Potencial alelopático de cinco espécies da família Annonaceae

Allelopathy refers to the ability that certain plant has to interfere in the metabolism of another by substances released into the environment, causing harmful or beneficial effects. The aim of this work was to evaluate the allelopathic effects of metanolic extracts from shoots (leaves and stems) of Annona crassiflora, A. coriacea, A. dioica, A. sylvatica and Duguetia furfuracea (Annonaceae), at 1% (m/v) concentration on germination and early growth of lettuce seedlings. Treatments consisted of three replicates of 25 lettuce seeds distributed in Petri dishes containing two sheets of germitest paper and 3 mL of extracts, maintained at 25ºC with white light. The control treatment was only watered with distilled water. The counting of normal seedlings, time of germination and length of radicle and hypocotyl were evaluated at four and seven days after sowing. Extracts were characterized about pH and phytochemical prospection. The methanolic extracts from Annonaceae altered all the parameters analyzed, significantly reducing the germination percentage and vigor of lettuce seeds and affecting adversely the time of germination in relation to the control. Extracts also caused radicle and hypocotyls growth inhibition.Alelopatia se refere à capacidade que determinada planta tem de interferir no metabolismo de outra, por meio de substâncias liberadas no ambiente, causando efeitos danosos ou benéficos. O objetivo deste trabalho foi avaliar os efeitos alelopáticos de extratos metanólicos da parte aérea (folhas e caules) de Annona crassiflora, A. coriacea, A. dioica, A. sylvatica e Duguetia furfuracea (Annonaceae), na concentração de 1% (m/v) sobre a germinação e no crescimento inicial de plântulas de alface. Os testes foram realizados em triplicatas com 25 sementes de alface distribuídas em placas de Petri contendo duas folhas de papel germitest e 3 mL dos extratos, mantidas a 25ºC sob luz branca constante. Água destilada foi utilizada no tratamento controle. A contagem das plântulas normais, o tempo médio de germinação e comprimento de radícula e de hipocótilo foram avaliados aos quatro e sete dias após a semeadura. Os extratos foram caracterizados quanto ao pH e perfil fitoquímico. Os extratos metanólicos das plantas de Annonaceae alteraram todos os parâmetros analisados, reduzindo significativamente a porcentagem de germinação e o vigor de sementes de alface, além de afetarem negativamente o tempo médio de germinação em relação ao controle. Os extratos também causaram inibições no comprimento radicular e de hipocótilo

Effect of 1-(phenyl)-N’-(4-methoxybenzylidene)-9H-pyrido[3,4-b]indole-3-carbohydrazide on in vitropoliovirus replication

The effect of the alkaloid, 1-(phenyl)-N’-(4-methoxybenzylidene)-9H-pyrido[3,4-b]indole-3-carbohydrazide (PMC)on poliovirus (PV) replication cycle in Vero cells was assayed by inhibition of the cytopathic effect (CPE) and inhibition of plaque forming units (PFU). Both methodologies suggested that the mode of action was avoidance of infection progression in the host cell. The compound was able to prevent CPE and PFU formation when the cells were pretreated with PMC for 24 h prior to PV infection. In addition, when the alkaloid was continuously maintained in the infected cultures, the spread of PV to adjacent cells was impaired. The pre-exposure and post-exposure prophylactic applications are possible situations in which an anti-PV drug might be used. Future studies are needed to elucidate the PMC mode of action and verify the feasibility of PMC use of in vivo. No antipicornavirus agent is currently approved for clinical use

Synthesis, Antiproliferative Activity And Molecular Properties Predictions Of Galloyl Derivatives.

The present study was designed to investigate the in vitro antiproliferative activity against ten human cancer cell lines of a series of galloyl derivatives bearing substituted-1,3,4-oxadiazole and carbohydrazide moieties. The compounds were also assessed in an in silico study of the absorption, distribution, metabolism and excretion (ADME) in the human body using Lipinski's parameters, the topological polar surface area (TPSA) and percentage of absorption (%ABS). In general, the introduction of N'-(substituted)-arylidene galloyl hydrazides 4-8 showed a moderate antitumor activity, while the 2-methylthio- and 2-thioxo-1,3,4-oxadiazol-5-yl derivatives 9 and 10 led to increased inhibition of cancer cell proliferation. The precursor compound methyl gallate 2 and the intermediary galloyl hydrazide 3 showed greater antiproliferative activity with GI50 values < 5.54 µM against all human tumor cell lines tested. A higher inhibition effect against ovarian cancer (OVCAR-3) (GI50 = 0.05-5.98 µM) was also shown, with compounds 2, 3, 9 and 10 with GI50 ≤ 0.89 µM standing out in this respect. The in silico study revealed that the compounds showed good intestinal absorption.205360-537

Synthesis, antitumor and antimicrobial activity of novel 1-substituted phenyl-3-[3-alkylamino(methyl)-2-thioxo-1,3,4-oxadiazol-5-yl] &#946;-carboline derivatives

With the purpose of activity enhancement of 1-substituted phenyl-3-(2-thioxo-1,3,4-oxadiazol-5-yl) &#946;-carbolines 1a-c, reported as potential antitumor agents in our previous study, herein we report the synthesis and antitumor activity evaluation of several novel Mannich bases 2-7(a-c), by the introduction of different alkylamino(methyl) groups in the 1,3,4-oxadiazole unity of 1a-c. The antimicrobial activities of 1a-c and of 2-7(a-c) were also evaluated. Additionally, an in silico study of the ADME properties of novel synthesized &#946;-carboline derivatives 2-7(a-c) was performed by evaluation of their Lipinski's parameters and topological polar surface area (TPSA) and percentage of absorption (% ABS) data.Com o propósito de aumentar a atividade anticâncer demonstrada anteriormente pelas 1-fenilssubstituído-3-(2-tioxo-1,3,4-oxadiazol-5-il) &#946;-carbolinas 1a-c, neste trabalho foram realizadas a síntese e a avaliação in vitro da atividade antitumoral de novas bases de Mannich 2-7(a-c), derivadas da introdução de diferentes grupos alquilamino(metil) na unidade 1,3,4-oxadiazol de 1a-c. Os derivados 1a-c e 2-7(a-c) foram também avaliados quanto às atividades antibacteriana e antifúngica. Adicionalmente, um estudo in silico das propriedades de ADME dos novos compostos sintetizados 2-7(a-c) foi realizado pela avaliação de seus parâmetros de Lipinski e de dados de área de superfície topológica polar (TPSA) e de porcentagem de absorção (% ABS).288298Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES

Chemical composition and anti-inflammatory activity of the essential oil of Schinus terebinthifolius Raddi (Anacardiaceae) fruits

Traditional usage of Schinus terebinthifolius Raddi, popularly known as Brazilian pepper, includes the treatment of inflammatory diseases. Chemical composition of the essential oil extracted of fruits of S. terebinthifolius collected in Mato Grosso do Sul was investigated and the anti-inflammatory activity was evaluated. The essential oil (EOST) obtained in Clevenger and analyzed by GC-MS, exhibited predominance of monoterpenes. The oral administration of EOST significantly inhibited, in dose dependent manner, the carrageenan (Cg) induced rat paw oedema. The observed inhibitions after two hours of Cginjection were 57 ± 8% (100 mg kg-1) for EOST and 66 ± 6% for dexamethasone (DEXA). In another model of inflammation, the oral administration of EOST (100 mg kg-1) reduced 56 ± 11% while DEXA inhibited about 91 ± 5% the Cg-induced leukocyte migration in the air pouch model. Finally, in the persistent inflammation induced by complete Freund's adjuvant (CFA), the daily oral treatment with EOST (200 mg/kg) inhibited 33 ± 6% in 4 days after injection of CFA. The essential oil (EOST) exhibited a marked anti-inflammatory activity and these response profiles differ from others oils collected in different places.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Free radical scavenging and anti-edematogenic activities of essential oil obtained from trichilia silvatica dc. (meliaceae) leaves

The present study was focused in evaluating the chemical composition, the anti-edematogenic and antioxidant activities of essential oil obtained from Trichilia silvatica (EOTS) leaves. The EOTS was extracted by hydrodistillation and their analyses were performed by GC/MS. The main compounds identified in the EOTS were sesquiterpenes. Furthermore, the EOTS exhibited antioxidant and in vivo anti-inflammatory activity. The oral administration of EOTS (100 and 300 mg/kg), significantly inhibited the carrageenan (Cg) induced rat paw edema. The observed inhibitions were 54 ± 7 and 49 ± 6 % (100 mg/kg) for EOTS and 68 ± 6 % and 66 ± 11 % for dexamethasone after 2 and 4 h after Cg-injection, respectively. In conclusion, the present work showed for the first time, that the anti-inflammatory effects of essential oil seem to be mainly associated with the high levels of sesquiterpene in the leaves of this plant.Colegio de Farmacéuticos de la Provincia de Buenos Aire

PRODUÇÃO DE BIOMASSA E CONTEÚDO DE FENÓIS E FLAVONOIDES DE Schinus terebinthifolius CULTIVADA EM FILEIRA SIMPLES E DUPLA COM CAMA DE FRANGO

The aim of this study was to evaluate the influence of the addition of poultry litter on growth, biomass yield, flavonoid and phenol content, and antioxidant activity in leaves of pink pepper. The experiment was carried out at the Federal University of Grande Dourados, in Dourados, Mato Grosso do Sul state, from October 2009 to May 2010. Pink pepper was grown in single or double row in soil with incorporated poultry litter at doses of 0, 5, 10, 15 and 20 t ha-1. Treatments were arranged as 2 x 5 factorial in a randomized block design with four replications. There was a significant interaction between the doses of poultry litter and evaluation times for plant height and chlorophyll content. A linear increase in leaf area, fresh and dry weight of leaves and diameter of main stems with increasing doses of poultry litter was observed. Plants grown in single row showed higher fresh weight of stem with increasing doses of poultry litter. Poultry litter at 15 and 20 t ha-1 promoted an increase in flavonoid and phenolic contents in the leaves. No significant effect on the antioxidant activity was observed by the chemical method using DPPH. Therefore, it is recommended the cultivation of pink pepper plants with double row and 20 t ha-1 of poultry litter to higher growth, biomass yield, and flavonoid and phenol content.O objetivo deste estudo foi avaliar a influência da adição da cama de frango ao solo sobre o crescimento, produção de biomassa, conteúdo de fenóis e flavonoides e atividade antioxidante em folhas de pimenta-rosa. O experimento foi realizado na Universidade Federal da Grande Dourados, em Dourados-MS, de outubro de 2009 a maio de 2010. A pimenta-rosa foi cultivada em fileira simples e dupla com cama de frango incorporada nas doses de 0, 5, 10, 15 e 20 t ha-1. Os tratamentos foram arranjados em fatorial 2 x 5 em blocos casualizados com quatro repetições. Houve uma interação significativa entre doses de cama de frango e épocas de avaliação para altura de plantas e conteúdo de clorofila. Foi observado um aumento linear na área foliar, massa fresca e seca de folhas e diâmetro dos ramos principais com o aumento das doses de cama de frango. As plantas cultivadas em fileira simples apresentaram maior massa fresca de caules com o aumento das doses de cama de frango. A cama de frango nas doses de 15 e 20 t ha-1 promoveu um incremento no conteúdo de fenóis e flavonoides nas folhas. Nenhum efeito significativo na atividade antioxidante foi observado com o método químico utilizando DPPH. Portanto, recomenda-se o cultivo de plantas de pimenta-rosa em fileira dupla e 20 t ha-1 de cama de frango para maior crescimento, produção de biomassa, e conteúdo de fenóis e flavonoides

PRODU\uc7\uc3O DE BIOMASSA E CONTE aDO DE FEN 3IS E FLAVONOIDES DE Schinus terebinthifolius CULTIVADA EM FILEIRA SIMPLES E DUPLA COM CAMA DE FRANGO

The aim of this study was to evaluate the influence of the addition of poultry litter on growth, biomass yield, flavonoid and phenol content, and antioxidant activity in leaves of pink pepper. The experiment was carried out at the Federal University of Grande Dourados, in Dourados, Mato Grosso do Sul state, from October 2009 to May 2010. Pink pepper was grown in single or double row in soil with incorporated poultry litter at doses of 0, 5, 10, 15 and 20 t ha-1. Treatments were arranged as 2 x 5 factorial in a randomized block design with four replications. There was a significant interaction between the doses of poultry litter and evaluation times for plant height and chlorophyll content. A linear increase in leaf area, fresh and dry weight of leaves and diameter of main stems with increasing doses of poultry litter was observed. Plants grown in single row showed higher fresh weight of stem with increasing doses of poultry litter. Poultry litter at 15 and 20 t ha-1 promoted an increase in flavonoid and phenolic contents in the leaves. No significant effect on the antioxidant activity was observed by the chemical method using DPPH. Therefore, it is recommended the cultivation of pink pepper plants with double row and 20 t ha-1 of poultry litter to higher growth, biomass yield, and flavonoid and phenol content.O objetivo deste estudo foi avaliar a influ\ueancia da adi\ue7\ue3o da cama de frango ao solo sobre o crescimento,produ\ue7\ue3o de biomassa, conte\ufado de fen\uf3is e flavonoides e atividade antioxidante em folhas de pimentarosa. O experimento foi realizado na Universidade Federal da Grande Dourados, em Dourados-MS, de outubro de 2009 a maio de 2010. A pimenta-rosa foi cultivada em fileira simples e dupla com cama de frango incorporada nas doses de 0, 5, 10, 15 e 20 t ha-1. Os tratamentos foram arranjados em fatorial 2 x 5 em blocos casualizados com quatro repeti\ue7\uf5es. Houve uma intera\ue7\ue3o significativa entre doses de cama de frango e \ue9pocas de avalia\ue7\ue3o para altura de plantas e conte\ufado de clorofila. Foi observado um aumento linear na \ue1rea foliar, massa fresca e seca de folhas e di\ue2metro dos ramos principais com o aumento das doses de cama de frango. As plantas cultivadas em fileira simples apresentaram maior massa fresca de caules com o aumento das doses de cama de frango. A cama de frango nas doses de 15 e 20 t ha-1 promoveu um incremento no conte\ufado de fen\uf3is e flavonoides nas folhas. Nenhum efeito significativo na atividade antioxidante foi observado com o m\ue9todo qu\uedmico utilizando DPPH. Portanto, recomenda-se o cultivo de plantas de pimenta-rosa em fileira dupla e 20 t ha-1 de cama de frango para maior crescimento, produ\ue7\ue3o de biomassa, e conte\ufado de fen\uf3is e flavonoides

Evaluation of Antioxidant Activity, Total Flavonoids, Tannins and Phenolic Compounds in Psychotria Leaf Extracts

The antioxidant activity of Psychotria carthagenensis, P. leiocarpa, P. capillacea and P. deflexa (Rubiaceae) extracts were investigated, and the concentrations of total phenolics, flavonoids, condensed tannins and flavonols were determined. The chemical compositions of the extracts were investigated using the high performance liquid chromatography (HPLC/PAD) method. We used 1,1-diphenyl-1-picrylhydrazyl free radical (DPPH), β-Carotene bleaching and 2,2-azinobis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical cations to determine antioxidant activity. The ability to scavenge radical was measured in these experiments by the discoloration of the solution. Concentrations of constituents were measured spectrophotometrically. P. carthagenensis and P. capillacea exhibited the highest antioxidant activity, in the DPPH test, β-carotene bleaching and ABTS system. The highest phenolic, flavonoid, condensed tannin and flavonol concentration was found in P. carthagenensis and P. capillacea extracts. HPLC-PDA analysis of P. carthagenensis and P. capillacea revealed hydroxycinnamic acid (p-coumaric acid). This is the first report on the antioxidant properties and constituent analysis of these Psychotria extracts