Structure-activity relationship for aryl and heteroaryl boronic acid inhibitors of hormone-sensitive lipase

A range of aryl and heteroaryl boronic acids were tested for their in vitro hormone-sensitive lipase inhibitory properties. (2-Benzyloxy-5-fluorophenyl)boronic acid, (2-benzyloxy-5-chlorophenyl)boronic acid and 5-bromothiophene-2-boronic acid were found to be the most potent HSL inhibitors with IC(50) values of 140, 17 and 350 nM, respectively.     

Concentrations and ecological risks of metals in surface sediments of some coastal creeks in the Niger Delta,Nigeria

The concentrations of nine metals were measured by atomic absorption spectrophotometry in surface sediments of three coastal creeks, namely, the Ifie, Egbokodo and Ubeji creeks, in the Niger Delta of Nigeria, from August 2012 to January 2013. The aim of the study was to provide information on the spatial and seasonal distribution patterns, degree of contamination, and ecological risks of metals in these sediments. The mean concentrations of the nine metals in these creek sediments ranged from 0.30 to 3.20?mg kg^?1 Cd; 10.7 to 24.7?mg kg^?1 Pb, 125 to 466?mg kg^?1 Cr; 3.1.10 to 14.9?mg kg^?1 Cu; 4.7 to 14.3?mg kg^?1 Co; 61.1 to 115?mg kg^?1 Ni; 106 to 183?mg kg^?1 Mn; 52.0 to 170?mg kg^?1 Zn and 5 469 to 20 639?mg kg^?1 Fe. In general, the metal concentrations were higher in the dry season than the wet season, except for Cr. The concentrations of Cd, Cr, Ni and Zn were above their regulatory control limits in sediment as specified by the Nigerian Regulatory Authority and Cd was identified as the main ecological risk factor. The enrichment factors for the studied metals followed the order: Cd > Cr > Ni > Zn > Pb > Co > Mn > Cu. The average multiple pollution index values indicated that these sediments were severely polluted with significant inputs from Cd, Ni and Cr.     

Ability of laboratory methods to predict in-use efficacy of antimicrobial preservatives in an experimental cosmetic.

The abilities of nine antimicrobial systems to preserve an experimental water-based cosmetic formulation were evaluated by six microbiological challenge tests: the U.S. Pharmacopeia test; the British Pharmacopeia test; the Cosmetic, Toiletry, and Fragrance Association test; the rapid screen test; the sequential challenge test; and the post-use test. The antimicrobial systems contained various combinations and amounts of two parabens and a quaternary compound in order to provide a broad range of preservation. The results obtained were compared with the abilities of the formulations to support maintenance and growth of microorganisms in microfloras obtained from human axilla areas and finger skin during an 8-week simulated in-use test. Without statistical analysis all of the tests predicted the results obtained with well-preserved or poorly preserved formulations. The rapid screen test was the best test for predicting differences at intermediate levels of preservation. Statistically, all of the tests were equivalent predictors of preservation efficacy in the in-use test (P = 0.05). At the P = 0.10 level, only the U.S. Pharmacopeia, British Pharmacopeia, rapid screen, Cosmetic, Toiletry, and Fragrance Association tests were significantly predictive. The results of prediction by a test, based on the preservative levels used, agreed well with the in-use test results (P = 0.01). A total of 20% of the formulations that contained excessive microbial levels contained human axilla microorganisms. The levels of preservation in failed products were similar to the levels of preservation in unused controls.     

Assembly and disassembly of mammalian chromosome pellicle

By means of indirect double immunofluorescent staining,the coordination of PI antigen and perichromonucleolin(PCN),the constituent of nuclear periphery and nucleolus respectively,in the assembly and disassembly of chromosome pellicle during mitosis was studied.It was found that in 3T3 cells,during mitosis PI antigen began to coat the condensing chromosome surface earlier than PCN did.However,both of them completed their coating on chromosome at approximately the same stage of mitosis,prometaphase metaphase,The dissociation of mitosis,Prometaphase metaphase.The dissociation of PI antigen from chromosome pellicle to participate the formation of nuclear periphery took place also ahead of that of PCN,At early telophase PI antigen had been extensively involved in the formation of nuclear periphery,while PCN remained in association with the surface of decondensing chromosomes.At late telophase,when PI antigen was localized in an fairly well formed nuclear periphery,PCN was in a stage of forming prenucleolar bodies.     

Excess Mortality Attributable to Clostridium difficile and Risk Factors for Infection in an Historic Cohort of Hospitalised Patients Followed Up in the United Kingdom Death Register

Methods

We compared time from hospital admission to death in a probability sample of 100 Clostridium difficile infected cases and a probability sample of 98 non-cases admitted to an English teaching hospital between 2005 and 2007 with follow up in the UK national death register using survival analysis.

Results

Clostridium difficile infection was associated with a 50% increased risk of death (Hazard Ratio 1.51 (95% CI: 1.05–2.19 p = 0.03) at between five to eight years in Cox Regression analysis adjusting for age, sex, Charlson comorbidity index, diagnosis of a malignant condition and insertion of a nasogastric tube during admission. Acquisition of Clostridium difficile infection was independently associated with an almost six fold higher odds of being admitted with a diagnosis of infection of any other type (OR 5.79 (2.19, 15.25) p<0.001).

Conclusions

Our results strongly support continued priority being given to improve prevention and treatment of Clostridium difficile infection in the English National Health Service particularly in patients admitted with an infection. Our results may be applicable to other health systems.     

Vaccine coverage: recent trends and future prospects.

OBJECTIVE--To assess the feasibility of achieving the target of 95% coverage for the childhood immunisation schedule by 1995 and to determine the influence of sociodemographic factors and information systems on recent trends. DESIGN--Analyses of trends in quarterly vaccination data for diphtheria, pertussis, and measles in health districts between February 1988 and February 1991. SETTING--District health authorities in England and Wales, and health and social services boards in Northern Ireland. SUBJECTS--Cohorts of children whose youngest member had reached the target age of 18 months for receiving the third doses of diphtheria and pertussis vaccines and 2 years for receiving measles vaccine. RESULTS--Predicted coverage levels for mid-1995 were in excess of 95% for diphtheria, pertussis, and measles vaccines. In the 118 districts that continuously reported between February 1988 and February 1991 the increase in coverage was 6% for diphtheria and 13% for pertussis and measles vaccines. 1991 coverage depended primarily on 1988 coverage. The additional effects of deprivation, change in computer system, and child population size achieved at most only marginal statistical significance. CONCLUSIONS--The government''s target of 95% coverage by 1995 is realistic, although projections should be viewed with caution. Several national vaccination initiatives are likely to have contributed to the recent steady increase in coverage. Updating and validation exercises are likely to improve recorded coverage.