Purinergic receptors are divided into P1(adenosine)and P2(ATP)receptors.P2 receptor are divided into two subtypes,namely P2X(ligand-gated ion channels)and P2Y(G-protein coupled)receptors.Several kinds of purinoceptor subtypes have been expressed in endocrine pancreas and participate in regulating the secretion of insulin.Purinoceptor and ligand are correlated with pathogenesis of diabetes mellitus and complications and make it possible to provide a new target to treat diabetes mellitus and complications.

P2 receptors are divided into two subclasses:P2X receptors which are ligand-gated ion channels and P2Y receptors which are G-protein coupled.Several kinds of P2X and P2Y receptor subtypes express in vascular endothelial cells and vascular smooth muscle cells.Purinergic signalling plays an important role in vascular diseases such as atherosclerosis,cerebral vessels ageing and blood vessel remodeling.So this signalling pathway may provide a new target to treat vascular diseases.

To enhance in vitro dissolution of Cur by preparing Cur solid dispersions. The ability of HPMCAS-HF,HPMCAS-MF,HPMCAS-LF and PVPK30 to maintain supersaturated solution was investigated by supersaturation test. Amorphous solid dispersions were prepared by the solvent-evaporation method. The prepared samples were characterized using infrared spectroscopy( IR) and differential scanning calorimetry( DSC),and in vitro dissolution was investigated. DSC and IR results showed that in 1 ∶3 and 1 ∶9 solid dispersions,Cur was amorphously dispersed in the carrier,and the interaction existed between drug and carrier. The supersaturation test showed that the order of the ability of polymer to inhibit crystallization of Cur was MF>HF>LF>K30. The dissolution results showed that Cur-K30 amorphous solid dispersion had the highest drug release rate; Cur-K30 and Cur-LF amorphous solid dispersions had a quicker but not stable dissolution rate,and the drug concentration decrease after 4 h; Cur-MF and Cur-HF solid dispersions had a low dissolution,which however increased steadily,attributing to the strong ability of the polymers to inhibit the crystallization of Cur. HPMCAS could inhibit the degradation of Cur better than K30,especially MF and HF. The amorphous solid dispersions of cur significantly enhanced the dissolution of Cur and improved the chemical stability of Cur. This study can provide a basis for the rational selection of the polymer used for Cur solid dispersion.
Chemistry, Pharmaceutical ; Curcumin ; chemistry ; Drug Stability ; Methylcellulose ; analogs & derivatives ; chemistry ; Polymers ; Solubility

OBJECTIVE:To compare the clinical efficacy and safety of Kangshuling gel,mupirocin and lactate ethacridine in the treatment of diabetic foot. METHODS:90 patients with diabetic foot were randomly divided into Kangshuling group,mupiro-cin group and lactate ethacridine group. All the patients were treated by lowing blood glucose,nutritional support,improving micro-circulation and anti-infection,etc. On this basis,3 groups were given Kangshuling gel,Mupirocin ointment and Lactate ethacridine solution for wet compress by gauze. The course was 180 d. The clinic data was observed,including clinical efficacy,and wound ar-ea,healed patients’granulation,epithelial tissue,healing time and incidence of adverse reactions before and after treatment. RE-SULTS:The total effective rate in Kangshuling group was significantly higher than mupirocin group and lactate ethacridine group;healed patients’granulation,epithelial tissue and healing time were significantly shorter than mupirocin group and lactate ethacri-dine group,with significant differences(P<0.05). After treatment,wound area in each group were significantly smaller than be-fore,and Kangshuling group was smaller than mupirocin group and lactate ethacridine group,with significant differences(P<0.05);there were no significant differences between mupirocin group and lactate ethacridine group(P>0.05). There were no obvi-ous adverse reactions during treatment. CONCLUSIONS:Based on the conventional treatment,Kangshuling gel has better efficacy than mupirocin and lactate ethacridine in the treatment of diabetic foot,with good safety.

OBJECTIVE:To explore the clinical features and regularity of drug-induced liver injury (DILI),and to provide reference for clinical rational drug use. METHODS:104 DILI cases in our hospital from 2005 to 2014 were selected and analyzed retrospectively in respects of patient’s gender,age,allergic history,medication history,drug type and clinical manifestations. RE-SULTS:DILI hospitalized cases increased year by year. There were 47 males and 57 females,and average age was(8.71±13.90). The clinical symptoms appeared within 12 weeks after using the drug. The symptoms were no specific,including weak,anorexia, jaundice,yellow urine,etc. and 10.57% of patients were asymptomatic. Most of the DILI cases were hepatocyte type(80.77%), followed by cholestasis type(12.50%)and hybrid type(6.73%). The most common cause of drug-induced liver injury were TCM, antimicrobial drugs and the nervous system drugs. CONCLUSIONS:The incidence of DILI in females is slightly higher than males. DILI often occurs after 40 years old. The clinical symptoms have no specificity and are similar to viral hepatitis. The hepatic lesions can be caused by most of drugs. DILI by TCM should concerned. Clinical physicians should pay more attention to DILI.

Objective To investigate the changes of plasma microRNA-223(miR-223) and HMGB-1 in pediatric sepsis patients.Methods There were 49 children with sepsis enrolled in the study (sepsis group),severe sepsis group (n=25) and general group (n=24). Meanwhile, 50 healthy children (normal control group) were selected as control group. The expression levels of plasma miR-223and HMGB-1 (high mobility group box 1) were detected. The predictive values of miR-223and HMGB-1 in plasma of children with sepsis were evaluated by receiver operatingcharacteristic (ROC) curve.Results The plasma miR-223 and HMGB-1 expression levels in severe sepsis group and general group were up-regulated compared with those in the normal control group (F=63.02, 76.32,P<0.05). The area under ROC curve of miR-223,HMGB-1 predicting sepsis were 0.904 (95%CI 0.821-0.998), 0.748 (95%CI: 0.625-0.903). There was positive correlation between miR-223 and HMGB-1 (r=3.532, P<0.05). Conclusions The expression levels of plasma miR-223 in children with sepsis are signiifcantly up-regulated, which can be used as early diagnostic markers to relfect the severity of inlfammation in some degree.

This study bioinformatically analyzed the non-VP1 capsid proteins (VP2-VP4) of Coxasckievirus A6 (CVA6), with an attempt to predict their basic physicochemical properties, structural/functional features and linear B cell eiptopes. The online tools SubLoc, TargetP and the others from ExPASy Bioinformatics Resource Portal, and SWISS-MODEL (an online protein structure modeling server), were utilized to analyze the amino acid (AA) sequences of VP2-VP4 proteins of CVA6. Our results showed that the VP proteins of CVA6 were all of hydrophilic nature, contained phosphorylation and glycosylation sites and harbored no signal peptide sequences and acetylation sites. Except VP3, the other proteins did not have transmembrane helix structure and nuclear localization signal sequences. Random coils were the major conformation of the secondary structure of the capsid proteins. Analysis of the linear B cell epitopes by employing Bepipred showed that the average antigenic indices (AI) of individual VP proteins were all greater than 0 and the average AI of VP4 was substantially higher than that of VP2 and VP3. The VP proteins all contained a number of potential B cell epitopes and some eiptopes were located at the internal side of the viral capsid or were buried. We successfully predicted the fundamental physicochemical properties, structural/functional features and the linear B cell eiptopes and found that different VP proteins share some common features and each has its unique attributes. These findings will help us understand the pathogenicity of CVA6 and develop related vaccines and immunodiagnostic reagents.
Amino Acid Sequence ; Capsid Proteins ; genetics ; immunology ; Computational Biology ; Enterovirus ; genetics ; pathogenicity ; Epitopes, B-Lymphocyte ; genetics ; immunology ; Humans

OBJECTIVETo study the extraction technology with CO2 supercritical fluid in Chinese Traditional Medicine by extracting the anthraquinones ingredients from Salvia miltiorrhiza and Polygonum caspidatum.

METHODExtractions were made under different pressure, temperature, extraction time, entrainer, and the extracts were analyzied by TLC and HPLC.

RESULTThe technology could be used in extraction and isolation. Under certain conditions, different contents of the extracts could be obtained.

CONCLUSIONCO2 supercritical fluid is good at extracing low polarity ingredients, and it shows the evident individurity in extraction of Chinese herb. The technological factors in industrial usage must be thought of all over.

Carbon Dioxide ; Chromatography, Supercritical Fluid ; methods ; Diterpenes, Abietane ; Drugs, Chinese Herbal ; isolation & purification ; Emodin ; analogs & derivatives ; isolation & purification ; Phenanthrenes ; isolation & purification ; Plants, Medicinal ; chemistry ; Polygonum ; chemistry ; Pressure ; Salvia miltiorrhiza ; chemistry ; Temperature

AIMTo study the relationship between resonance Rayleigh scattering(RRS) and the formation of association nanoparticle, and to develop a new and sensitive RRS method for the determination of trace berberine (BB).

METHODSThe association nanoparticle between BB and tetraphenylboron (TPB) was investigated by means of RRS, absorption spectral method and transmission electron microscope (TEM).

RESULTSIn pH 5.0 NaAc-HAc buffer solution, BB and TPB combine to BB-TPB association complex. The association complexes aggregate to (BB-TPB)n association nanoparticles, due to the strong hydrophobic force and Van der Waals force. It exhibits a resonance Rayleigh scattering peak at 470 nm, a maximum absorption peak at 368 nm. A new RRS method was proposed for the determination of 0.06 to 5.28 mg.L-1 BB in real samples with satisfactory results. The detection limit is 26 micrograms.L-1.

CONCLUSIONThe TEM of (BBjAgp-TPBj + p)h composite association nanoparticles was observed by means of composite association nanoreaction both TPB- and BB+ or Ag+. The results indicated that the formation of (BB-TPB)n association nanoparticles and interface of solid-liquid results in the enhanced resonance light-scattering. This new RRS method showed high sensitivity, and had been successfully applied to the determination of BB in real samples.

Berberine ; administration & dosage ; analysis ; Drug Carriers ; Drugs, Chinese Herbal ; administration & dosage ; analysis ; Nanotechnology ; Scattering, Radiation ; Spectrum Analysis ; Tablets ; Technology, Pharmaceutical ; methods ; Tetraphenylborate ; chemistry

Seventeen compounds were isolated from the 95% ethanol extract of the stems and leaves of Sapium discolor by using various chromatographic techniques,including silica gel,Sephadex LH-20,MCI,ODS,and semi-preparative HPLC. Their structures were elucidated as sapiumin F( 1),kadsulignan C( 2),ciwujiatone( 3),ethylbrevifolin carboxylate( 4),7-hydroxy-8-methoxycoumarin( 5),fraxetin( 6),fraxidin( 7),isofraxidin( 8),6,7,8-trimethoxycoumarin( 9),5,6,7,8-tetramethoxycoumarin( 10),8-hydroxy-5,6,7-trimethoxycoumarin( 11),3,3'-di-O-methylellagic acid( 12),3,3',4'-tri-O-methylellagic acid( 13),3'-methoxyellagic acid 4'-O-α-rhamnopyranoside( 14),4,5-didehydro-chebulic acid triethyl ester( 15),ent-kaurane-3-oxo-16α,17-diol( 16),and abscisic acid( 17) by spectroscopic data. Compound 1 is a new compound. Except for compounds 4,11,and 13,the remaining compounds were isolated from this plant for the first time. All the isolates were evaluated for their in vitro antineuroinflammatory activities,and the results showed that compounds 6 and 15 significantly inhibited nitric oxide production in lipopolysaccharide-induced BV-2 microglial cells,with IC50 values of 6. 06 and 6. 05 μmol·L-1,respectively.
Animals ; Cell Line ; Chromatography, High Pressure Liquid ; Mice ; Phytochemicals ; analysis ; Plant Leaves ; chemistry ; Plant Stems ; chemistry ; Sapium ; chemistry