Resumen Introducción: Los protistas del género Labyrinthula causan la denominada “Enfermedad del desgaste” en el pasto marino, Thalassia testudinum. Desde el 2008 los monitoreos en el Caribe colombiano han mostrado variación espacial y temporal en la incidencia de la enfermedad, pero sin la alta mortalidad observada en otras regiones del mundo. Objetivo: Analizar algunos parámetros epidemiológicos en T. testudinum y comparar metabolitos entre plantas sanas e infectadas. Métodos: Registramos la severidad, incidencia y prevalencia de esta enfermedad en el Parque Nacional Natural Tayrona e Isla de Providencia, y analizamos muestras de agua y sedimentos. Además, aplicamos cromatografía líquida y de gases, junto con espectrometría de masas, a extractos metanólicos de muestras de hojas y rizomas de brotes sanos e infectados. Resultados: Las praderas se encontraban en buen estado, a pesar de la escasez de brotes de fanerógamas marinas en Tayrona y una alta incidencia (15 %) y severidad (355 %) de la enfermedad en Providencia. Las plantas infectadas tenían niveles más bajos de fenoles, flavonoides y azúcares. Las flavonas sulfatadas con aglicona luteolina y diosmetina, los esteroles (sitosterol y estigmasterol) y las oxilipinas volátiles se acumularon en las hojas (3-hidroxi-2-isopentanona) y los ácidos isopentanoico y octadecatrienoico en los rizomas. Conclusiones: Estos pastos marinos colombianos tienen producción diferencial de metabolitos. Probablemente como una defensa exitosa, aún a niveles bajos de severidad (0.1 %) e incidencia (1 %) de la enfermedad.

Abstract Introduction: Protists of the genus Labyrinthula cause the so-called “Wasting Disease” in seagrass, Thalassia testudinum. Monitoring in the Colombian Caribbean since 2008 has shown spatial and temporal variation in the disease’s incidence, but without the high mortality observed in other regions of the world. Objective: To analyze some epidemiological parameters in T. testudinum and to compare metabolites between healthy and infected plants. Methods: We recorded severity, incidence and prevalence of this disease in Tayrona National Natural Park and Providencia Island, and we analyze water and sediment samples. Additionally, we applied gas and liquid chromatography, coupled with mass spectrometry, to methanolic extracts from leaf and rhizome samples of healthy and infected shoots. Results: The meadows were in good condition, despite the scarce seagrass shoots in Tayrona and a high incidence (15 %) and severity (35.5 %) of the disease in Providencia. Infected plants had lower levels of phenols, flavonoids and sugars. Sulphated flavones with aglycone luteolin and diosmetin, sterols (sitosterol and stigmasterol) and volatile oxylipins are accumulated in leaves (3-hydroxy-2-isopentanone) and isopentaenoic and octadecatrienoic acids in rhizomes. Conclusions: These Colombian seagrasses have differential production of metabolites. Probably as a successful defense, even at low levels of severity (0.1 %) and incidence (1 %) of the disease.

Resumen En el presente estudio se describe el acondicionamiento de algunos parámetros con fines de obtención eficiente de extractos apoplásticos enriquecidos en compuestos polares, principalmente fenólicos. Este flujo de trabajo descrito, incluso, puede ser aplicado a diferentes especies vegetales para ser empleado en el análisis particular o global de metabolitos en este espacio extracelular periférico. Para ello, usando raíces y tallos de clavel (Dianthus cariophyllus L), se evaluaron diferentes soluciones de infiltración para la extracción de los metabolitos apoplásticos. El mejor resultado se logró con la disolución amortiguadora NaH2PO4-Na2HPO4 0,1 M pH 6,5/NaCl 50 mM, porque se obtiene la mayor cantidad de metabolitos fenólicos apoplásticos, con la menor contaminación de compuestos intracelulares. Los metabolitos se separaron mediante HPLC-DAD-ESI-MS, obteniendo perfiles cromatográficos con parámetros de calidad razonables basados en resolución, selectividad y número de platos teóricos. Con estas condiciones, fue posible identificar ocho compuestos diferenciales (una flavona y siete flavonoles), cuyas estructuras básicas comprendían flavonoides del tipo (iso)pratol, kaempférido, (dihidro) kaempferol, quercetina y miricetina, según el órgano de prueba y la variedad. Los flavonoides identificados están relacionados con metabolitos de tipo fitoanticipina en el clavel, como hidroxi-metoxiflavona, di-o-benzoilquercetina y kaempférido disaliciloilrhamnósido, abundantemente presentes en la variedad resistente. Las condiciones descritas en este trabajo son fundamentales para profundizar en el papel de los metabolitos fenólicos apoplásticos relacionados con los mecanismos de defensa de esta planta ornamental.

Abstract The present study outlines the conditioning of various parameters for the efficient removal of the apoplastic fraction of carnation enriched in polar compounds, mainly phenolics. Several studies can apply the described workflow to different plant species in the particular or global analysis of those metabolites in this peripheral extracellular space. Hence, using carnation (Dianthus caryophyllus L) roots and stems, we evaluated different infiltration solutions for removing apoplastic metabolites. The best outcome was obtained by using the buffer solution NaH2PO4-Na2HPO4 0.1 M pH 6.5/NaCl 50 mM, since the highest amount of apoplastic phenolic metabolites can be obtained with the slightest contamination of intracellular compounds. The metabolites were separated using HPLC-DAD-ESI-MS, affording chromatographic profiles with reasonable quality parameters based on resolution, selectivity, and number of theoretical plates. It was possible to identify eight differential compounds (one flavone and seven flavonols), whose core moieties consisted of (iso)pratol, kaempferide, (dihydro)kaempferol, quercetin, and myricetin-type flavonoids according to the test organ and the cultivar. We deduced that identified flavonoids are related to phytoanticipin-type metabolites in carnation, such as hydroxy-methoxyflavone, di-o-benzoylquercetin, and kaempferide disalicyloylrhamnoside, which are abundantly present in the resistant cultivar. The conditions described in this work are fundamental for delving into the role of apoplastic phenolic metabolites related to the defense mechanisms of this ornamental plant.

Resumo O presente estudo descreve o condicionamento de alguns parâmetros para a obtenção eficiente de extratos apoplásticos enriquecidos em compostos polares, principalmente fenólicos. Este fluxo de trabalho descrito pode até mesmo ser aplicado a diferentes espécies de plantas para serem usadas na análise particular ou global de metabólitos neste espaço extracelular periférico. Para isso, utilizando raízes e caules de craveiro (Dianthus cariophyllus L), diferentes soluções de infiltração foram avaliadas para a extração de metabólitos apoplásticos. O melhor resultado foi obtido com a solução tampão NaH2PO4-Na2HPO40 0.1 M pH 6.5/NaCl 50 mM, pois a maior quantidade de metabólitos fenólicos apoplásticos é extraída. Os metabólitos foram separados por HPLC-DAD-ESI-MS, obtendo-se perfis cromatográficos com parâmetros de qualidade razoáveis baseados na resolução, seletividade e número de pratos teóricos. Nessas condições, foi possível identificar oito compostos diferenciais (uma flavona e sete flavonóis), cujas estruturas básicas compreendem flavonóides do tipo (iso) pratol, kaempferida, (dihidro)kaempferol, quercetina e miricetina, de acordo com o órgão e a variedade de craveiro utilizado. Os flavonóides identificados estão relacionados a metabólitos do tipo fitoanticipinas no craveiro, como hidroxi-metoxiflavona, di-O-benzoilquercetina e kaempférido disaliciloilramnósido, abundantemente ocorridos na cultivar resistente. As condições descritas neste trabalho são essenciais para se aprofundar no papel dos metabólitos fenólicos apoplásticos relacionados aos mecanismos de defesa dessa planta ornamental.

Resumo A murcha vascular causada por Fusarium oxysporum f. sp. Dianthi (Fod) é a doença mais relevante para o cultivo de cravo. Compreender os mecanismos bioquímicos envolvidos na resistência ao Fod permitirá o desenvolvimento de novas estratégias de controle de doenças. Nesta pesquisa, os níveis de alguns fitohormônios como ácido salicílico (SA), salicilato de metil (MeSA) e jasmonato de metil (MeJA) foram avaliados em simplastos de raízes de cravo infectadas com este patógeno. O acúmulo desses hormônios foi então correlacionado com os níveis de expressão das peroxidases simplásticas, enzimas envolvidas na resistência da planta ao patógeno durante a interação. Nossos resultados sugeriram que a infecção do patógeno causa um acúmulo diferencial de SA, MeSA e MeJA em um cultivar resistente (‘Golem’), sendo mais precoce e superior do que o observado em um suscetível (‘Solex’). Simultaneamente, um aumento da atividade enzimática da peroxidase de guaiacol (GPX) e os níveis de transcrição de um gene que codifica para uma peroxidase simplástica foram apresentados como parte da resposta de resistência. A correlação estatística positiva entre o acúmulo de SA e MeJA e a expressão de peroxidases (atividade GPX e níveis de mRNA) indica a possível relação celular desses fenômenos durante a ativação da resistência ao Fod. Nossos resultados sugeriram alguns mecanismos de sinalização hormonal atuando nas raízes durante a regulação da resposta bioquímica associada à resistência contra Fod .

Abstract The vascular wilting caused by Fusarium oxysporum f. sp. dianthi (Fod) is the most relevant disease for carnation cultivation. Understanding the biochemical mechanisms involved in resistance to Fod will allow the development of new disease control strategies. In this research, the levels of some phytohormones such as salicylic acid (SA), methyl salicylate (MeSA), and methyl jasmonate (MeJA) were evaluated in symplast of carnation roots infected with this pathogen. The accumulation of these hormones was then correlated with the expression levels of symplastic peroxidases, enzymes involved in the plant resistance against pathogen during interaction. Our results suggested that pathogen infection causes a differential accumulation of SA, MeSA, and MeJA in a resistant cultivar (i.e. ‘Golem’), being earlier and higher than that observed in a susceptible one (i.e. ‘Solex’). Simultaneously, an increase of guaiacol peroxidase enzymatic activity (GPX) and transcriptional levels of a gene coding for a symplastic peroxidase were presented as part of the resistance response. The positive statistical correlation between the accumulation of SA and MeJA and the expression of peroxidases (GPX activity and mRNA levels) indicates the possible cellular relationship of these phenomena during the activation of the resistance to Fod. Our findings suggested some hormonal signaling mechanisms acting at the roots during the regulation of the biochemical response associated with resistance against Fod.

Control of fungal pathogens is mainly addressed by the use of chemically synthesized fungicides which result in environmental pollution, developing resistance after prolonged use. In this context, endophytes have been recognized as potential biocontrollers, and also as a promising source of antifungal metabolites. Therefore, as part of our research on phytopathogen controllers, 355 fungal endophytes were isolated from Protium heptaphyllum and Trattinnickia rhoifolia (Burseraceae), both ethnobotanically important tree species that produce secondary metabolites of agronomic and industrial interest. Endophytes were tested by in vitro dual culture against Fusarium oxysporum, a phytopathogen of agronomic importance. Five endophytes exerted at least 40% inhibition on F. oxysporum growth. Ethyl acetate (EtOAc) extracts were obtained from the most active antagonistic fungi, after growing them in three different liquid media. The extracts were tested against a conidial suspension of F. oxysporum by direct bioautography. Two extracts derived from fungi identified as Chaetomium globosum, F211JJMNG and Meyerozima sp. F281.UMNG showed inhibition of pathogen growth. Isolate C. globosum, F211JJMNG was selected for a chemical analysis by RP-HPLC-DAD-ESI-MS and antifungal molecules such as cladosporin, chaetoatrosin A and chaetoviridin A were annotated and identified based on their MS data.

El control de patógenos fúngicos se basa principalmente en el uso de fungicidas de síntesis química, los que pueden dar lugar a la contaminación del medio ambiente y el desarrollo de resistencia después de un uso prolongado. En este contexto, los endófitos han sido reconocidos como potenciales biocontroladores y también como fuentes prometedoras de metabolitos secundarios antifúngicos. En el marco de nuestra investigación sobre controladores de fitopatógenos, se aislaron 355 hongos endófitos de Protium heptaphyllum y Trattinnickia rhoifolia (Burseraceae), especies arbóreas de valor etnobotánico que producen metabolitos secundarios de interés agronómico e industrial. Los endófitos fueron evaluados in vitro en cultivos duales frente a Fusarium oxysporum, un fitopatógeno de importancia agronómica. Cinco endófitos mostraron al menos un 40% de inhibición en el crecimiento de F. oxysporum. Una vez determinados los hongos más activos, estos se cultivaron en 3 medios líquidos diferentes y a partir de ellos se preparó una serie de extractos solubles en acetato de etilo. Los extractos fueron probados contra una suspensión de conidios de F. oxysporum por bioautografía directa. Dos extractos derivados de los hongos identificados como Chaetomium globosum (F211.UMNG) y Meyerozima sp. (F281JJMNG) mostraron inhibición del crecimiento del patógeno. En el extracto derivado del hongo C. globosum se anotaron e identificaron los compuestos antifúngicos cladosporina, chaetoatrosina A y chaetoviridina A mediante el análisis por RP-HPLC-DAD-ESI-MS.

Phenolic lipids are a series of natural origin compounds which are produced, among others, by species of the family Poaceae, such as barley (Hordeum vulgare L.). Such compounds have been described with significant antimicrobial properties. Therefore, as part of a program for the search for antifungal compounds, an acetone extract and depurated fractions were obtained from grain flour of barley (andina variety) and tested in-vitro against Furarium oxysporum. The acetone extract showed high alkylrecorcinols content compared to previous works, whose chromatographic profile led to identify at least eight major alkylresorcinols. The purification of the extract (monitored with specific revealer) led to obtain three alkylrecorcinol-enriched fractions. Both the crude extract and the purified fractions showed antifungal activity at different levels, with a dose-dependent response. Thus the treatments showed ED50 values were between 3,3-24,0 μg mL-1. However, enriched fractions showed greater activity to that of crude extract, indicating that the direct effect of alkylresorcinols on the phytopathogen is representative to inhibit their growth. All of the above mentioned facts suggest these compounds as good candidates for controlling this phytopathogen

Los lípidos fenólicos son una serie de compuestos de origen natural que son producidos, entre otros, por especies de la familia Poaceae, como es el caso de la cebada (Hordeum vulgare L.). Tales compuestos se han descrito en algunos trabajos con propiedades antimicrobianas importantes. Por tanto, como parte de un programa de búsqueda de compuestos anti fúngicos, se realizó la evaluación de la actividad in-vitro contra Furarium oxysporum del extracto en acetona y de tres fracciones depuradas, obtenidas a partir de la harina de granos de la variedad andina de cebada. En comparación con trabajos previos, el extracto en acetona presentó contenidos más altos de alquilresorcinoles, cuyo perfil cromatográfico permitió identificar al menos ocho alquilresorcinoles mayoritarios. La depuración del extracto bajo monitoreo con revelador específico, llevó a la obtención de tres fracciones enriquecidas en alquilresorcinoles. Tanto el extracto crudo como las fracciones depuradas mostraron actividad anti fúngica a diferentes niveles, con respuesta dependiente de la dosis. Así, los valores de ED50 de tales tratamientos estuvieron entre 3,3-24,0 μg mL-1. Las fracciones enriquecidas mostraron mayor actividad, indicando que el efecto directo de los alquilresorcinoles sobre el fitopatógeno es representativo para inhibir su crecimiento. Todo lo anterior sugiere a estos compuestos como buenos candidatos para ser estudiados en trabajos futuros en el control de este fitopatógeno

The calyxes of Hibiscus sabdariffa are used in traditional medicine around the world. However, quality assurance protocols and chemical variability have not been previously analyzed. In the present study, chemical characterization of a set of samples of H. sabdariffa calyxes commercialized in Colombia was accomplished with the aim to explore the chemical variability among them. Chemometrics-based analyses on the data obtained from the HPLC-UV-DAD-derived profiles were then performed. Thus, the pre-processed single-wavelength data were subjected to principal component analysis (PCA). The PCA-derived results evidenced different groups which were well-correlated to the corresponding total phenolic and total anthocyanin contents. Multi-wavelength chromatographic (HPLC-UV-DAD surfaces) data were additionally examined via parallel factor analysis (PARAFAC) as data reduction method and the obtained loadings were subsequently submitted to PCA and orthogonal partial least squares discriminant analysis (OPLS-DA). Results were thus consistent with those from single-wavelength data. PCA loadings were employed to determine those chemical components responsible for the data variance and OPLS-DA model, constructed from PARAFAC loadings, and indicated differentiation according total anthocyanin contents among samples. The present chemometric analysis therefore demonstrated to be an excellent tool for differentiation of H. sabdariffacalyxes according to their chemical composition.

Las infecciones causadas por hongos continúan siendo un problema de salud pública en la actualidad. De hecho, existen diversos programas para el descubrimiento de fármacos enfocados en la búsqueda de estructuras plantilla. El mapeo virtual junto con docking molecular constituye una alternativa importante para encontrar potenciales estructuras promisorias. Mediante herramientas de docking molecular se pueden definir nuevos blancos terapéuticos para combatir diversas infecciones. Por tanto, se llevó a cabo el estudio del acoplamiento molecular a treinta y dos compuestos de origen natural, empleando la N-miristoil transferasa (NMT) como blanco enzimático antifúngico. De los compuestos ensayados, alcaloides, flavonoides, xantonas y quinonas mostraron interacción media más fuerte con la NMT que los terpenos, cumarinas y fenólicos. Particularmente, la afinidad encontrada para un alcaloide aporfínico, un flavonoide prenilado y dos xantonas resultó comparable con la encontrada para un inhibidor sintético reportado. En el presente trabajo se demostraron varias interacciones tanto hidrofóbicas como hidrofílicas mediante diversas herramientas computacionales. Los resultados encontrados permiten establecer tres posibles estructuras promisorias para el desarrollo de fármacos antifúngicos, aunque se requiere aún de estudios de relación estructura-actividad.

Fungal infections currently remain as a common problem in public health. Actually, drug discovery programs are oriented to the searching for lead structures. Virtual screening and molecular docking constitute great alternatives in order to find hit compounds. Novel infection targets can also be defined and employed together with molecular docking tools in drug discovery programs. Thus, thirty-two natural compounds were docked within the active site of N-myristoyl transferase (NMT) as antifungal enzyme target. From tested compounds, alkaloids, flavonoids, xanthones, and quinones exhibited strongest mean interaction with NMT than terpenoids, coumarins and phenolics. Particularly, affinities for one aporphine alkaloid, a prenylated flavonoid and two xanthones resulted to be comparable with that of previously reported synthetic inhibitor. Several hydrophobic and polar contacts were demonstrated by comparing different computational tools. The present results let to establish three possible lead structures to develop antifungal drugs although subsequent SAR analyses are still required.

Introduction: Lauraceae plants are considered as important sources of bioactive substances, as those acting as insecticides. As part of our program for bioprospecting studies on Colombian Lauraceae plants, seven medicinal species belonging to this family were studied for their acaricide activity against Dermatophagoides farinae and Blomia tropicalis, considered public health problems at domiciliary level. Objective: to evaluate acaricide activity of ethanol extracts from Lauraceae plants on domiciliary mites Dermatophagoides farinae and Blomia tropicalis as well as to characterize ethanol-soluble extracts by preliminary phytochemical assay. Methods: in vitro acaricide activity of extracts from seven plants belonging to the Lauraceae family, harvested in different regions of Colombia, was assessed on individual adults through direct contact test and fumigant action. Each plant extract was tested for chemical characterization by means of coloration and precipitation tests. Results: in direct contact bioassay, the leaf extract from Persea caerulea eliminated 100 % of Dermatophagoides farinae. In fumigant action bioassay, the leaf extract of Persea caerulea eliminated 100 % Dermatophagoides farinae and 83.37 % of Blomia tropicalis (after 120 minutes exposure at 0.1 mg/mL). The preliminary phytochemical testing identified the possible presence of metabolites according to the Lauraceae chemotaxonomy. Conclusions: obtained results indicated that Lauraceae plants could be catalogued as a source of potential biocontrol agents against specific domiciliary mites Dermatophagoides farinae and Blomia tropicalis.

Introducción: especies de la familia Lauraceae son fuentes importantes de sustancias bioactivas, como las que actúan de insecticidas. En los estudios de bioprospección de lauraceas colombianas, a siete especies medicinales pertenecientes a esta familia se les evaluó su actividad acaricida frente a Dermatophagoides farinae y Blomia tropicalis, considerados como un problema en salud pública a nivel intradomiciliario. Objetivo: determinar la actividad acaricida de los extractos etanólicos de las especies de Lauraceae sobre los ácaros intradomiciliarios Dermatophagoides farinae y Blomia tropicalis, así como caracterizar los extractos obtenidos mediante ensayo fitoquímico preliminar. Métodos: la actividad acaricida in vitro de los extractos de las siete especies, colectadas en diferentes regiones de Colombia, se evaluó sobre individuos adultos a través de las pruebas de contacto directo y acción fumigante. Cada uno de los extractos se caracterizó químicamente mediante ensayos de coloración o precipitación. Resultados: en la prueba de contacto, el extracto de hojas de Persea caerulea eliminó al 100 % de Dermatophagoides farinae. En la prueba de acción fumigante, el extracto de hojas de Persea caerulea, eliminó 100 % de Dermatophagoides farinae y 83,4 % de Blomia tropicalis (después de 120 min de exposición; a 0,1 mg/mL). El ensayo fitoquímico preliminar permitió identificar la posible presencia de metabolitos acorde con la quimiotaxonomía de las Lauraceae. Conclusiones: los resultados permiten sugerir que especies de la familia Lauraceae serían catalogados como fuente potencial de biocontroladores contra los ácaros domiciliarios Dermatophagoides farinae y Blomia tropicalis.

Os efeitos anti-inflamatórios in vitro de sete conhecidos lignanos e uma dihidrocalcona isolados das folhas de duas espécies da família Lauraceae (Pleurothyrium cinereum e Ocotea macrophylla) foram avaliados por meio da inibição da COX1, COX-2, 5-LOX e agregação de plaquetas de coelhos induzida por PAF, AA e ADP. A (+)-4"-O-metilmagnolina-4 foi encontrada como mais potente inibidora tanto da COX-2 quanto de 5-LOX e antagonista de PAF (COX-2 IC50 2,27 µM; 5- LOX IC50 5,05 µM; PAF IC50 2,51 µM). Entretanto, todos compostos mostram uma atividade em intensidades diferentes, indicando boas propriedades anti-inflamátorias a serem consideradas para futuros estudos de modificações e otimização estruturais.

The in vitro anti-inflammatory effects of seven known lignans and one dihydrochalcone isolated from the leaves of two Lauraceae species (Pleurothyrium cinereum and Ocotea macrophylla), were evaluated through the inhibition of COX-1, COX-2, 5-LOX and the aggregation of rabbit platelets induced by PAF, AA and ADP. (+)-de-4"-O--methylmagnolin 4 was found to be a potent COX-2/5-LOX dual inhibitor and PAF-antagonist (COX-2 IC50 2.27 µM; 5-LOX IC50 5.05 µM; PAF IC50 2.51 µM). However, all compounds exhibited an activity at different levels, indicating good anti-inflammatory properties to be considered in further structural optimization studies.

The antibacterial potential of 14 compounds obtained from three native Colombian species( [Pleurothyrium cinereum [van der Werff], Esenbeckia alata [Karst & Triana], Reputia heptaphylla [Pittier]) was assessed by agar diffusion method versus four bacterial species: Enterococcus faecalis 29212, Staphylococcus aureus 6539, Escherichia coli 25922 and Salmonella tiphymurium 14028s. The assessed compounds showed activity versus strains at different levels, maintaining a trend and selectivity according the base nucleus. The 4-methoxi-1-methyl-quinolin-2-(1H) alkaloid, other (8) was the compound with the highest activity.

El potencial antibacteriano de 14 compuestos obtenidos de 3 especies nativas colombianas (Pleurothyrium cinereum [van der Werff], Esenbeckia alata [Karst & Triana], y Raputia heptaphylla [Pittier]) fue evaluado mediante la inhibición del crecimiento bacteriano por el método de difusión en agar contra 4 cepas bacterianas: Enterococcus faecalis 29212, Staphylococcus aureus 6539, Escherichia coli 25922 y Salmonella tiphymurium 14028s. Los compuestos evaluados mostraron actividad frente a las cepas a diferentes niveles, observando una tendencia y selectividad según el núcleo base. El alcaloide 4-metoxi-1-metil-quinolin-2-(1H)-ona (8) fue el compuesto que presentó la mayor actividad.

Introduction: the Z. fagara species having multiple ethnobotanical uses, and a variety of secondary metabolites becomes a promising object of study at phytochemical and/or pharmacological settings. Objectives: to detect the possible presence of certain groups of secondary metabolites by means of a preliminary phytochemical analysis and to evaluate the antioxidant, anti-inflammatory and antiproliferative activities of the ethanolic extract from Zanthoxylum fagara (L.) Sarg. (Rutaceae)bark. Methods: the bark extract underwent preliminary phytochemical analysis using tests to evaluate antioxidant action (DPPH, TBARS test and FeSO4-induced peroxidation), anti-inflammatory activity (using mouse ear edema induced by acetate 12-O-tetradecanoylphorbol, TPA) and antiproliferative property (in treating tumor cells, sulphorodamine B protein (SRB) in microculture assay was used in addition to measuring cell viability and growth). Results: alkaloids, flavonoids, tannins and terpenes were found in the extract. The antioxidant activity at 10, 100 and 1000 ppm concentrations, exhibited inhibition percentages of 14.9; 84.5 and 92.5 % respectively [compared to DPPH]; 92.8 % (1 000 ppm) [TBARS test], and 4.2; 47.1; and 93.9 %, respectively, in the FeSO4-induced peroxidation. The anti-inflammatory activity showed inhibition percentage of 45.3 %, and in the case of anti-proliferation, the extract was moderately active against cancer cell lines K562, being the inhibition percentage equals to 55.5 %. In the other tested lines (U251, PC-3, HCT-15, MCF-7, and Skule) the inhibition percentage was lower than 50 %. Conclusions: the preliminary phytochemical testing showed the presence of alkaloids, flavonoids, tannins and terpenes. Antioxidant and anti-inflammatory properties were observed at above 100 ppm extract concentrations, whereas the antiproliferative activity was moderately effective against leukemia cancer cell lines K562.

Introducción: la especie Z. fagara, que presenta múltiples usos etnobotánicos y diversidad de metabolitos secundarios, se convierte en objeto de estudio promisorio a nivel fitoquímico y(o) farmacológico. Objetivo: detectar la posible presencia de ciertos grupos de metabolitos secundarios mediante análisis fitoquímico preliminar y evaluar la actividad antioxidante, antiinflamatoria y antiproliferativa del extracto etanólico de corteza de Zanthoxylum fagara (L.) Sarg. (Rutaceae). Métodos: el extracto de corteza se sometió a un análisis fitoquímico preliminar, evaluándose mediante ensayos de actividad antioxidante (DPPH, TBARS y peroxidación inducida con FeSO4), antiinflamatoria (edema de oreja de ratón inducido con TPA) y antiproliferativa (se trataron células tumorales, y se usó proteína sulforrodamina B [SRB] en ensayo de microcultivo, se midió viabilidad y crecimiento celular). Resultados: en el extracto se detectó la presencia de alcaloides, flavonoides, taninos y terpenos, principalmente. La actividad antioxidante, a concentraciones de 10, 100 y 1 000 ppm, exhibió porcentajes de inhibición de 14,9; 84,5 y 92,5 %, respectivamente (frente al DPPH); de 92,8 % (a 1 000 ppm) (prueba TBARS), y de 4,2; 47,1 y 93,9 %, respectivamente, en la peroxidación inducida con FeSO4. La actividad antiinflamatoria mostró 45,3 %, y en el caso de la antiproliferación fue moderadamente activo contra las líneas celulares cancerosas K562, con valor de 55,5 %. En otras líneas evaluadas (U251, PC-3, HCT-15, MCF-7, y SKUL) el porcentaje fue inferior a 50 %. Conclusiones: se evidenció la presencia de alcaloides, flavonoides, taninos y terpenos. La capacidad antioxidante y antiinflamatoria fue representativa a concentraciones superiores a 100 ppm, mientras que la actividad antiproliferativa fue moderadamente efectiva contra líneas de células cancerosas leucémicas K562.