Beta-Elemene is an antitumor drug which is isolated from the traditional Chinese medicinal herb Curcumae Phaeocaulis Rhizoma, it is the main component of elemene which is extracted from the plant and delivered via blood circulation after intravenous injection. The antitumor effect of beta-elemene in vitro and in vivo was definite, and beta-elemene could improve the patient immunity and no sever side effect, drug resistance or bone marrow suppression were found during the clinical studies. And human serum albumin (HSA) is a primary extracellular protein which has a high concentration distribution in blood plasma and has many characteristic physiological functions. Therefore, the binding of beta-elemene to protein may be very important for absorption, distribution, metabolism and elimination. Therefore, the study on the interaction of beta-elemene with drug-carrying protein is very important. In this work, molecular binding of beta-elemene to human serum albumin (HSA) was investigated by using spectrofluorometer. the binding constants suggested that a strong interaction and the formation of a complex between beta-elemene and HSA. This clearly implies that beta-elemene can be stored and removed by the proteins in the body. Furthermore, the fluorescence quenching results showed that the HSA fluorescence was quenched by beta-elemene through static quenching mechanism. Thermodynamic parameters showed that hydrophobic interactions play a role in the binding of beta-elemene to HSA. The negative deltaH(0) and positive deltaS(0) in case of beta-elemene therefore showed that electrostatic attraction play a role in the binding of beta-elemene to HSA.
Drugs, Chinese Herbal ; chemistry ; Humans ; Kinetics ; Protein Binding ; Serum Albumin ; chemistry ; Sesquiterpenes ; chemistry ; Spectrometry, Fluorescence ; Thermodynamics

Objective To discuss the clinical application value of ultrasound contrast on evaluating fallopian tube patency.Methods Ultrasound contrast examination was conducted on 84 patients suffering from infertility and the flowing status of contrast agent in the uterine cavity and the fallopian tube and the distribution condition in the pelvic cavity were observed under the real -time ultrasound to judge the patency condition of the fallopian tube.Results After 84 patients receiving ultrasound contrast,38 cases'bilateral fallopian tubes were unobstructed,26 cases'lateral fallopian tube were unobstructed and 20 cases'bilateral fallopian were obstructed.Comparing the result of ultrasound contrast with laparoscopy,the diagnosis accuracy was 89.5%,the specificity 86% and the sensitivity 94%.Conclusion Fallopian tube ultrasound contrast technique can make an accurate and objective evaluation on the fallopian tube patency,it is an effective method to check fallopian tube patency and it is of high clinical application value.

Objective To explore the changes and significances of serum leptin and interleukin-1?(IL-1?)before and after treatment with risperidone in children with schizophrenics.Methods Thirty-one cases with first-episode children with schizophrenia were chosen in patient group.Their body weight and height were measured before and 8 weeks after treatment with risperidone to calculate the body mass index(BMI),and their fasting serum leptin and IL-1? were assayed radio-immunity method.Thirty-one healthy controls were measured at the same time.Results BMI and the level of serum leptin in patients of post-treatment increased significantly compared with those of pre-treatment(all P

Methyl parathion hydrolase (MPH, E.C.3.1.8.1) coding gene mph from Pseudomonas sp. WBC-3, isolated and identified by our lab, was successfully expressed in E. coli AD494 (DE3)/ pET32a(+) system as soluble fusion form at high level. The recombinant MPH showed nearly 4～5 fold higher specific activity to parathion than the enzyme from Pseudomonas sp. WBC-3. In addition, the thermal stability of the recombinant enzyme was improved comparing with the wild type enzyme.

According to the designed specific primers of gene fragment based on the Salvia miltiorrhiza transcriptome data, a full-length cDNA sequence of SQS2 from S. miltiorrhiza f. alba was cloned by the method of reverse transcription polymerase chain reaction (RT-PCR). The SmSQS2 cDNA sequence was obtained, this sequence is named SmSQS2 and its GenBank registration number is KM244731. The full length of SmSQS2 cDNA was 1245 bp, encoding 414 amino acids including 5'UTR 115 bp and 3'UTR 237 bp. Sequence alignment and phylogenetic analysis demonstrated that SmSQS2 had relative close relationship to the SQS2 of S. miltiorrhiza. The induction of E. coli [pET28-SQS2] in different temperature, induction time, IPTG concentrations and density of inducing host bacterium (A600) were performed, Shaking the culture at 30 degrees C until the A600 is approximately 0.6 and add IPTG to final concentration of 0.2 mmol x L(-1), and then the optimal expression of SmSQS2 recombinant protein were accumulated after the induction time of 20 h. The research provided important base for the study of sterol and terpene biosynthesis of SQS2 in S. miltiorrhiza f. alba.
Cloning, Molecular ; Farnesyl-Diphosphate Farnesyltransferase ; chemistry ; genetics ; metabolism ; Models, Molecular ; Molecular Sequence Data ; Phylogeny ; Plant Proteins ; chemistry ; genetics ; metabolism ; Salvia miltiorrhiza ; chemistry ; classification ; enzymology ; genetics ; Sequence Alignment

Adult ; Air Pollutants, Occupational ; poisoning ; Humans ; Male ; Middle Aged ; Occupational Diseases ; etiology ; Occupational Exposure ; adverse effects ; Pneumoconiosis ; etiology ; Silicon Dioxide ; poisoning

Objective:To establish the test method for histamine-like substances in pirarubicin. Methods:According to the meth-od described in the appendix of Chinese Pharmacopoeia (2010 edition), the test for histamine-like substances was carried out. Re-sults:The test for histamine-like substances had no interference under the condition with pirarubicin concentration of 0. 01mg·ml-1 . The established test method for histamine-like substances in pirarubicin was applied in 10 samples, and the results were accordant with those of the test method for depressor substances. Conclusion:The test method for histamine-like substances in pirarubicin is feasible with the limit of 1 μg·mg-1 .

Objective To understand the prevalence,drug resistance and clinical features of children with acute lower respiratory tract infection(ALRI) caused by escherichia coli.Methods From Oct. 2005 to Oct. 2006,659 patients with ALRI who were admitted to hospital were chosen and their nasopharyngeal secretions were obtained and cultured.K-B disc diffusion for antibiotic susceptibility were performed for these clinical isolates.Results Among 659 patients,118 cases were isolated escherichia coli,the rate was 17.99% which had 90 boys and 28 girls.Eighty-seven of 118 E.coli strains were with extended-spectrum ?-lactamase(ESBLs),the rate was 73.73%.All of strains were sensitive to imipenem.For ESBLs-producing strains,the ratio of resistance tocefotaxime,ceftriaxone,cefuroxime,ampicillin,piperacillin were 78.81%,73.73%,73.73%,76.27%,78.81%,respectively.Conclusions The positive rate of ESBLs producing E coli in Kunming area is high and drug resistance is severe gradually.Imipenem can be the first selection for treatment on these infections.

BACKGROUNDLittle is known about the influence of liver transplantation on the pharmacokinetics of most anesthetic drugs. The goal of this study was to study the population pharmacokinetics of remifentanil in the different phases of orthotopic liver transplantation (OLT) and the influence of relevant factors.

METHODSThirteen adult patients undergoing OLT were enrolled. A single bolus infusion of remifentanil 5 microg/kg was administered during the preanhepatic, anhepatic and neohepatic phases of OLT. Arterial blood samples of 1.5 ml were collected at 0 (baseline), 1, 2, 3, 5, 7, 10, 15, 20, 25, 30, 45, 60 and 90 minutes after drug administration. Remifentanil concentration was assayed by high-performance liquid chromatography/mass spectrometry/mass spectrometry (HPLC/MS/MS). Population pharmacokinetic modeling was performed using nonlinear mixed-effects modeling (NONMEM).

RESULTSThe pharmacokinetics of remifentanil in patients undergoing OLT was best described by a two-compartment open model. The pharmacokinetic parameters were not influenced by age, gender, operative phase, blood temperature, rehydration volume, or blood loss volume during sampling. The volume of distribution in the central compartment (V(1)) and the volume of distribution in the peripheral compartment (V(2)) were influenced by body weight.

CONCLUSIONSThe population pharmacokinetics of remifentanil in patients undergoing OLT can be well described by a two-compartment open model. The functional status of the liver does not significantly affect the pharmacokinetics of remifentanil, but the body weight is an influential factor of V(1) and V(2).

Adult ; Chromatography, High Pressure Liquid ; Female ; Humans ; Liver Transplantation ; Male ; Middle Aged ; Piperidines ; administration & dosage ; pharmacokinetics ; Tandem Mass Spectrometry

OBJECTIVETo evaluate the cardiopulmonary exercise capacity in patients with essential hypertension (EH) complicating with or without left ventricular hypertrophy (LVH).

METHODSGraded maximal exercise test on the bicycle ergometer with respiratory gas analysis were performed in 30 gender and age matched normotensive controls, 40 EH patients without LVH and 30 EH patients with LVH (LVMI>125 g/m2 in males and > 120 g/m2 in females). Metabolic equivalents (METs), oxygen uptake (VO2), oxygen uptake to body mass ratio (VO2/kg) and oxygen uptake to heart beat ratio (VO2/HR) at time of reaching anaerobic threshold (AT) and at maximal oxygen uptake (VO2max) were measured and compared.

RESULTSMETs and VO2/kg were significantly reduced in EH patients with or without LVH compared with controls [at AT, METs: 3.57 +/- 0.8 and 4.34 +/- 1.47 vs. 5.21 +/- 1.45; VO2/kg: 12.38 +/- 2.85 and 14.42 +/- 4.33 vs. 18.48 +/- 4.52, all P < 0.01; at VO2max, METs: 4.94 +/- 1.24 and 5.90 +/- 1.51 vs. 6.96 +/- 1.85; VO(2)/kg: (17.20 +/- 4.34) mlxmin(-1)xkg(-1) and (20.41 +/- 4.59) mlxmin(-1)xkg(-1) vs. (24.04 +/- 5.21) mlxmin(-1)xkg(-1), all P < 0.01]. METs and VO2/kg at both time points were also significantly reduced in EH patients with LVH compared EH patients without LVH (all P < 0.05). The lower VO2/kg in hypertensive patients was significantly correlated to higher LVMI (P < 0.05).

CONCLUSIONSCardiopulmonary exercise capacity was reduced in hypertensive patients, especially in hypertensive patients with LVH.

Adult ; Aged ; Case-Control Studies ; Exercise Test ; Exercise Tolerance ; Female ; Heart ; physiopathology ; Humans ; Hypertension ; physiopathology ; Hypertrophy, Left Ventricular ; physiopathology ; Lung ; physiopathology ; Male ; Middle Aged ; Respiratory Function Tests