The aim of this study was to evaluate the incidence of catheter tip dislocation in patients with percutaneously implanted port-catheters for hepatic arterial chemotherapy with catheter tip fixation. Forty-seven patients (31 men and 16 women; mean age 66 years) with unresectable advanced liver cancers (primary liver cancer, n=19; metastatic liver cancer, n=28) underwent percutaneously implantable port-catheter system placement with the tip fixed at the gastroduodenal artery with coils and side hole opened at the common hepatic artery. In 39 patients, n-butyl cyanoacrylate (NBCA) mixed with Lipiodol was added for fixation. The position of the side hole after the indwelling port-catheter system was investigated, and the correction method in cases with catheter dislocation was determined. In 2 (25%) of the 8 patients without NBCA fixation, dislocation of the catheter was noted, in contrast to none (0%) of 37 patients with NBCA fixation. Two patients in whom NBCA was used could not undergo long-term intra-arterial chemotherapy because of hepatic arterial thrombotic occlusion which occurred after placement of the indwelling catheter, and were excluded from the evaluation. Fixation of the catheter tip with combined use of coils and NBCA--Lipiodol mixture to the gastroduodenal artery is important to prevent dislocation of the port-catheter system.

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The asymmetric intramolecular Michael reaction of acyclic compounds ethyl (Z) -4-[benzyl- (3oxobutyl)amino] but-2-enoate 9, and ethyl (E) -5- [benzyl-(3-oxobutyl)amino] pent-2-enoate 10 was investigated under a variety of conditions, and the pyrrolidine ethyl (4-acetyl-l -benzylpyrrolidin-3-yl)acetate 11 and piperidine ethyl (3-acetyl-1 -benzylpiperidin-4-yI)acetate 12, versatile chiral building blocks for alkaloid synthesis, were obtained in moderate to excellent optical yield. Cyclization of the aforementioned but-and pent-2-enoate using (R) -1 -phenylethylamine in THF in the presence of molecular sieves 5 A gave the (+)-pyrrolidine derivative (+)-11 and the (-)piperidine derivative (-)-12 in 60 and 90% ee, respectively. When (S)-1 -phenylethylamine was used, pyrrolidine ( -) -1 1 and piperidine derivatives (+) -1 2 were obtained in similar optical yields, respectively. The ee of (-)and (+) -piperidine derivatives increased up to 98% upon recrystallization of their hydrobromide salts. Ph> Ph> i natural products a,,, CO2Et 1 2 Scheme 1 Rrugent: i, chiral base experimental details of the asymmetric, intramolecular Michael reaction induced by the 1,3-allylic strain of chiral enamines.

Here, we assessed the effects of long-chain fatty acids (LCFAs) and the LCFA receptor agonist GW9508 on the transcription of the gonadotropin subunit genes Cga, Lhb and Fshb because LCFA receptor GPR120 was observed in mouse gonadotropes in our recent study. A transcription assay using LβT2 cells demonstrated that LCFAs, oleic acid, α-linolenic acid, docosahexaenoic acid and palmitate, repressed the expression of Cga, Lhb, and Fshb at concentrations between 50 and 100 µM. On the other hand, treatment with 10 µM unsaturated LCFAs, oleic acid, α-linolenic acid and docosahexaenoic acid, repressed only Fshb expression, while the same dose of a saturated LCFA, palmitate, had no effect on the expression of gonadotropin subunit genes. Furthermore, GW9508 did not affect promoter activity. Next, we examined deletion mutants of the upstream region of Fshb and found that the upstream regulatory region (-2824 to -2343 bp) of Fshb was responsible for the notable repression by 10 µM unsaturated LCFAs. Our results suggest that the upstream region of Fshb is susceptible to unsaturated LCFAs. In addition, unsaturated LCFAs play a role in repressing Fshb expression through the distal -2824 to -2343 bp region, which might be independent of the LCFA receptor GPR120 pathway.

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