OBJECTIVE: To establish an HPLC method for determing irinotecan (CPT-11) and its metabolite 7-ethyl-10 HCPT in rat liver microsome incubation system, and to optimize the incubation conditions. METHODS: CPT-11and SN-38 were determined by HPLC. Single factor design was used to optimize the incubation conditions. RESULTS: The linear range of CPT-11 and 7-ethyl-10 HCPT in rat liver microsome incubation system were 20-4000 ng · mL-1 and 2-400 ng · mL-1, respectively. The optimal incubation conditions were as follows: 10 μmol · L-1 CPT-11, 0.02 mg liver microsomes and incubation for 15 min. CONCLUSION: The HPLC method is accurate and suitable for the determination of CPT-11and 7-ethyl-10 HCPT in rat liver microsomes. The incubation condition can be applied in drug interaction studies of irinotecan.

OBJECTIVE: To establish a HPLC-MS/MS method for determing 5-hydroxylansoprazole/lansoprazole sulfone, and optimize the incubated conditions for rat liver microsomes. METHODS: 5-Hydroxylansoprazole/lansoprazole were determined by HPLC-MS/MS. Single factor design was used to optimize the incubated conditions and the enzymes kinetics value was evaluated by graphical analysis with Lineweaver-Burk double reciprocal plots. RESULTS: The linear range of 5-hydroxy lansoprazole and lansoprazole sulphone in liver microsome incubation system were 5.57-2 520 and 5.42-2 480 ng · mL-1, respectively. The optimal incubated conditions were 10 μmol · L-1 lansoprazole, 0.16 mg liver microsomes, and 10 min incubation, respectively. CONCLUSION: The HPLC-MS/MS method is accurate and suitable for the determination of 5-hydroxy lansoprazole and lansoprazole sulfone in rat liver microsomes. The incubated condition can be applied for study in the drug interaction with lansoprazole.

Objective:To establish the quality control for Yangxueyin oral liquids. Methods:TLC was applied to identify Angeli-cae Sinensis Radix and Fructus Ziziphi Jujubae. The content of astragaloside A in Yangxueyin oral liquids was determined by HPLC-ELSD. A Luna C18(250 mm ×4.6 mm,5 μm)column was used, the mobile phase was acetonitrile-water (38∶62)with the flow rate of 0. 8 ml·min-1 , and the column temperature was 40℃. The temperature of the drift tube was 85℃, and the flow rate of the carrier air was 2.0 L·min-1. Results: The linear range of astragaloside A was 0.522-4.176 μg(r =0.999 8). The average recovery was 97. 9% with RSD of 1. 03% (n=6). Conclusion:The method is convenient, sensitive and accurate, which can be used in the quality control of Yangxueyin oral liquids.

Objective:To investigate the significance of CT imaging features in the diagnosis of first-episode paranoid schizophrenia.Methods:Forty-five patients with first-episode paranoid schizophrenia admitted to Shaoxing 7 th People's Hospital from January 2018 to January 2019 were included in the study group. An additional 40 healthy controls who received health examination were included in the control group. All participants underwent head CT scans and CT values of cerebral lobes were measured. CT imaging features of first-episode paranoid schizophrenia were analyzed. The recurrence rate of paranoid schizophrenia was calculated. The diagnostic effect of CT imaging on paranoid schizophrenia was evaluated. Results:The CT value of the frontal lobe in the study group was significantly lower than that in the control group [(33.1 ± 1.4) HU vs. (36.9 ± 2.1) HU, t = 9.914, P < 0.001]. The proportions of patients having ventricular enlargement, sulcus widening, arachnoid cyst and cisterna magna in the study group were 51.1%, 24.4%, 31.1% and 20.0% respectively, which were significantly higher than 5.5%, 2.5%, 2.5% and 2.5% respectively in the control group ( χ2 = 21.688, 8.411, 11.928, 4.675, all P < 0.05). The recurrence rate of paranoid schizophrenia in the study group was 22.2% (10/45). The CT value of the left and right frontal lobe in patients with recurrent paranoid schizophrenia was (32.1 ± 1.7) HU and (32.5 ± 1.6) HU respectively, which was significantly lower than (35.0 ± 1.9) HU and (34.9 ± 1.7) HU in patients without recurrent paranoid schizophrenia ( t = 4.348 and 3.985, both P < 0.001). Conclusion:Patients with first-episode paranoid schizophrenia have brain structural abnormalities, as manifested by ventricular enlargement, sulcus widening, arachnoid cyst, and cisterna magna. CT imaging features are of great value in the diagnosis of first-episode paranoid schizophrenia. It deserves wide popularization and has a great innovation value.

To study the chemical constituents of Alchornea trewioides, silica gel column chromatography, Sephadex LH-20, reverse phase ODS column chromatography, MCI and semi-preparative HPLC were used to separate the 95% EtOH extract of the root of Alchornea trewioides. The structures were elucidated on the basis of spectroscopic studies including ESI-TOF-MS, 1H NMR, 13C NMR, HSQC and HMBC. Eight phenolic acids were obtained and identified as 1-O-galloyl-6-O-vanilloyl-beta-glucose (1), gallic acid (2), ethyl gallate (3), syringic acid (4), glucosyringic acid (5), erigeside C (6), 3, 4-dimethoxyphenyl-(6'-O-alpha-L-rhamnosyl)-beta-D-glucopyranoside (7) and 3, 4, 5-trimethoxyphenyl-(6'-O-galloyl)-O-beta-D-glucopyranoside (8). Among them, compound 1 is a new compound, compounds 4-8 are isolated from the genus Alchornea for the first time, and the others are isolated from the plant for the first time.

BACKGROUND:Duchenne muscular dystrophy is recognized as a fatal X-linked recessive inheritance. It is caused by the dystrophin gene mutation, resulting in the deficiency of dystrophin and consequent degeneration and necrosis of muscle fibers gradual y. Becker muscular dystrophy is also caused by the mutation of the same gene, but presented with less severe clinical symptoms compared with Duchenne muscular dystrophy. Frameshift mutation destroys the reading frames, and thus the translation cannot proceed smoothly to transcript functional proteins. In-frame mutation cannot destroy the reading frames and hence the translation can proceed smoothly. But in-frame mutation involves the whole hydrophobic regions. The three-dimensional structure of these regions and their functionality are not interpreted clearly. The effects of these regions on disease development need to be clarified in detail from the point of structure and function.
OBJECTIVE:By analyzing Kate and Dolittle scale mean hydrophobicity profile, to investigate the dystrophin hydrophobic regions using Swiss-model so as to provide the supplement explanation on the reading frame rule.
METHODS:Form 2002 to 2013, 1 038 cases diagnosed as Duchenne muscular dystrophy or Becker muscular dystrophy were col ected in the First Hospital of Sun Yat-sen University in China and Leiden DMD information database was searched with deletion of codon mutation information available. The correlation between clinical types and genotypes was analyzed upon resources col ected above. The mean hydrophobicity profile of dystrophin was analyzed by Bioedit as wel as the reconstruction of hydrophobic domains using Swiss-model. Thus, the important functional domain of dystrophin was confirmed by analysis and the correlation between clinical types and genotypes.
RESULTS AND CONCLUSION:Four hydrophobic regions were confirmed:Calponin homology domain CH2 on actin-binding domain, repeat 16 domain, Hinge Ⅲ domain and EF Hand domain. Duchenne muscular dystrophy was developed as a result of the destruction of the 1st, 2nd and 4th hydrophobic regions which were the conjunction of dystrophin and associated protein in dystrophin-glycoprotein complex. When the 3rd hydrophobic was deleted, the repeat domain located on central rob domain remained its continuity so that the clinical symptoms were less severe. These findings indicate that the dystrophin hydrophobic regions act as an important role on the pathogenesis of Duchenne muscular dystrophy.

Objective To compare the therapeutic effects of closed reduction and transverse fixation with Kirschner wires and open reduction and fixation with mini-plates or Kirschner wires for the fifth metacarpal base fracture.Methods Data of 50 patients,who had been treated in our hospital for the fifth metacarpal base fracture from August 2005 to May 2012,were enrolled in this study.Twenty-six patients underwent closed closed reduction and transverse fixation with Kirschner wires,including 22 males and 4 females,aged from 17 to 41 years; according to the OTA classification,there were 8 of type A1,11 of type B1,and 7 of type C1.Twenty-four patients underwent open reduction and fixation with mini-plates or Kirschner wires,including 21 males and 3 females,aged from 19 to 46 years (average,26 years); according to the OTA classification,there were 11 of type A1,8 of type B1 and 5 of type C1.The total active motion (TAM) score of Chinese Medical Associaition was used to evaluate the range of motion of the joint.Results In closed reduction group,the operation time ranged from 14 to 33 min; the treatment costs ranged from 2018 to 2995 yuan; 23 patients were followed up for 6 to 26 months; X-rays showed the anatomic reduction was achieved in all patients,and the fracture healing time ranged from 4 to 7 weeks; according to the TAM score,the result was excellent in 15,good in 6 and fair in 2,and the excellent and good rate was 91.3％.In open reduction group,the operation time ranged from 45 to 105 min; the treatment costs ranged from 3874 to 4793 yuan; 22 patients were followed up for 6 to 21 months; X-rays showed the anatomic reduction was achieved in all patients,and the fracture healing time ranged from 4 to 8 weeks; according to the TAM score,the result was excellent in 13,good in 7 and fair in 2,and the excellent and good rate was 90.9％.Conclusion Closed reduction and transverse fixation with Kirschner wires is an effective method for the fifth metacarpal base fracture,which has several advantages,such as simple operation,stable fixation,satisfactory results,short operation time and low treatment costs.

Objective To explore the effects of smoking on serum paraoxonase1 (PON1) activity and carotid atherosclerosis.Methods 478 subjects from residents of health screening for cardiovascular disease were enrolled from June 2012 to July 2014 in Huangpu district,shanghai.Smoking,drinking,exercise and cardiovascular disease risk factor data were recorded and gathered.All subjects accepted carotid artery ultrasound examination and were measured serum PON1 activity.The lowest quartile of serum PON1 activity level was taken as low PON1 activity level.Results (1) Serum PON1 activity in smokers was lower than that in non-smokers ((206.5±25.6) kU/L vs (230.9±38.1)kU/L,P＜0.01),incidence of carotid artery atherosclerosis in smoking group was higher than non-smoking group(75.7％ vs 56.1％,P＜0.01).(2) Multivariate logistic regression analyses indicated smoking,lack of exercise,creatinine,LDL-C were the independence factors of PON1 activity.(3) Multivariate logistic regression analyses indicated smoking,serum PON1 activity,age,gender,systolic pressure,were the independence factors of carotid atherosclerosis.Conclusion Smoking reduces serum activity.Smoking and lower serum PON1 activity level are independent risk factors of carotid atherosclerosis.

Objective:To measure the voice samples of the normal aged in order to systemically study the fea-tures of the voice changes. Method :To collect and analyze 146 voice samples of the normal aged with sonogram.Result:The fundamental frequency of the voice of the aged decreases and rises in the male more than 80 yearsolder. The low frequency harmonics are regulation and the intensity is strong in the formant of the aged. Thedifference reduces in voice between male and female. The harmonics to noise ratio tends downwards and the am-plitude perturbation quotient tends upwards along with the growth of age in the aged male. The changes of the above-mentioned parameters are not significant in the aged female. Conclusion:The voice changes are normalphysiological ones in the normal aged. The changes of the parameters are used to evaluate normal aged voice andabnormal one. The changes show that the function in the aged phonation tends to decline to a certain extent andit must be protected and be trained.

Objective:To establish a liquid chromatography-mass spectrometry(LC-MS) method for determining the concentration of amlodipine besylate in human plasma and to evaluate the bioequivalence of 2 kinds of amlodipine besylate tablets.Methods: Twenty healthy male volunteers were enrolled into a single crossover study.A single dose of the suspension equivalent to 10 mg amlodipine besylate or a reference preparation was given in a crossover way.The plasma concentrations of amlodipine besylate were determined by LC-MS method in the volunteers at different time points;the pharmacokinetic parameters and relative bioavailability were calculated and the bioequivalence of the 2 preparations were evaluated.Results: The pharmacokinetic parameters for experimental and the reference preparations were: C_max(6.21?1.88) vs(6.03?1.08) ng/ml;AUC_0-120(250.68?52.61) vs(246.14?52.11) ng h/ml;T_max(6.0?2.3) vs(6.1? 2.5) h;t_1/2(40.45?6.68) vs(43.74?9.05) h,respectively.The linear range of the present method was 0.1-20.0 ng/ml;the lowest detectable concentration of amlodipine besylate was 0.1 ng/ml.There was no significant difference in pharmacokinetic parameters between the 2 tablets.Conclusion: The present method is simple to use,fast,and accurate.The 2 preparations of amlodipine besylate are bioequivalent.