Aminocyanopyridines as anti-lung cancer agents by inhibiting the STAT3 pathway.

Lung cancer is a leading cause of cancer-related death worldwide. Cyanopyridines and aminocyanopyridines with carbon-nitrogen bonds have been proved to exert significant anticancer, antibacterial, and anti-inflammatory effects. In this study, we showed that aminocyanopyridine 3o and 3k displaying potent antitumor activity via inhibiting the signal transducer and activator of transcription 3 (STAT3) pathway. They blocked the constitutive STAT3 phosphorylation in a dose- and time-dependent manner and regulated the transcription of STAT3 target genes encoding apoptosis factors. Most importantly, 3o also inhibited interleukin-6-induced STAT3 activation and nuclear localization. Furthermore, 3o significantly inhibited the tumor growth of H460-derived xenografts. Taken together, these findings suggest that 3o and 3k are promising therapeutic drug candidates for lung cancer by inhibiting persistent STAT3 signaling.

Short- and medium-term follow-up of transcatheter closure of perimembranous ventricular septal defects.

BACKGROUND: Transcatheter closure of perimembranous ventricular septal defects is one of the greatest challenges in interventional cardiology. Short- and midium-term follow-up data for large samples are limited. This report presents our experience with transcatheter closure of perimembranous ventricular septal defects using an occluder. METHODS: Two hundred fifty-three patients included in the database of the Second Affiliated Hospital and Yuying Children's Hospital from January 2011- December 2015 with transcatheter closure of perimembranous ventricular septal defects and discharged from follow-up. All patients were invited for clinical and transthoracic echocardiography, electrocardiogram, and thoracic radiography check-up. RESULTS: Device implantation was successful in 252 of 253 patients (99.6%). The median age was 42 months (range 27-216 months). The median follow-up duration was 36 months (range 6-60 months). The mean defect diameter was 3.5 ± 1.4 mm and the mean size of the ventricular septal defect rim below the aortic valve was 3.7 ± 1.8 mm. The mean diameter of the devices used was 4 mm. Thirty-seven patients developed arrhythmia after the procedure and recovered within 24 months; four patients had hemolysis and four had moderate tricuspid valve regurgitation. No other serious adverse event occurred during the follow-up period. CONCLUSION: Transcatheter closure of perimembranous ventricular septal defects using an occluder is safe and effective in most patients.

[Composition analysis,antioxidative and antibacterial activities comparison of agarwood oils extracted by supercritical and steam distillation].

Agarwood is a traditional and precious medicinal material and natural spice in China and other southeast Asian countries.As the head of all spices,agarwood has many pharmacological activities such as analgesia,antidiarrheal,anti-inflammatory and antibacterial effects. Due to its high price and scarce resources,there were just a few previous studies on it,mainly focusing on the chemical compositions of the agarwood essential oil and solvent extract mixture. The components of agarwood oils obtained by supercritical extraction and steam distillation were analyzed by using Gas Chromatography-Mass Spectrometer( GC-MS),and then the agarwood oils compositions and contents were compared between the traditional extraction method and the recently emerging supercritical extraction method. Antioxidant experiments of scavenging DPPH,ABTS,hydroxyl radical,total reducing power and MIC experiments of five kinds of tester strains such as staphylococcus aureus were combined to illustrate the differences between these two kinds of agarwood oils in terms of antioxidant and bacteriostatic activities. The results showed that the main components of agarwood oil were sesquiterpenoids( 68. 68%) in steam distillation extraction method,but sesquiterpenoids( 23. 78%) and chromones( 29. 42%) in supercritical extraction method. Fourteen common components included benzyl acetone,α-santalol,γ-eudesmol,agarospirol and guaiol etc. The antioxidant activity and inhibitory MIC of agarwood oils in supercritical extraction method were better than those in steam distillation method,and the inhibitory effect of agarwood oil on the growth of bacillus subtilis was found for the first time.

Oxidised Low-Density Lipoprotein and Its Receptor-Mediated Endothelial Dysfunction Are Associated with Coronary Artery Lesions in Kawasaki Disease.

The study aimed to investigate the role of oxidised low-density lipoprotein (oxLDL)/lectin-like-oxLDL receptor-1 (LOX-1) in coronary artery lesions (CALs) in Kawasaki disease (KD) and of plasma oxLDL concentration in the early prediction of CALs in KD. This prospective study included 80 KD patients, 20 febrile and 20 healthy children. oxLDL, LOX-1 and other parameters were analysed in the acute phase. Plasma oxLDL concentration and LOX-1 mRNA expression in peripheral blood mononuclear cells (PBMCs) were significantly increased in KD patients compared with febrile and healthy children (P < 0.001 and P = 0.022, respectively), particularly in the group with CALs (P < 0.001 and P = 0.027, respectively). Coronary Z-score was significantly correlated with plasma oxLDL concentration and LOX-1 mRNA expression (r = 0.739 and 0.637, respectively; P < 0.01). The sensitivity and specificity of predicting CALs were 71.4% and 77.2%, respectively, at plasma oxLDL concentration ≥ 12.38 mU/L. oxLDL/LOX-1 may be involved in CAL development. The plasma oxLDL concentration in the acute phase is a potentially useful biological indicator for predicting CAL in KD patients.

Surface Properties and Structural Transformation Behaviors of mPEG-Maleic Rosin Copolymer in Water.

mPEG (monomethoxy poly(ethylene glycol))-maleic rosin copolymer was successfully prepared. The surface properties of the copolymer were investigated by surface tension and resonance scattering techniques. The critical micelle concentration (CMC) was obtained. The adsorption behaviors and the conformational changes of the surfactant molecules at the air-water interface were described. The adsorption amount of state 1 presented a sinusoid shape and that of state 2 presented a sigmoid with the growth of П. The free energy of adsorption is more negative than that of micellization, thus, the surfactant molecules adsorb on the surface firstly, and then form micelles after saturation adsorption. Accordingly, structural transformation and aggregation behaviors of various concentration mPEG-maleic rosin copolymers with changing temperature were explored in water. The mPEG-maleic rosin chains experienced transformation from unimers to aggregates, to contracted aggregates, to cohesive aggregates with increasing temperature when the concentration is lower than CMC. This process is almost reversible with decreasing temperature. Transformation from micelle to aggregate with increasing temperature happened when the concentration is higher than CMC. The phenomena were assessed by DLS (dynamic light scattering) and SEM (scanning electron microscopy) techniques.

[Simultaneous determination of five effective components in Qingrejiedu oral liquid using high performance liquid chromatography-mass spectrometry].

A high performance liquid chromatography-electrospray ionization mass spectrometry (HPLC-ESI/MS) method for the simultaneous determination of five effective components in Qingrejiedu oral liquid was developed. The HPLC separation was performed on a Zorbax SB C18 column (250 mm x 3.0 mm, 5 microm) using 0.4 mmol/L sodium acetate solution containing 0.2% formic acid (A) and acetonitrile (B) as the mobile phase with gradient elution (0 min, 10% B; 0 --> 6 min, 10% B --> 30% B; 6 --> 15 min, 30% B --> 39% B; 15 --> 16 min, 39% B --> 80% B) at a flow rate of 0.35 mL/min. The analytes were detected by ESI(+)-MS under selected ion monitoring mode (0 --> 9.7 min, m/z 377; 9.7 --> 12 min, m/z 411; 12 --> 14.7 min, m/z 447; 14.7 --> 18 min, m/z 557; 18 --> 25 min, m/z 263). The linear ranges were 0.050-50 mg/L, 0.020-20 mg/L, 0.005-30 mg/L, 0.010-15 mg/L and 0.010-10 mg/L with detection limits of 0.010, 0.005, 0.001, 0.002 and 0.003 mg/L for chlorogenic acid, geniposide, baicalin, forsythin and indirubin, respectively. The average recoveries ranged from 97.0% to 101.7%. The relative standard deviations were less than 2.2%. This method is rapid, accurate, and suitable for the quality control of the five effective components in Qingrejiedu oral liquid.