The contents of secondary plant substances in solvent extracts of various byproducts (barks, kernels, peels, and old and young leaves) in a range of Brazilian mango cultivars were identified and quantitated. The results show that the profiles of secondary plant substances such as xanthone C-glycosides, gallotannins, and benzophenones in different byproducts vary greatly but are fairly consistent across cultivars. The free radical scavenging activity of the solvent extracts was evaluated using a high-performance liquid chromatography-based hypoxanthine/xanthine oxidase assay and revealed dose-dependent antioxidant capacity in all extracts. Four (mangiferin, penta- O-galloyl-glucoside gallic acid, and methyl gallate) of the major phenolic compounds detected were also evaluated in additional in vitro bioassay systems such as oxygen radical absorbance capacity, 2,2-diphenyl-1-picrylhydrazyl, and ferric reducing ability of plasma. Mangiferin in particular, detected at high concentrations in young leaves (Coite = 172 g/kg), in bark (Momika = 107 g/kg), and in old leaves (Itamaraka = 94 g/kg), shows an exceptionally strong antioxidant capacity.

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Ethanol extracts of powdered genipap (Genipa americana L.), umbu (Spondia tuberosa A.) and siriguela (Spondia purpurea L.) prepared from separate pulp, seeds and peel were investigated for their (i) antioxidant capacity, which was evaluated by various known methods; (ii) acetylcholinesterase (AChE) inhibitory activity; and (iii) cytotoxic effect on corneal epithelial cells of sheep. The highest values of total phenolic content were obtained with peel and seed extracts. Siriguela and umbu (seeds and peel) extracts displayed the highest antioxidant activities. Lipid peroxidation assays using mimetic biomembranes and mouse liver homogenates indicated that genipap pulp is a promising antioxidant. The investigation of phenols and organic acid contents revealed the presence of quercetin, citric and quinic acids, chlorogenic acid derivatives, among others, in several extracts, with the highest amount found in siriguela seeds. Genipap pulp and siriguela seed ethanol extracts presented an AChE inhibition zone similar to that of the positive control, carbachol. AChE inhibition assay with chlorogenic acid, one of the main constituents of siriguela seeds, revealed that this acid showed activity similar to that of the control physostigmine. These data suggest that these extracts are potentially important antioxidant supplements for the everyday human diet, pharmaceutical and cosmetic industries.

Recebido em 12/12/01; aceito em 5/11/02 SCREENING FOR ACETYLCHOLINESTERASE INHIBITORS FROM PLANTS TO TREAT ALZHEIMER'S DISEASE. Alzheimer's disease (AD) is a neurodegenerative disease characterized by cognite impairment and personality changes. The development of drugs for the treatment of the cognitive deficits of AD has focused on agents which counteract loss in cholinergic activities. These symptons of AD have been successfully treated with acetylcholinesterase (AchE) inhibitors (eg. galanthamine). There still is great interest in finding better AchE inhibitors. We use Ellmann's microplate assay and silica gel thin-layer chromatography (TLC) to screen natural products from plants as new sources of AchE inhibitors.Keywords: Alzheimer disease; plants; cholinesterase inhibitors. INTRODUÇÃONa última década, a maneira de se pesquisarem novos compostos biologicamente ativos sofreu grandes mudanças, principalmente devido aos avanços tecnológicos. A indústria farmacêutica tem um papel importante no desenvolvimento de novos métodos, os quais podem propiciar, de forma mais rápida, o surgimento de novos medicamentos no mercado 1 . Um dos mais importantes fatores para o sucesso no descobrimento de um fármaco novo é a diversidade química dos compostos a serem selecionados, cujas fontes podem ser: compostos sintéticos, produtos naturais ou química combinatória. Entre estas possibilidades, os produtos naturais são considerados como uma das maiores fontes de diversidade química 2 . A natureza é uma fonte de inestimável riqueza de novos medicamentos. Nos EUA e Inglaterra, aproximadamente 25% dos compostos ativos, nas prescrições atuais, foram identificados em plantas superiores 3 . A avaliação biológica 1 foi uma das mais significantes mudanças na área de produtos naturais nos últimos anos. O entendimento dos mecanismos da doença, acompanhado do aumento de testes com receptores e enzimas disponíveis, permitiram o desenvolvimento de sistemas eficientes e rápidos de bioensaios. Dessa forma, um bom sistema permite selecionar milhares de amostras em poucos dias 1,4 . A modernização dos ensaios permitiu a utilização de enzimas, receptores, DNA, entre outros alvos, para avaliação rápida de grandes quantidades de amostras. Dentre os bioensaios rápidos e sensí-veis, a utilização da enzima acetilcolinesterase é uma alternativa para a detecção e seleção de amostras com ação anticolinesterase.Entre os indivíduos idosos, ressaltam-se as anormalidades decorrentes da disfunção do sistema nervoso, como deficiências relativas à memória, à capacidade intelectual, à coordenação motora, ao equilíbrio, à postura, etc.A demência, embora possa ocorrer nas idades jovens por enfermidades cerebrais variadas, está ligada ao fenômeno de envelhecimento cerebral, acometendo indivíduos com idade superior a 65 anos. Admite-se que 10 a 15% destes indivíduos apresentam alguma forma de demência e, deste grupo, 50 a 60% sofrem de uma doença degenerativa de causa não totalmente conhecida denominada doença de Alzheimer 5-8 . A doença de Alzheimer está associada ...

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The complexes cis-[Ru(phen)(Apy)], Apy = 4-aminopyridine and 3,4-aminopyridine, are stable in aqueous solution with strong visible absorption. They present emission in the visible region with long lifetime that accumulates in the cytoplasm of Neuro2A cell line without appreciable cytotoxicity. The complexes also serve as mixed-type reversible inhibitors of human AChE and BuChE with high active site contact. cis-[Ru(phen)(3,4Apy)] competes efficiently with DMPO by the OH radical. Luminescence using fluorescence lifetime imaging (FLIM) enables real-time imaging of the conformational changes of the self-aggregation of Aβ with incubation of complexes (0-24 h) in phosphate buffer at micromolar concentrations. By this technique, we identified protofibrills in the self-assembly of Aβ and globular structures in the short fragment Aβ in aqueous solution.

This study aimed to assess the possible systemic antinociceptive activity of mangiferin and to clarify the underlying mechanism, using the acute models of chemical (acetic acid, formalin, and capsaicin) and thermal (hot-plate and tail-flick) nociception in mice. Mangiferin at oral doses of 10 to 100 mg/kg evidenced significant antinociception against chemogenic pain in the test models of acetic acid-induced visceral pain and in formalin- and capsaicin-induced neuro-inflammatory pain, in a naloxone-sensitive manner, suggesting the participation of endogenous opiates in its mechanism. In capsaicin test, the antinociceptive effect of mangiferin (30 mg/kg) was not modified by respective competitive and non-competitive transient receptor potential vanilloid 1 (TRPV1) antagonists, capsazepine and ruthenium red, or by pretreatment with L-NAME, a non-selective nitric oxide synthase inhibitor, or by ODQ, an inhibitor of soluble guanylyl cyclase. However, mangiferin effect was significantly reversed by glibenclamide, a blocker of K(ATP) channels and in animals pretreated with 8-phenyltheophylline, an adenosine receptor antagonist. Mangiferin failed to modify the thermal nociception in hot-plate and tail-flick test models, suggesting that its analgesic effect is only peripheral but not central. The orally administered mangiferin (10-100 mg/kg) was well tolerated and did not impair the ambulation or the motor coordination of mice in respective open-field and rota-rod tests, indicating that the observed antinociception was unrelated to sedation or motor abnormality. The findings of this study suggest that mangiferin has a peripheral antinociceptive action through mechanisms that involve endogenous opioids, K(ATP)-channels and adenosine receptors.

The antioxidant capacity of essential oils obtained by steam hydrodistillation from five species of the genus Ocimum, namely Ocimum basilicum var. purpurascens, Ocimum basilicum, Ocimum gratissimum, Ocimum micranthum, and Ocimum tenuiflorum (syn. O. sanctum), were evaluated using a high-performance liquid chromatography-based hypoxanthine/xanthine oxidase and the DPPH assays. The yield of oils from the leaves of the five species was variable with the greater amount obtained from Ocimum gratissimum (3.5%) and the least from Ocimum basilicum var. purpurascens (0.5%). In the hypoxanthine/xanthine oxidase assay, strong antioxidant capacity was evident in all the oils but the greater was shown by that obtained from Ocimum tenuiflorum (syn. O. sanctum) (IC50 = 0.46 microL/mL) compared to Ocimum basilicum var. purpurascens (IC50 = 1.84 microL/mL). Antioxidant capacity was positively correlated (r = 0.92, p < 0.05) with a high proportion of compounds possessing a phenolic ring such as eugenol, while a strong negative correlation (r = -0.77, p > 0.1) with other major volatiles was observed. These correlations were confirmed to a large extent in the DPPH assay. The results of a 24 h experiment with Ocimum tenuiflorum (syn. O. sanctum) shows that the antioxidant capacity factor (amount of essential oil obtained x free radical scavenging capacity; mg x %/100) reaches a threshold between 10 and 12.00 h, corresponding to maximum sunlight intensity in Brasil and furthermore exhibits a clear diurnal variation. The data generated with Ocimum species indicates that essential oils obtained from various herbs and spices may have an important role to play in cancer chemoprevention, functional foods, and in the preservation of pharmacologic products.