Synthesis, Biological Evaluation, and Molecular Docking Studies of Hydrazones as Novel Xanthine Oxidase Inhibitors.

A series of hydrazones, 2-cyano-N'-(4-diethylamino-2-hydroxybenzylidene)acetohydrazide (1), N'-(5-bromo-2-hydroxy-3-methoxybenzylidene)-3-chlorobenzohydrazide monohydrate (2·H2O), N'-(2-hydroxy-3-methylbenzylidene)-4-nitrobenzohydrazide (3), and N'-(2-hydroxy-3-trifluoromethoxybenzylidene)-4-nitrobenzohydrazide (4), were prepared and structurally characterized by elemental analysis, IR and 1H NMR spectra, and single crystal X-ray determination. Xanthine oxidase inhibitory activities of the compounds were studied. Among the compounds, 2-cyano-N'-(4-diethylamino-2-hydroxybenzylidene)acetohydrazide shows the most effective activity.

Dezocine relieves the postoperative hyperalgesia in rats through suppressing the hyper-action of Akt1/GSK-3β pathway.

The relieving role of dezocine in pain after surgery was previously reported, while the potential mechanism was not completely clear. Therefore, the current research probed into the regulatory mechanism of dezocine in pain after surgery. A postoperative pain model was established by performing plantar incision surgery on the juvenile Sprague-Dawley rats.

Identification of independent risk factors for intraoperative gastroesophageal reflux in adult patients undergoing general anesthesia.

Background: Gastroesophageal reflux (GER) affects up to 20% of the adult population and is defined as troublesome and frequent symptoms of heartburn or regurgitation. GER produces significantly harmful impacts on quality of life and precipitates poor mental well-being. However, the potential risk factors for the incidence and extent of GER in adults undergoing general anesthesia remain unclear.

Risk Factors for Fentanyl-Induced Cough Following General Anesthesia in Adults: A Retrospective Study from a Single Center in China.

BACKGROUND Fentanyl-induced cough (FIC) during general anesthesia induction and postoperative nausea and vomiting are common complications, yet the risk factors for FIC remain controversial. This retrospective study was conducted at a single center in China and aimed to investigate the risk factors for fentanyl-induced cough following general anesthesia in adults. MATERIAL AND METHODS A total of 601 adult patients undergoing elective surgery were enrolled, and the incidence of FIC during general anesthesia induction and postoperative adverse events were recorded.

Neuregulin-1 Protects the Rat Diaphragm during Sepsis against Oxidative Stress and Inflammation by Activating the PI3K/Akt Pathway.

Sepsis-induced diaphragm dysfunction (SIDD) which is mainly characterized by decrease in diaphragmatic contractility has been identified to cause great harms to patients. Therefore, there is an important and pressing need to find effective treatments for improving SIDD. In addition, acetylcholinesterase (AChE) activity is a vital property of the diaphragm, so we evaluated both diaphragmatic contractility and AChE activity.

Effect of Inhibiting p38 on HuR Involving in β-AChR Post-transcriptional Mechanisms in Denervated Skeletal Muscle.

Previous studies reported that RNA-binding protein human antigen R (HuR) mediates changes in the stability of AChR β-subunit mRNA after skeletal muscle denervation; also, p38 pathway regulated the stability of AChR β-subunit mRNA in C2C12 myotubes. However, the relationship between HuR and p38 in regulating the stability of AChR β-subunit mRNA have not been clarified. In this study, we wanted to examine the effect of inhibiting p38 on HuR in denervated skeletal muscle.

Neuregulin-1β attenuates sepsis-induced diaphragm atrophy by activating the PI3K/Akt signaling pathway.

The aim of this study was to investigate the protective effects of neuregulin-1β (NRG-1β) on sepsis-induced diaphragm atrophy and the possible underlying mechanisms. Sprague-Dawley rats were randomly divided into sham, sepsis and NRG groups. Sepsis was induced by cecal ligation and puncture (CLP).

γ-Acetylcholine Receptor Mediating Dynamic Changes of Resistance to Rocuronium in the Denervated Skeletal Muscle.

Background/aims: Denervation resulted in resistance to non-depolarizing muscle relaxants (NDMRs), the magnitude of which changed after denervation in the skeletal muscle. The aim of this study was to investigate whether changed potencies of rocuronium were due to altered γ-acetylcholine receptor (γ-AChR) expression after skeletal muscle denervation.

Methods: Innervated and denervated muscle cells were used in this study.

The Role of Oxidative Stress in Decreased Acetylcholinesterase Activity at the Neuromuscular Junction of the Diaphragm during Sepsis.

Our recent study demonstrated that acetylcholinesterase (AChE) activity at the neuromuscular junction (NMJ) of the diaphragm decreased during sepsis. However, the mechanisms were not clearly identified. In this study, we aimed to investigate whether the decreased AChE activity was related to oxidative stress by observing AChE activity in different grades of sepsis induced by caecal ligation and puncture (CLP).

A single dose of dezocine suppresses emergence agitation in preschool children anesthetized with sevoflurane-remifentanil.

Background: Emergence agitation (EA) is a common phenomenon in preschool children during emergence from general anesthesia. This study evaluated the safety and efficacy of dezocine for emergence agitation in preschool children anesthetized with sevoflurane-remifentanil.

Methods: A total of 100 preschool children, scheduled for elective laparoscopic repair of an inguinal hernia by high ligation of the hernia sac under sevoflurane-remifentanil anesthesia were randomized into two groups: Group C (n = 50) received Ringer's lactate 10 mL and Group D received Ringer's lactate 10 mL containing dezocine 0.

Sepsis decreases the activity of acetylcholinesterase by reducing its expression at the neuromuscular junction.

Our previous study demonstrated that sepsis may decrease the activity of acetylcholinesterase (AChE) at the neuromuscular junction (NMJ) of the diaphragm at 24 h, and thus improve the antagonistic action of neostigmine on rocuronium. The present study aimed to determine the effects of sepsis on AChE activity over 2 weeks, which is a more clinically relevant time period. Furthermore, the present study aimed to elucidate the association between AChE activity and its expression at the NMJ during sepsis.

[The Role of DNA Double-strain Damage Repairing Mechanisms in Diabetic Atheroscolersis].

Objectives: To identify the role of DNA double-strain damage repairing pathway in the development of diabetics atherosclerosis.

Methods: Wistar male rats were randomly divided into three groups: control group (group A), balloon injury group (group B) and diabetes + balloon injury group (group C). Streptozotocin (STZ) was injected into rat abdomen to induce diabetes.

Effect of acute peritonitis on rocuronium-induced intraperitoneal pressure reduction and the uptake function of the sarcoplasmic reticulum.

Previous studies have reported the incomplete relaxation effect of neuromuscular blockers on skeletal muscles in acute peritonitis (AP) and other inflammatory processes; however, the underlying mechanisms responsible for this effect have not yet been satisfactorily identified. The impaired removal of cytosolic Ca through sarcoendoplasmic Ca-ATPase (SERCA) and defects in sarcoplasmic reticulum (SR) Ca uptake are the major contributing factors to diastolic dysfunction. Previous studies on the effects of neuromuscular blockers have primarily focused on neuromuscular transmission.

[Lowered sarcoendoplasmic reticulum calcium uptake and diaphragmatic SERCA1 expression contribute to diaphragmatic contractile and relaxation dysfunction in septic rats].

Objective: The explore the mechanism responsible for diaphragmatic contractile and relaxation dysfunction in a rat model of sepsis.

Methods: Thirty-six adult male Sprague-Dawley rats were randomized equally into a sham-operated group and two model groups of sepsis induced by cecal ligation and puncture (CLP) for examination at 6 and 12 h following CLP (CLP-6 h and CLP-12 h groups). The parameters of diaphragm contractile and relaxation were measured, and the calcium uptake and release rates of the diaphragmatic sarcoendoplasmic reticulum (SR) and the protein expressions of SERCA1, SERCA2 and RyR in the diaphragmatic muscles were determined.

Airflow behavior changes in upper airway caused by different head and neck positions: Comparison by computational fluid dynamics.

The feasibility of computational fluid dynamics (CFD) to evaluate airflow characteristics in different head and neck positions has not been established. This study compared the changes in volume and airflow behavior of the upper airway by CFD simulation to predict the influence of anatomical and physiological airway changes due to different head-neck positions on mechanical ventilation. One awake volunteer with no risk of difficult airway underwent computed tomography in neutral position, extension position (both head and neck extended), and sniffing position (head extended and neck flexed).

Functional expression of human α7 nicotinic acetylcholine receptor in human embryonic kidney 293 cells.

The functional expression of recombinant α7 nicotinic acetylcholine receptors in human embryonic kidney (HEK) 293 cells has presented a challenge. Resistance to inhibitors of cholinesterase 3 (RIC‑3) has been confirmed to act as a molecular chaperone of nicotinic acetylcholine receptors. The primary objectives of the present study were to investigate whether the co‑expression of human (h)RIC‑3 with human α7 nicotinic acetylcholine receptor in HEK 293 cells facilitates functional expression of the α7 nicotinic acetylcholine receptor.

Sepsis Strengthens Antagonistic Actions of Neostigmine on Rocuronium in a Rat Model of Cecal Ligation and Puncture.

Background: The antagonistic actions of anticholinesterase drugs on non-depolarizing muscle relaxants are theoretically related to the activity of acetylcholinesterase (AChE) in the neuromuscular junction (NMJ). However, till date the changes of AChE activity in the NMJ during sepsis have not been directly investigated. We aimed to investigate the effects of sepsis on the antagonistic actions of neostigmine on rocuronium (Roc) and the underlying changes of AChE activity in the NMJ in a rat model of cecal ligation and puncture (CLP).

Slowed relaxation of diaphragm in septic rats is associated with reduced expression of sarco-endoplasmic reticulum CA -ATPase genes SERCA1 and SERCA2.

Introduction: The aim of this study was to study the effects of sepsis on diaphragm relaxation properties and the associated expression of sarco-endoplasmic reticulum Ca -ATPase genes SERCA1 and SERCA2.

Methods: Rats were randomized to undergo either sham surgery or cecal ligation and puncture (CLP). Diaphragm isometric relaxation parameters were measured after 24 h.

Immuno-enhancement effects of Lycium ruthenicum Murr. polysaccharide on cyclophosphamide-induced immunosuppression in mice.

Lycium ruthenicum Murr. is commonly used in traditional Tibetan medicine, and the fruits of Lycium ruthenicum Murr. contain an immunologically active pectin which improves immune function against chronic diseases.

Beneficial effects of dantrolene on sepsis-induced diaphragmatic dysfunction are associated with downregulation of high-mobility group box 1 and calpain-caspase-3 proteolytic pathway.

Background: Intracellular calcium overload is a major contributing factor to diaphragmatic dysfunction triggered by sepsis. In this study, the possible role of dantrolene, a ryanodine receptor inhibitor, in preventing the release of calcium from the sarcoplasmic reticulum in diaphragmatic dysfunction and weakness was explored.

Methods: A middle-grade severity sepsis rat model was established for the effects of treatment with dantrolene, on diaphragm harvested 24 h after cecal ligation and puncture (CLP), and analyzed using functional, histologic, and biomarker assays.

Effects of skeletal muscle denervation on the potency of succinylcholine.

The aim of the present study was to investigate the time‑dependent effects of denervation on the sensitivity of skeletal muscles to the relaxant succinylcholine (SuCh) and to assess the possible association of the de novo expression of γ‑acetylcholine receptor (AChR). Innervated as well as denervated mouse muscle cells and human embryonic kidney (HEK293) cells expressing γ‑AChR and ε‑AChR were used in the present study. The effects of SuCh on the current of nicotinic (n)AChRs were examined using a whole‑cell patch clamp technique.

The effect of infraorbital nerve block on emergence agitation in children undergoing cleft lip surgery under general anesthesia with sevoflurane.

Background: Sevoflurane is widely used in pediatric anesthesia. However, a high incidence of emergence agitation (EA) after general anesthesia with sevoflurane has been reported and pain has been regarded as a significant contributing factor. The objective of this prospective randomized, placebo-controlled trial was to determine whether infraorbital nerve block reduces EA in children undergoing repair of cleft lip after sevoflurane.

Dexmedetomidine May Produce Extra Protective Effects on Sepsis-induced Diaphragm Injury.

Objective: The objective was to evaluate the protective effects of dexmedetomidine (DEX), a selective agonist of α2-adrenergic receptor, on sepsis-induced diaphragm injury and the underlying molecular mechanisms.

Data Sources: The data used in this review were mainly from PubMed articles published in English from 1990 to 2015.

Study Selection: Clinical or basic research articles were selected mainly according to their level of relevance to this topic.

Receptor analysis of differential sensitivity change to succinylcholine induced by nerve injury in rat gastrocnemius.

Background: Urgent tracheal intubation is common in intensive care units and the emergency room, and succinylcholine is a first-line neuromuscular blocker used in these situations. Paraplegic or critically ill patients may be at a high risk of receiving succinylcholine because the denervation stage changes nicotinic receptors, which affect the efficacy and safety of succinylcholine. The objective of this study was to determine the receptor subtypes associated with changes in the pharmacodynamics of succinylcholine and its time-line trend.