Effects and mechanism of pterostilbene on wound healing in diabetic skin ulcer model rats / 中国药房

OBJECTIVE To explore the effects of pterostilbene （PTE） on wound healing in diabetic skin ulcer model rats and its mechanism. METHODS Ten SD rats were grouped into control group； after diabetic skin ulcer model of other rats was induced by giving high-fat and high-sugar diet+intraperitoneal injection of streptozotocin+cutting off the skin and subcutaneous tissue in the marked area of the back， model rats were randomly divided into model group， PTE low-dose group （40 mg/kg）， PTE high-dose group （80 mg/kg）， PTE high-dose+PP2 group （80 mg/kg PTE+2 mg/kg SRC inhibitor PP2）， with 10 rats in each group. On the second day after modeling， the rats in each drug group were intraperitoneally injected with corresponding drug solutions， while the rats in control group and model group were intraperitoneally injected with normal saline， once a day， for 14 consecutive days. The wound healing rate of rats in each group was measured on the 7th and 14th day of administration； the contents of interleukin-1β （IL-1β）， IL-6， tumor necrosis factor-α （TNF-α） and vascular endothelial growth factor （VEGF） in the serum of rats were detected； the pathological changes of wound granulation tissue were observed， and the expressions of SRC/mitogen-activated protein kinase kinase （MEK）/extracellular signal-regulated kinase （ERK） signaling pathway-related proteins in wound granulation tissue were detected. RESULTS Compared with control group， the wound healing rate， serum content of VEGF， the phosphorylation levels of SRC， MEK1/2 and ERK1/2 were decreased significantly （P＜0.05）， while serum contents of IL- 1β， IL-6 and TNF-α were increased significantly （P＜0.05）； there was obvious infiltration of inflammatory cells in the wound granulation tissue， and the number of new blood vessels decreased. Compared with model group， above indexes of PTE low-dose and high-dose groups were improved significantly （P＜0.05）， and the pathological injury of granulation tissue in wound was improved. PP2 significantly reversed the improvement effects of PTE on the above indexes （P＜0.05）. CONCLUSIONS PTE can promote the wound healing of diabetic skin ulcer model rats， the mechanism of which may be related to activating SRC/MEK/ERK signaling pathway.

Data Analysis of Therapeutic Drug Monitoring for Three New Pediatric Antiepileptic Drugs / 中国药师

Objective:To analyze the situation of therapeutic drug monitoring ( TDM) for 3 new antiepileptic drugs including leve-tiracetam, lamotrigine and oxcarbazepine in our hospital to provide reference for the individualized drug treatment for the children with epilepsy. Methods:The basic information, dose and TDM data of levetiracetam, lamotrigine and oxcarbazepine of the children with ep-ilepsy during 2015 and 2016 were collected and statistically analyzed in our hospital. Results: Without obvious difference in mean dose, the average plasma concentrations of oxcarbazepine in 3-6-year-old,6-10-year-old and 10-18-year-old children were significantly higher than those in less than 3-year-old children(P<0. 05). The mean dose and the average plasma concentrations of lamotrigine in children at different ages had no statistical significance(P>0. 05). The average plasma concentration of levetiracetam in less than 3-year-old children was significantly higher than that in the other children (P<0. 05). The effective rate of clinical treatment within dif-ferent plasma concentration ranges had statistical significance(P<0. 05). Conclusion: There are inter-individual differences in the plasma concentrations of antiepileptic drugs among the children with epilepsy at different ages. So the plasma concentration of antiepi-leptic drugs should be monitored regularly in order to ensure the safety and effectiveness of medication for children.

Data Analysis of Therapeutic Drug Monitoring for Three New Pediatric Antiepileptic Drugs / 中国药师

Objective:To analyze the situation of therapeutic drug monitoring ( TDM) for 3 new antiepileptic drugs including leve-tiracetam, lamotrigine and oxcarbazepine in our hospital to provide reference for the individualized drug treatment for the children with epilepsy. Methods:The basic information, dose and TDM data of levetiracetam, lamotrigine and oxcarbazepine of the children with ep-ilepsy during 2015 and 2016 were collected and statistically analyzed in our hospital. Results: Without obvious difference in mean dose, the average plasma concentrations of oxcarbazepine in 3-6-year-old,6-10-year-old and 10-18-year-old children were significantly higher than those in less than 3-year-old children(P<0. 05). The mean dose and the average plasma concentrations of lamotrigine in children at different ages had no statistical significance(P>0. 05). The average plasma concentration of levetiracetam in less than 3-year-old children was significantly higher than that in the other children (P<0. 05). The effective rate of clinical treatment within dif-ferent plasma concentration ranges had statistical significance(P<0. 05). Conclusion: There are inter-individual differences in the plasma concentrations of antiepileptic drugs among the children with epilepsy at different ages. So the plasma concentration of antiepi-leptic drugs should be monitored regularly in order to ensure the safety and effectiveness of medication for children.

Application of computer-aided approaches to the PUMC classification of scoliosis

Surgical planning for scoliosis relies on the classification of the spinal curve pattern. To improve the reliability of the Peking Union Medical College (PUMC) classification system for scoliotic spinal curves, a computer-aided system is proposed and its reliability is evaluated. First, the reliability of curve measurements was improved by the computer-aided Cobb measurement approach. Second, judgmental errors were reduced by the computer program through the automation of the PUMC classification procedure. Four observers divided into an expert group and a resident group participated in the experiments. The kappa statistic was used to evaluate the variability. Classifications of 65 scoliotic cases by the four observers showed that with the computer's aid, the average intraobserver and interobserver kappa values were improved from 0.86 to 0.93 and from 0.75 to 0.86, respectively. The results indicate that the proposed computerized system can assist a surgeon in the PUMC classification of scoliosis and is especially useful for inexperienced surgeons.

Contents Determination of Chlorogenic Acid and Vitexin in Lophatherum gracile by HPLC / 中国药房

OBJECTIVE:To establish a method for the simultaneous determination of chlorogenic acid and vitexin in Lophather-um gracile. METHODS:HPLC was performed on the column was Waters Atlantis C18 with mobile phases of acetonitrile- water (gradient elution)at a flow rate of 1.0 ml/min,detection wavelength was 280 nm,column temperature was 35 ℃,and the injec-tion volume was 10 μl. RESULTS:The linear range was 0.041 0-1.228 8 μg for chlorogenic acid(r=0.999 8)and 0.264 0-7.920 0μg for vitexin(r=0.999 9);RSDs of precision, stability and reproducibility tests were lower than 2%;recoveries were 97.6%-102.3%(RSD=1.85%,n=9) and 97.1%-101.3%(RSD=1.19%,n=9),respectively. CONCLUSIONS:The method is simple,stable and reproducible,and can be used for the simultaneous determination of chlorogenic acid and vitexin in L. gracile.

Systematic Review of the Efficacy and Safety of Rosiglitazone and Metformin in the Treatment of Type 2 Dia-betes / 中国药房

OBJECTIVE:To systematically review the efficacy and safety of rosiglitazone and metformin in the treatment of type 2 diabetes,and provide evidence-based reference for the clinical treatment. METHODS:Retrieved from PubMed,Medline, EMBase,Cochrane Library,CJFD,VIP and Wanfang database,randomized controlled trials (RCT) about rosiglitazone (test group)and metformin(control group)in the treatment of type 2 diabetes. After data extract and quality evaluation,Meta-analysis was performed by using Rev Man 5.0 statistics software. RESULTS:A total of 5 RCT were included involving 636 patients. Re-sults of Meta-analysis showed the incidence of diarrhea [RR=0.23,95%CI(0.07,0.81),P=0.000] in test groupwere significantly lower than control group,the HbA1c level [MD=0.22,95%CI(0.07,0.38),P=0.004],the incidence of edema [RR=0.20,95%CI (0.05,0.57),P=0.011] in test group was significantly higher than control group,and there was no significant difference in the fast-ing blood glucose level[MD=0.27,95%CI(-0.26,0.79),P=0.32],the incidence of nausea/vomiting [RR=0.94,95%CI(0.06, 0.89),P=0.692]between 2 groups. CONCLUSIONS:Metformin is more effective than rosiglitazone in the treatment of type 2 dia-betes,however,the incidence of diarrhea should be noticed. Due to the limit of methodological quality and sample size,it remains to be further verified with more rigorously designed and long-term follow-up of large-scale RCT.

Association of KCNJ5 gene rs3740835(C/A) and rs2604204(A/C) polymorphism with unilateral and bilateral primary aldosteronism / 中华医学遗传学杂志

<p><b>OBJECTIVE</b>To assess the association between polymorphisms of rs3740835(C/A) and rs2604204(A/C) in KCNJ5 gene with the susceptibility to unilateral and bilateral primary aldosteronism (PA).</p><p><b>METHODS</b>A total of 1043 subjects were studied, which included 83 unilateral PA patients,142 bilateral PA patients and 818 essential hypertensive(EH) patients. The polymorphism of KCNJ5 gene at rs3740835(C/A) and rs2604204(A/C) position were analyzed with a TaqMan genotyping technique.</p><p><b>RESULTS</b>Frequencies of A allele and AA+AC genotype at rs3740835(C/A) in unilateral PA group were significantly higher than EH group (P < 0.05). However, the above frequencies did not show a statistical significance between bilateral PA group and EH group (P > 0.05). No statistical difference was detected in the distribution of alleles or genotypes at rs2604204 (A/C) between unilateral PA and EH group or between bilateral PA and EH group. Haplotypic frequencies of C-A and A-A in unilateral PA group were significantly higher and lower than EH group, respectively. However, there was no statistical difference in the haplotype distribution between bilateral PA and EH groups.</p><p><b>CONCLUSION</b>Rs3740835(C/A) polymorphism may be associated with unilateral PA but not with bilateral PA. rs2604204(A/C) polymorphism is not associated with either unilateral or bilateral PA. Haplotype C-A and A-A may respectively be susceptibility factor and protective factor for unilateral PA. No haplotype has been found to associate with bilateral PA.</p>

The association between KCNJ5 gene polymorphism and primary hyperaldosteronism / 中华内分泌代谢杂志

Objective To investigate the association between KCNJ5 gene polymorphism and primary hyperaldosteronism(PA).Methods A total of 248 PA patients and 816 essential hypertension (EH) patients were enrolled in this study,TaqMan assay was used to detect the rs1221497 polymorphism of KCNJ5 gene.Results The genotypes of rs1221497 were in Hardy-Weinberg equilibrium in both PA group and EH group,the genotype frequencies ofGG,GC,CC were 208,39,1 in PA group and 631,177,8 in EH group respectively,the allele frequencies in the two groups were 455,41 and 1 439,193 respectively.The frequencies of GG genotype and G allele in PA group were significantly higher than those in EH group.Logistic regression showed that GG genotype was closely associated with PA after adjusting age.Conclusions GG genotype and G allele may contribute to the occurrence of PA.

Genetic aspects in primary aldosteronism / 中华内分泌代谢杂志

Primary aldosteronism (PA) is one of the common forms of secondary hypertension.Compared with essential hypertension patients,PA patients have a higher incidence of target organ damage and cardiovascular events.Elucidation of the underlying molecular mechanisms will likely aid the development of targeted treatments and improve prognosis for PA patients.At present,studies have elucidated the pathogenesis of familial hyperaldosteronism type Ⅰ,while the study of the pathogenesis of other subtypes is still in progressing.This review introduces the current studies on the molecular genetics of primary aldosteronism.

Characteristics of left ventricular structural damage in patients with primary aldosteronism / 中华内分泌代谢杂志

ObjectiveTo investigate the characteristics of left ventricular structural damage in patients with primary aldosteronism(PA).MethodsA total of 438 inpatients with hypertension from January 2007 to June 2010 were screened for PA,and diagnosis was made in 213 PA patients and 225 patients with essential hypertension (EH).The left ventricular structure of all subjects was evaluated according to the results of echocardiographic measurements.Results The duration of hypertension and plasma aldosterone level in patients with PA were significantly higher (P＜ 0.01 ),while the serum potassium and plasma renin activity were significantly lower (P＜0.01 ) than those in patients with EH.The interventricular septum thickness,left ventricular end-diastolic dimension,left ventricular mass index (LVMI),left ventricular end-diastolic volume,and stroke volume in patients with PA were significantly higher than those in EH patients( P＜0.01 ) after the duration of hypertension was corrected.In patients with PA,the prevalence of left ventricular hypertrophy (LVH) was higher than that in EH patients ( 53.1％ vs 33.8 ％,x2 =16.57,P ＜ 0.01 ). Normal left ventricular geometry ( NG ),concentric remodeling ( CCR ),concentric hypertrophy( CCH),and eccentric hypertrophy (ECH) were found respectively in 24.9％,22.1％,22.1％,and 30.9％ of patients with PA.Multiple stepwise regression analysis showed that the seated plasma aldosterone level (β=0.43,P ＜ 0.01 ) and systolic blood pressure (β =0.45,P ＜ 0.01 ) were the main factors that influenced LVMI.The course was the main parameter that influenced relative wall thickness(β=0.011,P＜0.05 ).Conclusion The prevalence of LVH is higher in patients with PA than that in EH patients.The eccentric hypertrophy is the most common left ventricular geometrical pattern in patients with PA.

Clinical analysis of 330 patients with primry aldosteronism / 中华内分泌代谢杂志

The clinical data of 330 patients with primary aldosteronism (PA) from January 2006 to March 2010 were retrospectively analyzed. The prevalence of 1, 2, and 3 stage hypertension in these subjects was 3.64％,20. 91％, and 75.45 ％, respectively. Of all PA patients, 89.09％ were young adults and 81.82％ were overweight or obese. There was a marked preponderance of male patients in the overweight or obese group ( P＜0. 01 ). The incidence of hypokalemia was 32. 12％. The concentration of serum potassium was not associated with the disease course. Logistic regression showed that the concentration of plasma aldosterone was an independent risk factor of hypokalemia in PA patients( P＜0. 01 ). 79. 09％ PA patients presented the plasma aldosterone level over 12 ng/dl and the renin activity level of less than 1 ng · ml-1 · h-1. The aldosterone-to-rennin activity ratio was ＞20 in 94.24％ of the patients with PA.

DNA-EGS1386 in cells induced RNase P inhibits the expression of human cytomegalovirus UL49 gene / 生物工程学报

External Guide Sequences (EGSs) represents a novel nucleic acid based gene interference approach to modulate gene expression. They are oligonucleotides that consist of a sequence complementary to a target mRNA and recruit intracellular RNase P for specific degradation of the target RNA. DNA-based EGS1386 with a size of 12 nt was chemically synthesized to target the mRNA coding for the UL49 gene of human cytomegalovirus (HCMV). The DNA-based EGS1386 molecule efficiently directed human RNase P to cleave the target mRNA sequence in vitro. A reduction of more than 50% in the levels of UL49 expression was observed in human cells treated with the DNA-based EGS1386 targeted UL49 assayed by fluorescent quantization PCR and Western blotting. This results showed that the DNA-EGS1386 can effectively guide the RNase P cut the target mRNA. Therefore, DNA-EGS can develop into a new gene silencing technology and potential of the anti-viral reagents.

An in vivo study on pharmacodynamics of 4-aminosalicylic acid oral colon-specific delivery coated tablets / 中国新药与临床杂志

AIM: To examine the pharmacodynamics of a self-developed oral colon-specific delivery coated tablets of 4-aminosalicylic acid (4-ASA) on rats. METHODS: Ulcerative colitis rat model was developed by intrarectal administration of 2, 4, 6-trinitrobenzenesulfonic acid (TNBS) in alcohol. Rats were divided randomly into healthy control group, TNBS control group, TNBS + lower dose (coated tablets) group, TNBS +medium dose (coated tablets) group, TNBS + higher dose (coated tablets) group, TNBS + sulfasalazine (SASP) group, TNBS + medium dose non-coated tablet group. Several indices including macroscopic change,histological damage, and tissue myeloperoxidase (MPO) activity were examined after 5 consecutive oral drug administration to assess pharmacodynamics of the coated tablets. RESULTS: An experimental ulcerative colitis in rats was induced by TNBS. Compared with 4-ASA non-coated tablet group, decreased macroscopic and histological damage score and lower MPO activity were observed after the oral administration of 4-ASA coated tablets or SASP. There was no significant difference between the effects on the indices of higher dose of coated tablets and SASP (P ＞ 0.05) CONCLUSION: The self-made 4-ASA oral colon-specific delivery coated tablet showes higher effect than non-coated tablets to treat ulcerative colitis in rats.

Colon-specific delivery tablets of sodium 4-aminosalicylic acid / 药学学报

Aim To prepare a new oral colon-specific delivery formulation and to investigate the release profile in vitro and the colon-specific delivery property in vivo in dogs. Methods Sodium 4-aminosalicylic acid was selected as the model drug. The combination of Eudragit RL30D and RS30D were used as sustained-release film, and Eudragit FS30D used as enteric film, which was expected to release drug depending on pH and time. The release profile of tablets was studied in three phosphate buffers with the pH 6.5, 7.0 or 7.4 for 12 h after a simulated gastric presoak for 2 h in 0.1 mol · L-1 HCl. The tablets were radiolabelled with 99mTc to make their release times and positions in the gastrointestinal tract be followed using a gamma camera. Results For the in vitro study, there was no drug released in 0. 1 mol ·L- 1 HCl for 2 h, and release occurred slowly when pH was above 6.5. Drug was released faster while pH was higher. For the in vivo study, the coated tablets remained intact in the upper gastrointestinal tract, and drug release began after the colonic arrival. The uncoated tablets, however, disintegrated in the stomach of the dogs rapidly. Conclusion The coating could protect the drug until the tablets reached the ascending colon, where drug was released slowly for over 10 h.

The Effects of Extracts of Different Constitutes of Vernonia Anthelmintica Willd on the Serum Levels of Cu and Zn in Mice / 中国药房

OBJECTIVE:To investigate the effects of extracts of different constitutes of Vernonia Anthelmintica Willd different on the serum levels of Cu and Zn in mice METHODS:Different groups of mice were given separately with (B) 1/10,(C)1/30,(C′)1/50 doses of LD50 of extracts of different constitutes of Vernonia Anthelmintica Willd for 7 days,and the levels of Cu and Zn in serum were determined RESULTS:The levels of Cu and Zn in serum were different in different groups of mice(P

Study on the Preparation and Quality Control of Indapamide Capsules / 中国药房

OBJECTIVE:To prepare indapamide capsules and study the quality control methods METHODS:The content of indapamide in capsules was determined by UV-spectrophotometry The other ingredients were determined by HPLC RES_ULTS:The calibration curve was linear within the concentration range of 3 7～11 1?g/ml(r=0 9 997);the recovery of indapamide was 99 50%,RSD=0 43% The RSDs of indapamide and other ingredients were 0 43% and 0 1% respectively The relative percentage contents of 3 batches of sample were 99 07%,99 34%,99 58% respectively The uniformity A+1 80S of contents of indapamide in all samples detected was

Depermination of the Serum Concentrations of Three Kinds of Antiepileptic Drugs and the Experience of Individualized Drug Administration / 中国药房

AIM： To give some information for rational administration of oral antiepileptic drugs to epileptic patients in clinic METHODS： The serum concentrations of oral phenytoin sodium， phenobarbital and carbamazepine were determined in 88,63 and 63 epileptic patients（ total 214 times） by fluorescence polarization immunoassay， respectively The individualized drugs administration schemes were provided RESULTS： The sensitivity to the three kinds of antiepileptic drugs varied in different patients CONCLUSIONS： The administration of oral antiepileptic drugs to epileptic patients must be based on the data of drug concentration in serum We must comprehensively consider the other factors

Study on Quality Control Method of Compound Lidocaine Cream / 中国药房

OBJECTIVE： To develop a HPLC method for the determination of the contents of lidocaine and prilocaine in compound lidocaine cream as a quality control means.METHODS： Lidocaine and prilocaine in compound lidocaine cream were determined by high-performance liquid chromatography on C18 column with the detection wavelength at 254nm.The mobile phase was 0.5％ ammonium dihydrogen phosphate(pH=7)-methanol(20∶ 80).RESULTS： The calibration curves of both lidocaine and prilocaine were linear within the concentration range of 130～250μ g/ml(r=0.9 996).The recovery rates of lidocaine and prilocaine were 99.05％ and 99.27％ respectively， RSDs were 0.67％ and 1.15％ ， intra-day RSDs 0.81％ and 1.45％ ， inter-day RSDs 0.55％ and 0.63％ respectively.CONCLUSION： The method was sensitive， stable and accurate.It can be used to determine and control the quality of compound lidocaine cream.

ATPase inhibitory factor 1-a host cell protein molecule interacting with human cytomegalovirus pUL23 protein / 中国病理生理杂志

AIM:pUL23,the product of human cytomegalovirus (HCMV) gene UL23 was identified as one of tegument proteins. The aim of this research is to investigate the function of pUL23 during HCMV life cycle.METHODS:GAL4 yeast two-hybrid assay was performed to screen the human fetal kidney cDNA library to obtain host cell protein molecules which interact with pUL23 of HCMV. Then the GST-pulldown experiment was applied to confirm the protein interactions identified by yeast two-hybrid.RESULTS:ATPase inhibitory factor 1 (ATIF1) was selected from host cells using yeast two-hybrid assay. GST-pulldown experiments in vitro further confirmed the interaction between ATIF1 and pUL23.CONCLUSION:pUL23 of HCMV can interact with ATIF1 in host cell,which may provide the evidence for understanding the function of pUL23 in the life cycle of HCMV.

Pharmacokinetics of hydroxyl-?-dextrin sodium new houttuyfonate injection in beagle dogs / 中成药

AIM:To establish the method of determining sodium new houttuyfonate in plasma and study its pharmacokinetics in beagle dogs.METHODS:The HPLC was employed with chromatographic conditions,such as octa-silicane bond silica gel column(250 mm?4.6 mm,5 ?m)as analytical column,methanol-water-ammonium hydroxide with 4 butyls(70 ∶30 ∶0.3)as mobile phase and at the flow-rate of 1.0 mL/min.The UV detection was set at 286 nm.The pharmacokinetic parameters were calculated by DAS(ver 1.0)program and compared by statistic analysis.RESULTS:The calibration curve was linear in blood plasma over the concentration range of 0.128～25.575 mg/L(r= 0.999 2),good precision and high recoveries.The parameters were T_ max= 5.0 min,C_ max= 4.982 mg/L,T_ 1/2=8.67 min.CONCLUSION:The analytical method established in this study is sensitive and exact,and can be used to measure the pharmacokinetics of sodium new houttuyfonate in beagle dog.The sodium new houttuyfonate can metabolize quickly following intravenous injection.