AIM:To establish HPLC method for the determination of amodiaquine in human plasma.METHODS: Amodiaquine and internal standard(hydroxychloroquine) were analyzed on C18 column(150 mm ×4.6 mm, 5 μm) with methanol: water:triethylamine: orthophosphoric acid (21:77.5:1:0.5 )as mobile phase at the flow rate of 1.0 mL · min-1The UV detector was set at 294 nm. RESULTS: The retention times of amodiaquine and internal standard were 5.82, 8.56 min, respectively. The calibration curve was linear in the range from 10 to 1 000 μg ·L- 1 ( r = 0.999 8, n = 9 ). The limit of quantitation was5 μg· L-1. The extraction recovery was between 75.5 % and 82.7 %, and the methodological recovery was between 97.0 % and 104.8 %. The intra-day and inter-day RSD were less than 6.0 % and 7.5 %, respectively. CONCLUSION: This HPLC method is simple, sensitive and suitable for pharmacokinetic study of amodiaquine.

OBJECTIVE: To establish a HPLC method for content determination of gatifloxacin in human plasma.METHODS: The Analytical column was C18,the mobile phase consisted of acetonitrile-30mmol/L ammonium acetate-triethylamine-orthophosphoric acid (20∶80∶1.0∶0.7) with a flow rate of 1.0ml/min,the detection was performed at UV 294nm.RESULTS: The calibration curve was linear in the concentrations ranging from 0.1 to10.0?g /ml (r=0.9 992).The detection limit was 0.05?g/ml.The intraday RSD was less than 8% and interday RSD was less than 10%.The average recovery was (101.67?3.06)%.CONCLUSION: The method is simple, sensitive, accurate and suitable for determination of gatifloxacin in human plasma and pharmacokinetic study.

Aim To investigate the reversal effect of cinobufacine(Cino)on adrimycin(ADM)resistant human breast cancer cell line MCF-7/ADM.Methods The cytotoxic effect of Cino or ADM and the sensitivity of ADM to cells was determined by MTT assay.The intracellular concentration of ADM was detected by HPLC. The expression of P-glycoprotein(P-gp)was examined by flow cytometric(FCM) .Results The maximum non-toxic dose Cino(15 mg?L-1) increased the sensitivity of ADM in MCF-7/ADM,decreased the IC50 of ADM in MCF-7/ADM from 38.14 mg?L-1 to 12.93 mg?L-1, and significantly increased the intracellular concentration of ADM in MCF-7/ADM and reduced the expression of P-glycoprotein.Conclution The results showed that Cino can partially reverse multidrug resistance(MDR)of MCF-7/ADM cells and the mechanism might be associated with the increase of intracellular accumulation of ADM and the reduced expression of P-glycoprotein(P-gp)in MCF-7/ADM cells.

OBJECTIVETo study the effects of Ginkgo biloba extract (GBE) on the pharmacokinetics and pharmacodynamics of warfarin and observe the anticoagulant activity of GBE.

METHODA randomized, double-blinded, placebo-controlled, two-way cross-over trial was conducted. Twelve healthy volunteers (sex ratio was 1: 1) were randomized into two groups and received GBE (three pill, tid) or placebo (three pill, tid) for 5 weeks respectively. the subjects received a single dose of warfarin (5 mg) on the day 29. Blood samples for pharmacokinetics and pharmacodynamics assessment were collectd.

RESULTCompared with placebo, BE had no significant pharmacodynamics effects on warfarin and had no effects on prothrombin time (PT) and activated partial thromboplastin time (APTT). GBE extract increased C(max), AUC(0-144 min), AUC(0-infinity), t1/2, of warfarin significantly and decreased CL(F) of warfarin significantly (P < 0.05), and there were no singnificant difference of V(d) (F).

CONCLUSIONGBE has limited effects on the pharmacokinetics but no effects on the pharmacodynamics of single dose warfain in health subjects. GBE has no effects on clotting process alone.

Adult ; Anticoagulants ; pharmacology ; Double-Blind Method ; Female ; Ginkgo biloba ; Herb-Drug Interactions ; Humans ; Male ; Plant Extracts ; pharmacology ; Warfarin ; blood ; pharmacology ; Young Adult

OBJECTIVETo observe the effect of heart protection on diabetic cardiomyopathy in rats by tripterysium glucosides.

METHODThe rat diabetic cardiomyopathy rats model are made by streptozotocin, then divided into tripterysium glucosides group (n=8) and model group (n=8). In addition, the control group is established (n=8). Glucosides group was orally administrated tripterysium glucosides (18 mg x kg(-1)), the control groups was orally administrated same volume NS for 3 months. Blood sugar, heart function and cardiac index were detected after 3 months. Immunohistochemical techniques were used to detect NF-kappaB and ICAM-1 expression. Ultrastructure of cardiac muscle cell were observed by electronmicroscope.

RESULTCompared with model group, cardiac index was decreased after tripterysium glucosides administration, and LVSP, LVEDP, + dp/dtmax, -dp/dtmax, were improved, and the expression of nuclear Factor-kappaB (NF-kappaB) and intercellular adhension molecule-1 (ICAM-1) was inhibited. Ultrastructure of cardiac muscle cell such as mitochondrion and cardiac muscle fibers was atttenuated.

CONCLUSIONTripterysium glucosides could protect rat diabetic cardiomyopathy rats heart. These function may be related to inflammatory reaction inhibition and immunosuppression of tripterysium glucosides.

Animals ; Blood Glucose ; metabolism ; Cardiomyopathies ; etiology ; metabolism ; pathology ; physiopathology ; Diabetes Mellitus, Experimental ; complications ; Gene Expression Regulation ; drug effects ; Glucosides ; administration & dosage ; pharmacology ; therapeutic use ; Heart ; drug effects ; Intercellular Adhesion Molecule-1 ; metabolism ; Male ; Myocardium ; ultrastructure ; NF-kappa B ; metabolism ; Rats

Objective To investigate the anti-tumor effect of ultrasound-targeted microbubble destruction (UTMD) mediated herpes simplex virus thymedine kinase (HSV-TK) on mice ovarian cancer.Methods Forty female BALB/c-nu mice were randomly divided into four groups after the models of subcutaneous transplantation tumors were established:(A)HSV-TK + Microbubbles + Ultrasound (HSV-TK+ MBs + US);(B) HSV-TK+ Ultrasound (HSV-TK + US);(C) HSV-TK;(D) PBS.TheTK protein and mRNA expression were separately detected by western-blot and real time RT-PCR.TUNEL staining was used to detect the tumor cell apoptosis.The inhibition rates and survival time of the animals were compared among all groups.Results The HSV-TK gene transfection efficacy and tumor inhibitory effect of HSV-TK on mice transplantable tumor in group A (HSV-TK + MBs + US) were significantly improved compared with group B (HSV-TK + US),group C (HSV-TK) and group D (PBS) (P ＜0.05).However,group A has no significant difference (P ＞0.05) with other groups in improving the survival time of tumor-bearing mice.Conclusions Ultrasound-targeted microbubble destruction can effectively transfect HSV-TK gene into target tissues and play a significant inhibition effect on ovarian cancer in mice.However,this new method is not able to improve the survival time of mice for a short-term observation.

0.05)in healthy volunteers.

Objective: To explore the changes of pulmonary function in type 2 diabetes and its related factors.Methods: The pulmonary functions of 72 patients with type 2 diabetes and 22 healthy objects were measured,and the related factors,such as duration of DM,HbA1c,BMI,were analysed with linear regression analysis.Ninteen of them underwent a 12-week-long intensive insulin therapy and pulmonary function tests before and after the treatment.Results: Vital capacity(VC),forced vital capacity(FVC),forced expiratory volume in the first second(FEV1),total lung capacity(TLC) and carbon monoxide diffusion in the lung(DLco) were significantly decreased in the diabetes patients.Correlation analysis revealed that DLco was negatively correlated with the duration of DM.which was shown by linear regression analysis to be the only significant predictor.After a 12-week-long intensive insulin therapy,DLco and DLco/VA decreased significantly.Conclusion:Patients with type 2 diabetes have abnormal pulmonary ventilatory function and impaired pulmonary diffusive function,and the latter is related to the time of hyperglycemia,and can not ameliorated by short-term glycemic control.

Objective:To establish the fingerprint analysis method for the root of Rosa laevigata Michx from different regions by UPLC. Methods:The column was ACQUITY UPLC? Phenyl(2.1 mm × 100 mm,1.7 μm). The mobile phase consisted of methanol-water with gradient elution. The flow rate was 0. 2 ml·min-1 , the detection wavelength was 210 nm, the column temperature was 30℃, and the injection volume was 3 μl. Results:The fingerprint consisted of 15 common peaks. The range of similarity for twelve bat-ches of the root of R. laevigata Michx was 0. 489-0. 942. And the reference fingerprint of the root of R. laevigata Michx was estab-lished by UPLC. Conclusion:The fingerprint method is simple and reproducible, which can provide basis for the quality control and the medicinal resources exploration.

Objective:To evaluate the static symmetry in patients with early facial paralysis after masseteric-to-facial nerve transfer combined with fascia lata graft.Methods:Clinical data of paralyzed patients who treated with masseteric-to-facial nerve transfer combined with fascia lata graft in Shanghai Jiao Tong University School of Medicine Affiliated Ninth People’s Hospital from January 2016 to December 2018 were retrospectively analyzed. Patients were divided into two groups according to the degree of preoperative oral commissure dropping: slight asymmetry (Scale Ⅱ, Group A) and severe asymmetry (Scale Ⅲ, Group B). Facial muscle contraction was evaluated by Terzis Facial Grading System to evaluate smile function, which was divided into Score Ⅰ, Ⅱ, Ⅲ, Ⅳ and Ⅴ. The higher the score, the better the facial muscle contraction and the better the dynamic symmetry during preoperatively and one year postoperatively. The static symmetry of oral commissure was evaluated by Symmetry Scale of Oral Commissure to evaluate symmetry at rest, which was divided into Scale Ⅰ, Ⅱ, Ⅲ and Ⅳ, the higher the scale, the worse the static symmetry. Face-gram software was adopted to measure bilateral vertical differences(D 1) or horizontal differences(D 2) in the oral commissure position of the patients with facial paralysis for evaluating the postoperative static symmetry objectively. Statistical analyses were performed with SPSS version 26.0. Numeration data were analyzed by chi-square test. Intragroup quantitative data was analyzed by paired t-test and intergroup quantitative data was analyzed by two-sample t-test. The significance level was set at 0.05. Results:A total of 58 patients were included, including 30 patients in group A [male 12, female 18, age (43.5 ±8.1) years], and 28 patients in group B[male 12, female 16, age (40.6 ±9.6) years]. There was no significant difference in sex, age at surgery, paralyzed side and denervation time between groups ( P>0.05). The patients were scored Ⅰ on Terzis’ smile functional evaluation scale preoperatively. The score of smile function in postoperative percentage in all patients was improved to Score Ⅲ (Group A, 9/30, 30.0%; Group B, 10/28, 35.7%) or Score Ⅳ (Group A, 21/30, 70.0%; Group B, 18/28, 64.3%), according to the Terzis Facial Grading System. There was no significant difference in the improvement of smile function between groups ( P>0.05). In Group A, 73.3% patients had postoperative improvement in static symmetry (Scale Ⅱ to Scale Ⅰ, 22/30) and 26.7% patients were still Scale Ⅱ according to Symmetry Scale of Oral Commissure to evaluate symmetry at rest. In Group B, 39.3% of patients achieved static symmetry effect (Scale Ⅲ to Scale Ⅰ, 11/28), 42.9% patients had postoperative improvement (Scale Ⅲ to Scale Ⅱ, 12/28) and 17.8%(5/28) of them were still Scale Ⅲ. The proportion of achieving static symmetry effect (Scale Ⅰ) in Group A was higher than that in Group B ( P<0.01). D 1 values of one-year postoperation were smaller than that of preoperation [Group A: (5.27 ±0.74) mm vs. (2.24 ±0.57) mm; Group B: (8.22 ±1.37) mm vs. (4.42 ±0.95) mm, P<0.01]. Similarly, D 2 values of one-year postoperation were smaller than that of preoperation [Group A: (6.11 ±1.18) mm vs. (2.98±1.13) mm; Group B: (8.84 ±2.16) mm vs. (5.24 ±1.85) mm, P<0.01]. There were significant differences between groups in preoperative comparison and one-year postoperative comparison( P<0.01). Conclusions:Masseteric-to-facial nerve transfer combined with fascia lata graft achieved dynamic and static symmetry in patients with different levels of asymmetry. The postoperative static symmetry effect at rest may be influenced by the different levels of oral commissure asymmetry preoperatively.