An integrative metabolomics and network pharmacology method for exploring bioactive components and preliminary pharmacodynamics in medicinal parts of Harrisonia perforata / 中国中药杂志

In this paper,metabolomics and network pharmacology were used to investigate the bioactive components of Harrisonia perforata and their possible mechanisms of action. Metabolites in the flowers,fruits,branches,leaves and stalks of H. perforata were analyzed by ultra-high performance liquid chromatography-quadrupole-time-of-flight mass spectrometry. Meanwhile,multiple statistical analysis methods including principal component analysis( PCA) and orthogonal partial least squares discriminant analysis( OPLS-DA)were applied to screen and identify differential compounds. With metabolomics method,9 differential compounds were preliminarily identified from leaves and other non-traditional medicinal parts. Subsequently,these compounds were explored by using network pharmacology. With gastrointestinal absorption and drug-likeness as limiting conditions,they were imported into the Swiss ADME,from which 7 compounds with potential medicinal activity were obtained. Then,their targets were predicted by PharmMapper,with Human Protein Targets Only and Normalized Fit Score>0. 9 set as limiting conditions,and 60 standardized potential targets were identified with Uniprot. KEGG( Kyoto encyclopedia of genes and genomes) pathway data was obtained using metascape and the " potential active ingredients-target-pathway" network was constructed with Cytoscape 3. 7. 2. The enrichment analysis of KEGG demonstrated that the 60 targets were enriched in 78 signaling pathways( min overlap: 3,P value cutoff: 0. 01,min enrichment: 1. 5),many of which are related to anti-bacteria,anti-inflammation and anti-virus,such as IL-17 signaling pathway,RIG-I-like receptor signaling pathway and NOD-like receptor signaling pathway. Finally,depending on the clinical activity of H. perforata,the relevant signaling pathways were analyzed through experimental data and literature. Dehydroconiferyl alcohol was reported to have the anti-inflammatory effect and perforamone D to possess the antimycobacterial activity. The KEGG pathway enrichment analysis showed that dehydroconiferyl alcohol could act on the Alzheimer's disease( AD) signaling pathway by targeting CDK5 R1 and BACE1. ACh E inhibitor is the most promising drug to treat AD,while dehydroconiferyl alcohol has been proved to inhibit ACh E according to literature. The experimental results revealed that the extract of leaves of H. perforata can effectively inhibit the growth of Staphylococcus aureus. These are consistent with the enrichment analysis results of KEGG. This study explored the bioactive components and pharmacodynamics of the leaves of the H. perforata,laying a theoretical foundation for its in-depth development and rational application.

Ensaios preliminares em ratas wistar com extrato hidroetanólico de calunga (Simaba ferruginea St. Hil. ) v. o., nas fases gestacionais de implantação, organogênese e período fetal: interferências na prole / Preliminary trials on female Wistar rats with hydroethanolic extract from "calunga" (Simaba ferruginea St. Hil. ) in the gestational stages of implantation, organogenesis and fetal period: interference on offspring

RESUMO A susceptibilidade dos conceptos a agentes químicos varia muito em cada estágio do desenvolvimento. Devido a isto, a maioria dos países passou a exigir a análise do potencial para afetar todos os aspectos da reprodução (espermatogênese, acasalamento, prenhez, parto e lactação) para o desenvolvimento de novos medicamentos e fitoterápicos. O presente trabalho objetivou avaliar o efeito do extrato hidroetanólico de Simaba ferruginea St. Hil (calunga) (EHSF) v.o., em ratas da linhagem Wistar tratadas durante a prenhez e verificar a interferência no desenvolvimento intra-uterino da prole. As ratas foram tratadas com EHSF 50 e 100 mg Kg-1 ou água destilada, do seguinte modo: a) do 1º ao 6º dia de prenhez (período da formação do blastocisto e implantação); b) do 8º ao 16º dia de prenhez (fase embrionária de organogênese); c) do 15º ao 19º dia de prenhez (fase do desenvolvimento fetal). O tratamento do 1º ao 6º dia, mostrou redução no número de fetos com ambas doses e não alterou o peso do útero / ovário nem peso corporal das mães. Quando as ratas foram tratadas na fase da organogênese verificou-se, redução estatisticamente significante do número de fetos vivos com a dose 50 mg Kg-1, e o aparecimento de fetos mortos em 30% das fêmeas tratadas com EHSF 50 mg Kg-1 e em 20% nas fêmeas tratadas com a dose de 100 mg Kg-1, não houve alteração no peso do útero / ovário nem no peso corporal das matrizes. Finalmente, o tratamento no período fetal não afetou o número de filhotes vivos, não provocou malformações anatômicas visíveis a olho nu, nem reabsorção fetal; porém, observou-se que 10% das mães tratadas com 50 mg Kg-1 apresentaram 2 fetos mortos e 20% das mães tratadas com 100 mg Kg-1 apresentaram, em média, 4 fetos mortos. Com estes dados, pode ser concluído que o EHSF apresenta baixa ou nenhuma toxicidade materna para ratas Wistar, embora seja letal para alguns descendentes, independente da fase da prenhez em que foram realizados os tratamentos ...

ABSTRACT The susceptibility of concepts to chemical agents varies a lot at each development stage. Because of that, most countries started requiring the analysis of potential to affect all aspects of reproduction (spermatogenesis, mating, pregnancy, birth and lactation) for the development of new drugs and herbal medicines. This study aimed to evaluate the effect of the hydroethanolic extract of Simaba ferruginea St. Hil ("calunga") (EHSF) on female Wistar rats treated during pregnancy in order to check the interference on the intrauterine development of the offspring. The rats were treated with EHSF 50 and 100 mg/kg-1or distilled water, as follows: a) from day 1 to day 6 of pregnancy (period of blastocytes formation and implantation); b) from day 8 to day 16 of pregnancy (embryonic phase of organogenesis); c) from day 15 to day 19 of pregnancy (fetal development phase). The treatment from day 1 to day 6 showed reduction on the amount of fetuses with both doses and it did not alter neither the weight of the uterus / ovary nor the body weight of the mothers. When the female rats were treated in the organogenesis phase, it was verified both statistical significant decrease on the number of live fetuses for the 50 mg / Kg-1, and also appearance of dead fetuses in 30% of the female rats treated with EHSF 50 mg / Kg-1. In 20% of the female rats treated with 100 mg / Kg-1, there was no alteration neither in the weight of the uterus / ovary or in the body weight of the matrixes. Finally, the treatment in the fetal period did not affect the number of live descendants, or caused anatomical malformations visible to naked eye and fetal reabsorption. However, 10% of the mothers treated with 50 mg / Kg-1presented 2 dead fetuses and 20% of the mothers who had 100 mg / Kg-1showed, on average, 4 dead fetuses. With this data, we can conclude that EHSF presents low maternal toxicity for Wistar rats, although being fatal to some descendants, not mattering in which pregnancy phase the treatments have been performed, being more evident in the earlier phases. For this reason, it is recommended to avoid the use of this plant in pregnancy case.

Chemical constituents from the twigs and leaves of Harrisonia perforate / 药学学报

This study was performed to investigate the chemical constituents in the twigs and leaves of Harrisonia perforate. Six compounds were isolated from the 95% EtOH extract of the twigs and leaves of Harrisonia perforate by silica gel, ODS, Sephadex LH-20 column chromatographies and preparative HPLC. On the basis of chemical properties and spectra data, these compounds were identified as harriperfin E (1), kihadanin A (2), kihadanin B (3), 6α-acetoxyobacunol acetate (4), gardaubryone C (5), and β-sitosterol methyl ether (6), respectively. Compound 1 is a new chromone, and compounds 2-6 are isolated from this plant for the first time.

Inhibitory effect of Quassia amara Linn. crude bark extract on Entamoeba histolytica in vitro

BACKGROUND: Entamoeba histolytica is an important etiologic agent of diarrhea. Globally, it is estimated to infect 40 to 50 million people and cause 40,000 to 100,000 deaths per year. Metronidazole is effective but can cause adverse reactions in certain individuals. In search of alternatives, traditional medicinal plants are being studied. Several plants in Family Simaroubaceae have shown anti-amoebic activity. Quassia amara, a member of this family has not been tested.OBJECTIVE: To determine the effect of Q. amara crude extract on Entamoeba histolytica in vitro.METHODS: Initial testing of 104 µg/ml ethanolic bark extract was performed. Counts were made after 72 hours. Three trials in triplicates were performed.Nine (9) dilutions of extract were then tested (18.8 to 5,00 µg/ml). Test tubes were checked for viable amoeba after 24-hour and 72-hour incubation. Minimum inhibitory concentrations (MIC) were determined for the two incubation periods. At least two trials in triplicates for each dilution were performed. metronidazole served as positive control.RESULTS: At 104 µg/ml incubated for 72 hours, no viable amoeba was obtained and counted. The MIC after 24 hours was 5,000 µg/ml, while the MIC at 72 hours was 37.5 µg/ml.CONCLUSION: Q. amara crude extract has inhibitory effects on E. histolycain vitro.

Tripanocide and antibacterial activity ofAlvaradoa subovata Cronquist extracts / Actividad tripanocida y antibacteriana de extractos de Alvaradoa subovata Cronquist

We studied antioxidant, antibacterial and tripanocide activities of Alvaradoa subovata extracts. The ethanolic extracts showed the greatest DPPH radical scavenging capacity, especially that of bark with an IC50 = 4.7 +/- 0.18 ug/mL. Wood dichloromethane extract displayed growth inhibition of the phytopathogenic bacteria Xanthomona axonopodis in the disk diffusion assay and showed a MIC value of 100 ug/ml. It also showed growth inhibition of Trypanosoma cruzi (IC50 = 0.063 +/- 0.003 mg/mL). A fraction of this extract, which has emodin as the main component, showed tripanocide activity (60 percent of growth inhibition at 100 ug/mL). The main compounds in wood dichloromethane extract were anthraquinones, identified as chrysophanol and emodin, and coumarins, of which scopoletin was identified. These three compound s could serve as analytical markers of the extract. The results of this study show that wood extract of A. subovata constitute a source of bioactive compounds such as antiparasitic and pesticides agents.

En el presente trabajo se estudió la actividad antioxidante, antibacteriana y tripanocida de extractos de Alvaradoa subovata. La mayor actividad depuradora de radicales libres se observó en el extracto etanólico de corteza (CI50 = 4.7 +/- 0.18 ug/mL). El extracto en diclorometano de madera inhibió el crecimiento de la bacteria fitopatógena Xanthomona axonopodis con una CIM = 100 ug/mL. El mismo extracto mostró inhibición del crecimiento de Trypanosoma cruzi (CI50 = 0.063 +/- 0.003 mg/mL). Una fracción de este extracto (100 ug/mL), cuyo componente mayoritario es emodina, inhibió en un 60 por ciento el crecimiento del parásito. Los compuestos mayoritarios detectados en el extracto de madera fueron antraquinonas, entre las cuales se identificaron emodina y crisofanol, y la cumarina escopoletina. Estos tres compuestos podrían servir como marcadores analíticos del extracto. Los resultados de este trabajo muestran que los extractos de A. subovata constituyen una fuente de compuestos bioactivos con potencial como antiparasitarios y plaguicidas.

Intoxicação experimental por Simarouba versicolor (Simaroubaceae) em ovinos e indução de resistência ao consumo da planta / Experimental poisoning by Simarouba versicolor (Simaroubaceae) in sheep and induced resistance to consumption of the plant

Simarouba versicolor é uma árvore semidecídua pertencente à família Simaroubaceae. Um surto de intoxicação por S. versicolor em bovinos por brotos da planta presente no pasto em Mato Grosso do Sul e sua reprodução experimental foram descritos. Esse estudo teve por objetivos verificar experimentalmente se os ovinos podem ser utilizados como modelo clínico-patológico no estudo da intoxicação por Simarouba versicolor St. Hil. (fam. Simaroubaceae), determinar se há indução de resistência pela ingestão de pequenas e repetidas doses e, se a planta mantém sua toxicidade quando dessecada. Foram realizados dois experimentos, sendo o primeiro com folhas verdes ou folhas dessecadas e trituradas de S. versicolor em doses únicas de 5g/kg, 5g/kg e 3g/kg a três ovinos (Ovino 1, 2 e 3 respectivamente). O experimento 2, foi realizado com diferentes doses diárias de folhas dessecadas e trituradas de S. versicolor em quatro ovinos que receberam 1,5g/kg, 0,75g/kg, 0,6g/kg e 0,3g/kg e, com um ovino que recebeu 3g/kg como controle positivo (Ovino 4). A administração foi suspensa quando os ovinos apresentaram sinais clínicos da intoxicação. Após doze dias de recuperação, os animais sobreviventes foram desafiados com a mesma dose diária da planta ingerida anteriormente para avaliar o desenvolvimento de resistência. Os sinais clínicos observados nos dois experimentos caracterizaram-se por anorexia, mucosas oculares congestas, polidipsia, sialorreia, fezes pastosas que evoluíram para diarreia líquida fétida esverdeada, decúbito lateral e morte para os Ovinos 1 a 7. As principais lesões histológicas observadas foram necrose do tecido linfoide (linfonodos, baço, placas de Peyer) e enterite necrosante. Com os resultados obtidos, pode-se concluir que os ovinos podem ser utilizados como modelo experimental clínico-patológico na intoxicação por S. versicolor. Com o método utilizado, não houve resistência ao consumo diário de folhas da planta pelos ovinos e, as folhas mantiveram sua toxicidade quando dessecadas.(AU)

Simarouba versicolor St. Hil. is a semideciduous tree belonging to the Simaroubaceae family. An outbreak of poisoning in cattle by shoots of S. versicolor present in the pasture in Mato Grosso do Sul and experimental reproduction of the poisoning was described. This study aimed to verify experimentally whether sheep could be used as a clinical-pathological model in the study of the poisoning caused by S. versicolor, to determine if there develops resistance induced by ingestion of small and repeated doses of the leaves, and if the plant keeps its toxicity when dried. Two experiments were conducted: Experiment 1 with green leaves or dried and powdered leave of S. versicolor, given in single doses of 5g/kg, 5g/kg and 3g/kg to three sheep (Sheep 1, 2 and 3 respectively). Experiment 2 was made with different daily doses of dried and powdered leaves of S. versicolor; to four sheep was given 1.5g/kg, 0.75g/kg, 0.6g/kg and 0.3g/kg, and the positive control (Sheep 4) received 3g/kg. The administration was suspended when the animals showed clinical signs of poisoning. After twelve days of recovery, the surviving sheep were challenged with the same daily dose given previously, to assess the development of resistance. Clinical signs observed in both experiments were characterized by anorexia, congested ocular mucosa, polydipsia, drooling, loose stools which evolved into fetid greenish watery diarrhea, lateral decumbency and death of Sheep 1 to 7. The main histological lesions observed were necrosis of lymphoid tissue (lymph nodes, spleen, Peyer's patches) and necrotizing enteritis. With the results it can be concluded that sheep can be used as experimental model for the clinic-pathological aspects of poisoning by S. versicolor. The method used has not shown resistance to the daily consumption of the plant by the sheep, and the leaves kept their toxicity when dried.(AU)

Actividad antioxidante, análisis fitoquímico y micrografía analítica de hojas de Castela tweedii (Simaroubaceae) / Antioxidant activity, phytochemical analisys and micrographic characterization of Castela tweedii (Simaroubaceae) leaves

Castela tweedii is a small tree belonging to Simaroubaceae family. Infusions of its leaves are used in folk medicine to treat gastrointestinal disorders and diarrhea. In this work, we evaluated the antioxidant activity of ethanol and dicloromethane leaves extracts against DPPH radical (2,2-difenilpicrilhidrazil) in order to justify, at least in part, its popular use. Ethanol extract showed scavenging activity, with an IC50=0.1288 mg/mL. Responsible compounds for these activity were tannins, flavonoids and phenylcarboxilic acids, among them we identified rutine and chlorogenic acid. Microscopic and histochemical analysis of leaves was carry out to developed useful characterizations that will allow a future identification and authentication of raw material: such as, the presence of mucilaginous hypodermis, leaf of dorsiventral structure, 1 to 2 rows of empalisade parenchyma with tannin deposits, anomocytic stomata in low epidermis and simple, unicellular trichomes in both epidermis.

Castela tweedii es un árbol de bajo porte perteneciente a la Familia Simaroubaceae, las infusiones de sus hojas son utilizadas en la medicina popular Argentina para el tratamiento de desordenes gastrointestinales y diarreas. Con el objetivo de fundamentar el uso popular de esta especie se evaluó la actividad antioxidante de los extractos etanólicos y diclorometánicos de forma cuantitativa y cualitativa frente al radical 2,2-difenilpicrilhidrazilo (DPPH); el extracto etanólico demostró actividad obteniéndose una CI50= 0,1288 mg/mL. El análisis fitoquímico mostró que los compuestos responsables de esta actividad fueron taninos, flavonoides y ácidos fenilcarboxílicos, entre ellos se identificó rutina y ácido clorogénico. Además se realizó el estudio morfoanatómico e histoquímico de las hojas que aportó datos de valor diagnostico para el control de calidad de la droga vegetal: presencia de una hipodermis mucilaginosa, estructura dorsiventral con una a dos hileras de parénquima en empalizada conteniendo taninos, estomas anomocíticos solo en la epidermis abaxial y tricomas simples unicelulares en ambas epidermis.

Anatomía foliar de arbustos y árboles medicinales de la región chaqueña semiárida de la Argentina / Foliar anatomy of medicinal trees and shrubs of the semi-arid Chaco region of Argentina

Se estudió la anatomía foliar de 32 arbustos y árboles medicinales de los Distritos Chaqueños Occidental y Serrano (Argentina). El objetivo de este trabajo fue proveer una clave para el reconocimiento de estos taxones a partir de hojas fragmentadas, desmenuzadas o pulverizadas. Para el estudio las muestras de herbario fueron reconstituidas y fijadas en FAA; y, en cuanto a las preparaciones, se utilizaron técnicas histológicas convencionales. Algunos de los principales caracteres de identificación fueron: los tricomas estrellados en Capparicordis tweediana y Ruprechtia triflora, cistolíticos en Celtis spp.; escamoso-peltados en Zanthoxylum coco; epidermis papilosa (e.g., Schinopsis lorentzii); los estomas ciclocíticos en Bulnesia sarmientoi, Maytenus vitis-idaea, Moya spinosa y Schinopsis spp.; idioblastos cristalíferos epidérmicos en Scutia buxifolia; la epidermis cristalífera en Maytenus vitis-idaea; la epidermis pluristrata en Jodina rhombifolia; la presencia de hipodermis en Castela coccinea, Maytenus vitis-idaea, Prosopis ruscifolia y Ziziphus mistol; los haces bicolaterales en Lycium cestroides; la presencia de arena cristalina en Calycophyllum multiflorum y Lycium cestroides; la ausencia total de cristales en la familia Capparaceae. Para la identificación de las especies estudiadas se presenta una clave dicotómica e ilustraciones originales.

Gram-scale isolation of isobrucein B and neosergeolide from Picrolemma sprucei Hook. f. / Isolamento de isobruceina B e neosergeolida de Picrolemma sprucei Hook. f. em escala-grama

Quassinoids neosergeolide and isobrucein B, obtained from Picrolemma sprucei, have proven in vitro antitumor, antimalarial, anthelminthic, cytotoxic, insecticide and leishmanicidal activities. There is interest in the in vivo pharmacological study of these natural compounds and their semi-synthetic derivatives, however, the quantities obtained in previous extraction processes have been shown to be a limiting factor for continuation of these studies. Herein, we describe a method for obtaining grams of these quassinoids whose purification relies only on recrystallization.

Os quassinóides neosergeolida e isobruceína B, obtidos de Picrolemma sprucei, possuem atividades antitumoral, antimalárica, anti-helmíntica, citotóxica, inseticida e anti-leishmania comprovadas em estudos in vitro. Há interesse no estudo farmacológico in vivo dessas substâncias naturais e de seus derivados semi-sintéticos, porém a quantidade obtida nos processos de extração tem se mostrado um fator limitante à continuação desses estudos. No presente trabalho, descrevemos um método para obtenção de gramas desses quassinóides cuja purificação depende apenas de cristalização fracionada.

Biological activity of neosergeolide and isobrucein B (and two semi-synthetic derivatives) isolated from the Amazonian medicinal plant Picrolemma sprucei (Simaroubaceae)

In the present study, in vitro techniques were used to investigate a range of biological activities of known natural quassinoids isobrucein B (1) and neosergeolide (2), known semi-synthetic derivative 1,12-diacetylisobrucein B (3), and a new semi-synthetic derivative, 12-acetylneosergeolide (4). These compounds were evaluated for general toxicity toward the brine shrimp species Artemia franciscana, cytotoxicity toward human tumour cells, larvicidal activity toward the dengue fever mosquito vector Aedes aegypti, haemolytic activity in mouse erythrocytes and antimalarial activity against the human malaria parasite Plasmodium falciparum. Compounds 1 and 2 exhibited the greatest cytotoxicity against all the tumor cells tested (IC50 = 5-27 µg/L) and against multidrug-resistant P. falciparum K1 strain (IC50 = 1.0-4.0 g/L) and 3 was only cytotoxic toward the leukaemia HL-60 strain (IC50 = 11.8 µg/L). Quassinoids 1 and 2 (LC50 = 3.2-4.4 mg/L) displayed greater lethality than derivative 4 (LC50 = 75.0 mg/L) toward A. aegypti larvae, while derivative 3 was inactive. These results suggest a novel application for these natural quassinoids as larvicides. The toxicity toward A. franciscana could be correlated with the activity in several biological models, a finding that is in agreement with the literature. Importantly, none of the studied compounds exhibited in vitro haemolytic activity, suggesting specificity of the observed cytotoxic effects. This study reveals the biological potential of quassinoids 1 and 2 and to a lesser extent their semi-synthetic derivatives for their in vitro antimalarial and cytotoxic activities.

phytopharmacological review on genus Ailanthus

The various species of Ailanthus find extensive use in the indigenous system of medicine for various ailments. The phytochemical and biological evaluation by researchers have authenticated their usage in traditional system of medicine. In the present paper the authors compile here a comprehensive review of their use in the light of present day research

In vitro inhibition of Plasmodium falciparum by substances isolated from Amazonian antimalarial plants

In the present study, a quassinoid, neosergeolide, isolated from the roots and stems of Picrolemma sprucei (Simaroubaceae), the indole alkaloids ellipticine and aspidocarpine, isolated from the bark of Aspidosperma vargasii and A. desmanthum (Apocynaceae), respectively, and 4-nerolidylcatechol, isolated from the roots of Pothomorphe peltata (Piperaceae), all presented significant in vitro inhibition (more active than quinine and chloroquine) of the multi-drug resistant K1 strain of Plasmodium falciparum. Neosergeolide presented activity in the nanomolar range. This is the first report on the antimalarial activity of these known, natural compounds. This is also the first report on the isolation of aspidocarpine from A. desmanthum. These compounds are good candidates for pre-clinical tests as novel lead structures with the aim of finding new antimalarial prototypes and lend support to the traditional use of the plants from which these compounds are derived.

Pharmacognostic evaluation of the stem bark of balanites aegyptiaca delile "Hingot"

Balanites aegyptiaca [Hingot] is one of the important Kasthausadhi of Indian System of medicine, which is botanically identified as Balanites aegyptiaca of family Simaroubaceae. All the parts of this plant as well as its extracts are particularly useful to mankind. According to Ayurvedic concept it is pungent bitter, purgative, anthelmintic and is useful in cough and colic, ulcer as well as in hypertension. Chemically it contains a lot of saponins whose concentration varies in different parts of the plant. The present paper deals with its literature survey regarding distribution, cultivation, chemical information, and medicinal importance. The detailed botanical and pharmacognostical parameters have been performed on the stem bark, for the identification of the genuine sample, detection of the adulteration in the market sample and study of the quality control parameters of the drug

In vitro studies of the anthelmintic activity of Picrolemma sprucei Hook. f. (Simaroubaceae)

1300 ppm (1.3 g / L), water and ethanol extracts prepared from stems or roots of Picrolemma sprucei Hook. f. were lethal (85-90 percent mortality) in vitro to Haemonchus contortus (Barber Pole Worm) larvae, a gastrointestinal nematode parasite found in domestic and wild ruminants. Neosergeolide and isobrucein B were isolated in 0.0083 and 0.0070 percent yield from dry, ground P. sprucei stems (0.89 kg). Neosergeolide, isobrucein B and the anthelmintic drug standard levamisole all caused comparable mortality rates (68-77 percent) in vitro to H. contortus at similar concentrations (81-86 ppm). The anthelmintic activity of P. sprucei infusions (teas), alcohol extracts, and neosergeolide and isobrucein B, has therefore been demonstrated for the first time.

Na concentração de 1300 ppm (1.3 g / L), extratos aquosos e etanólicos preparados a partir dos caules ou raízes de Picrolemma sprucei Hook. f. apresentaram letalidade (85-90 por cento de mortalidade) in vitro para Haemonchus contortus, um nematóide parasítico do aparelho gastrointestinal de ruminantes domesticos e silvestres. Neosergeolida e isobruceina B foram isoladas dos caules em rendimentos de 0.0083 and 0.0070 por cento, respectivamente. Essas últimas e a droga anti-helmíntica levamisole provocaram mortalidade semelhante in vitro (68-77 por cento) em H. contortus em concentrações semelhantes (81-86 ppm). A atividade anti-helmíntica in vitro de infusões e extratos alcoólicos dos caules, bem como da neosergeolida e isobruceina B isoladas de P. sprucei, foi demonstrada pela primeira vez.

Effect of aqueous leaf extract of Irvingia gabonensis on gastrointestinal tract in rodents.

Effect of the aqueous leaf extract of I. gabonensis on the gastrointestinal tract was investigated on isolated rabbit jejunum, guinea pig ileum, gastrointestinal motility, castor oil-induced diarrhoea in mice and castor oil-induced fluid accumulation in rats. The results showed that the extract exhibited a concentration-dependent relaxation of spontaneous pendular movement of isolated rabbit jejunum and guinea pig ileum, and attenuated both acetylcholine-induced contraction of rabbit jejunum and histamine-induced contraction of guinea pig ileum. The extract (100, 200 and 400 mg/kg) also caused a significant dose-dependent decrease of gastrointestinal motility in mice (40.12, 39.45 and 37.45%), intestinal fluid accumulation in rats (71.43, 81.63 and 83.27%), and remarkably protected mice against castor oil-induced diarrhoea [58.33, 75 and 91.67% (Di Carlo score)] respectively. Preliminary phytochemical screening of the aqueous leaf extract of I. gabonensis revealed the presence of saponins, tannins, phenols and phlobatanins.

Screening of plants found in the State of Amazonas, Brazil for activity against Aedes aegypti larvae

Extratos aquosos, etanólicos e metanólicos, representando principalmente espécies vegetais nativas encontradas na região Amazônica, foram preparados, respectivamente, por infusão, maceração e extração contínua líquido-sólido, seguida de evaporação e liofilização. Os extratos liofilizados foram testados para atividade contra larvas de Aedes aegypti, na concentração única de 500 mg / mL. Os extratos metanólicos foram, em geral, os que apresentaram maior atividade larvicida. Os seguintes 7 extratos metanólicos das (partes das) espécies vegetais indicadas foram os mais ativos, provocando 100% de mortalidade em larvas de A. aegypti: Tapura amazonica Poepp. (raiz), Piper aduncum L. (folha e raiz), P. tuberculatum Jacq. (folha, fruto e galho) e Simaba polyphylla (Cavalcante) W.W. Thomas (galho).

Chemical constituents of Simarouba versicolor

From the roots, stems and fruits of Simarouba versicolor (Simaroubaceae) were isolated quassinoids (3, 5-7), triterpenoids (8-14), a mixture of steroids (15-17), the flavonoid kaempferol (18) and the squalene derivative 11,14-diacetoxy-7,10; 15,18-diepoxy-6,19-dihidroxy-6,7,10,11,14,15,18,19-octahydrosqualene (19). Spectral data were used for structural characterization

Autenticación citohistológica de cuatro plantas medicinales nativas / Cytohistological authentication of four native medicinal plants

El objetivo del presente trabajo de tesis fue autentificar citohistológicamente 4 plantas utilizadas como antimicrobiana y a las cuales se les ha comprobado esta actividad farmacolóica. El estudio identificó las características citohistológicas de los órganos de las siguientes plantas medicinales: folios de Simarouba glauca DC. (aceituna), hoja de Psidium Guajava L. (guayaba), hojas de Tagetes lucida Cav. (pericón) y corteza de Byrsonima crassifolia L. (nance).