de BanLec aos animais foi capaz de modular citocinas importantes na resposta imunológica, provavelmente causando um efeito que pode ser interpretado como mais protetor do que patogênico. Com base nos resultados obtidos, podemos concluir que existem diferenças nos teores de BanLec dependendo da cultivar e estádio de maturação analisado, sendo que essa proteína não está presente na polpa de todas as variedades de banana e finalmente, que ela tem grande potencial imunomodulador in vivo, uma vez que ativou citocinas de resposta anti-inflamatória. / Lectins are proteins which bind specifically and reversibly to carbohydrates. BanLec is the lectin present in banana pulp, and it binds to mannose and glucose, being capable of inducing T-cell proliferation, and to stimulate the immune response. There are some evidence that the amount of BanLec may vary depending on the maturation stage of the fruit and the cultivar (cv.), which may affect the amount of BanLec and the possible immune response after consumption of banana. Thus, this study aimed to evaluate the amount of BanLec and its hemagglutinating activity in crude extracts of bananas from cultivars Pacovan, Figo, Terra, Mysore and Nanicão, in both unripe and ripe maturation stage, and also fruits which were treated with 1-MCP and low temperature. In addition, in order to access their immunomodulatory effects in vivo, BanLec was purified by affinity chromatography and administered orally to BALB/c mice. The hemagglutinating activity assays indicate higher amount of BanLec in ripe fruit. Moreover, the possible was undetectable in the pulp of banana Figo. The immunological parameters of mice orally fed with BanLec showed that the immunological response is dependent on the amount of protein administrated, in agreement to previous in vitro studies. Besides, 50 &#181;g of BanLec, were able to modulate some cytokines in immune response, causing an effect that seems to be more protective than pathogenic. We conclude that there are important differences in amount of BanLec depending on the cultivar and the maturation stage, and BanLec has a dose-dependent immunomodulatory effect in vivo.

O objetivo deste trabalho foi produzir pigmentos em pó a partir dos subprodutos de vinificação da uva tinta, variedade Bordô (Vitis labrusca), através da secagem em spray dryer utilizando maltodextrina como agente carreador. Foram estudados os efeitos das condições de processo sobre algumas propriedades físico-químicas, além da estabilidade e da atividade biológica do material obtido. Extratos etanólicos das cascas e sementes da uva foram obtidos e concentrados até um terço do volume inicial. Este extrato foi então misturado com o agente carreador maltodextrina 10 DE nas concentrações de 10, 20 ou 30% e atomizado em spray dryer, com vazão de alimentação de 44 mL/min e temperaturas do ar de entrada de 130, 150 ou 170°C, num total de nove ensaios. Além disso, foi obtida uma amostra de extrato concentrado liofilizado, sem a presença do agente carreador, para efeito de comparação. Avaliou-se o rendimento do processo de atomização; e para as amostras obtidas determinou-se o teor de umidade, retenção de antocianinas, higroscopicidade e solubilidade em água, a fim de verificar a influência das condições de processo sobre essas características. Estas amostras também foram avaliadas quanto à morfologia, distribuição do tamanho de partículas e isotermas de sorção de umidade. Todas as amostras obtidas (atomizadas e liofilizada) foram avaliadas quanto à cor instrumental, espectroscopia de infravermelho, estabilidade durante a estocagem, presença de compostos bioativos (fenólicos, flavonóides, antocianinas e proantocianidinas), além de atividade antioxidante, antimicrobiana e de inibição da arginase de Leishmania. As condições de processo avaliadas (temperatura de secagem e concentração de agente carreador) tiveram forte influência nas características estudadas. O teor de umidade, a retenção de antocianinas, a morfologia e o tamanho das partículas, foram bastante influenciados pela temperatura de secagem e pela concentração de agente carreador, enquanto que a higroscopicidade sofreu maior influência da concentração de agente carreador. Esse parâmetro também apresentou grande influência nas isotermas de sorção de umidade das amostras. Não houve grande interferência do processo de secagem na composição química do material obtido, evidenciada pelos espectros de infravermelho. Quanto à avaliação da estabilidade durante a estocagem, foi observado que as amostras contendo maltodextrina conservaram mais as antocianinas e a cor, quando comparadas com as amostras sem carreador e os extratos líquidos, indicando, que o processo de secagem e a presença do carreador, promoveram um efeito protetor aos compostos e sua cor. Todas as amostras apresentaram altos teores de flavonóides totais, antocianinas, proantocianidinas e elevados valores de atividade antioxidante variando de 314,06 a 441,04 &micro;molesTE/g de extrato seco pelo método DPPH e de 993,32 a 1138,68 &micro;molesTE/g de extrato seco pelo método FRAP. Apresentaram atividade antimicrobiana principalmente contra Staphylococcus aureus e Listeria monocytogenes. Além disso, tiveram grande capacidade de inibir a enzima arginase de Leishmania com porcentagem de inibição variando de 54,60 a 83,43%. Os resultados encontrados sugeriram que o processo de secagem em spray dryer com maltodextrina, dos extratos obtidos dos subprodutos da uva Bordô, produziu pós com diversas características interessantes, como baixa higroscopicidade, alta solubilidade e estabilidade, além de grande potencial biológico. Tais resultados evidenciam que este subproduto da indústria vinícola pode ser aproveitado como fonte natural de ingredientes funcionais. / The aim of this work was to produce powder pigments from grape byproducts of Bordo variety (Vitis labrusca) by spray drying using maltodextrin as carrier agent. The effects of process conditions on some physicochemical properties, stability and biological activity of the product were studied. Ethanol extracts were obtained from grape pomace (skins and seeds) and concentrated to one-third the initial volume. This extract was then mixed with the carrier agent 10 DE maltodextrin at concentrations of 10, 20 or 30% and atomized in a spray dryer, with feed flow rate of 44 mL/min and inlet drying air temperatures of 130, 150 or 170°C a total of nine tests. In addition, a sample of freeze-dried concentrated extract without carrier agent was obtained for comparison. It was evaluated process yield and the samples obtained were initially evaluated for moisture content, anthocyanins retention, hygroscopicity and solubility in water, in order to verify the influence of process conditions on these characteristics. These samples were also evaluated for morphology, particle size distribution and moisture sorption isotherms. All samples (spray-dried powders and freeze-dried extract) were evaluated for instrumental color, infrared spectroscopy, stability during storage, presence of bioactive compounds (phenols, flavonoids, anthocyanins and proanthocyanidins) plus antioxidant activity, antimicrobial activity and inhibition of Leishmania arginase. Process conditions evaluated (inlet drying air temperature and carrier agent concentration) had a strong influence on the characteristics studied. The moisture content, anthocyanin retention, morphology and particle size of the samples were strongly influenced by drying temperature and carrier agent concentration while the hygroscopicity suffered greater influence of the carrier agent concentration. The concentration of carrier agent also had great influence on the moisture sorption isotherms of the samples. There was no significant interference of the drying process on the chemical composition of the material evidenced by infrared spectroscopy. Regarding the evaluation of stability during storage, it was observed that the samples containing maltodextrin, retained much more anthocyanins and original color when compared with the sample without a carrier or liquid extracts, indicating both, the drying process and the presence of carrier, promoted a protective effect to the compounds and its color. All samples showed high levels of flavonoids, anthocyanins, proanthocyanidins and high levels of antioxidant activity ranging from 314.06 to 441.04 &micro;molTE/g of extract (dry weight), by DPPH and 993.32 to 1138.68 &micro;molTE/g of extract (dry weight) by FRAP method. Most samples showed antimicrobial activity against Staphylococcus aureus and Listeria monocytogenes. Moreover, had great ability to inhibit the enzyme arginase of Leishmania with inhibition percentage ranging from 54.60 to 83.43%. The results suggest that the drying process of Bordo grape pomace extracts in a spray dryer with maltodextrin, produced powders with various interesting characteristics such as low hygroscopicity, high solubility and stability, and large biological potential. This shows that this byproduct of wine industry can be used as a natural source of functional ingredients.