Dopaminergic profile of new heterocyclic N-phenylpiperazine derivatives

Dopamine constitutes about 80% of the content of central catecholamines and has a crucial role in the etiology of several neuropsychiatric disorders, including Parkinson's disease, depression and schizophrenia. Several dopaminergic drugs are used to treat these pathologies, but many problems are attributed to these therapies. Within this context, the search for new more efficient dopaminergic agents with less adverse effects represents a vast research field. The aim of the present study was to report the structural design of two N-phenylpiperazine derivatives, compound 4: 1-[1-(4-chlorophenyl)-1H-4-pyrazolylmethyl]-4-phenylhexahydropyrazine and compound 5: 1-[1-(4-chlorophenyl)-1H-1,2,3-triazol-4-ylmethyl]-4-phenylhexahydropyrazine, planned to be dopamine ligands, and their dopaminergic action profile. The two compounds were assayed (dose range of 15-40 mg/kg) in three experimental models: 1) blockade of amphetamine (30 mg/kg, ip)-induced stereotypy in rats; 2) the catalepsy test in mice, and 3) apomorphine (1 mg/kg, ip)-induced hypothermia in mice. Both derivatives induced cataleptic behavior (40 mg/kg, ip) and a hypothermic response (30 mg/kg, ip) which was not prevented by haloperidol (0.5 mg/kg, ip). Compound 5 (30 mg/kg, ip) also presented a synergistic hypothermic effect with apomorphine (1 mg/kg, ip). Only compound 4 (30 mg/kg, ip) significantly blocked the amphetamine-induced stereotypy in rats. The N-phenylpiperazine derivatives 4 and 5 seem to have a peculiar profile of action on dopaminergic functions. On the basis of the results of catalepsy and amphetamine-induced stereotypy, the compounds demonstrated an inhibitory effect on dopaminergic behaviors. However, their hypothermic effect is compatible with the stimulation of dopaminergic function which seems not to be mediated by D2/D3 receptors

Atividade antibacteriana de extratos de erva mate (Ilex paraguariensis A.St.-Hil.) Antibacterial activity of yerba mate (Ilex paraguariensis A.St.-Hil.) extracts

Através de testes de diluição, em sistema de tubos múltiplos, determinou-se a intensidade de atividade de inibição bacteriana (IINIB) e intensidade de atividade de inativação bacteriana (IINAB) de extratos hídricos (decocto), etanólicos (alcoolatura e hidroalcoolatura) de cambitos e de folhas de Ilex paraguariensis A.St.-Hil.(Aquifoliaceae) sobre as bactérias Staphylococcus aureus (ATCC 25.923), Enterococcus faecalis (ATCC 19.433), Salmonella enteritidis (ATCC 11.076) e Escherichia coli (ATCC 11.229). Todas as formas de extração apresentaram capacidade de inativação e/ou inibição seletivas sobre as bactérias avaliadas, porém os extratos originados por destilação etanólica apresentaram os melhores resultados. Salmonella enteritidis demonstrou maior sensibilidade, seguida por Enterococcus faecalis. Posteriormente, estes dois agentes foram submetidos a testes de suspensão, no mesmo sistema, na presença e ausência de matéria orgânica (soro bovino), sob controle do fator tempo. A presença de matéria orgânica diminuiu, enquanto o tempo de exposição aumentou a sensibilidade de Salmonella enteritidis e de Enterococus faecalis aos diferentes extratos de Ilex testados.<br>Dilution tests in multiple tube system were employed to evaluate the intensity of bacterial inhibition activity (IINIB) and bacterial inactivation activity (IINAB) of aqueous extracts (decoctions) and ethanolic extracts (alcoholic and hydroalcoholic extracts) from "cambitos" of Ilex paraguariensis St. Hil. (Aquifoliaceae) leaf on the bacteria Staphylococcus aureus (ATCC 25.923), Enterococcus faecalis (ATCC 19.433), Salmonella enteritidis (ATCC 11.076), and Escherichia coli (ATCC 11.229). All extraction procedures presented selective inactivation and/or inhibition capacity on the evaluated bacteria; however, extracts from ethanolic distillation yielded the best results. Salmonella enteritidis had the highest sensitivity, followed by Enterococus faecalis. Later, such agents were subjected to suspension tests, in the same system, in absence or presence of organic matter (bovine serum), under controlled time. Salmonella enteritidis and Enterococus faecalis sensitivity to the different tested Ilex extracts decreased in the presence of organic matter and increased with exposure time

Caracterização de frutos e sementes em acessos de maracujá silvestre (Passiflora foetida L.) Characterization of fruits and seeds of wild passion fruit (Passiflora foetida L.).

A espécie Passiflora foetida L.é uma trepadeira exótica cujas folhas e frutos possuem propriedades medicinais. No Brasil, a erva é utilizada na forma de extratos ou emplastros para erisipelas e doenças de pele com inflamação. O objetivo deste trabalho foi caracterizar cinco acessos de Passiflora foetida L. baseados em 17 descritores morfológicos O experimento foi conduzido em casa de vegetação em delineamento inteiramente ao acaso, com 15 repetições por genótipo. As variáveis analisadas foram cor da casca do fruto, formato do fruto, comprimento do fruto, diâmetro do fruto, massa fresca do fruto, comprimento do pedicelo, cor da polpa do fruto, espessura da casca, acidez titulável, sólidos solúveis, potencial hidrogeniônico, razão sólidos solúveis/ acidez titulável, comprimento da semente, diâmetro da semente, espessura da semente, massa fresca das sementes e o número de sementes por fruto. Os dados foram submetidos à análise de variância e teste de médias pelo teste Tukey a 5% de probabilidade. Houve diferença significativa pelo teste F a 5% de probabilidade, entre os genótipos para quase todas as características com exceção da espessura da casca, massa fresca do fruto, comprimento da semente e massa fresca das sementes. A característica que apresentou maior variação foi o teor de sólidos solúveis. E entre os genótipos, o acesso 5 foi o que apresentou as maiores médias pelo teste de Tukey a 5% de probabilidade, em todas as características analisadas, podendo ser utilizado em programas de melhoramento da espécie.<br>The species Passiflora foetida L. é an exotic vine, which leaves and fruit have medicinal properties. In Brazil, the herbis used in the form of extracts or poultices for erysipelas and skin diseases with inflammation. The aim of this study was to characterize five Passiflora foetida L. accessions based on 17 morphological descriptors The experiment was conducted in a greenhouse in a completely randomized design with 15 replicates per genotype. The variables were the fruit skin color, fruit shape, fruit length, fruit diameter, fresh fruit, length of pedicel, flesh color of the fruit, skin thickness, acidity, soluble solids, hydrogen potential ratio soluble solids / acidity, seed length, seed diameter, thickness of seed, fresh seed and seed number per fruit. The data were submitted to analysis of variance and the means were compared by Tukey test at 5% of probability. There was a significant difference by F test at 5%,of probability among the genotypes for nearly all traits, except the thickness of the shell, fresh fruit mass, seed length and fresh weight of seed. The variable that most variation was the soluble solids. The genotype 5 had the highest means by Tukey test at 5% of probability on all characteristics that can be used in breeding programs of the species