Synthesis and Antileukemic Activity of Novel 2-(4-(2,4-dimethoxybenzoyl)phenoxy)-1-(4-(3-(piperidin-4-yl)propyl)piper idin-1-yl)ethanone Derivatives

A series of novel 2-(4-(2,4-dimethoxybenzoyl)phenoxy)-1-(4-(3-(piperidin-4-yl)propyl) piperidin-1-yl)ethanone derivatives 9(ae) and 10(ag) were synthesized and characterized by 1H NMR, IR, mass spectral, and elemental analysis. These novel compounds were evaluated for their antileukemic activity against two human leukemic cell lines (K562 and CEM) by using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazoliumbromide assay. Some of the tested compounds showed good antiproliferative activity with IC50 values ranging from 1.6 to 8.0 mu m. Compound 9c, 9e, and 10f with an electron-withdrawing halogen substituent at the para position on the phenyl ring showed excellent in vitro potency against tested human leukemia cells (K562 and CEM).

Piper and Vismia Species from Colombian Amazonia Differentially Affect Cell Proliferation of Hepatocarcinoma Cells

There is an increasing interest to identify plant-derived natural products with antitumor activities. In this work, we have studied the effects of aqueous leaf extracts from Amazonian Vismia and Piper species on human hepatocarcinoma cell toxicity. Results showed that, depending on the cell type, the plants displayed differential effects; thus, Vismia baccifera induced the selective killing of HepG2, while increasing cell growth of PLC-PRF and SK-HEP-1. In contrast, these two last cell lines were sensitive to the toxicity by Piper krukoffii and Piper putumayoense, while the Piperaceae did not affect HepG2 growth. All the extracts induced cytotoxicity to rat hepatoma McA-RH7777, but were innocuous (V. baccifera at concentrations < 75 mu g/mL) or even protected cells from basal death (P. putumayoense) in primary cultures of rat hepatocytes. In every case, cytotoxicity was accompanied by an intracellular accumulation of reactive oxygen species (ROS). These results provide evidence for the anticancer activities of the studied plants on specific cell lines and suggest that cell killing could be mediated by ROS, thus involving mechanisms independent of the plants free radical scavenging activities. Results also support the use of these extracts of the Vismia and Piper genera with opposite effects as a model system to study the mechanisms of the antitumoral activity against different types of hepatocarcinoma.

Studies on the content variation of chemical constituents during the combination of ginseng with veratrum nigrum by ESI-MS and HPLC-ESI-MS

To study the content variation of ginsenosides and alkaloids during combination of ginseng with veratrum nigrum, the ginsenosides and alkaloids in the decoction of ginseng with veratrum nigrum were analyzed and compared by high performance liquid chromatography-electrospray ionization-mass spectrometry (HPLC-ESI-MS) and electrospray ionization-mass spectrometry (ESI-MS). In the compatible decoction, eight ginsenosides and eight alkaloids. were detected, and the contents of six ginsenosides were found to be reduced, on the contrary, the contents of six alkaloids were increased. During combination of ginseng with veratrum nigrum, the contents of ginsenosides were reduced and those of the toxic alkaloids were increased. From the chemical point of view, the traditional theory is right that ginseng and veratrum nigrum are incompatible with each other.

A murcha-bacteriana (Ralstonia solanacearum) em pimenta longa (Piper hispidinervium).

A murcha-bacteriana é a principal doença vascular de plantas em todo o mundo. É causada pela bactéria Ralstonia solanacearum e ocorre em todas as regiões do Brasil, principalmente nas regiões Norte, Nordeste e Centro-Oeste em que predominam temperaturas e umidades elevadas

Protocolo de avaliação isoenzimática para a pimenta longa (Piper hispidinervum).

Considerando o alto valor comercial do safrol, bem como a ocorrência natural de pimenta longa no Acre, esta espécie poderá constituir-se em mais uma alternativa econômica de produção para os pequenos, médios e grandes produtores do Estado. Sendo uma espécie pouco conhecida geneticamente, desenvolveu-se um protocolo de análise isoenzimática com o objetivo de avaliar a estrutura genética e distribuição da variabilidade genética entre as populações nativas da espécie, visando traçar uma estratégia de coleta de material vegetal mais adequada para conservação da variabilidade ex situ e detectar populações superiores com relação aos teores de safrol, rendimento em base livre de umidade, resistência a pragas e/ou doenças e outros parâmetros de interesse.

Manejo de capoeira com alta densidade de pimenta longa (Piper hispidinervum) em área de assentamento extrativista no Acre.

O objetivo deste trabalho é gerar conhecimento quanto ao comportamento ecológico da Pimenta longa e propor técnicas de manejo que assegurem a exploração das populações nativas em bases autossustentadas, garantindo o uso e a conservação desse recurso. Com isso, espera-se oferecer uma alternativa para a diversificação do produto, especialmente nas Reservas Extrativistas, visando sua sustentabilidade econômica. Os estudos estão sendo desenvolvidos no Projeto de Assentamento Extrativista Chico Mendes (seringal Cachoeira), onde foi instalada uma unidade piloto de manejo da espécie.

Potencialidades da pimenta-de-macaco (Piper aduncum L.): características gerais e resultados de pesquisa.

A diversidade da flora brasileira, em especial a da Região Amazônica, apresenta um imenso potencial para a produção de compostos secundários de plantas, que têm sido demandados continuamente pela indústria nas últimas décadas, devido ao incremento da utilização de produtos naturais na agropecuária. Estima-se que existam 500 mil espécies de plantas no mundo, sendo .16% delas encontradas na florésta amazônica. No entanto, a pesquisa de substâncias ativas derivadas de plantas no Brasil ainda é muito incipiente. Mesmo considerando os incrementos significativos da pesquisa nas últimas duas décadas, há, evidentemente, uma grande lacuna de conhecimento da nossa flora a ser preenchida. A partir da década de 90 a Embrapa Acre vem intensificando atividades de pesquisa no sentido de viabilizar a utilização de recursos não-madeireiros das florestas do Acre. Destacam-se dentre eles, produtos promissores oriundos de piperáceas, como o óleo essencial rico em safrol, produzido a partir da biomassa da Piper hispidinervum e, mais recentemente, o óleo essencial de P. aduncum com altos teores de dilapiol. P. aduncum é uma espécie de planta que vem apresentando um crescente interesse, principalmente quanto à extração em escala industrial do seu óleo essencial. A elaboração deste documento tem como finalidade contribuir para o conhecimento da potencialidade do emprego dessa planta na elaboração de produtos para o controle de pragas de interesse agropecuário e utilização na medicina humana.

Pied Piper of Hamelin due date card

This is a due date card for the book titled Pied Piper of Hamelin, with stamped dates from 1939-1940.

Chill unit models for blackcurrant (Ribes nigrum L.) cultivars 'Ben Gairn', 'Ben Hope' and 'Ben Tirran'

Temperate-zone crops require a period of winter chilling to terminate dormancy and ensure adequate bud break the following spring. The exact chilling requirement of blackcurrant (Ribes nigrum), a commercially important crop in northern Europe, is relatively unknown. Chill unit models have been successfully utilized to determine the optimum chilling temperature of a range of crops, with one chill unit equating to I h exposure to the optimum temperature for chill satisfaction. Two-year-old R. nigrum plants of the cultivars 'Ben Gairn', 'Ben Hope' and 'Ben Tirran' were exposed to temperatures of -10.1 degrees C. -3.4 degrees C. 0.1 degrees C, 1.5 degrees C, 2.1 degrees C, 3.4 degrees C or 8.9 degrees C (+/- 0.7 degrees C) for durations of 0, 2, 4, 6, 8 or 10 weeks and multiple regression analyses used to determine the optimum temperature for chill satisfaction. (C) 2009 Elsevier B.V. All rights reserved.

Effect of a cellulase treatment on extraction of antioxidant phenols from black currant (Ribes nigrum L.) pomace

The effect of a commercial cellulase preparation on phenol liberation and extraction from black currant pomace was studied. The enzyme used, which was from Trichoderma spp., was an effective "cellulase-hemicellulase" blend with low P-glucosidase activity and various side activities. Enzyme treatment significantly increased plant cell wall polysaccharide degradation as well as increasing the availability of phenols for subsequent methanolic extraction. The release of anthocyanins and other phenols was dependent on reaction parameters, including enzyme dosage, temperature, and time. At 50 degrees C, anthocyanin yields following extraction increased by 44% after 3 h and by 60% after 1.5 h for the lower and higher enzyme/substrate ratio (E/S), respectively. Phenolic acids were more easily released in the hydrolytic mixture (supernatant) and, although a short hydrolysis time was adequate to release hydroxybenzoic acids (HBA), hydroxycinnamic acids (HCA) required longer times. The highest E/S value of 0.16 gave a significant increase of flavonol yields in all samples. The antioxidant capacity of extracts, assessed by scavenging of 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) radical cation, the oxygen radical absorbance capacity, and the ferric reducing antioxidant potential depended on the concentration and composition of the phenols present.

Extraction of polyphenols from processed black currant (Ribes nigrum L.) residues

The total phenol and anthocyanin contents of black currant pomace and black currant press residue (BPR) extracts, extracted with formic acid in methanol or with methanol/water/acetic acid, were studied. Anthocyanins and other phenols were identified by means of reversed phase HPLC, and differences between the two plant materials were monitored. In all BPR extracts, phenol levels, determined by the Folin-Ciocalteu method, were 8-9 times higher than in the pomace extracts. Acid hydrolysis liberated a much higher concentration of phenols from the pomace than from the black currant press residue. HPLC analysis revealed that delphinidin-3-O-glucoside, delphinidin-3-O-rutinoside, cyanidin-3-O-glucoside, and cyanidin-3-O-rutinoside were the major anthocyanins and constituted the main phenol class (approximate to 90%) in both types of black currant tissues tested. However, anthocyanins were present in considerably lower amounts in the pomace than in the BPR. In accordance with the total phenol content, the antioxidant activity determined by scavenging of 2,2'-azinobis(3-ethylbenzothiazoline-6- sulfonic acid) radical cation, the ABTS(center dot+) assay, showed that BPR extracts prepared by solvent extraction exhibited significantly higher (7-10 times) radical scavenging activity than the pomace extracts, and BPR anthocyanins contributed significantly (74 and 77%) to the observed high radical scavenging capacity of the corresponding extracts.

The influence of geographic origin and food type on the susceptibility of Callosobruchus maculatus (Fabricius) to Piper guineense (Schum and Thonn)

The tolerance of Callosobruchus maculatus from different geographical locations reared on two cowpea varieties, pale brown Ife Brown (IFBV) and dark brown IAR48 (IAR48V), to seed powder of Piper guineense (Schum and Thonn) was investigated. C. maculatus populations were collected from nine different locations across Osun state in the South Western part of Nigeria. The main and interactive effects of cowpea variety, population origin and dose on C. maculatus tolerance to P. guineense were explored. It was observed that bruchids that emerged from IAR48V had greater tolerance of P. guineense than bruchids reared on IFBV. There were significant effects (P < 0.001) of cowpea variety, population and dose, and significant interactions among these factors (except variety � dose, P > 0.05) on the response of bruchids to P. guineense. When reared on IAR48V, bruchid populations from the North-Eastern part of the state show greater tolerance to P. guineense than their counterparts from the SoutheWest. This study underscores the importance of knowledge of the origin of the population and the cowpea variety on which C. maculatus developed when managing bruchids damage using P. guineense

Composition and antifungal activity against Candida albicans, Candida parapsilosis, Candida krusei and Cryptococcus neoformans of essential oils from leaves of Piper and Peperomia species

This study was addressed to investigate the composition and antifungal activity of essential oils from leaves of Piperaceae species (Piper aduncum, Piper amalago, Piper cernuum, Piper diospyrifolium, Piper crassinervium, Piper gaudichaudianum, Piper solmsianum, Piper regnellii, Piper tuberculatum, Piper umbelata and Peperomia obtusifolia) against Candida albicans, C. parapsilosis, C. krusei and Cryptococcus neoformans. The essential oils from P. aduncum, P. gaudichaudianum and P. solmsianum showed the highest antifungal activity against Cryptococcus neoformans with the MIC of 62.5, 62.5 and 3.9 mg.mL-1, respectively. The oil from P. gaudichaudianum showed activity against C. krusei with MIC of 31.25 mg.mL-1.