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Estudo de produtos naturais e derivados sintéticos buscando inibidores seletivos das catepsinas L e V
(Universidade Federal de São Carlos, 2011-01-31) Marques, Emerson Finco; Vieira, Paulo Cezar; https://lattes.cnpq.br/8923844563320377; https://lattes.cnpq.br/0976272219606258
The present work describes the search of bioactive secondary metabolites in plant species of genus Zanthoxylum and synthetic derivatives seeking specific inhibitors of cathepsins L and V. The natural products are involved in approximately 50% of all drugs marketed. Cathepsins represent a class of enzymes that has the primary function of randomly degrade proteins at lysosomes, but are also involved in different pathologies, such as, atherosclerosis, rheumatoid arthritis, osteoporosis and various cancers. This work was carried out monitoring Zanthoxylum extracts by fluorimetric assays and by Highperformance liquid chromatography (HPLC). Among the species studied, the most promising extracts were methanol and dichloromethane extracts of Zanthoxylum acuminatum, the latter being selected for isolation. The chromatographic methodology afforded the isolation of a triterpene: lupeol (1), the coumarins umbelliferone (2), heradenol (3), nordentatin (4), anisocoumarin (5), derivated of 6´,7´-epoxy-7-geranyloxycoumarin (6); canthinonic alkaloids 5-methoxycantin-6-one (7), 4,5-dimehoxycantin-6-ona (8); β-carboline alkaloid; 7-hydroxi-1-ethyl-β-carboline (9); and acridone alkaloid arborinine (10). All were tested at concentration of 25 mM and coumarin 5 inhibited over 50%, showing more activity and selective against cathepsin L. The value potency (IC50) of this compound was 30 μM for cathepsin L and 102 μM for cathepsin V. Furthermore, were determined the potency values, selectivity and mechanism of action acridones alkaloids isolated from Swinglea glutinosa, N-aryl anthranilic acids, synthetic acridone alkaloids and a series of alkaloids 4-quinoline-2-substituted. The most promising compound was the alkaloid acridone AC_05 with a IC50 of 0.5 μM and Ki of 0.18 μM. Moreover, the compound AC_05 presented as a competitive inhibitor against both cathepsins, which is consistent with the interaction model proposed by molecular modeling.
História da agricultura no município de Araras (SP) e a caracterização da restauração da mata ciliar no Ribeirão das Furnas
(Universidade Federal de São Carlos, 2011-01-31) Quintas, Domingos Antonio Cerveira; Stolf, Rubismar; https://lattes.cnpq.br/5786606684404295
The objectives of this study were to characterize the evolution of agriculture in the history of the city of Araras, SP and the study of the current stage of development of reforestation began in 1998 in the fragment of the riparian forest of Ribeirao das Furnas. The colonization of land in the municipality began in 1727 in a scenario where an estimated 82% of the land was occupied by forests and 18% were fields and swampy areas. There were distinct cycles of occupation and properties of lands that culminated in the current scenario of monoculture of cane sugar and a few fragments of native forest remnants. The almost total destruction of riparian vegetations during the colonial occupation, agricultural and urban of Sao Paulo, caused a large impact on water quality and its preservation. The heavy siltation of rivers and lakes undertook the main sources of supply. The Association of Environmental Preservation and Protection of Araras promoted the recovery of degraded areas, recomposing riparian vegetations, producing and planting seedlings of native species. Through four plots 5X20m equidistant, carried out the floristic and phytosociological survey, distributed in the central position in relation to the width of riparian vegetation. After the quantification and identification of species were applied index of diversity, equability and importance value of arboreal species. Were identified 48 arboreal individuals with DBH ≥ 5 cm, grouped into 13 families, 19 genera and 22 species. The most important value, IVI, 52,84, was the species Schinus terebinthifolius (Anacardiaceae). The indices of Shannon had amplitudes from 0,301 to 1,035 and the indices of equability in vii plots varied between 0,224 and 0,771, indicating the occurrence of gradients, characterizing the development of reforested vegetation is not uniform. The equability index (e) indicates that the forest is fragmenting into two islands of vegetation. Conclude that the restoration of forests is a process that goes beyond the planting of seedlings of arboreal species, demand fundamental care in the early years of the project, until the forest reaches a stage of development which allows its sustainability.