Течение реакции прев ращения Δ4-андростен-3,17-диона в тестостерон дрожжам и Saccharomyces cerevisiae не зависит ни от вида , ни от концентрации применяемого сахара. Такая же продукция тестост ерона (около 80%) была пол учена и в дестиллированной во де. рН в пределах от 3 до 9 не оказывает вл ияния на течение прев ращения Оптимальная темпера тура для этого превращения на ходится в пределах 27– 30°С. Оптимальная концент рация дрожжей составляет 5% на 0,4% приба вленного Δ4-андросте н-3,17-диона при 28-часовой полунепр ерывной трансформации. Внесе ние стероидов в ферме нтационный раствор по частям сущ ественно улучшает течение пре вращения.
A series of derivatives of (phenylsulfanyl) benzoic acids bearing quinoline, 2,4-dihydroxy-3- propylacetophenone and 2,4-difluorobiphenyl moieties were prepared and their antileukotrienic activities evaluated. Some of the compounds were found to display multiple antileukotrienic effect in the inhibition of LTB4 biosynthesis, binding to LTD4 and LTB4 receptors, superior to the standards ( zileuton and zafirlukast) used. The compounds had an antiinflammatory effect, manifested with quinoline derivatives by a significant inhibition of bronchospasm induced by LTD4 and/or albumin. The results of regression analysis correspond to the observation that the most active compounds belong to quinoline derivatives with the lowest lipophilicity. X-ray analysis of the quinoline compounds revealed that an intramolecular hydrophobic interaction of their aromatic rings does not occur in the solid state.
Celiac disease, induced by dietary gluten, is characterized by mucosal atrophy and local inflammation associated with cell infiltration and activation. Unlike other food proteins, gluten and its proteolytic fragments, besides inducing a specific immune response, were shown to activate components of innate immunity and cause, e.g., direct stimulation of TNF-alpha and IL-10 and a significant rise in NO production by peritoneal macrophages. The identity of the active fragments was established by separating the peptic digest of gliadin by RP-HPLC chromatography. The purest fraction with the highest activity was analyzed by mass spectrometry, and the gliadin peptide sequence was identified as VSFQQPQQQYPSSQ. This peptide (T) and its N- and C-terminally shortened forms (A, B, C and D, E, F) were synthesized. Peptide B (FQQPQQQYPSSQ) elicited the highest TNF-alpha, IL-10, and RANTES secretion and increase in IFN-gamma-primed NO production by mouse macrophages. In contrast, C-terminally shortened peptides had a lower ability to stimulate macrophages than the native form.
3-Substituted 1-benzothiophene-2-carboxanilides 2 - 5 and their corresponding sulfones 6 - 8 were synthesized. The antiinflammatory effect of compounds 2 - 8 was evaluated in tests of LTB 4 biosynthesis, carrageenin edema and ear inflammation. With the exception of 3-hydroxyamides 5a - 5c , low inhibitory activities against COX and LT biosynthesis were observed.
A series of epibatidine analogues and their positional isomers bearing an 8-azabicyclo[3.2.1]octane moiety is described. Some of the compounds, especially those containing 8-azabicyclo[3.2.1]oct-2-ene moiety show high affinity for the nicotinic cholinergic receptor.
