Synthesis and evaluation of novel 8,5-fused bicyclic peptidomimetic compounds as interleukin-1beta converting enzyme (ICE) inhibitors

An 8,5-fused bicyclic peptidomimetic ring system generated by a stereoselective ring metathesis reaction was elaborated into potent inhibitors of interleukin-1beta converting enzyme (ICE, caspase-1). Multiple compounds were found that exhibited ICE IC50 values < 10 nM and were selective over caspase-3 and caspase-8. These active analogs generally possessed good activity (IC50 values < 100 nM) in a whole cell assay measuring IL-1beta production. Pharmacokinetic analysis of the ethyl acetal prodrug form of a selected active lead revealed a compound with a reasonable plasma half-life (1.1 h) and good oral bioavailability (30%).     

Composition and distribution of vascular epiphytes in a tropical semideciduous forest,Ghana

The composition and distribution of vascular epiphytes were studied in two 1‐ha plots in the KNUST Botanic garden, Ghana. One‐hectare plot each was randomly set up in secondary and cultivated forests for the identification and enumeration of trees and shrubs (≥10 cm dbh), and epiphytes. Each tree was carefully examined, noting the presence, positions and life‐forms of all epiphytes. Twenty‐nine epiphyte (29) species belonging to fourteen genera and eleven families were identified in the study. These were hosted by 48 tree species and occurred in three life‐forms: hemi‐epiphytes (45%), casual epiphytes (45%) and true epiphytes (10%). The vascular epiphyte species made up 25.7% of all the identified plant species (excluding herbs and climbers) encountered. Host species (P < 0.001), habitat (P = 0.001) and their interaction (P < 0.001) had strong effects on epiphyte composition in the forests. Moraceae was the most dominant family (44.8%), while Nephrolepis undulata J. Sm. and N. biserrata (Sw.) Scott. were the commonest species of epiphytes. In terms of vertical distribution, most epiphytes were located on the trunk, while a few occurred in the canopy.     

Fructose oligosaccharides: Possible markers of phylogenetic relationships among dicotyledonous plant families

Stems from more than 555 species representing 440 genera of approximately 210 dicotyledonous families were surveyed for the presence of fructose oligosaccharides. The tissues from 372 species representing 312 genera and 187 families did not contain such oligosaccharides. The sugars occurred sporadically or in small amounts in members of the following families: Crossosomataceae, Lauraceae, Malpighiaceae, Cornaceae, Myrisinaceae, Melianthaceae, Greyiaceae, and Simaroubaceae. The fructosyl sucrose trisaccharide, isokestose, aswell as its fructose tetrasaccharide homolog (but not higher inulin oligosaccharides) were present in members of the families Hippocastanaceae and Limnathaceae. Stems from members of the families Clethraceae and Monotropaceae, and some members of the Polemoniaceae, contained two series of fructose oligosaccharides: one based on isokestose (the inulin series) and the other one based on kestose (the levan series). The inulin or isokestose-based series of fructose oligosaccharides, alone, was present in members of the following families: Menyanthaceae, Boraginaceae, Campanulaceae, Goodeniaceae, Stylidiaceae, Brunoniaceae, Calyceraceae and Compositae. The primary metabolites occur ubiquitously and consistently in tissues of plants of these families. We hypothesize that this conservative character represents several phylogenetic alliances among them.