新化合物 A-失碳-17β-羟基-17α-乙炔基-Δ3(5),9(10)-雌甾二烯-2-酮的合成

报道新化合物A-失碳-17β-羟基-17α-乙炔基-Δ^3(5),9(10)-雌甾二烯-2-酮2的合成。文中探讨了用炔钾粗品对A-失碳-Δ^3(5),9(10)-雌甾二烯-2，17-二酮１和Ａ-失碳-６β，１９-环氧-Δ³-雄甾-2，17-二酮3的选择性炔化，分别得标题化合物2（44%）及Ａ-失碳-17β-羟基-17α-乙炔基-６β，１９-环氧-Δ³雄甾-2-酮４（６５％），４经还原性破开环氧、去羟甲基和去醋酰氧基合成了标题化合物２。四步总收率为３４％。     

Ureteral calculi: percutaneous removal using modified basket extractors and fluoroscopy

Two modified helical basket extractors are described that have increased the success rate of removing ureteral calculi using fluoroscopy from 63% to 92%. Initially a rather stiff and expandable basket with a 20-cm filiform tip is used with coaxial catheters and sheath (stage 1). If this procedure is unsuccessful, a basket with two long cable ends is passed from the nephrostomy out through the urethra (stage 2). When used with coaxial bladder catheters, this technique allows dilatation of the vesicoureteric junction and retrograde catheterization and injection of fluids or gas to dislodge the stone prior to extraction. In a series of 38 patients, stones were removed in all but three (a success rate of 92%). In five cases small stones (less than 5 mm) were not retrieved but subsequent studies were normal. Ureteral stones were found in the abdominal ureter in 28 cases, in the pelvic ureter in seven cases, and in multiple sites in three cases. Stones were larger than 1 cm in 27.7% of cases. Postextraction mucosal edema with reduced ureteral patency was common but usually cleared in 2-3 days. Occasional complications were related to the nephrostomy.     

Evaluation of left ventricular mechanical dyssynchrony as determined by phase analysis of ECG-gated SPECT myocardial perfusion imaging in patients with left ventricular dysfunction and conduction disturbances

Background  Cardiac resynchronization therapy (CRT) is approved for the treatment of patients with advanced systolic heart failure and evidence of dyssynchrony on electrocardiograms. However, a significant percentage of patients do not demonstrate improvement with CRT. Echocardiographic techniques have been used for more accurate determination of dyssynchrony. Single photon emission computed tomography (SPECT) myocardial perfusion imaging has not previously been used to evaluate cardiac dyssynchrony. The objective of this study is to evaluate mechanical dyssynchrony as described by phase analysis of gated SPECT images in patients with left ventricular dysfunction, conduction delays, and ventricular paced rhythms. Methods and Results  A novel count-based method is used to extract regional systolic wall thickening amplitude and phase from gated SPECT images. Five indices describing the phase dispersion of the onset of mechanical contraction are determined: peak phase, phase SD, bandwidth, skewness, and kurtosis. These indices were determined in consecutive patients with left ventricular dysfunction (n=120), left bundle branch block (n=33), right bundle branch block (n=19), and ventricular paced rhythms (n=23) and were compared with normal control subjects (n=157). Phase SD, bandwidth, skewness, and kurtosis were significantly different between patients with left ventricular dysfunction, left bundle branch block, right bundle branch block, and ventricular paced rhythms and normal control subjects (all P<.001) Peak phase was significantly different between patients with right ventricular paced rhythms and normal control subjects (P=.001). Conclusions  A novel SPECT technique for describing left ventricular mechanical dyssyn-chrony has been developed and may prove useful in the evaluation of patients for CRT. This study was funded in part by a research grant from the Medtronic-Duke Strategic Alliance, of which Dr Borges-Neto is the primary investigator.     

Modulation of the hypolipidemic effect of fish oils by dietary fiber in rats: studies with rice and wheat bran

Adult male rats were fed a purified diet containing rice bran or wheat bran with or without a marine fish oil to investigate the possible effects of such dietary combinations on lipid metabolism. Plasma and hepatic triacylglycerols and hepatic lipogenesis were lowered significantly by feeding fish oil with rice bran but not with wheat bran. Plasma cholesterol and hepatic cholesterol synthesis were significantly lower in animals fed fish oil with either bran. Liver microsomal free cholesterol was significantly lower in rats fed rice bran alone than in all other groups. Hepatic low density lipoprotein (LDL) receptor activity was significantly higher in the two groups fed rice bran than in the two groups fed wheat bran. Fish oil significantly decreased hepatic LDL receptor activity and increased hepatic high density lipoprotein (HDL) binding activity with wheat bran but had no significant effects on these parameters when added to the rice bran diet. However, when the data for all groups were pooled, there was a significant negative correlation between hepatic HDL binding activity and LDL receptor activity. Cecal volatile fatty acids were significantly higher in rats fed rice bran, were unaffected by adding fish oil to either bran diet and did not appear to mediate any of the effects of the brans and fish oil on plasma lipids and hepatic lipid metabolism. The combination of rice bran plus fish oil therefore appears to have more beneficial effects on lipid metabolism than wheat bran plus fish oil.     

Comparative effects of dietary wheat bran and its morphological components (aleurone and pericarp-seed coat) on volatile fatty acid concentrations in the rat

Adult male rats were fed on diets containing 100 g dietary fibre/kg either as alpha-cellulose or wheat bran or the pericarp-seed coat or aleurone layers prepared from that bran by sequential milling and air elutriation and electrostatic separation. After 10 d, concentrations of total volatile fatty acids (VFA) in caecal fluid were significantly different between groups and fell in the order: aleurone greater than wheat bran greater than pericarp-seed coat greater than cellulose. This ranking probably reflected the ease of fermentation of fibre polysaccharides by colonic bacteria which also resulted in a considerably higher faecal bacterial mass in the aleurone group. Because of the differences in the volume of caecal digesta, the mass of caecal VFA was considerably the highest in the aleurone group, intermediate with wheat bran and equally low in the pericarp-seed coat and cellulose groups. The diet based on aleurone gave a relatively higher proportion of propionate but with both pericarp-seed coat and wheat bran the contribution of butyrate was raised. VFA concentrations in hepatic portal venous plasma were proportional to caecal concentrations with very high (greater than 3 mM) values being recorded in the aleurone group. The findings are discussed in relation to the apparent susceptibility of the morphological components of wheat bran to fermentation by large bowel bacteria.