消旋15(R)-15-甲基PGE2甲酯的合成

d,l-15(R)-15-Methyl-PGF_2α methyl ester 11-trimethylsilyl ether(II)wasprepared from selective monosilylation of d,l-15(R)-15-methyl-PGF_2αmethyl ester(I) withtrimethylsilyldiethylamine in acetone. Oxidation of(II ) with Collin's reagent gave d,l-15(R)-15-methyl-PGE₂ methyl ester 11-trimethylsilyl ether(III)which,without purification,was converted to d,l-15(R)-15-methyl-PGE₂ methyl ester(IV)under mild acidic conditions.     

Prevention in practice: results of a 2-year follow-up of routine health promotion interventions in general practice

BACKGROUND.: The effectiveness of health promotion activity in general practiceon risk factor reduction for coronary heart disease remainsthe subject of active debate. OBJECTIVE.: The study aimed to assess the impact of practice-based healthcheck-ups on health behaviours over a 2-year period. METHOD.: A general practice cohort of 7123 patients from 18 practiceswas surveyed. Eight hundred and forty (12%) patients had beenoffered a heafth check within a 12-month period from September1992 and 621 (9%) received one. Two hundred and fifty patients(40%) were asked back for follow-up after their health check. RESULTS.: Over a 2-year period there was no difference in smoking cessation,alcohol consumption, weight loss nor the amount of exercisetaken between those who attended for a health check and thosewho did not. The food score chosen to assess dietary change(Oxcheck) showed a statistically significant 1.16-point risefor the whole sample over the survey period. There was a significantdifference in mean food score change between heafth check attendersand non-attenders (Mann-Whitney U test: P << 0.002). Maintenanceof dietary improvement over a 2-year period was not affectedby health check attendance. CONCLUSIONS.: This study confirms the low impact of health checks on the selfreported modification of cardiovascular risk factors and showsthat maintenance of appropriate health behaviour change is nomore likely in those who have received a health check. Keywords. Health promotion, general practice.     

Effects of antenatal thyrotropin-releasing hormone, antenatal corticosteroids, and postnatal ventilation on surfactant mobilization in premature rabbits.

OBJECTIVE: The effects of antenatal hormones on postnatal surfactant mobilization were evaluated in preterm rabbits. STUDY DESIGN: Pregnant rabbits were treated with vehicle, betamethasone, or thyrotropin-releasing hormone for 2 days before cesarean section at 29 days' gestation (term 31 days). Newborns were mechanically ventilated or allowed to spontaneously breathe, and groups were compared by analysis of variance. RESULTS: Neither antenatal corticosteroids nor thyrotropin-releasing hormone increased radiolabeled precursor incorporation, alveolar wash or total lung saturated phosphatidylcholine pools, lung clearance of radiolabeled rabbit surfactant, or estimated net secretion of saturated phosphatidylcholine. However, saturated phosphatidylcholine pools in alveolar wash increased 2.7-fold during the first 24 hours in spontaneously breathing rabbits versus 2.1-fold in mechanically ventilated thyrotropin-releasing hormone-treated and control rabbits (p less than 0.05). In addition, estimated net secretion of precursor-derived saturated phosphatidylcholine was 50% higher after 24 hours in spontaneously breathing rabbits. CONCLUSION: Mechanical ventilation may have hindered the mobilization of surfactant saturated phosphatidylcholine pools to the alveolar space after birth in preterm rabbits, but maternal hormonal therapies did not appear to influence this adaptive process or change surfactant metabolism.     

Quantitative liver function in patients with rheumatoid arthritis treated with low-dose methotrexate: a longitudinal study

The objectives were to determine quantitative liver function prospectively in patients with rheumatoid arthritis (RA) treated with low-dose methotrexate (MTX), to search for risk factors for a loss of quantitative liver function and to assess the relationship between quantitative liver function and histological staging. A total of 117 patients with RA (ACR criteria, 85 women, mean age 59 yr) had measurements of galactose elimination capacity (GEC), aminopyrine breath test (ABT) and liver enzymes [aspartate amino transferase (AST), alanine amino transferase (ALT), alkaline phosphatase (AP), 7-glutamyl transferase (GGT), bile acids, bilirubin, albumin] before treatment with weekly i.m. MTX injections and every year thereafter. In 16 patients, liver biopsies were performed. Before the introduction of MTX, mean GEC was 6.6 mg/min/kg [5th to 95th percentile (5-95 PC) 5.1- 8.5; reference range 6.0-9.1] and mean ABT was 0.80% kg/mmol (5-95 PC 0.42-1.30: reference range 0.6-1.0). During treatment with MTX [mean weekly dose 11.8 mg (5-95 PC 5.4-20.2), mean observation period 3.8 yr (5-95 PC 0.4-6.9)], significant declines of GEC (-0.12 mg/min/kg per year. t = 3.30, P < 0.002) and ABT (-0.06% kg/mmol per year, t = 4.81, P < 0.001) were observed. Negative correlations were found between the annual change in GEC and GEC at baseline (Rs = -0.40, P < 0.0001), and the annual change in ABT and ABT at baseline (Rs = -0.43, P < 0.0001). No correlations were found between the annual change in GEC or ABT and weekly MTX dose, age or percentage of increased liver enzymes, and no effect of a history of alcohol consumption > 30 g/week became evident. Two patients with Roenigk grade III had impaired quantitative liver function, while 14 patients with Roenigk grades I and II exhibited a high variability of GEC and ABT from normal to abnormal values. The continuous declines in GEC and ABT observed deserve attention in patients with prolonged treatment. Patients with a low GEC or ABT at baseline seem not to be at increased risk for a further loss of quantitative liver function. An impaired GEC or ABT does not necessarily concur with hepatic fibrosis on histological examination.