Effects of psycho–physical stress (competitive rafting) on saliva interleukin‐1 beta

The effects of psycho‐physical stress on immune function were evaluated by investigating the secretion rate of salivary interleukin‐1 beta (IL‐1β) during competitive rafting. Ten female and 20 male volunteers participated in this study. The concentration of IL‐1 β was determined in saliva using ELISA. We examined the statistical differences between T2/T1 (the changes observed during the training period) and C2/C1 (the changes before and after the competitive rafting) ratios by a Wilcoxon signed rank test. The ratio of IL‐1 β was significantly increased during competitive rafting (C2&sol;C1 = 3.6; p < 0.01), compared to the control ratio (T2&sol;T1 = 0.95; p < 0.01). The level of IL‐1 β at 8.00 a.m. decreased significantly between the first (11.9 ± 8.71 pmol/l) and the third day (7.9 ± 5.52 pmol/l) in all subjects (p < 0.01). In addition, the basal IL‐1 β levels significantly decreased between the beginning (8.00 a.m.) and the end of the day (6.00 p.m.), during the three consecutive days of collection (p < 0.01). These results may correspond to a circadian secretion rhythm of human saliva IL‐1 β. In conclusion, a disturbance of IL‐1 β salivary secretion is observed either after psycho‐physical stress or during intensive training. It may potentially affect the immune and endocrine status. Copyright © 2001 John Wiley & Sons, Ltd.     

Serendipitous Discovery of a Prodrug of a PARP‐1 Inhibitor

During SAR development of previously reported pyrrolocarbazole 1 , a potent PARP‐1 inhibitor, compound 14 , was discovered serendipitously to be a prodrug of compound 1 .     

Predictive factors of morbidity and mortality in grade IV and V liver trauma undergoing perihepatic packing: Single institution 14 years experience at European trauma centre

PurposeMajor liver trauma in polytraumatic patients accounts for significant morbidity and mortality. We aimed to assess prognostic factors for morbidity and mortality in patients with severe liver trauma undergoing perihepatic packing.MethodsProspectively collected records of 293 consecutive polytrauma patients with liver injury admitted at a level I trauma centre between 1996 and 2008 were reviewed. 39 patients with grade IV–V AAST liver injury and treated with peri-hepatic packing were identified and included for analysis. Univariate and multivariate analyses were performed to assess prognostic factors for morbidity and mortality.ResultsMean age of patients was 41 years. 34 patients were haemodynamically unstable at initial presentation. Ten of 39 patients were treated with angiographic embolization in addition to perihepatic packing. The overall mortality rate was 51.3%. Liver-related death occurred in 23.1%. Overall and liver-related morbidity rates were 90% and 28%, respectively. Glasgow Coma Scale (GCS), respiratory rate, packed red blood cells (PRBC) transfusion, pH and Base Excess (BE), Revised Trauma Score (RTS) and Trauma Injury Severity Score (TRISS), need for angiographic embolization as well as early OR and ICU admission were associated with significant decrease of early mortality.ConclusionsRevised Trauma Score, haemodynamic instability, blood pH and BE are important prognostic factors influencing morbidity and mortality in polytrauma patients with grade IV/V liver injury. Furthermore, fast and effective surgical damage control procedure with perihepatic packing, followed by early ICU admission is associated with lower complication rate and shorter ICU stays in this patient population.     

Synthesis and substance P receptor binding activity of androstano[3,2-b]pyrimido[1,2-a]benzimidazoles.

Several heterosteroids containing a dihydroethisterone skeleton were prepared and shown to displace substance P in a receptor binding assay. Further biochemical (kinetic and Scatchard analyses) and pharmacological evaluation (substance P-induced plasma extravasation and salivation in the rat) of a representative example in this series (5a) established that these compounds are competitive antagonists at the substance P receptor.     

Ring-Opening polymerization of cycloolefins with catalysts derived from ruthenium and iridium

An investigation was carried out on the polymerization of norbornene, cyclopentene and cyclooctene by the following iridium and ruthenium compounds: chlorobis(cyclooctene)iridium ( 1 ), carbonylchlorobis(cyclooctene)iridium ( 2 ), trifluoroacetatobis(cyclooctene)iridium ( 3 ), chloroiridic(IV) acid ( 4 ), dichloro(2,7-dimethylocta-2,6-diene-1,8-diyl)-ruthenium ( 5a ), and bis(trifluoroacetato)-(2,7-dimethylocta-2,6-diene-1,8-diyl)ruthenium ( 5b ). All the above catalysts were found to be very active for the polymerization of norbornene via ring-opening. Iridium catalysts were practically inactive for the polymerization of cyclopentene and cyclooctene, but gave copolymers of norbornene with cyclopentene and cyclooctene via ring-opening. The ruthenium catalysts displayed no activity for the polymerization of cyclopentene and cyclooctene, but it was found that after treatment with H₂ they became active for the polymerization of cyclopentene. The results obtained from the reaction of norbornene and aliphatic olefins suggest that the above catalysts act by metathesis. The particular features of these catalysts were examined.