Effect of isoquinoline alkaloids from two Hippeastrum species on in vitro acetylcholinesterase activity.

The treatment of neurological disorders and neurodegenerative diseases is related to the levels of acetylcholine (ACh) through the inhibition of acetylcholinesterase (AChE). Galanthamine, an important alkaloid isolated from the Amaryllidaceae family, is approved for the pharmacological treatment of Alzheimer's disease (AD) and acts by inhibiting the acetylcholinesterase (AChE) activity. In the present study, Ellman's method was used to verify the inhibition of AChE activity of some isoquinolines alkaloids such as galanthamine, montanine, hippeastrine and pretazettine. At the concentrations 1mM, 500 microm and 100 microm, galanthamine presented an AChE inhibition higher than 90%. Montanine inhibited, in a dose-dependent manner, more than 50% of the enzyme at 1mM concentration. With the concentrations 500 microm and 100 microm, 30-45% of AChE activity inhibition was detected. The alkaloids hippeastrine and pretazettine presented no significant inhibition of the AChE activity. The results demonstrate that montanine significantly inhibits AChE activity at the tested concentrations, suggesting the necessity of further investigations on this alkaloid use in treating neurological disorders.

Cryptofolione derivatives from Cryptocarya alba fruits.

Cryptofolione (1) and the new cryptofolione derivative 6-(4,6-dimethoxy-8-phenyl-octa-1,7-dienyl)-4-hydroxy-tetrahydro-pyran-2-one (2) were isolated from the fruits of Cryptocarya alba. The structures were elucidated by spectroscopic methods. Cryptofolione showed activity towards Trypanosoma cruzi trypomastigotes, reducing their number by 77% at 250 microg mL(-1). Cryptofolione showed moderate cytotoxicity in both macrophages and T. cruzi amastigotes. It also displayed a mild inhibitory effect on the promastigote form of Leishmania spp. As both cytotoxic and trypanocidal effects are similar, the compound presented little selectivity in our assay models.

Hyaline membrane disease (HMD) therapy in Latin America: impact of exogenous surfactant administration on newborn survival, morbidity and use of resources.

Impact of surfactant administration, on neonatal mortality, morbidity and resource use, was assayed in a historically controlled study in 19 NICUs from 5 Latin American countries. Data from clinical records of infants with HMD were retrospectively reviewed for the previous 2 years (PRE phase n = 666 cases), and prospectively in cases that received surfactant (SURF phase, 348 cases). Birth weight stratified relative risk, with 95% confidence interval (RR +/-95% CI) for death, in the SURF as compared to the PRE was 0.60 (0.49-0.74), 0.79 (0.68-0.92) and 0.82 (0.71-0.94), for days 7, 28 and at discharge, respectively. At all ages mortality was significantly lower during SURF. Significant increases were observed in the occurrence of pulmonary interstitial emphysema, pulmonary hemorrhage, patent ductus arteriosus, bronchopulmonary dysplasia, intrahospital infection and necrotizing enterocolitis. Resource use increased significantly. It is concluded that the use of surfactant in the region is an important advance, and the efficacy of management of the late complications of the very premature and labile HMD survivors must increase. More attention should be given to thermal regulation, nutrition and management of infection in the survivors, before a more marked effect of surfactant can be seen.