OBJECTIVE:To develop an HPLC method for the determination of 5-ISMNconcerntrations in human plasma and study the pharmacokinetics of 5-ISMN orally disintegrating tablets and the reference tablets.METHODS:A single oral dose test capsule(orally disintegrating tablets)or reference capsule of 5-ISMN(60 mg)were administered by randomized crossover way in 20 healthy male volunteers with plasma 5-ISMN concentrations determined by HPLC.The pharmacokinetic parameters were calculated with 3p87 pharmacokinetic program and the bioavailability of the two preparations was evaluated.RESULTS:The main pharmacokinetic parameters of the test preparation vs.the reference preparation were as follows:Cmax:(613.42?73.83)vs.(368.64?38.66)?g?mL-1;tmax:(26.52?2.00)vs.(95.73?4.16)min;AUC0～∞:(73 872.24?543.89)vs.(77 978.47?646.37)ng?min?mL-1,respectively.CONCLUSION:The assay was proved to be sensitive,accurate and suitable for pharmacokinetic study of 5-ISMN.The results of pharmacokinetic study after oral administration of test and reference preparations of 5-ISMN showed that the two preparations were bioequivalent while the test preparation had a higher peak concentration and could reach peak level in less time,and the test preparation showed a rapid drug releasing behavior.

Chemical constituents of Inula japonica were isolated and purified by repeated column chromatographies, over silica gel, and Toyopearl HW-40, and preparative HPLC. On the basis of spectral data analysis, including NMR and MS data, the structures of the isolates were elucidated and their anti-inflammatory activities were assayed. Fifteen compounds were isolated from the ethyl acetate extract of I. japonica, and their structures were elucidated as dihydrosyringenin (1), (3S, 5R, 6S, 7E)-5,6-epoxy-3-hydroxy-7-megastigmen-9-one (2), (6R, 7E) -9-hydroxy-4,7-megastigmadien-3-one (3), arnidiol (4), taraxasterol acetate (5), 8,9,10-trihydroxythymol (6), taxifolin (7), luteolin (8), napetin (9), eupatin (10), spinacetin (11), quercetin (12), p-hydroxycinnamic acid (13), caffeic acid (14), and caffeoyl acetate (15). Compounds 1, 2, 7, 13 and 15 were isolated from the genus Inula for the first time, and compounds 3, 4, 9-11 and 14 were isolated from this plant for the first time. The anti-inflammatory activity result showed that compounds 3, 6-12 and 14 exhibited inhibition effect against leukotriene C4 (LTC4) synthesis and degranulation definitely in c-Kit Ligand (KL) induced mast cells, and compound 8 and 12 also had the suppression effect against lipopolysacharide(LPS) induced nitric oxide (NO) activity in RAW264.7 macrophages. It is firstly reported that compounds 7 and 9-11 possessed potent inhibition activities against LTC4 generation and degranulation in mast cells.
Animals ; Anti-Inflammatory Agents ; chemistry ; pharmacology ; Cell Line ; Inula ; chemistry ; Macrophages ; drug effects ; Mast Cells ; drug effects ; Mice ; Mice, Inbred BALB C ; Plant Extracts ; chemistry ; pharmacology

Objectives To investigate the changes of cystatin C in the serum of patients with acute kidney injury ( AKI) or end-stage renal disease ( ESRD), and study its significance in the early diagnosis of AKI and its correlation with the degree of renal function injury. Method The cases in Xiangya hospital were enrolled in this study according to the RIFLE criteria, including 20 cases of slight acute kidney injury, 30 cases of medium-severe acute kidney injury, 48 cases of victims of the 5. 12 wenchuan earthquake, 32 cases of end-stage renal disease and 20 healthy patients. The microparticle-enhanced immunoturbidimetry method was used to detect serum cystatin C, and the colorimetric method was used to detect urine N-acetyl-beta-D-glucosaminidase (NAGase). The enzymic method was used to detect serum creatinine. The correlation between serum cystatin C and serum creatinine was analyzed, and the sensitivity and specificity of serum cystatin C were evaluated with the receiver operator characteristic curve (ROC curve). Results Compared with healthy control group, the serum cystatin C increased obviously in acute kidney injury group and ESRD group( P <0. 05 and P <0. 01). The serum cystatin C was positively correlated with serum creati-nine( P <0.01). The serum cystatin C in the 5. 12 wenchuan earthquake injured group was also higher than that in healthy control group ( P <0.05), an the serum cystatin C had an AUC - ROC of 0.931 ( P <0. 01). Conclusion Compared to the conventional biomarkers, the earlier emergence of serum cystatin C can contribute better to early clinical diagnosis of AKI. The serum cystatin C is positively correlated with renal function, and reflect changes in renal function accurately.

Objective To investigate the clinical significance of transvaginal ultrasound, hysteroscopy and MRI in the assessment of endometrial cancer lesions size. Methods Data from 56 patients who successively underwent transvaginal ultrasound, MRI and hysteroscopy inspection preoperative endometrial carcinoma were retrospectively analyzed to assess the accuracy of lesions size. Results The pathologic lesions size measured mean maximum diameter of 56 cases was (3.05 ± 0.23) cm, while the mean maximum diameter measured by vaginal ultrasound, MRI and hysteroscopy were respectivelly (2.46±0.31) cm, (3.12± 0.08) cm, and (3.18 ± 0.21) cm. Compared with the pathologic measured values, the compliance rates of transvaginal ultrasound, hysteroscopy and MRI were respectively 54%(30/56), 71%(40/56)and 75%(42/56), which vaginal ultrasound measurement value was significantly different than that by pathologic measured ( P=0.031), while there were significant difference between the hysteroscopy measured lesion size and pathologic measured, or between MRI measured values and pathologic measured (all P>0.05). Conclusion Preoperative assess the endometrial cancer lesions size, significance of vaginal ultrasound examination is limited, and MRI and hysteroscopy examination is accurate, but easy to over-estimated lesion size.

?ig-h_3 was first identified as a transforming growth factor-beta1-inducible gene in human lung adenocarcinoma cell line. It encodes for a secreted extracellular matrix (ECM) protein, which is thought to act on cell attachment and ECM composition. Previous study showed that ?ig-h_3 were highly expressed in human hepatoma cell lines and lowly expressed in human normal hepatic cells. The present study aimed to transfect ?ig-h_3 into 7721 cells to investigate its effect on secretion of MMPs in the transfected human hepatoma cells. Full-length ?ig-h_3 gene,cloned by reverse transcription polymerase chain reaction (RT-PCR) was inserted into the eukaryotic expression vector pEGFP-C_2. The recombinant plasmid was transfected into 7721 cells with Lipofectamine2000 and Gelatin-Zymography were adopted to detect the production of MMPs in the transfected cells. Results showed that ?ig-h_3/pEGFP-C_2 recombinant expression plasmid was successfully constructed and achieved high transfection efficiency. MMPs expression of the transfected cells was promoted significantly. These results suggest that overexpression of ?ig-h_3 promoted the production of MMPs, indicating that ?ig-h_3 may play roles in the invasive and metastatic processes of hepatoma.

OBJECTIVEThere was consanguineous relationship between caspase-3 and early damage after hypoxia and ischemia. Caspase-3 plays a key role in the process of apoptosis in neuron. Magnesium sulfate could protect neuron from injuries, but the mechanism was not clear. The study was to investigate the expression of caspase-3 mRNA in the hippocampus of seven-day-old hypoxic-ischemic rats and the possible mechanism of neural protection with magnesium sulfate.

METHODSThe model of seven-day-old hypoxia-ischemia rats was established. The rats were divided randomly into 6 groups as follows: (1) normal control (n = 4); (2) sham surgery control (n = 4); (3) hypoxia-ischemia (n = 4); (4) sodium chloride injection with hypoxia-ischemia (n = 4); (5) magnesium sulfate pre-injection with hypoxia-ischemia (n = 4); (6)magnesium sulfate post-injection with hypoxia-ischemia (n = 4). The therapy groups received a bolus injection of 500 mg/kg magnesium sulfate intraperitoneally 0.5 hour before or after hypoxia-ischemia. Semi-quantitative RT-PCR was used to measure caspase-3 mRNA expression in the hippocampus 24 hours after hypoxia-ischemia.

RESULTSThe expression of caspase-3 mRNA was significantly increased in the hippocampus of the hypoxia-ischemia pups (1.88 +/- 0.36 vs 0.97 +/- 0.46, P < 0.05). The expression of caspase-3 mRNA in rats with magnesium sulfate pre-injection and post-injection decreased significantly (1.54 +/- 0.49, 1.65 +/- 0.48 vs 1.88 +/- 0.36, P < 0.05).

CONCLUSIONCaspase-3 was activated in the hippocampus of the seven-day-old rats 24 hours after hypoxia-ischemia. The suppression of the expression of caspase-3 mRNA in the hippocampus was probably related to the protective effect of magnesium sulfate on the brain injury of hypoxia-ischemia.

Animals ; Animals, Newborn ; Caspase 3 ; Caspases ; genetics ; Female ; Gene Expression Regulation, Enzymologic ; Hippocampus ; blood supply ; metabolism ; Hypoxia-Ischemia, Brain ; physiopathology ; prevention & control ; Magnesium Sulfate ; therapeutic use ; Male ; RNA, Messenger ; genetics ; metabolism ; Rats ; Rats, Sprague-Dawley ; Reverse Transcriptase Polymerase Chain Reaction

Adolescent ; Central Nervous System Infections ; complications ; Child ; Epilepsy ; etiology ; Female ; Fever ; complications ; Humans ; Seizures, Febrile ; etiology ; Syndrome

OBJECTIVETo study the outcomes of very or extremely low birth weight (VLBW/ELBW) infants born between 2000 and 2008 in a single NICU and the medical factors associated with the termination of treatment in some infants.

METHODSIn this case control study, the clinical data of 148 VLBW/ELBW infants were retrospectively studied and the surviving infants were followed up. Both univariate analysis and multivariate logistic regression analysis were used to investigate the medical factors associated with terminating treatment in infants.

RESULTSTwenty infants (13.5%) failed to respond to the therapy and died in the hospital. Three infants (2.0%) died after discharge. Nineteen infants (12.8%) did not receive treatment due to decision of the guardian and died. Thirty infants (20.3%) were not followed up after discharge. Seventy-six infants (51.4%) survived, including 47 healthy infants, 2 cases of congenital diseases and 27 cases with poor prognosis. Multivariate logistic regression analysis showed there were 2 significant factors associated with terminating treatment: neonatal respiratory distress syndrome (P=0.030, OR=11.396, 95%CI 1.-102.701) and hospitalization periods (the year 2004-2006) (P=0.039, OR=9.869, 95%CI 1.118-87.140).

CONCLUSIONSThe survival status of VLBW and ELBW infants needs to be improved. It is important to decrease the incidence of neonatal respiratory distress syndrome for decreasing the proportion of terminating treatment in the infants.

Female ; Follow-Up Studies ; Humans ; Infant Mortality ; Infant, Extremely Low Birth Weight ; Infant, Newborn ; Infant, Very Low Birth Weight ; Intensive Care Units, Neonatal ; Logistic Models ; Male

Objective To monitor the co-infection status of Borrelia burgdorferi sensu lato (R.b.s.1) and spotted fever group Rickettsia (SFGR) in tourist areas of Heilongjiang province.Methods Polymerase chain reaction (PCR) was used to detect the 5S-23S rRNA intergenic spacer of B.b.s.1 and ompA of SFGR in ticks,dynamically collected from tourist areas of Heilongjiang province in 2010.Amplification products from positive ticks were sequenced,and phylogenetic analysis was conducted by Mega 5.0 software package.Results 849 ticks were collected from two tourist points,with the dominant ticks in Tiger Mountain and Jingpo Lake were Ixodes persulcatus and Haemaphysalis concinna.Regarding the Ixodes persulcatus from Tiger Mountain,the infection rates of B.b.s.1 and SFGR were 26.15％ and 10.05％.The infection rate of SFGR was 13.33％ in Haemaphysalis concinna and the B.b.s.1 was tndiscovered in the same ticks from Jingpo Lake.However,the co-infection could only be detected in Ixodes persulcatus of both tourist areas.Surveillance data showed that the major ticks were more likely to be appeared in July at Tiger Mountain and in June at Jingpo Lake.Data from the sequence analysis on B.b.s.1 showed that the B.b.s.1 in tourist areas could be classified into three different genotypes,other than B.garinii and B.afzelii.We first detected B.valaisiana-like group genotype in northeast of China.Results from the sequence analysis of SFGR positive products showed that the two DNA sequences of newly detected agents were completely the same as Rickettsia sp.HL-93 which was detected in Hulin and Rickettsia sp.H820 found in northeast,China.Conclusion The co-infection of B.b.s.1 and SFGR was detected in ticks from the tourist areas of Heilongjiang province,and data from the sequencing of specific fragment showed that various kinds of genotypes existed in this area.However; the rates of co-infectionitis-different according to environment,time and population that contributed to the kinds of and the index of ticks existed in the surveys points,also the infection rate of the ticks was studied.