Pharmacological study of anti-allergic activity of Syzygium cumini (L) Skeels

Myrtaceae is a plant family widely used in folk medicine and Syzygium and Eugenia are among the most important genera. We investigated the anti-allergic properties of an aqueous leaf extract of Syzygium cumini (L.) Skeels (SC). HPLC analysis revealed that hydrolyzable tannins and flavonoids are the major components of the extract. Oral administration of SC (25-100 mg/kg) in Swiss mice (20-25 g; N = 7/group) inhibited paw edema induced by compound 48/80 (50 percent inhibition, 100 mg/kg; P <= 0.05) and, to a lesser extent, the allergic paw edema (23 percent inhibition, 100 mg/kg; P <= 0.05). SC treatment also inhibited the edema induced by histamine (58 percent inhibition; P <= 0.05) and 5-HT (52 percent inhibition; P <= 0.05) but had no effect on platelet-aggregating factor-induced paw edema. SC prevented mast cell degranulation and the consequent histamine release in Wistar rat (180-200 g; N = 7/group) peritoneal mast cells (50 percent inhibition, 1 æg/mL; P <= 0.05) induced by compound 48/80. Pre-treatment of BALB/c mice (18-20 g; N = 7/group) with 100 mg/kg of the extract significantly inhibited eosinophil accumulation in allergic pleurisy (from 7.662 ± 1.524 to 1.89 ± 0.336 x 10(6)/cavity; P <= 0.001). This effect was related to the inhibition of IL-5 (from 70.9 ± 25.2 to 12.05 ± 7.165 pg/mL) and CCL11/eotaxin levels (from 60.4 ± 8.54 to 32.8 ± 8.4 ng/mL) in pleural lavage fluid, using ELISA. These findings demonstrate an anti-allergic effect of SC, and indicate that its anti-edematogenic effect is due to the inhibition of mast cell degranulation and of histamine and serotonin effects, whereas the inhibition of eosinophil accumulation in the allergic pleurisy model is probably due to an impairment of CCL11/eotaxin and IL-5 production.

Aplicação de cromatografia centrífuga de contra-corrente na purificação de ácido ursólico das folhas de Eugenia brasiliensis Lam. / Aplication of counter-current chromatography in the purification of ursolic acid from leavesof Eugenia brasiliensis Lam.

Os ácidos triterpênicos são metabólitos comuns na família Myrtaceae, especialmente no gênero Eugenia. O ácido ursólico foi descrito como um dos principais constituintes, nas folhas de Eugenia brasiliensis, coletada no Sudoeste do Brasil. Uma partição prévia, por solventes, do extrato etanólico ou do extrato clorofórmico de E. brasiliensis, seguida por uma purificação por cromatografia de contra-corrente de alta velocidade (CCCAV), conduziu ao isolamento do ácido ursólico com alto grau de pureza (> 97 por cento). Esta substância, também foi isolada por cromatografia convencional de coluna aberta (rendimento de 0.22 por cento a partir do extrato etanólico), e caracterizada por 13C-RMN, GC-EM e co-injeção com padrão comercial em CG-DIC, na forma do éster metílico. A técnica de CCCAV, usualmente usada para triterpenos glicosilados, foi aqui aplicada para a aglicona. As fases móvel e estacionária, no experimento de CCCAV, foram geradas pela mistura de n-hexano : acetato de etila : metanol : água, na proporção 10:5:2,5:1. A seleção do sistema de solventes (fases estacionária e móvel) foi determinada pela máxima distribuição eqüitativa do ácido ursólico em ambas as fases, medida por densitometria e monitorada por cromatografia em camada delgada, CCD, usando-se ácido ursólico comercial como referência.

Triterpene acids are common metabolites in the Myrtaceae family, especially in the genus Eugenia. Ursolic acid was found in Eugenia brasiliensis collected in Southeastern Brazil. A previous solvent partition of the ethanol or chloroform extracts of the leavesof E. brasiliensis, followed by rapid high-speed counter-current chromatography (HSCCC) afforded ursolic acid in high purity (> 97 percent). This compound was also purified apart by conventional column chromatography (yield of 0.22 percent from the ethanolic extract) and characterized by 13C-NMR, GC-MS and co-injection of its methyl ester with standards in GC-FID. The HSCCC technique, usually applied to triterpene glycosides, was here applied successfully to an aglycone, to which examples are rarely described. The mobile and stationary phase for the HSCCC experiment were derived from the two-phase solvent system composed by n-hexane : ethyl acetate : methanol : water in the proportion of 10:5:2.5:1. The choice of the developing solvent system for optimum HSCCC separation was determined by TLC coupled to densitometric measurements of ursolic acid in both stationary and mobile phase, generated by the upper and lower layer of the system above. Commercial ursolic acid was used as standard.

Peripheral modulation of pain in conscions guinea pigs: effect of morphine nalorphine and clonidine

Morphine and nalorphine were shown to have a peripheral effect on conscious guinea pigs, producing a decrease in the vocalization response to noxious electrical stimulation. Naloxone antagonized the effect of morphine and nalorphine. Locally administered clonidine had a peripheral effect on conscious guinea pigs, producing a decrease in the vocalization response to noxious electrical stimulation. The peripheral analgesia of clonidine was antagonized by yohimbine and naloxone. The analgesic effect clonidine was 250-300 times more potent than that of lidocaine. It is suggested that alfa2-adrenergic receptor agonists may active enkephalin-like substances released at the peripheral level

O uso da bromoergocriptina no tratamento da infertilidade. / The use of bromoergocriptine in the treatment of infertility

Sessenta pacientes inferteis e hiperprolactinemicas tratadas pela bromoergocriptina foram estudadas em dois grupos um de 35 pacientes, que engravidaram durante ou nas quatro primeiras semanas apos o termino do tratamento, e outro de 25 pacientes, que engravidaram entre cinco e 70 semanas apos o termino do tratamento. O primeiro grupo era composto de seis pacientes com ciclo ovulatorio normal, 10 com ciclo anovulatorio, das quais cinco com ovarios policisticos, e 19 com ciclo ovulatorio mas com deficiencia secretora de progesterona ou estrogenios. O segundo grupo era composto de uma paciente com ciclo ovulatorio normal, cinco com ciclo anovulatorio, das quais duas com ovarios policisticos, e 19 com deficiencia secretora ou de estrongenios. Nois dois grupos a posologia utilizada da bromoergocriptina unica terapeutica instituida, variou entre 2,5 e 7,5mg por dia, de acordo com o necessario para reduzir os niveis de prolactina. As gestacoes do total das pacientes assim evoluiram: 50% , ate o termo; 8,5% terminaram em parto prematuro; 8,5%, em abortamento: ha 33% em evolucao. Nenhuma gravidez ectopica foi registrada

Infertilidade: conceito, etiopatologia e diagnostico. / Infertility: concept, etiopathology and diagnosis

O autor discute conceito, etiopatologia e diagnostico da infertilidade. Distinguem-se tres entidades nosologicas: o aborto habitual ou de repeticao, a morte fetal precoce e a morte fetal tardia. Relacionam-se todas as causas etiopatogenicas conforme os periodos da fertilizacao, nidacao e desenvolvimento, e no final discutem-se fatores psicogenicos e o coito como outras causas da infertilidade