Antileishmanial Activity and In Silico Molecular Docking Studies of Malachra alceifolia Jacq. Fractions against Leishmania mexicana Amastigotes.

Malachra alceifolia Jacq. (family Malvaceae), known as "malva," is a medicinal plant used as a traditional therapy in many regions of America, Africa and Asia. Traditionally, this plant is used in the form of extracts, powder and paste by populations for treating fever, stomachache, inflammation, and parasites. However, the ethnopharmacological validation of M. alceifolia has been scarcely researched. This study showed that the chloroform fraction (MA-IC) and subfraction (MA-24F) of the leaves of M. alceifolia exhibited a potential antileishmanial activity against axenic amastigotes of Leishmania mexicana pifanoi (MHOM/VE/60/Ltrod) and had high and moderate cytotoxic effects on the viability and morphology of macrophages RAW 264.7. This study reports, for the first time, possible terpenoid metabolites and derivatives present in M. alceifolia with activity against some biosynthetic pathways in L. mexicana amastigotes. The compounds from the subfractions MA-24F were highly active and were analyzed by gas chromatography-mass spectrometry (GC-MS) and by a molecular docking study in L. mexicana target protein. This study demonstrates the potential modes of interaction and the theoretical affinity energy of the metabolites episwertenol, α-amyrin and methyl commate A, which are present in the active fraction MA-24F, at allosteric sites of the pyruvate kinase, glyceraldehyde-3-phosphate dehydrogenase, triose phosphate isomerase, aldolase, phosphoglucose isomerase, transketolase, arginase and cysteine peptidases A, target proteins in some vital biosynthetic pathways were responsible for the survival of L. mexicana. Some phytoconstituents of M. alceifolia can be used for the search for potential new drugs and molecular targets for treating leishmaniases and infectious diseases. Furthermore, contributions to research and the validation and conservation of traditional knowledge of medicinal plants are needed globally.

An Overview of Genus Malachra L.-Ethnobotany, Phytochemistry, and Pharmacological Activity.

The genus Malachra L. belongs to the family Malvaceae. It includes herbs or subshrubs of nine accepted species with approximately thirty synonyms, and it has been widely used in community folk medicine to treat health problems including inflammation, nasal obstruction, leishmaniasis, malaria, childbirth, kidney disorders, fever, respiratory tract diseases, among others. From the genus Malachra L., flavonoids, steroids, triterpenes, anthocyanins, leucoanthocyanins, saponins, carbohydrates, phenols, glycosides, and alkaloids have been isolated and identified. Some pharmacological reports have indicated that the genus has antidiarrheal, antiepileptic, antiulcerogenic, antioxidant, anticonvulsant, antiviral, anticancer, antibacterial, anthelmintic, and hepatoprotective properties. However, there have been limited studies of bioactive molecules with pharmacological and biological activities associated with Malachra alceifolia Jacq., Malachra capitata (L.) L., Malachra fasciata Jacq., Malachra radiata (L.) L., Malachra ruderalis Gürke., Malachra rudis Benth., Malachra helodes Mart., Malachra urens Poit. ex Ledeb. & Alderstam., and Malachra officinalis Klotzsch. In this review, we consider the conservation of these species to save the ancestral knowledge of their traditional use in populations, and their pharmacological potential for future studies in search of alternatives for solutions to diseases in humans and animals and tools for the design and search of potential bioactive compounds against infectious and non-infectious agents.

In vivo evaluation of the toxic activity and genotoxicity of the Hymenaea courbaril L.'s resin in Drosophila melanogaster.

Due to the negative consequences carried by the usage of synthetic insecticides, a global interest into finding substitutes for these chemical compounds through natural products has arisen. When yielded to external attacks, plants generally produce metabolites to defend themselves. The physicochemical characteristics of this kind of compounds have allowed their usage as potential bioinsecticides. The Hymenaea courbaril L. (algarrobo) has proven to be a plant rich in metabolites with outstanding biological activity, in such a way that some of its extracts have been tested as insecticides. The goal of this study was to know the phytochemical composition of Hymenaea courbaril L.'s resin and perform evaluations in vivo of its toxic and genotoxic effects in the biological model Drosophila melanogaster. For this, two resin extracts were prepared and both a phytochemical analysis were carried out on them, having found in the ethanolic total extract the presence of terpenes, flavonoids and coumarins, while in the partial ethanolic extract only presence of terpenes and flavonoids was found. Drosophila larvae were submitted to different concentrations of the extracts and both the survival and the sexual ratio were evaluated, finding that larvae are more sensitive to the partial ethanolic extract. Subsequently, the induction of somatic mutation and mitotic recombination (SMART) was evaluated in the flies' eyes. The most significant affectations at a genotoxic level were found when larvae were tested with the partial extract, indicating that possibly the coumarins absence makes this insect more susceptible to damages at a genetic material level.

Homology Modeling of Leishmanolysin (gp63) from Leishmania panamensis and Molecular Docking of Flavonoids.

Leishmaniasis is a chronic disease caused by protozoa of the distinct Leishmania genus transmitted by sandflies of the genus Phlebotomus (old world) and Lutzomyia (new world). Among the molecular factors that contribute to the virulence and pathogenesis of Leishmania are metalloproteases, e.g., glycoprotein 63 (gp63), also known as leishmanolysin or major surface protease (MSP). This protease is a zinc-dependent metalloprotease that is found on the surface of the parasite, abundant in Leishmania promastigote and amastigote. This study describes the prediction of three-dimensional (3D) structures of leishmanolysin (UniProt ID A0A088RJX7) of Leishmania panamensis employing a homology modeling approach. The 3D structure prediction was performed using the SWISS-MODEL web server. The tools PROCHECK, Molprobyty, and Verify3D were used to check the quality of the model, indicating that they are reliable. Best docking configurations were identified applying AutoDock Vina in PyRx 0.8 to obtain a potential antileishmanial activity. Biflavonoids such as lanaroflavone, podocarpusflavone A, amentoflavone, and podocarpusflavone B showed good scores among these molecules. Lanaroflavone appears to be the most suitable compound from binding affinity calculations.

Antibacterial activity of Cordia dentata Poir, Heliotropium indicum Linn and Momordica charantia Linn from the Northern Colombian Coast / Actividad antibacterial de Cordia dentata Poir, Heliotropium indicum Linn y Momordica charantia Linn de la costa norte de Colombia

SUMMARY Cordia dendata Poir, Heliotropium indicum Linn and Momordica charantia Linn are used for treatment of the most common human diseases and health disorders in folk medicine of the population from the northern Colombian coast. In this study, chemical composition and antibacterial activity of the ethanol extract and fractions from C. dentata, H. indicum and M. charantia were investigated. The chemical constituents of qualitative detection were examined by Thin Layer Chromatography (TLC). The antibacterial activity was determined by agar gel diffusion and broth microdilution method. The main identified compounds were flavonoids, cardiac glycosides, alkaloids, saponins, terpenoids, tannins and coumarins. The minimal inhibitory concentration (MIC) was 31.25 to 1000 µg /mL for Gram-positive and Gram-negative bacteria, respectively. These results indicated that ethanol extract and fractions from C. dentata, H. indicum and M. charantia significantly inhibited the growth of standard strains. Potent antibacterial activities of C. dentata, H. indicum and M. charantia may be considered in future study, particularly against antibiotic-resistant cases.

RESUMEN Cordia dendata Poir, Heliotropium indicum Linn y Momordica charantia Linn son usadas para el tratamiento de las enfermedades más comunes y trastornos de salud en la medicina popular de la población de la costa norte de Colombia. En este estudio se investigó la composición química y la actividad antibacterial de los extractos etanólicos y fracciones de C. dentata, H. indicum y M. charantia. Los constituyentes químicos se examinaron por detección cualitativa cromatografía de capa fina (TLC, por sus siglas en inglés). La actividad antibacterial se determinó por difusión en agar y microdilución en caldo. Los mayores compuestos identificados fueron flavonoides, glucósidos cardiotónicos, alcaloides, saponinas, terpenoides, taninos y cumarinas. La concentración inhibitoria mínima (MIC, por sus siglas en inglés) fue de 31,25 a 1000 /µg/mL para bacterias Gram-positivas y Gram-negativas, respectivamente. Estos resultados indican que el extracto etanólico y las fracciones de C. dentata, H. indicum y M. charantia inhibieron de manera significa el crecimiento de las cepas estándar. La potente actividad antibacterial de C. dentata, H. indicum y M. charantia puede considerarse en posteriores estudios, en particular frente a casos de antibióticos resistentes.

Validación de una metodología analítica USP por HPLC para la cuantificación de warfarina sódica en tabletas / Validation of an analytical HPLC method for the quantification of warfarin sodium in tablets

La metodología analítica para la cuantificación de warfarina sódica en tabletas de 5 mg fue estandarizada y validada mediante cromatografía líquida de alta eficiencia acoplada a detector de arreglo de diodo (HPLC-DAD). Se usó como fase móvil una mezcla compuesta por MeOH-AcOH-H2O (68:1:32), una columna cromatográfica C8e Phenomenex® de 150 x 4,6 mm y tamaño de partícula de 5 μm. Los resultados analíticos muestran que el método es preciso, exacto y selectivo para este fármaco. La curva de calibración se realizó en un intervalo del 80 al 120%, en una concentración nominal de 0,1mg/mL, demostrando ser lineal con un coeficiente de correlación a r²> 0,990; el porcentaje de recuperación fue de 98,1% ± 1,3, la precisión medida a través de la repetibilidad y la precisión intermedia fue adecuada (%RSD<2). En la prueba de disolución se encontró un porcentaje de 92,3% ± 3.0. Por lo tanto, la metodología desarrollada cumple con las especificaciones establecida por la USP 38/ NF33.

The analytic methodology for the quantification of sodium warfarin tablets of 5 mg was standardized and validated by High Efficiency Liquid Chromatography coupled to Diode Array Detector (HPLC-DAD). A mixture of MeOH-AcOH-H2O (68:1:32) was used like mobil phase, a chromatographic column C8e Phenomenex® of 150x4.6 mm and a particle size of 5 μm. The analytic results show that the method is precise, accurate and selective for this drug. The calibration curve was performed in the range of 80 to 120% at a nominal concentration of 0.1 mg/mL, demonstrating to be linear with a correlation coefficient at r²> 0.990; recovery rate was 98.1% ± 1.3 and the precision measured through repeatability and intermediate accuracy was adequate (% RSD <2). A percent of 92.3% ± 3.0 was found in dissolution test, thus, the methodology developed complies with the specifications established by USP 38/NF33.

Perfil fitoquímico, actividad anti-Leishmania, hemolítica y toxicológica de Cordia dentata Poir. y Heliotropium indicum L. / Phytochemical profile and antileishmanial, hemolytic and toxicological activity of Cordia dentata Poir. and Heliotropium indicum L.

Introducción: la leishmaniasis constituye un grave problema de salud pública a nivel mundial. En Colombia, la forma clínica cutánea tiene la mayor incidencia y es causada principalmente por especies de Leishmania (Viannia) panamensis. Dado que los tratamientos disponibles para esta enfermedad resultan ineficaces, es necesaria la búsqueda de nuevos agentes terapéuticos en especies vegetales utilizadas por la medicina popular. Objetivo: evaluar el perfil fitoquímico, la actividad hemolítica, citotóxica y anti-Leishmania in vitro de extractos y fracciones provenientes de hojas de Cordia dentata y Heliotropium indicum. Métodos: al extracto etanólico total y fracciones obtenidas de hojas de C. dentata y H. indicum, se les realizó perfil fitoquímico, determinación de actividad hemolítica, efecto tóxico en larvas de Artemia salina y sobre la línea celular promonocítica humana U937 (CRL-1593.2™), así como también, la actividad anti-Leishmania sobre amastigotes intracelulares de L. (V.) panamensis (MHOM/CO/87/UA140) transfectados con Green Fluoresence Protein. Resultados: los extractos y fracciones de ambas especies no exhibieron actividad hemolítica en las condiciones evaluadas. Las fracciones de H. indicum fueron más tóxicas que las de C. dentata frente a larvas de A. salina y células U937. La actividad de la fracción de diclorometano de H. indicum (Hi-I-5B) sobre los amastigotes intracelulares está fuertemente relacionada con la presencia de alcaloides. Conclusiones: el extracto etanólico de las hojas de H. indicum exhibe propiedades antileishmaniales, a diferencia de la especie C. dentata, por lo que se podría pensar que la primera especie vegetal, representa una fuente potencial de moléculas útiles en el tratamiento de leishmaniasis cutánea.

Introduction: leishmaniasis is a serious public health problem worldwide. In Colombia, its cutaneous clinical form has the greatest incidence, and is mainly caused by species of Leishmania (Viannia) panamensis. Given the ineffectiveness of the available treatments, it is necessary to find new therapeutic agents in plant species used in folk medicine. Objective: evaluate the phytochemical profile and the hemolytic, cytotoxic and antileishmanial in vitro activity of extracts and fractions from leaves of Cordia dentata and Heliotropium indicum. Methods: the total ethanolic extract and fractions obtained from leaves of C. dentata and H. indicum underwent phytochemical profiling and determination of their hemolytic activity, toxic effect on Artemia salina larvae and on human promonocytic cell line U937 (CRL-1593.2™), as well as their antileishmanial activity against intracellular amastigotes of L. (V.) panamensis (MHOM/CO/87/UA140) transfected with Green Fluorescence Protein. Results: hemolytic activity was not observed in the extracts and fractions from either species under the study conditions. H. indicum fractions were more toxic than C. dentata fractions against A. salina larvae and U937 cells. Activity of the H. indicum dichloromethane fraction (Hi-I-5B) on intracellular amastigotes is closely related to the presence of alkaloids. Conclusions: the ethanolic extract from H. indicum leaves has antileishmanial properties, unlike the extract from the species C. dentata. This suggests that the former plant species is a rich potential source of molecules useful for the treatment of cutaneous leishmaniasis.

Tamizaje fitoquímico preliminar de especies de plantas promisorias de la costa atlántica colombiana / Preliminary phytochemical screening of promising plant species of the Colombian Atlantic coast

Introducción: Colombia es el segundo país con mayor biodiversidad del mundo, posee 10 % del recurso vegetal mundial representado en 50 000 especies vegetales, de las cuales la costa norte colombiana posee cerca de 3 400. Esta región se caracteriza por mantener una rica tradición de uso de este recurso natural para tratar sus problemas de salud. Objetivo: realizar el estudio químico sobre 45 extractos etanólicos de 39 especies vegetales, que son utilizadas en la medicina tradicional de la costa atlántica colombiana, con el propósito de contribuir al conocimiento con base científica, de los metabolitos secundarios presentes en estas plantas. Métodos: se recolectaron cada uno de los órganos de las especies; la droga fresca fue sometida a extracciones sucesivas con etanol 98 % y en los extractos se identificaron los diferentes grupos de metabolitos secundarios presentes. Resultados: en los diferentes extractos etanólicos se detectó una alta diversidad de metabolitos secundarios, con predominio de los flavonoides, derivados antracénicos, triterpenos, compuestos cardiotónicos y alcaloides. Por primera vez se reportaron estudios químicos para las especies Sarcostemma clausum (Jacq) Schult., Diospyros inconstans Jacq., Sterculia apetala (Jacq.) H. Karst., Ceratopteris pteridoides Hooker., Cecropia peltata L., Cordia dentata Poir. y Gustavia superba (Kunth) O. Berg. Conclusiones: se evidenció presencia de flavonoides como fitoconstituyentes más abundantes en las especies seleccionadas. Los resultados constituyen un apoyo para continuar con los estudios químicos y farmacológicos de estas especies.

Introduction: Colombia is the second country with the highest biodiversity in the world, about 10 % of the world's plant resources are represented by 50,000 species of plants, and the north Colombian´s coast has about 3,400 of these species. This region is characterized by maintaining a rich tradition of use of this natural resource to treat several primary health problems. Objective: to conduct a phytochemical study of 45 ethanol extracts of 39 plants, which are used in traditional medicine in the Colombian Atlantic coast, with the aim of contributing to science-based knowledge of secondary metabolites present in these plants. Methods: different organs from each species were collected, fresh drug was subjected to successive extractions with 98 % ethanol and were identified in the extracts different groups of secondary metabolites present in each plants. Results: in the different ethanol extracts was detected high diversity of secondary metabolites; flavonoids, anthracene derivatives, triterpenes, cardiotonic compounds and alkaloids were predominantly present in each extracts. This studies were reported for first time the phytochemical study for species such as Sarcostemma clausum (Jacq) Schult., Diospyros inconstans Jacq., Sterculia apetala (Jacq.) Karst., Ceratopteris pteridoides Hooker., Cecropia peltata L., Cordia dentata Poir. and Gustavia superba (Kunth) O. Berg. Conclusions: there was evidence the presence of flavonoids as phytoconstituents most abundant in the species selected. The results provide support for further chemical and pharmacological studies of these species.

Actividad Antibacteriana in vitro de extractos y fracciones de Physalis peruviana L. y Caesalpinia pulcherrima (L.) Swartz / In vitro antibacterial activity of extracts and fractions of Physalis peruviana L. and Caesalpinia pulcherrima (L.) Swartz

We evaluated the in vitro antibacterial activity of extracts and fractions of Physalis peruviana L. calyces and flowers and leaves of Caesalpinia pulcherrima (L.) Swartz against ATCC strains Staphylococcus aureus, Klebsiella pneumoniae and Pseudomonas aeruginosa, determining the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC). We find potent activity with MIC < 0,256 mg/mL for the chloroform fraction of P. peruviana calyces, the ethanol fraction of flowers of C. pulcherrima and ethanol and ether fractions of leaves of C. pulcherrima. Based on these results, we conclude that both species are promising and it is recommended to continue exploring them in order to isolate, purify and to elucidate the chemical structure from those compounds responsible for the biological activity of each active fraction.

Se evaluó la actividad antibacteriana in vitro de extractos y fracciones de los cálices de Physalis peruviana L. y flores y hojas de Caesalpinia pulcherrima (L.) Swartz frente a cepas ATCC de Staphylococcus aureus, Klebsiella pneumoniae y Pseudomonas aeruginosa, determinando la concentración mínima inhibitoria (CMI) y la concentración mínima bactericida (CMB). Encontramos potente actividad, con valores de CMI < 0,256 mg/mL para la fracción en cloroformo de los cálices de P. peruviana, la fracción en etanol de las flores de C. pulcherrima y las fracciones en etanol y éter de las hojas de C. pulcherrima. En función de los resultados obtenidos, concluimos que ambas especies son promisorias y se recomienda continuar su estudio intentando aislar, purificar y dilucidar la estructura química de los compuestos responsables de la actividad biológica en cada fracción activa.

Actividad larvicida de extractos etanólicos de Tabernaemontana cymosa y Trichilia hirta sobre larvas de estadio III y IV de Aedes aegypti (Diptera: Culicidae) / Larvicidal activity of ethanol extracts of Tabernaemontana cymosa and Trichilia hirta against III and IV stage larvae of Aedes aegypti (Diptera: Culicidae)

Introducción: el mosquito Aedes aegypti es el principal vector de los virus del dengue y la fiebre amarilla. Una de las formas actuales para combatir estas enfermedades es el control del vector. Sin embargo, los problemas causados por los insecticidas sintéticos y la resistencia adquirida por los mosquitos, hacen cada vez más difícil esta lucha. Las plantas constituyen una fuente alternativa al uso de insecticidas sintéticos. Objetivos: evaluar la actividad larvicida para el mosquito Aedes aegypti, de los extractos etanólicos y fracciones activas, de diferentes órganos vegetales de las especies Trichilia hirta L. y Tabernaemontana cymosa Jacq. Métodos: en este estudio se utilizaron larvas de Aedes aegypti en estadios III y IV. Los extractos etanólicos totales se obtuvieron por maceración del material vegetal seco y molido, durante una semana y posterior secado a presión reducida con un rotoevaporador. La obtención de fracciones y subfracciones, se realizó por cromatografía de columna abierta, usando solventes de diferentes polaridades. La actividad larvicida se evaluó bajo protocolos recomendados por la Organización Mundial de la Salud. Resultados: los extractos etanólicos de corteza de Trichilia hirta y flores, corteza y hojas de Tabernaemontana cymosa, no mostraron actividad larvicida. El extracto de semillas de Trichilia hirta mostró una actividad moderada con una CL50 y CL90 de 219,2 y 331,4 mg/L respectivamente. El extracto etanólico de semillas de Tabernaemontana cymosa, la fracción F008 y la subfracción F011, mostraron una buena actividad larvicida con CL50 de 35,1; 20,9, y 14,98 mg/L, respectivamente. Conclusiones: según los resultados, se consideró como promisorio el extracto de semillas de Tabernaemontana cymosa para la obtención de metabolitos secundarios con actividad larvicida.

Introduction: Aedes aegypti is the main vector of dengue and yellow fever. One way to combat these diseases today is the vector control. However, the problems caused by synthetic insecticides and the acquired resistance by mosquitoes, turn this control into a more difficult struggle every day. The plants offer an alternative source to the use of synthetic insecticides. Objectives: the objective of this study was to evaluate the larvicidal activity of the ethanol extracts and active fractions of different organs of Trichilia hirta L. and Tabernaemontana cymosa Jacq. Methods: in this study, Aedes aegypti larvae in III and IV stages were used. The total ethanol extracts were obtained by maceration of dried and ground plant material for a week and then dried at reduced pressure. The fractionation was performed by open column chromatography with the use of different polarity solvents. The larvicidal activity was assessed following protocols recommended by the World Health Organization. Results: the ethanol extracts from Trichilia hirta bark and flowers, and Tabernaemontana cymosa bark and leaves showed no larvicidal activity. The Trichilia hirta seed extract showed a moderate activity with an LC50 and LC90 of 219.2 and 331.4 mg/L respectively. The ethanol extract from Tabernaemontana cymosa seeds, the fraction F008 and the subfraction F011, showed good larvicidal activity with LC50 of 35.1, 20.9, and 14.98 mg/L, respectively. Conclusions: according to the results obtained in this study, the extract from Tabernaemontana cymosa seeds could be considered as a potential source of secondary metabolites with larvicidal activity.

In vitro antimalarial activity of fractions and constituents isolated from Tabebuia billbergii / Actividad antimalárica in vitro de fracciones y constituyentes aislados de Tabebuia billbergii

Introduction: in vitro antimalarial activity of naphthoquinones (1-5), isolated from Tabebuia billbergii (Bureau & K. Schum.) Standl., was investigated. Tabebuia billbergii, commonly known as guayacán, is a plant traditionally used in the Amazon in numerous conditions like bacterial and fungal infections, fever, syphilis, malaria, trypanosomiasis, as well as stomach and bladder disorders, and tumours. Objective: to study the dichloromethane extracts of both the trunk and the inner bark of Tabebuia billbergii and to demonstrate the antimalarial activity of some of its bioactive components. Methods: some bioactive components were evaluated for the antimalarial activity against Plasmodium berghei, by using the inhibition of the differentiation cycle of the parasite measure by the ³H-hypoxanthine incorporation and compared to that obtained for chloroquine. Results: conventional chromatographic techniques and bioassay-guided fractionation (Artemia salina) allowed isolating from the active fractions one naphthoquinone (lapachol) and four naphtho-furan-4,9-diones. These compounds proved to have an important antiplasmodial effect, with very encouraging IC50's, especially when compared to the results shown by Chloroquine in the same experiment. In addition, two triterpenes, β-sitosterol and stigmasterol, were obtained from the bark. Conclusions: the activity-guided fractionation (A. salina) of dichloromethane extracts of the trunk and the inner bark of Tabebuia billbergii led to the isolation and the identification of five quinonoid compounds with antiplasmodial effect. The significant inhibitory activity in vitro against Plasmodium berghei observed for compound 2-acetyl-naphtho-[2,3b]-furan-4,9-dione allow us to present them as a potential antimalarial compound.

Introducción: se evaluó la actividad antimalárica in vitro de una serie de naftoquinonas (1-5), aisladas de Tabebuia billbergii (Bureau & K. Schum.) Standl., que es conocida comúnmente como guayacán, una planta utilizada tradicionalmente en la Amazonía en numerosos problemas de salud como infecciones bacterianas y fúngicas, fiebre, sífilis, paludismo, tripanosomiasis, así como en problemas estomacales, tumores y trastornos de la vejiga. Objetivo: estudiar los extractos en diclorometano tanto del tronco como la corteza interna de Tabebuia billbergii y evaluar la actividad antimalárica de algunos de sus componentes bioactivos. Métodos: la actividad antimalárica contra Plasmodium berghei se evaluó en algunos componentes bioactivos, por la inhibición del ciclo de la diferenciación de la medida de los parásitos mediante la incorporación de 3H-hipoxantina y se comparó con la obtenida para la cloroquina. Resultados: a través de técnicas cromatográficas convencionales y el fraccionamiento guiado por bioensayo (Artemia salina) se aislaron de las fracciones activas, una naftoquinona (lapachol) y 4 nafto-furan-4,9-dionas. Estos compuestos presentaron un efecto antiplasmodial importante, con buenos valores de IC50, especialmente cuando se compara con los resultados mostrados por la cloroquina en el mismo experimento. Además, se obtuvieron de la corteza 2 triterpenos, β-sitosterol y estigmasterol. Conclusiones: el fraccionamiento guiado por Artemia salina de los extractos en diclorometano del tronco y la corteza interna de Tabebuia billbergii, condujo al aislamiento y la identificación de 5 compuestos de naturaleza quinoidal con efecto antiplasmódicol. La actividad in vitro contra Plasmodium berghei observada para el compuesto 2-acetil-nafto-[2,3 b]-furan-4,9-diona, permite proponerlo como un potencial compuesto antimalárico.

Química y biología del extracto etanólico del epicarpio de Crescentia cujete L. (totumo) / Chemistry and biology of ethanol extract from the epicarp of Crescentia cujete L. (totumo)

Introducción: el árbol de Crescentia cujete L. (Bignonaceae), conocido en Colombia como totumo, es una especie característica de climas tropicales. Su rasgo más distintivo es el fruto, el cual es una calabaza esférica con cáscara dura y leñosa, y una pulpa gelatinosa con numerosas semillas. Objetivo: realizar el estudio químico y biológico sobre el extracto etanólico del epicarpio de Crescentia cujete L. Métodos: se recolectó el material vegetal y se obtuvo el extracto etanólico total. Luego se realizó el tamizaje preliminar fitoquímico, los ensayos físico-químicos directos sobre el material vegetal, la cuantificación de metales pesados y, finalmente, el estudio biológico frente a larvas de Aedes aegypti L. (Culicidae) en estadios III y IV, larvas de Artemia salina Leach. (Artemiidae) y células apicales de raíces de Allium cepa L. (Amaryllidaceae). Resultados: se identificó la presencia de tres grupos de metabólitos secundarios: flavonoides, esteroides y triterpenos. Asimismo, se cuantificó el contenido de agua y cenizas en base seca, y se determinaron las concentraciones de algunos metales pesados como cadmio, cromo, mercurio y plomo. En el estudio biológico se puso de manifiesto que el extracto no presenta toxicidad aguda en ninguno de los sistemas biológicos ensayados, a las concentraciones y tiempos de experimentación. Conclusiones: la información obtenida en la presente investigación, constituye un recurso importante para la comunidad científica porque proporciona elementos relacionados con la naturaleza química y el comportamiento biológico del epicarpio del totumo, antes no reportados.

Introduction: Crescentia cujete L. (Bignonaceae) tree known in Colombia as totumo, is a characteristic species of tropical climates. Its most distinctive feature is the fruit, which is a spherical pumpkin with hard and woody peel, and a gelatinous pulp having a lot of seeds. Objective: to conduct the chemical and biological ethanol extract of Crescentia cujete L. epicarp. Methods: vegetal material was harvested and the total ethanol extract was obtained. Then, preliminary phytochemical screening, direct physical and chemical tests on vegetal material, the quantification of heavy metals and finally the biological study against Aedes aegypti L. (Culicidae) larvae in stages III and IV, Artemia salina Leach. (Artemiidae) larvae and apical cells of Allium cepa L. (Amaryllidaceae) roots. Results: the presence of three groups of secondary metabolites, that is, flavonoids, steroids and triterpenes were identified. Likewise, the water and ash content on dry basis was quantified as well as the levels of concentration of some heavy metals such as cadmium, chromium, mercury and lead were estimated. The biological study revealed that the extract did not show acute toxicity either in any of the tested biological systems or at the concentrations and the time of experimentation. Conclusions: the information obtained in this research is an important resource for the scientific community and provides elements associated to the chemical nature and the biological behavior of the totumo ´s epicarp not contained in previous reports.

Folk medicine in the northern coast of Colombia: an overview.

BACKGROUND: Traditional remedies are an integral part of Colombian culture. Here we present the results of a three-year study of ethnopharmacology and folk-medicine use among the population of the Atlantic Coast of Colombia, specifically in department of Bolívar. We collected information related to different herbal medicinal uses of the local flora in the treatment of the most common human diseases and health disorders in the area, and determined the relative importance of the species surveyed. METHODS: Data on the use of medicinal plants were collected using structured interviews and through observations and conversations with local communities. A total of 1225 participants were interviewed. RESULTS: Approximately 30 uses were reported for plants in traditional medicine. The plant species with the highest fidelity level (Fl) were Crescentia cujete L. (flu), Eucalyptus globulus Labill. (flu and cough), Euphorbia tithymaloides L. (inflammation), Gliricidia_sepium_(Jacq.) Kunth (pruritic ailments), Heliotropium indicum L. (intestinal parasites) Malachra alceifolia Jacq. (inflammation), Matricaria chamomilla L. (colic) Mentha sativa L. (nervousness), Momordica charantia L. (intestinal parasites), Origanum vulgare L. (earache), Plantago major L. (inflammation) and Terminalia catappa L. (inflammation). The most frequent ailments reported were skin affections, inflammation of the respiratory tract, and gastro-intestinal disorders. The majority of the remedies were prepared from freshly collected plant material from the wild and from a single species only. The preparation of remedies included boiling infusions, extraction of fresh or dry whole plants, leaves, flowers, roots, fruits, and seeds. The parts of the plants most frequently used were the leaves. In this study were identified 39 plant species, which belong to 26 families. There was a high degree of consensus from informants on the medical indications of the different species. CONCLUSIONS: This study presents new research efforts and perspectives on the search for new drugs based on local uses of medicinal plants. It also sheds light on the dependence of rural communities in Colombia on medicinal plants.

Actividad antiinflamatoria de productos naturales / Anti-inflammatory activity of natural products

Some natural products have been reported effects on the production of proinflammatory cytokines (IL-1b, IL-6, IL-8, GM-CSF and TNF-), enzyme mediators (MMP-3, MMP-13, iNOS and COX-2) and their catabolites (NO and PGE2). These activities have been associated with inactivation of NF-B by preventing IkBphosphorylation and degradation, or regulation of AP-1 transcription factors, which may be the mechanistic basis for the anti-inflammatory effects of some compounds. This article tries to review the behavior of various medicinal plants or isolated compounds, whose antiinflammatory action is known by previous trials carried in a number of in vivo and in vitro experimental inflammatory models.

Se ha reportado que algunos productos naturales presentan efectos sobre la expresión de: citoquinas proinflamatorias (IL-1b, IL-6, IL-8, GM-CSF and TNF-), enzimas mediadoras (MMP-3, MMP-13, iNOS y COX-2) y catabolitos (NO y PGE2). Esta actividad ha sido asociada con: la inactivación del NF-B, por la prevención de la fosforilación- degradación de IkBo la regulación ciertos factores de trascripción, entre otros, lo cual constituye el mecanismo de acción de tales compuestos. En este trabajo se da una visión general de la química y los diferentes modelos in vivo e in vitro de evaluación del proceso inflamatorio de compuestos de origen natural.