17 documents found, page 1 of 2

Chemical Prospection of Qualea grandiflora Mart. Fruit and Stem Extracts and Th...

Qualea grandiflora Mart. (“pau-terra”) is a medicinal plant symbolic from Cerrado biome. Qualea species reportedly have antiparasitic properties, but their active compounds have yet to be identified. In this study, we investigated the antiplasmodial activity of Q. grandiflora fruit and stem extracts against Plasmodium falciparum. The polar extracts of both fruits and stems showed promising in vitro antiplasmodi...

In vitro Antiplasmodial Activities of Alkaloids Isolated from Roots of Worsleya...

A combined phytochemical, crystallographic and biological study of Worsleya procera roots was performed. Fifteen alkaloids were identified by gas chromatography mass spectrometry (GC-MS) and seven of them were isolated. The structures of the alkaloids were elucidated by spectroscopic methods, and a detailed crystallographic study of tazettine was carried out. The isolated alkaloids and the obtained extracts wer...

Isolation of Tiliroside from Spiranthera odoratissima as Inhibitor of Trypanoso...

Glyceraldehyde-3-phosphate dehydrogenase (GAPDH) is a key enzyme involved in the Trypanosoma cruzi glycolytic pathway, parasite that causes Chagas' disease. There are only few drugs available to treat this disease, most of which present strong side effects. Natural products constitute a prime source for the discovery of new scaffolds potentially useful for the treatment of several diseases, including Chagas' di...

Doenças tropicais negligenciadas: uma nova era de desafios e oportunidades

In an article recently published in Química Nova, entitled "Chemistry Without Borders" ("Química Sem Fronteiras") [Pinto, A. C.; Zucco, C.; Galembeck, F.; Andrade, J. B.; Vieira, P. C. Quim. Nova 2012, 35, 2092], the authors highlighted the important aspects of science and technology with special emphasis on the field of Chemistry and its contributions toward a more prosperous Brazil of future. As a second step...

Nobel de química 2012: receptores acoplados à proteína G

Enzyme kinetics, structural analysis and molecular modeling studies on a series...

The enzyme purine nucleoside phosphorylase from Schistosoma mansoni (SmPNP) is an attractive molecular target for the development of novel drugs against schistosomiasis, a neglected tropical disease that affects about 200 million people worldwide. In the present work, enzyme kinetic studies were carried out in order to determine the potency and mechanism of inhibition of a series of SmPNP inhibitors. In additio...

Planejamento de fármacos, biotecnologia e química medicinal: aplicações em doen...

Estratégias modernas de planejamento de fármacos se fundamentam no conhecimento da fisiopatologia das doenças, no estudo de vias bioquímicas e na seleção de alvos moleculares. As ferramentas biotecnológicas modernas têm fornecido informações valiosas para a descoberta e o desenvolvimento de novos fármacos. A química medicinal possui papel central em vários processos que visam à identificação de substâncias bioa...

Biochemical evaluation of a series of synthetic chalcone and hydrazide derivati...

Chagas' disease, a parasitic infection widely distributed throughout Latin America, is a major public health problem with devastating consequences in terms of human morbidity and mortality. The enzyme cruzain is the major cysteine protease from Trypanosoma cruzi, the etiologic agent of American trypanosomiasis or Chagas' disease, and has been selected as an attractive target for the development of novel trypano...

Structural insights into the molecular basis responsible for the effects of imm...

The development of fast and reliable methods for the identification of new bioactive compounds is of utmost importance to boost the process of drug discovery and development. Immobilized enzyme reactors (IMERs), integrated with high performance liquid chromatography (HPLC), are attractive and versatile tools for screening collections consisting of natural products and synthetic small molecules. Standard kinetic...

Screening of Trypanosoma cruzi glycosomal glyceraldehyde-3-phosphate dehydrogen...

The inhibitory activity of crude extracts of Meliaceae and Rutaceae plants on glycosomal glyceraldehyde-3-phosphate dehydrogenase (gGAPDH) enzyme from Trypanosoma cruzi was evaluated at 100 μg/mL. Forty-six extracts were tested and fifteen of them showed significant inhibitory activity (IA % > 50). The majority of the assayed extracts of Meliaceae plants (Cedrela fissilis, Cipadessa fruticosa and Trichilia rama...