Therapeutic drug monitoring of teicoplanin:an overview / 国际药学研究杂志

Teicoplanin is a new glycopeptide antibiotic marketed after vancomycin for the treatment of Staphylo- coccus aureus(SAU)infection. Previous studies have shown that teicoplanin is safer than vancomycin,especially in the nephrotoxicity,so the routine serum concentration monitoring was not performed in the clinical application of teico- planin. In recent years,it has been found that the individual differences frequently appeared in the clinical application of teicoplanin,and thus it has been suggested that the serum concentration monitoring should be carried out in its clinical application. However,the domestic studies on the serum teicoplanin concentration monitoring are rarely conducted,and its clinical application experience is insufficient in China. This paper reviews the therapeutic drug monitoring of teico- planin,in terms of the pharmacokinetic characteristics of teicoplanin,the correlation between the blood concentration with the efficacy and adverse reactions,and the factors influencing the blood concentration of teicoplanin,so as to pro- vide a reference for the therapeutic drug monitoring and the rational clinical application of teicoplanin.

Effect of proton pump inhibitors on tacrolimus blood concentration in organ transplant recipients / 国际药学研究杂志

Tacrolimus,a macrolide immunosuppressive agent,has been used as a first-line drug for the inhibi- tion of rejection after organ transplantation. In general, the organ-transplanted patients need to administer proton pump in- hibitors to prevent gastrointestinal syndrome when tacrolimus is used,and a high proportion of patients use the two drug combination. However,the combined use of tacrolimus with the proton pump inhibitor often gives rise to the fluctuation in the tacrolimus blood concentration. This fluctuation has been suggested to be likely related to the competition of the CYP3A4 metabolic enzyme between the two drugs. In this paper,the interaction between tacrolimus and different kinds of proton pump inhibitors is reviewed in order to provide reference for their clinical application.

Physicochemical properties of medicinal fungus Polyporus umbellatus sclerotial exudate / 中国中药杂志

This study was conducted to investigate the physicochemical properties of Polyporus umbellatus sclerotial exudate. Morphological characteristics of the sclerotia and its exudate were observed during different stages of sclerotial formation. The pH of the exudate was detected at different time during cultivation. A phenol-sulfuric acid method was employed to determine the polysaccharide content of P. umbellatus sclerotial exudate during cultivating time. Additionally, the protein content was measured by means of BCA protein assay. Furthermore, CAT content was detected using ultraviolet absorption method. That the protein content of the exudate and CAT specific activity rose gradually during the passage of the cultivating time indicated a high level of oxidative stress during P. umbellatus sclerotial exudate formation. The results showed that the pH of the exudate increased gradually and then dropped down during sclerotial formation. That the pH of the exudate maintained the acidity state during the cultivation indirectly indicated that acidic environment would help sclerotial formation. The exudate produced gradually and was absorbed by the sclerotia itself.

Dynamic gadoteridol-enhanced MR imaging in the end of growing long bone of piglets / 中华医学杂志(英文版)

<p><b>BACKGROUND</b>It is of value to identify the non-invasive means that can accurately reflect the blood supply of epiphysis and is more sensitive in detection of early ischemia of epiphysis than the conventional gadoteridol (Gd)-enhanced SE T1WI. The aim of this study was to evaluate the blood supply of various anatomic regions at the end of normal growing long bone using dynamic Gd-enhanced MR imaging and compare the sensitivities between dynamic Gd-enhanced MR imaging and conventional Gd-enhanced SE T1WI in the detection of decreased blood perfusion of early epiphyseal ischemia.</p><p><b>METHODS</b>Twenty-seven two-week-old piglets were used in this study. For the study of the end of normal growing long bone, unilateral MR imaging of the distal femur and proximal tibia was performed on eleven piglets. The comparison was made among various anatomic regions (physeal and epiphyseal cartilage, metaphyseal spongiosa, the secondary ossification center and metaphysis) using MRI in terms of the enhancement ratio and speed. Their relationships with the histological findings, including RBC/mm(2) and vessel distribution, were evaluated. To examine ischemic femoral head, 16 piglets were divided into two groups, with the control group having 8 piglets (involving 16 normal hips) and an ischemic group having 8 piglets (involving 16 hips with hyperabduction). In the ischemic group, MR imaging was performed on the hips in the hyperabduction immobilized persistently for 30 minutes. After MRI, the piglets were allowed to ambulate freely for 1 day and the same MR scanning was then repeated in a neutral position. The difference in enhancement ratio and speed of the femoral head between the control and ischemic group were evaluated.</p><p><b>RESULTS</b>With regard to the end of normal growing long bone, the enhancement ratio of the metaphyseal spongiosa was greatest among all the anatomic regions (P < 0.001). The enhancement ratio of physeal cartilage was greater than that of epiphyseal cartilage (P < 0. 001), which was the lowest in all tissues (P < 0.001). The enhancement speed of the spongiosa was greater than that of physis but the difference was not significant (P > 0.05). The enhancement speed of physis was greater than that of epiphyseal cartilage (P < 0.05), which was the lowest among all the tissues (P < 0.05). The enhancement ratio and speed were found to be related to the histological findings, including RBC/mm(2) (R > 0.75) and distribution of vessels in the tissues. With ischemic femoral head, the enhancement ratios of physis, anterior part and posterior part of capital femoral epiphysis were significantly lower (P < 0.05) and enhanced more slowly (P < 0.05) than those of normal femoral head on dynamic Gd-enhanced MR imaging. On conventional Gd-enhanced SE T1WI, however, no apparent decrease in enhancement ratio and speed in ischemic hips was found (P < 0.05), when they were compared with those in the normal hips.</p><p><b>CONCLUSIONS</b>Dynamic gadoteridol-enhanced MR imaging can reveal the blood supply in various anatomic regions of the end of normal growing long bone. It is more sensitive than conventional Gd-enhanced SE T1WI in the detection of early epiphyseal ischemia.</p>

Overactivated mitogen-activated protein kinase by anisomycin induces tau hyperphosphorylation / 生理学报

One of the pathological feathers of Alzheimer's disease (AD) is neurofibrillary tangles (NFTs), which consist of paired helical filaments (PHFs) formed by hyperphosphorylated microtubule-associated protein tau. To study the role of mitogen-activated protein kinase (MAPK) in tau hyperphosphorylation and the underlying mechanism, wild type mouse neuroblastoma cells (N2a) were dealt with different concentrations (0.1 microg/mL, 0.2 microg/mL and 0.4 microg/mL) of anisomycin (an activator of MAPK) for 6 h. The relationship between MAPK activity and tau phosphorylation at some Alzheimer-sites was analyzed, and the activities of protein kinase A (PKA) and glycogen synthase kinase-3 (GSK-3) were detected. The results showed that anisomycin activated MAPK in a dose-dependent manner, but tau hyperphosphorylation at Ser-198/199/202 and Ser-396/404 sites was only observed when the concentration of anisomycin was at the level of 0.4 microg/mL, and the alteration of tau phosphorylation at Ser-214 showed no significant difference in different groups. 0.2 microg/mL and 0.4 microg/mL of anisomycin led to an increase in the activity of GSK-3, respectively, but had no effect on the activity of PKA. Lithium chloride, a specific inhibitor of GSK-3, completely abolished the anisomycin-induced elevation of tau phosphorylation without any effect on the activity of MAPK. In conclusion, overactivation of MAPK up to a certain degree induces tau hyperphosphorylation at Ser-198/199/202 and Ser-396/404 sites, and this is probably related to the effect of activated GSK-3 by MAPK.

Identificition of Endophytic Bacteria EBS05 from Cinamonum camphra and Property of Its Antimicrobial Compound / 微生物学通报

An endophytic bacterium strain EBS05 from Cinamonum camphra was identified as Bacillus subtilis by morphological taxonomy and sequence analysis of 16S~23S rRNA intergenic spacer regions. Properties of antimicrobial compound produced by EBS05 were assayed. The active compound had the maximum absorbance peak at ?213.5 nm. The antimicrobial activity was stable in solution with pH value from 5 to 8, and decreased significantly in solution with pH value less than 4.0 or more than 9.0. The antimicrobial compound had thermodynamics stability. Its activity changed a little after treated at 60?C~80?C for two hours, and compared with 65% original activity after treated at 1?105 Pa for 30 minutes. The active substance had high resistance to ultraviolet radiation and protease K. Antimicrobial compound was soluble in alcohol solu- tion, which was easily dissolved in methanol and ethanol, but not dissolved in ethyl acetate, acetonitrile and petroleum et al.