DMAP-promoted oxidative functionalization of α-amino ketones via oxygen delivery from water/alcohols.

This paper shows a novel oxidative functionalization of α-amino ketones to yield the corresponding α-ketoamides and α-acylimidates. The reaction proceeds via oxygen delivery from water/alcohols in conjunction with an electron acceptor and 4-dimethylaminopyridine (DMAP). Mechanistic study indicates that DMAP exhibits a dual function of nucleophilic catalysis and proton abstraction.

Analgesic Effects and Adverse Reactions of Lidocaine for Patient-Controlled Intravenous Analgesia on Patients Undergoing Open Hepatectomy: A Retrospective Analysis.

PURPOSE: The aim of this study was to investigate the effect of lidocaine for patient controlled intravenous analgesia (PCIA) in patients who underwent open hepatectomy. DESIGN: A retrospective analysis. METHODS: A total of 281 patients who underwent open hepatectomy from July 2018 to December 2018 were included. All patients were assigned into two groups: the lidocaine group (PCIA consisted of lidocaine, sufentanil, tramadol and granisetron) and the control group (PCIA consisted of sufentanil, tramadol and granisetron). The postoperative visual analogue scale (VAS) and complications (including respiratory depression, hypotension, nausea and vomiting, pruritus, numbness of the corners of the mouth, dizziness) between the groups were compared. FINDINGS: There were no significant differences between the characteristics, duration of surgery and anesthesia, and recovery of postoperative activity between the two groups. In the first 3 days after the operation, the postoperative VAS score of the lidocaine group was lower than that of the control group at resting state, while after activity, the postoperative VAS contrast results were completely opposite. In particularly, the resting state at 48 hours (h) (1.05 ± 1.25 vs 1.57 ± 1.54) after surgery and the activity state at 72 h (3.02 ± 1.51 vs 2.2 ± 1.66) after surgery (P < 0.05). The incidence of mouth numbness and dizziness were significantly increased in the lidocaine group (P < 0.05). CONCLUSION: The addition of lidocaine in PCIA was not beneficial to improve the pain during activities and increased the incidence of perioral numbness and dizziness.

Patients with gastroenteric tumor after upper abdominal surgery were more likely to require rescue analgesia than lower abdominal surgery.

OBJECTIVES: To find out the reasons why patients still need to use rescue analgesics frequently after gastrointestinal tumor surgery under the patient-controlled intravenous analgesia (IV-PCA), and the different abdominal surgery patients using the difference of analgesics. METHODS: A total of 970 patients underwent abdominal operation for gastrointestinal tumors were included. According whether patients used dezocine frequently for rescue analgesics within 2 days after surgery, they assigned into two groups: RAN group (Patients who did not frequently use rescue analgesia, 406 cases) and RAY group (Patients who frequently used rescue analgesia, 564 cases). The data collected included patient's characteristics, postoperative visual analogue scale (VAS), nausea and vomiting (PONV), and postoperative activity recovery time. RESULTS: No differences were observed in the baseline characteristics. Compared with the RAN group, patients in the RAY group had a higher proportion of open surgery, upper abdominal surgery, VAS score at rest on the first 2 days after surgery and PONV, and a slower recovery of most postoperative activities. Under the current use of IV-PCA background, the proportion of rescue analgesics used by patients undergoing laparotomy and upper abdominal surgery was as high as 64.33% and 72.8%, respectively. Regression analysis showed that open surgery (vs laparoscopic surgery: OR: 2.288, 95% CI: 1.650-3.172) and the location of the tumor in the upper abdomen (vs lower abdominal tumor: OR: 2.738, 95% CI: 2.034-3.686) were influential factors for frequent salvage administration. CONCLUSIONS: In our patient population, with our IV-PCA prescription for postoperative pain control, patient who underwent open upper abdominal surgery required more rescue postoperative analgesia.

Neuropeptide Y suppresses epileptiform discharges by regulating AMPA receptor GluR2 subunit in rat hippocampal neurons.

The present study aimed to investigate the effects of neuropeptide Y (NPY) on the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor glutamate receptor 2 (GluR2) subunit in epileptiform discharge hippocampal neurons. Hippocampal neurons were harvested from neonatal Sprague­Dawley rats aged <24 h and primarily cultured in vitro. At day 12 following culture, hippocampal neurons were divided into the following groups: Control, Mg2+­free, NPY+Mg2+­free and BIBP3226+NPY+Mg2+­free. The action potential of neurons was measured using the whole cell patch clamp technique in the control, Mg2+­free and NPY+Mg2+­free groups. AMPA current (IAMPA) was detected and peak current density was calculated in each group. Alterations in total protein and phosphorylation of the GluR2 subunit were detected by western blot analysis, and GluR2 mRNA expression levels were detected by reverse transcription­quantitative polymerase chain reaction, in each group. The whole cell patch clamp technique demonstrated an abnormal action potential in the Mg2+­free group. The frequency and amplitude of the action potential were significantly greater in the Mg2+­free group compared with the control group, and significantly reduced in the NPY+Mg2+­free group compared with the Mg2+­free group (P<0.05). In the Mg2+­free group, compared with the control group, peak current density was significantly reduced (P<0.05), GluR2 subunit protein content was slightly reduced (P>0.05), phosphorylation levels of GluR2 subunit were significantly greater (P<0.05) and GluR2 mRNA was significantly reduced (P<0.05). In the NPY+Mg2+­free group, compared with the Mg2+­free group, peak current density was significantly greater (P<0.05), phosphorylation levels of GluR2 subunit were significantly reduced (P<0.05) and GluR2 mRNA expression was significantly greater (P<0.05). In the BIBP3226+NPY+Mg2+­free group, compared with the NPY+Mg2+­free group, peak current density was significantly reduced (P<0.05), phosphorylation levels of GluR2 subunit were significantly greater (P<0.05) and GluR2 mRNA expression was significantly reduced (P<0.05). After 3 h of treatment with Mg2+­free extracellular fluid, epileptiform discharge was detected in the cells. NPY inhibited the discharge and its underlying mechanism may be that epileptiform discharge suppressed the function of the AMPA receptor GluR2 subunit. NPY relieved the inhibition of the GluR2 subunit via the Y1 receptor. This may provide a novel direction for future studies on the pathogenesis and treatment of epilepsy.

Percussion, diuresis, and inversion therapy for the passage of lower pole kidney stones following shock wave lithotripsy.

BACKGROUND: Lower pole kidney stones typically have poor rates of spontaneous clearance from the body. Some studies have suggested that diuresis, percussion and inversion therapy could be beneficial for people with lower pole kidney stones following shock wave lithotripsy. There is however controversy about the relative benefits, harms, and efficacy of these interventions for the management of lower pole kidney stones. OBJECTIVES: To identify the benefits and harms of percussion, diuresis, and inversion therapy to facilitate the passage of lower pole kidney stones following shock wave lithotripsy. SEARCH METHODS: We searched the Cochrane Renal Group's specialised register up to 27 November 2013 through contact with the Trials' Search Co-ordinator using search terms relevant to this review. SELECTION CRITERIA: All randomised controlled trials (RCTs) and quasi-RCTs looking at the benefits and harms of percussion, diuresis, and inversion therapy for aiding passage of lower pole kidney stones following shock wave lithotripsy were sought for assessment. The first phases of randomised cross-over studies were also eligible for inclusion. DATA COLLECTION AND ANALYSIS: Two authors independently assessed study quality and extracted data. Results were expressed as relative risk (RR) for dichotomous outcomes and mean difference (MD) or standardised mean difference (SMD) for continuous data with 95% confidence intervals (CI). MAIN RESULTS: We identified two small studies (177 participants) for inclusion and analysis. One study (69 participants) compared percussion, diuresis and inversion therapy following shock wave lithotripsy versus observation-only after shock wave lithotripsy. This study reported significantly higher stone-free rates in the intervention group (RR 0.62, 95% CI 0.47 to 0.82) and a significant reduction in stone burden (MD -3.30, 95% CI -3.58 to -3.03) compared to the observation-only group. They reported no significant differences in complication rates (RR 3.00, 95% CI 0.12 to 76.24).The second study (108 participants) compared percussion, diuresis, and inversion therapy plus shock wave lithotripsy with shock wave lithotripsy therapy alone. This study reported significantly higher stone-free rates in the intervention group (RR 0.36, 95% CI 0.17 to 0.80) and a significant reduction in stone burden (MD -0.30, 95% CI -0.04 to -0.56) compared to the control group. They reported no significant differences in complication rates (RR 2.54, 95% CI 0.10 to 63.72).For both studies selection bias was unclear; there was high risk of bias for performance bias; and detection, attrition and reporting bias were low. AUTHORS' CONCLUSIONS: Limited evidence from two small studies indicated that percussion, diuresis, and inversion therapy may be safe and effective therapies to assist clearance of lower pole kidney stone fragments following shock wave lithotripsy. Methodological quality in both studies was assessed as moderate. Further well-designed and adequately powered studies are required to inform clinical practice.

[Drug distribution in gastric cancer and adjacent tissues by preoperative intraperitoneal chemotherapy with Co-fluorouracil liposome].

OBJECTIVE: To examine the distribution of fluorouracil in gastric cancer (CA), lymph node (LN), normal gastric mucosa (NG), peritoneum (PE), greater omentum (GO) and lesser omentum (LO) by preoperative intraperitoneal chemotherapy with Co-fluorouracil liposome (Co 5-Fu), and offer an experimental basis for clinic practice. METHODS: Ninety-six gastric cancer patients were divided into four groups: Co 5-Fu i.v. injection group (Co 5-Fu i.v.), Co 5-Fu intraperitoneal perfusion group (Co 5-Fu i.p.), 5-Fu i.v. injection group (5-Fu i.v.) and intraperitoneal perfusion group (5-Fu i.p.) given on day-2, day-1 and 60 minutes before operation. Fluorouracil concentration in all tissues collected during operation were examined by high performance liquid chromatography (HPLC). RESULTS: The fluorouracil concentration in the tissues in Co 5-Fu i.p. group was significantly higher than that in Co 5-Fu i.v. or 5-Fu i.p. group (P < 0.05 or P < 0.01), and that in 5-Fu i.p. group was greatly higher than that at 5-Fu i.v. group (P < 0.01). In Co 5-Fu i.p. group, the concentration of drug in LN, CA, PE, NG, GO and LO decreased gradually with the former 3 tissues significantly higher than the latter 3 tissues (P < 0.01), and adjacent lymph node was the highest. In Co 5-Fu i.v. group, the ranking was LN, CA, NG, PE, GO and LO with the former 3 tissues significantly higher than the latter 3 tissues (P < 0.01) and showing tumor tissues higher than the other tissues (P < 0.01). In 5-Fu i.p. group, the ranking was PE, LN, CA, NG, GO and LO with the former 2 tissues significantly higher than the latter tissues (P < 0.01). CONCLUSION: Co 5-Fu possesses drug targeting, slow release and long effect in gastric cancer tissues and adjacent lymph nodes. Preoperative chemotherapy with Co 5-Fu i.p. is more advantageous than 5-Fu given i.v. or 5-Fu i.p.