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.

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.

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.

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.

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

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

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.

0.05)in healthy volunteers.

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 determine the effect of transforming growth factor-β1 (TGF-β1) on the expression of telomerase in hepatic stellate cells (HSCs) in rats and the role of TGF-β1 in the development of liver fibrosis. METHODS: Primary HSCs were isolated from normal rats by density gradient separation and divided into 2 groups for culturing. The morphology of HSCs was identified by the inverted fluorescence microscope. The purity of HSCs was identified by immunohistological expression and fluorescence analysis. One group of HSCs was treated with different concentrations (0, 0.1, 1, and 10 ng/mL) of TGF-β1 for 24 h, while the other group was treated with 1 ng/mL TGF-β1 and cultured for 3, 6, and 9 days. The mRNA expression of telomerase reverse transcriptase (TERT) was assessed and compared by polymerase chain reaction. RESULTS: Cell morphology showed that TGF-β1 triggered the differentiation of HSCs from a quiescent phenotype into highly activated myofibroblasts. TERT mRNA expression in the primary HSCs showed slight increase with the culture time, though with no statistical difference between the results at various time points (P>0.05). TGF-β1 at 0.1 ng/mL did not significantly affect the TERT mRNA level compared with the 0 ng/mL group, while 1 ng/mL and 10 ng/mL TGF-β1 significantly decreased the level of TERT mRNA (P<0.05). TGF-β1 at 1 ng/mL had only weak effect on TERT mRNA expression after the 3 day treatment compared with the 0 ng/mL group (P>0.05). TGF-β1 at 1 ng/mL significantly inhibited TERT mRNA expression 6 days after the treatment (P<0.05). TGF-β1 inhibited the expression of TERT mRNA level in the HSCs in both dose- and time-dependent manner. CONCLUSION TGF-β1 may contribute to the transdifferentiation of HSCs by reducing TERT levels to develop hepatic fibrosis.
Animals ; Cell Transdifferentiation ; Cells, Cultured ; Hepatic Stellate Cells ; drug effects ; metabolism ; RNA, Messenger ; Rats ; Telomerase ; metabolism ; Transforming Growth Factor beta1 ; pharmacology