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Browsing by Autor "Alberto Giménez"

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    Active sesquiterpene lactones against <i>Leishmania amazonensis</i> and <i>Leishmania braziliensis</i>
    (Taylor & Francis, 2016) A Sosa; Susana Amaya; Efraín Salamanca; Miguel Gilabert; Alicia Bardón; Alberto Giménez; Nancy Vera; Susana Borkosky
    Seventeen sesquiterpene lactones (SLs) isolated from five species of the tribe Vernonieae were evaluated for their in vitro activity against promastigotes of Leishmania amazonensis and Leishmania braziliensis. Additionally, a quantitative structure activity relationship has been made, since all these natural compounds were found to have potent to mild antileishmanial properties. The most active compounds against L. braziliensis were 16 and 17 (IC<sub>50</sub> values 1.45 and 1.34 μM, respectively), followed by compound 15 with IC<sub>50</sub> value of 1.60 μM against L. amazonensis. The three glaucolide-type SLs (4-6) were the least active against both parasites. The computational study allowed us to establish that lipophilicity and polarisability play an important role in the antiparasitic activity. This is the first report of the known germacradiendiolides 16 and 17 from Elephantopus mollis. The activity data of the compounds 1-17 assayed against Leishmania parasites are reported here for the first time.
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    Anti-Leishmanial Lindenane Sesquiterpenes from<i>Hedyosmum angustifolium</i>
    (Thieme Medical Publishers (Germany), 2009) Lucia Acebey; Valérie Jullian; Denis Séréno; Séverine Chevalley; Yannick Estevez; Claude Moulis; Stephan Beck; Alexis Valentin; Alberto Giménez; Michel Sauvain
    The aim of this work is the isolation of anti-leishmanial compounds from the ethyl acetate extracts of the bark of HEDYOSMUM ANGUSTIFOLIUM. We have successfully isolated and characterized five sesquiterpenes: one new compound (oxyonoseriolide, 1), one compound isolated for the first time from a natural source (hedyosmone, 2), and three known sesquiterpenes (onoseriolide, 3; chloranthalactone A, 4; and spathulenol, 5) that had not been previously isolated from H. ANGUSTIFOLIUM. The biological activities of 1- 5 showed that onoseriolide ( 3) was the most active compound against axenic amastigotes from LEISHMANIA AMAZONENSIS and L. INFANTUM. Moreover, it was still active on the intramacrophagic amastigotes of L. INFANTUM. The isolated compounds have also been tested on PLASMODIUM FALCIPARUM and against various mammalian cell lines.
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    Anti-Trypanosoma activity of some natural stilbenoids and synthetic related heterocyclic compounds
    (Elsevier BV, 2001) Esther del Olmo; Marlon Garcı́a Armas; José Luis López‐Pérez; Grace Ruiz; Fernando F. Vargas; Alberto Giménez; Eric Deharo; Arturo San Feliciano
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    Antileishmanial metabolites from Lantana balansae
    (Springer Science+Business Media, 2016) Eliana M. Maldonado; Efraín Salamanca; Alberto Giménez; Olov Sterner
    Eleven compounds, 12-oxo-phytodienoic acid (1), persicogenin (2), eriodictyol 3′,4′,7-trimethyl ether (3), phytol (4), spathulenol (5), 4-hydroxycinnamic acid (6), onopordin (7), 5,8,4′-trihydroxy-7,3′-dimethoxyflavone (8), quercetin (9), jaceosidin (10), and 8-hydroxyluteolin (11), were isolated from an ethanol extract of Lantana balansae Briq., Verbenaceae, that was found to possess antileishmanial activity. The structures of the compounds were determined by NMR spectroscopy and HR mass spectrometry, and 1, 2, 3, 7, 8 and 9 were investigated for antiprotozoal activity toward promastigotes of Leishmania amazonensis and Leishmania braziliensis. Compound 1 was shown to be the most potent, with the IC50 values 2.0 μM toward L. amazonensis and 0.68 μM toward L. braziliensis, although less potent than the positive control Amphotericin B. All compounds have been reported previously, but this is the first report of the isolation of a cyclopentenone fatty acid (1) and flavanones (2 and 3) from a Lantana species.
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    Antileishmanial metabolites from Trixis antimenorrhoea
    (Elsevier BV, 2014) Eliana M. Maldonado; Efraín Salamanca; Alberto Giménez; Gloria Saavedra; Olov Sterner
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    Antimalarial activity of imidazo[2,1-a]isoindol-5-ol derivatives and related compounds
    (Elsevier BV, 2011) Esther del Olmo; Bianca Barboza; Louise Domeneghini Chiaradia; Alicia Moreno‐Sabater; Juana Carrero-Lérida; Dolores González‐Pacanowska; Victoria Muñoz; José Luis López‐Pérez; Alberto Giménez; Agustín Benito
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    Antiparasitic activity of prenylated benzoic acid derivatives from Piper species
    (Elsevier BV, 2009) Ninoska Flores; Ignacio A. Jiménez; Alberto Giménez; Grace Ruiz; David Gutiérrez; Geneviève Bourdy; Isabel L. Bazzocchi
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    Antiparasitic activity of two Brazilian plants: <i>Eugenia mattosii</i> and <i>Marlierea eugeniopsoides</i>
    (Taylor & Francis, 2020) Giovana Vechi; Adrielli Tenfen; Efraín Salamanca; Alberto Giménez; Valdir Cechinel Filho
    Parasitoses are very common throughout the world, generating serious consequences for public health. Leishmaniosis and giardiasis are examples of fairly recurrent, but neglected diseases. Several higher plants have demonstrated promising activity against the parasites. The aim of this study was to evaluate the biological activity of extracts, fractions and isolated compounds from the leaves and stems of two Brazilian plants: <i>Eugenia mattosii</i> and <i>Marlierea eugeniopsoides</i> (Myrtaceae) against <i>Leishmania</i> and <i>Giardia</i>. XTT and the fluorimetric method were used to for this evaluation, respectively. Cytotoxicity was evaluated against HeLa cells. The results demonstrated that chloroform fractions of <i>E. matosii</i> and pinostrobin presented the most pronounced antiparasitic activity, with the CLF-stems being the most effective against <i>Leishmania amazonensis</i> and <i>Leishmania braziliensis</i>. Pinostrobin also presented activity against <i>G. lamblia</i>. Therefore, <i>E. mattosii</i> stems and pinostrobin may be considered possible targets for the continuity of studies against other parasites.
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    Antiprotozoal Activity of Ethanol Extracts of Some<i>Bomarea</i>Species
    (Taylor & Francis, 2008) Fernando Álzate; Nora Jiménez; Bernard Weniger; Jaume Bastida; Alberto Giménez
    The antiprotozoal activity of 26 ethanol extracts derived from 13 species of the genus Bomarea (Alstroemeriaceae) were evaluated against the promastigote forms of three Leishmania species (L. amazonensis L., L. braziliensis Vianna, and L. donovani Laveran & Mesnil) and the epimastigote form of Trypanosoma cruzi Chagas. IC50 values for leishmanicidal activities were between 4.9 and 98.6 μ g/mL, B. setacea extracts being the most active against the three species of Leishmania. Amphotericin B (IC50 = 0.2 μ g/mL) and pentamidine (IC50 = 10 μ g/mL) were used as control in this assay. IC50 values for antitrypanosomal activities were between 65.2 and 92.7 μ g/mL, whereas the control benznidazole had an IC50 value of 2 μ g/mL.
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    Antiprotozoal and cytotoxic activities in vitro of Colombian Annonaceae
    (Elsevier BV, 2007) Edison Osorio; Gabriel Jaime Murillo Arango; Nora Jiménez; Fernando Álzate; Grace Ruiz; David Gutiérrez; Marco Antonio Paco; Alberto Giménez; Sara M. Robledo
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    Avaliação biológica de híbridos pirazolino-aminopirimidinas como protótipos com potencial antiparasitário para o tratamento da Leishmaniose
    (2025) Karla Seniuk Alferi; Efraín Salamanca; Alberto Giménez; Fátima de Campos Buzzi
    As Doenças Tropicais Negligenciadas (DTNs) compreendem um grupo de enfermidades infecciosas que afetam principalmente populações em situação de vulnerabilidade socioeconômica em regiões tropicais e subtropicais. Apesar de sua elevada prevalência e impacto na saúde global, ainda recebem investimentos limitados em pesquisa e desenvolvimento de novos fármacos, o que contribui para a escassez de terapias eficazes, seguras e acessíveis. Nesse cenário, compostos heterocíclicos surgem como alternativas promissoras, em virtude de sua versatilidade estrutural, potencial bioativo e ampla aplicabilidade farmacológica. Estudos prévios do grupo de pesquisa em Química Farmacêutica avaliaram uma série de aminopirimidinas frente a protozoários como&nbsp;Leishmania&nbsp;e&nbsp;Giardia lamblia&nbsp;que apresentaram atividade antiparasitária relevante e resultados biológicos promissores. Entre as moléculas avaliadas, as que continham os substituintes metil e dimetilamino foram as mais ativas. A partir desses resultados, e considerando os medicamentos atualmente disponíveis para o tratamento da leishmaniose, como o isotionato de pentamidina, planejaram-se novas moléculas mantendo os substituintes mais ativos, visando aprimorar sua eficácia antiparasitária e contribuir para o desenvolvimento de candidatos a fármacos mais eficazes e com menores efeitos colaterais. Assim, este estudo teve como objetivo avaliar a atividade biológica de híbridos pirazolino-aminopirimidinas sintetizados quanto ao seu potencial antiparasitário. Inicialmente, foram sintetizadas duas chalconas substituídas por meio de condensação aldólica clássica: (2E)-3-(4-metilfenil)-1-fenilprop-2-en-1-ona (CHM), obtida a partir da reação entre acetofenona (0,025 mmol) e tolualdeído (0,062 mmol) em etanol sob agitação magnética, e (2E)-3-[4-(dimetilamino)fenil]-1-fenilprop-2-en-1-ona (CHNM), obtida pela reação entre acetofenona (0,025 mmol) e dimetilaminobenzaldeído (0,062 mmol) em etanol sob agitação magnética. Após isso, as chalconas obtidas foram empregadas como precursores para a obtenção de derivados contendo o grupo carboximidamida. A chalcona CHM (2,2493 mmol) foi submetida à reação em refluxo com cloridrato de aminoguanidina (4,4986 mmol) em etanol, assim como, a chalcona CHNM (1,9894 mmol) reagiu sob as mesmas condições com cloridrato de aminoguanidina (3,9788 mmol). Os produtos obtidos foram isolados, purificados e caracterizados por RMN¹H, RMN¹³C, IV, espectrometria de massas e ponto de fusão, confirmando a formação dos compostos desejados. Posteriormente, os derivados sintetizados foram avaliados quanto à atividade antiparasitária, utilizando o método colorimétrico XTT para promastigotas de Leishmania spp. e epimastigotas de&nbsp;Trypanosoma cruzi, e o método fluorométrico com Resazurina para trofozoítos de&nbsp;Giardia lamblia, além da avaliação de citotoxicidade em macrófagos RAW. Foram obtidas duas moléculas caracterizadas como híbridos pirazolino-aminopirimidinas, a 4-(4-metilfenil)-2-[3-(fenil)-5-(4-metilfenil)-4,5-dihidro-1H-pirazol-1-il]-6-(fenil)-pirimidina (PZN-P1) com rendimento de 39% e 4-[4-(dimetilamino)-fenil]-2-[3-(fenil)-5-[4-(dimetilamino)-fenil]-4,5-dihydro-1H-pyrazol-1-il]-6-(fenil)-pirimidina (PZNM) com rendimento de 28,4%. Os resultados da avaliação biológica dos compostos demonstraram que a molécula PZN-P1 apresentou atividade moderada contra&nbsp;Leishmania amazonensis&nbsp;(CI50 = 80,2 ± 8,1 µg/mL) e Leishmania braziliensis (CI50 = 79,1 ± 1 µg/mL), enquanto PZNM não demonstrou efeito significativo (CI50 &gt; 100 µg/mL). Para Trypanosoma cruzi&nbsp;e&nbsp;Giardia lamblia, ambos os híbridos foram inativos (CI50 &gt; 100 e &gt; 200 µg/mL, respectivamente), além de apresentarem baixa citotoxicidade em macrófagos RAW (CI50 &gt; 100 µg/mL). Em comparação com as aminopirimidinas previamente avaliadas (AMM e AMNM), os compostos híbridos foram menos potentes, sugerindo que a presença do núcleo pirazolina pode reduzir a eficácia antiparasitária. Os achados indicam que os híbridos sintetizados ainda demandam otimizações estruturais, mas reforçam o potencial dos derivados heterocíclicos como protótipos para o desenvolvimento de novos agentes antiparasitários.
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    Avtividad antiplamódica in vitro e inhibición de la formación de la beta-hematina de plantas colombianas de la familia Annonaceae
    (2005) Edison Osorio; Gabriel Jaime Murillo Arango; Edison Parra; Katalina Muñoz-Durango; Grace Ruiz; David Gutiérrez; Marco Antonio Paco; Alberto Giménez
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    Benzoic Acid Derivatives from <i>Piper</i> Species and Their Antiparasitic Activity
    (American Chemical Society, 2008) Ninoska Flores; Ignacio A. Jiménez; Alberto Giménez; Grace Ruiz; David Gutiérrez; Geneviève Bourdy; Isabel L. Bazzocchi
    Piper glabratum and P. acutifolium were analyzed for their content of main secondary constituents, affording nine new benzoic acid derivatives (1, 2, 4, 5, 7, and 10-13), in addition to four known compounds (3, 6, 8, and 9). Their structures were elucidated on the basis of spectroscopic data. Riguera ester reactions and optical rotation measurements established the new compounds as racemates. In the search for antiparasitic agents, the compounds were evaluated in vitro against the promastigote forms of Leishmania spp., Trypanosoma cruzi, and Plasmodium falciparum. Among the evaluated compounds, methyl 3,4-dihydroxy-5-(3'-methyl-2'-butenyl)benzoate (7) exhibited leishmanicidal effect (IC50 13.8-18.5 microg/mL) against the three Leishmania strains used, and methyl 3,4-dihydroxy-5-(2-hydroxy-3-methylbutenyl)benzoate (1), methyl 4-hydroxy-3-(2-hydroxy-3-methyl-3-butenyl)benzoate (3), and methyl 3,4-dihydroxy-5-(3-methyl-2-butenyl) benzoate (7) showed significant trypanocidal activity, with IC50 values of 16.4, 15.6, and 18.5 microg/mL, respectively.
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    Chemical composition of essential oils of Piper jacquemontianum and Piper variabile from Guatemala and bioactivity of the dichloromethane and methanol extracts
    (Springer Science+Business Media, 2011) Sully M. Cruz; Armando Cáceres; Luis E. Álvarez; Jorge Alexander Diaz Morales; Miriam Anders Apel; Amélia Teresinha Henriques; Efraín Salamanca; Alberto Giménez; Yelkaira Vásquez; Mahabir P. Gupta
    The essential oils from two native species from Guatemala were studied for their chemical composition and the dichloromethane and methanol extracts for their biological activity. A GC-MS analysis of the essential oil from Piper jacquemontianum Kunth, Piperaceae, showed 34 constituents, consisting mainly of linalool (69.4%), while Piper variabile C. DC. essential oil had 36 constituents, camphor (28.4%), camphene (16.6%) and limonene (13.9%) being the major components. Dichloromethane extracts of both species were cytotoxic against MCF-7, H-460 and SF-268 cell lines (<7 µg/mL). Dichloromethane extract of P. jacquemontianum was slightly active against bacteria (0.5 mg/mL), was active against promastigotes of Leishmania (20.4-61.0 µg/mL), and epimastigotes of Trypanosoma cruzi (51.9 µg/mL). The methanol extract of P. variabile showed antimalarial activity against Plasmodium falciparum F32 (4.5 µg/mL), and the dichloromethane extract against Leishmania (55.8-76.3 µg/mL) and T. cruzi (45.8 µg/mL). None of the extracts from the two species was active against Aedes aegypti larvae and Artemia salina nauplii.
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    Chemical profiling and antioxidant activity of Bolivian propolis
    (Wiley, 2015) Nélida Nina; Cristina Quispe; Felipe Jiménez‐Aspee; Cristina Theoduloz; Alberto Giménez; Guillermo Schmeda‐Hirschmann
    High chemical diversity and differential antioxidant effects were found in Bolivian propolis. Our results provide additional evidence on the chemical composition and bioactivity of South American propolis.
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    DETERMINACIÓN GENOTÓXICA DEL EXTRACTO TOTAL DICLOROMETÁNICO DE CORTEZA DE GALIPEA LONGIFLORA KRAUSE, MEDIANTE EL TEST DE MUTACIÓN Y RECOMBINACIÓN SOMÁTICA (SMART)
    (Universidad Autónoma del Estado de México, 2006) Pseidy L. Mamani; Mónica Gonzales; Araceli Pillco; Alberto Giménez; Eduardo L. Gonzales
    "En el presente estudio se determinó la actividad genotóxica del extracto total diclorometánico de corteza de Evanta (Galipea longiflora Krause), mediante la Prueba de Mutación y Recombinación Somática (SMART) versión alas, que emplea a Drosophila melanogaster como organismo experimental. Larvas de tercer instar procedentes de los cruces Estándar (con bioactivación normal) y Alta bioactivación (con incremento del citocromo P-450) fueron tratadas con concentraciones de 30, 60, 125, 250 y 500 ug/mL del extracto y un control negativo, que fue el diluyente. Los resultados obtenidos mediante el estadístico de Kastenbaum-Bowman (α=0,05.), sugieren que el extracto diclorometánico de Evanta no produce daño genotóxico, a las concentraciones evaluadas mediante la prueba SMART, en las condiciones experimentales empleadas en el presente trabajo."
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    Drimanes from Drimys brasiliensis with leishmanicidal and antimalarial activity
    (Instituto Oswaldo Cruz, Ministério da Saúde, 2013) Vanessa D. Claudino; Kesia Caroline da Silva; Valdir Cechinel Filho; Rosendo A. Yunes; Franco Delle Monachè; Alberto Giménez; Efraín Salamanca; David Gutierrez-Yapu; Ângela Malheiros
    This paper evaluates CHCl3 and CH3OH extracts of the stem bark, branches and leaves of Drimys brasiliensis and drimane sesquiterpenes isolated from the stem bark against strains of Leishmania amazonensis and Leishmania braziliensis promastigotes and Plasmodium falciparum trophozoites. All of the extracts and compounds were tested in cell lines in comparison with reference standards and cell viability was determined by the XTT method. The CHCl3 and CH3OH extracts from the stem bark and branches yielded promising results against two strains of Leishmania, with 50% inhibitory concentrations (IC50 ) values ranging from 39-100 µg/mL. The CHCl3 extract of the stem bark returned IC50 values of 39 and 40.6 µg/mL for L. amazonensis and L. braziliensis, respectively. The drimanes were relatively effective: 1-β-(p-coumaroyloxy)-polygodial produced IC50 values of 5.55 and 2.52 µM for L. amazonensis and L. braziliensis, respectively, compared with 1-β-(p-methoxycinnamoyl)-polygodial, which produced respective IC50 values of 15.85 and 17.80 µM. The CHCl3 extract demonstrated activity (IC50 of 3.0 µg/mL) against P. falciparum. The IC50 values of 1-β-(p-cumaroyloxyl)-polygodial and 1-β-(p-methoxycinnamoyl)-polygodial were 1.01 and 4.87 µM, respectively, for the trophozoite strain. Therefore, the results suggest that D. brasiliensis is a promising plant from which to obtain new and effective antiparasitic agents.
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    ESTUDIOS QUÍMICOS, BIOLÓGICOS Y FARMACOLÓGICOS DE Galipea longiflora, KRAUSE
    (Universidad Autónoma del Estado de México, 2005) Alberto Giménez; J. Antonio Avila; Grace Ruiz; Magali Paz; Enrique Udaeta; Juan C. Ticona; Efraín Salamanca; Crispín Paredes; Norka Rodríguez; Katia Quints
    "La especie medicinal Galipea longiflora (Evanta) es utilizada por las etnias amazónicas: Tacana, Mosetene y Tsimane, como antiparasitario. Los alcaloides totales de esta especie vegetal serán centro de estudios clínicos como tratamiento alternativo para la leishmaniasis cutánea. Nuestros estudios detallan el aislamiento y caracterización de alcaloides quinolínicos, de la corteza y hojas, todos con actividad leishmanicida evaluada sobre promastigotes de: L. amazonensis, L. braziliensis, L. donovani y L. chagasi. Mediante modelos toxico cinéticos, se ha determinado la toxicidad aguda, subcrónica y parámetros fármaco-cinéticos, para el extracto crudo, en modelo murino. Se establecen las condiciones para el cultivo semi-continuo, in vitro, de células de Evanta."
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    Evaluación de la capacidad biocontroladora de metabólicos de Trichoderma inhamatum Bol12 QD sobre cepas nativas de Phytophthora infestans in vitro
    (Selva Andina Research Society, 2011) Ramon Puño; Enrique Terrazas; Teresa Alvares; Alberto Giménez; Laura Mendoza; Hugh Smeltekop; Manuel Gregorio Loza-Murguia
    Phytophthora infestans es un fitopatgeno causante de la disminucin del rendimiento de los cultivos del tomate, para controlar estas prdidas los agricultores utilizan productos qumicos.Esto trae consecuencias al medio ambiente, la salud humana y los organismos benficos del ecosistema.El objetivo fue obtener e identificar aislados nativos de Trichoderma spp., en suelos sembrados con tomate en Tlayacapan, Morelos (Mxico), con problemas de Alternaria solani y Phytophthora infestans; asimismo, determinar su capacidad antagnica in vitro.Trichoderma se aisl directamente del suelo por el mtodo de dilucin en placa con medio de cultivo papa-dextrosa-agar (PDA).Por otro lado se realizaron diluciones en placa del fermento de T. inhamatum Bol12 QD producido en cultivos batch durante 30 das para comparar la efectividad del biocontrolador.Los fermentos filtrados inhibieron el crecimiento cintico micelial del agente causal en laboratorio; con la dilucin 1:2 el crecimiento fue de 32,5%, para la dilucin 1:4 el crecimiento micelial fue de 69,1% y finalmente para la dilucin de 1:8 del fermento biocontrolador el micelio creci hasta un 95,2%.Para demostrar la actividad inhibitoria sobre el patgeno en campo, se produjeron cultivos de 3 L en batch durante 4 meses.La aplicacin de tres dosis (puro, dilucin 1:2 y dilucin 1:4 ms un testigo solamente agua) se realiz en un diseo de bloques completos al azar con cuatro repeticiones con el cultivo de tomate, perteneciente a la variedad Santa Cruz Kada Gigante, en las parcelas de la Unidad Acadmica Campesina-Carmen Pampa.El anlisis estadstico por el test de Duncan mostr que el fermento puro redujo la infeccin de Phytophthora infestans de manera significativa en el tomate.Apareci otro fitopatgeno del tomate, Septoria lycopersici, durante el desarrollo del trabajo de campo.Se evalu tambin el efecto de las dosis del fermento a esta enfermedad, y se not igualmente una reduccin significativa con todas las dosis del fermento.Con estos experimentos se demuestra que los fermentos de T. inhamatum Bol12 QD tienen efecto biocontrolador sobre el cultivo de tomate.La capacidad antagnica se evalu mediante el mtodo del papel celofn y la clase de antagonismo con la tcnica de cultivos duales.Los datos se sometieron a un anlisis de varianza y pruebas de Tukey.Se obtuvieron 20 aislados de Trichoderma.El rango de porcentajes de inhibicin del crecimiento micelial de los fitopatgenos por los aislados vari desde 38.8 a 81.3% en A. solani; y desde 16.3 a 85.5% en P. infestans.Se seleccionaron 10 aislados que inhibieron al menos el 65% del crecimiento, que pertenecen a las especies: T. harzianum (Thz), T. longibrachiatum (Tl) y T. koningii (Tk).Los aislados y Tk-4, seleccionados contra A. solani, presentan antagonismo clase 1, sobrecreciendo al fitopatgeno y esporulando sobre l.Los aislados THz-17, Thz-18, Tl-17, Tl-18 y Tl-19 seleccionados contra P. infestans, presentan antagonismo clase 2 y Thz19 antagonismo clase 3. Por su accin antagnica in vitro sobre P. infestans y A. solani, puede considerarse a Trichoderma como agente promisorio en el control biolgico de las enfermedades que ocasionan estos fitopatgenos
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    Evaluation of Antileishmanial Activity of Selected Brazilian Plants and Identification of the Active Principles
    (Hindawi Publishing Corporation, 2013) Valdir Cechinel Filho; Christiane Meyre‐Silva; Rivaldo Niero; Luísa Nathália Bolda Mariano; Fabiana Gomes do Nascimento; Ingrid Vicente Farias; Vanessa Fátima Gazoni; Bruna dos Santos Silva; Alberto Giménez; David Gutierrez-Yapu
    This study evaluated extracts, fractions, and isolated compounds from some selected Brazilian medicinal plants against strains of promastigotes of Leishmania amazonensis and L. brasiliensis in vitro. The cell viability was determined, comparing the results with reference standards. The dichloromethane fractions of the roots, stems, and leaves of Allamanda schottii showed IC50 values between 14.0 and 2.0 μ g/mL. Plumericin was the main active compound, with IC50 of 0.3 and 0.04 μ g/mL against the two species of Leishmania analyzed. The hexane extract of Eugenia umbelliflora fruits showed IC50 of 14.3 and 5.7 μ g/mL against L. amazonensis and L. brasiliensis, respectively. The methanolic extracts of the seeds of Garcinia achachairu and guttiferone A presented IC50 values of 35.9 and 10.4 μ g/mL, against L. amazonensis, respectively. The ethanolic extracts of the stem barks of Rapanea ferruginea and the isolated compound, myrsinoic acid B, presented activity against L. brasiliensis with IC50 of 24.1 and 6.1 μ g/mL. Chloroform fraction of Solanum sisymbriifolium exhibited IC50 of 33.8 and 20.5 μ g/mL, and cilistol A was the main active principle, with IC50 of 6.6 and 3.1 μ g/mL against L. amazonensis and L. brasiliensis, respectively. It is concluded that the analyzed plants are promising as new and effective antiparasitic agents.
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