4.Determination of yogliptin and its metabolite in Wistar rat plasma by liquid chromatography-tandem mass spectrometry.
Jun-Ting DAI ; Zhi-Yun MENG ; Xiao-Xia ZHU ; Hui GAN ; Ruo-Lan GU ; Bo YANG ; Li-Ying YU ; Gui-Fang DOU
Acta Pharmaceutica Sinica 2014;49(7):1044-1048
A rapid, sensitive and simple liquid chromatography-tandem mass spectrometric (LC-MS/MS) method was developed for the simultaneous determination of yogliptin and its metabolite in Wistar rat plasma. Linagliptin and dexamethasone were chosen as the internal standards of yogliptin and its metabolite, (R)-8-(3-hydroxypiperidine- -yl)-7-(but-2-yn-1-yl)-1-((5-fluorobenzo[d]thiazol-2-yl)methyl)-3-methyl- H-purine-2, 6 (3H, 7H)-dione, respectively. After a simple protein precipitation using acetonitrile as the precipitating solvent, both analytes and ISs were separated on a Grace Altima HP C18 column (2.1 mm x 50 mm, 5 microm) with gradient elution using methanol (containing 0.1% formic acid, 4 mmol x L(-1) ammonium acetate)-0.1% formic acid (containing 4 mmol x L(-1) ammonium acetate) as the mobile phase. A chromatographic total run time of 4.4 min was achieved. Mass spectrometric detection was conducted with electrospray ionization under positive-ion and multiple-reaction monitoring modes. Linear calibration curves for yogliptin and its metabolite were over the concentration range of 0.5 to 500 ng x mL(-1) with a lower limit of quantification of 0.5 ng x mL(-1). The intra- and inter- assay precisions were all below 14%, the accuracies were all in standard ranges. The method was used to determine the concentration of yogliptin and M1 in Wistar rat plasma after a single oral administration of yogliptin (27 mg x kg(-1)). The method was proved to be selective, sensitive and suitable for pharmacokinetic study of yogliptin and M1 in Wistar rat plasma.
Animals
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Chromatography, Liquid
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Dexamethasone
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blood
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Dipeptidyl-Peptidase IV Inhibitors
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blood
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pharmacokinetics
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Linagliptin
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blood
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Rats
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Rats, Wistar
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Tandem Mass Spectrometry
5.Clinical significance of (18)F-FDG PET/CT evaluation of response to treatment in T-cell lymphoma.
Juan CHENG ; Xiao-yi YANG ; Wen-gui XU ; Xiu-yu SONG ; Dong DAI ; Yan-jia ZHU
Chinese Journal of Hematology 2012;33(1):16-19
OBJECTIVETo investigate the usefulness of (18)F-FDG PET/CT imaging in restaging, evaluating the treatment outcome, monitoring relapse and predicting prognosis of T-cell lymphoma.
METHODSRetrospective analysis of PET/CT image results of thirty-four patients with T-cell lymphoma, and to evaluate its clinical significance in restaging, treatment efficiency, relapse monitor and prognosis prediction.
RESULTSClinical restaging among the 20 stage I and II patients, 6 were ascended, 9 descended and 5 unchanged. Restaging among the other 14 stage III and IV patients, 3 were ascended, 4 descended and 7 unchanged. There were 12 patients in complete remission (CR), 11 in partial remission (PR), 2 in stable disease (SD) and 9 in progressive disease (PD) among all the 34 patients. There is obvious statistical difference of the standardized uptake value (SUV) between the efficacy group and the inefficacy group after treatment of 6 courses at least in 25 patients among all the 34 patients (P = 0.009). There is obvious statistical difference of the SUV value before and after treatment in 8 patients among all the 34 patients (P = 0.000). There is obvious statistical difference in the survival time between the efficacy group and the inefficacy group after treatment of 6 courses at least in 25 patients among all the 34 patients (P = 0.015).
CONCLUSIONS(18)F-FDG PET/CT imaging plays an very important role in guiding clinical restaging, evaluating the treatment outcome, monitoring relapse and predicting prognosis of T-cell lymphoma. It is helpful to establish personalized treatment planning.
Adolescent ; Adult ; Aged ; Female ; Fluorodeoxyglucose F18 ; Humans ; Lymphoma, T-Cell ; diagnostic imaging ; therapy ; Male ; Middle Aged ; Positron-Emission Tomography ; methods ; Prognosis ; Retrospective Studies ; Tomography, X-Ray Computed ; methods ; Treatment Outcome ; Young Adult
6.Clinical observation on electroacupuncture combined with catgut implantation at acupoints for treatment of simple obesity of heart and spleen deficiency type.
Chun-lin TANG ; De-chun DAI ; Gui-feng ZHAO ; Wei-fang ZHU ; Lin-feng MEI
Chinese Acupuncture & Moxibustion 2009;29(9):703-707
OBJECTIVETo observe the interventional effect of electroacupuncture combined with catgut implantation at acupoints for treatment of simple obesity of heart and spleen deficiency type.
METHODSSixty five cases were randomly divided into an observation group (33 cases) and a control group (32 cases). The observation group was treated with electroacupuncture combined with catgut implantation at acupoint therapy, the electroacupuncture was applied at Zhongwan (CV 12), Xiawan (CV 10), Guanyuan (CV 4), Tianshu (ST 25), ect. and catgut implantation was given at Zhongwan (CV 12), Tianshu (ST 25), Qihai (CV 6), etc. The control group was treated with electroacupuncture only. The body weight, body mass index (BMI), waistline, waist hip ratio (WHR), Pittsburgh sleep quality index (PSQI), Hamilton anxiety scale (HAMA) and Hamilton depression scale (HAMD, 17 items) were evaluated before and after treatment, and these were also compared with those of 35 nomal cases.
RESULTSThe total effective rate of 93.9% in the observation group was higher than that of 84.4% in the control group (P < 0.05); the body weight, BMI, waistline, WHR, PSQI, HAMD and HAMA of simple obesity cases were obviously higher than those of normal cases (all P < 0.05). The scores of above indexes were all obviously decreased in both groups after treatment (all P < 0.05), and the improvement was more significant in observation group (P < 0.05).
CONCLUSIONThe sleep quality reduction and mental and psychology disorder exist in simple obesity patients, and electroacupuncture combined with catgut implantation at acupoints can reduce weight effectively, and at the same time improve the sleep quality and regulate psychological state.
Acupuncture Points ; Adult ; Catgut ; Electroacupuncture ; Female ; Heart ; physiopathology ; Humans ; Male ; Middle Aged ; Obesity ; physiopathology ; psychology ; surgery ; therapy ; Prostheses and Implants ; Prosthesis Implantation ; Spleen ; physiopathology ; Treatment Outcome ; Young Adult
7.Value of dual-time-point (18)F-fluorodeoxyglucose integrated positron emission and computed tomography in differentiation of malignant from benign gastrointestinal diseases.
Xiu-xia XU ; Juan CHENG ; Wen-gui XU ; Dong DAI ; Xiu-yu SONG ; Wen-chao MA ; Lei ZHU ; Xiang ZHU
Chinese Journal of Oncology 2012;34(5):364-368
OBJECTIVETo explore the value of dual-time-point (18)F-fluorodeoxyglucose integrated positron emission and computed tomography ((18)F-FDG PET-CT) in differentiation of malignant from benign gastrointestinal diseases.
METHODSSixty five patients with suspected gastrointestinal lesions underwent dual-time-point (18)F-FDG PET-CT imaging. Standardized uptake value (SUV) was calculated for semi-quantitative assessment. The SUV of the two acquisitions were signed SUV(early) and SUV(delayed), respectively. Then the change of SUVmax (ΔSUVmax) was calculated. The ROC curves of the SUV(early), SUV(delayed) and ΔSUV were drawn to find the best cut-off point value for differential diagnosis, and then the sensitivity, specificity, positive predictive value, negative predictive value and accuracy were calculated, respectively.
RESULTSOf the malignant lesions, the SUVmax in delayed imaging were significantly higher than those in early imaging, while there were no significant differences of SUVmax between the two images of the benign lesions. The ΔSUVmax of the malignant lesions were significantly higher than that of the benign ones. Taking the SUVmax higher than 9.2 in early imaging as positive diagnostic criteria, the sensitivity was 72.7%, the specificity was 85.7%, the positive predictive value was 91.4%, the negative predictive value was 60.0%, and the accuracy was 76.9%. Taking the SUVmax higher than 10.9 in delayed imaging as positive diagnostic criteria, the sensitivity was 75.0%, the specificity was 90.5%, the positive predictive value was 94.3%, the negative predictive value was 63.3%, and the accuracy was 80.0%. Taking the ΔSUVmax higher than 5.1% as positive diagnostic criteria, the sensitivity was 95.5%, the specificity was 85.7%, the positive predictive value was 93.3%, the negative predictive value was 90.0%, and the accuracy was 92.3%. The accuracy of dual-time-point (18)F-FDG PET-CT imaging was significantly higher than that of single-time point (18)F-FDG PET-CT imaging.
CONCLUSIONDual-time-point (18)F-FDG PET-CT imaging is a useful method for differentiating malignant from benign gastrointestinal diseases, and it is superior to the single-time point (18)F-FDG PET-CT imaging.
Adenocarcinoma ; diagnosis ; pathology ; Adult ; Aged ; Aged, 80 and over ; Colitis ; diagnosis ; pathology ; Colorectal Neoplasms ; diagnosis ; pathology ; Diagnosis, Differential ; Female ; Fluorodeoxyglucose F18 ; Follow-Up Studies ; Gastritis ; diagnosis ; pathology ; Gastrointestinal Diseases ; diagnosis ; pathology ; Gastrointestinal Neoplasms ; diagnosis ; pathology ; Humans ; Male ; Middle Aged ; Positron-Emission Tomography ; methods ; Predictive Value of Tests ; Proctitis ; diagnosis ; pathology ; Proctocolitis ; diagnosis ; pathology ; ROC Curve ; Radiopharmaceuticals ; Sensitivity and Specificity ; Stomach Neoplasms ; diagnosis ; pathology ; Tomography, X-Ray Computed ; methods
8.Relationship between the quantities of peripheral dendritic cells and of serum HBV DNA and the inflammatory reaction levels in the liver.
Bin GAO ; Hon-song CHEN ; Gui-ming ZHAO ; Ling ZHU ; Ying JI ; Ran FEI ; Chen-yang DAI ; Jian XU ; Li-min ZHU ; Lai WEI
Chinese Journal of Hepatology 2005;13(6):414-416
OBJECTIVESTo investigate the relationship between the quantity of peripheral dendritic cell (DC) and of serum HBV DNA and the inflammatory level in chronic hepatitis B (CHB).
METHODSThe myeloid DC (DC1) and plasmacytoid DC (DC2) in fresh peripheral blood were enumerated by using three-color flow cytometry in chronic hepatitis B patients and healthy donors. The hepatic inflammatory levels were evaluated by percutaneous liver biopsy. The serum HBV DNA levels were determined by real-time PCR.
RESULTSCHB patients with serum HBV DNA < or = 10(6) copies/ml exhibited a significant increase in the percentage of circulating DC2 in comparison with those of CHB patients with serum HBV DNA > or = 10(6) and with healthy donors (P < 0.05). The two latter groups showed no significant differences between each other. There was also no significant difference in the relative quantity of peripheral blood DC1 among the three groups mentioned above (P = 0.162). No evidence was found to support that the relative quantity of peripheral blood DC2 was associated with the clinical severity of the disease or the inflammatory level in the liver (P > 0.05).
CONCLUSIONThe relative quantity of peripheral blood DC2 is associated with HBV DNA level. It is suggested that DC2 may play a pivotal role in inhibiting HBV replication in CHB patients. There was no relationship found between relative quantities of DCs and the inflammatory level in the liver.
DNA, Viral ; blood ; Dendritic Cells ; cytology ; immunology ; Female ; Hepatitis B virus ; physiology ; Hepatitis B, Chronic ; immunology ; pathology ; virology ; Humans ; Liver ; pathology ; Male ; Virus Replication
9.Microbial transformation of sinenxan A, a rich constituent in callus cultures of Taxus.
Ji-xun ZHAN ; Jian-jiang ZHONG ; Jun-gui DAI ; Hong-zhu GUO ; Wei-hua ZHU ; Yuan-xing ZHANG ; De-an GUO
Acta Pharmaceutica Sinica 2003;38(7):555-558
AIMTo study the microbial transformation of sinenxan A.
METHODSChoose two strains of Fungi (Mucor spinosus AS 3.3450 and Cunninghamella echinulata AS 3.3400) and a strain of bacterium (Proteus vulgaris AS 1.1208) to transform the substrate.
RESULTSThree products were obtained and identified as 10-deacetylsinenxan A1, 6 alpha-hydroxy-10-deacetylsinenxan A2 and 9 alpha-hydroxy-10-deacetylsinenxan A3 respectively.
CONCLUSIONSinenxan A is facile to be transformed by microorganisms, the 10-acetyl group of which is an active group.
Acetates ; isolation & purification ; metabolism ; Biotransformation ; Culture Techniques ; Cunninghamella ; metabolism ; Diterpenes ; isolation & purification ; metabolism ; Mucor ; metabolism ; Plants, Medicinal ; chemistry ; Proteus vulgaris ; metabolism ; Taxus ; chemistry
10.Therapeutic potential of Naja naja atra venom in a rat model of diabetic nephropathy.
Gui Li DAI ; Jing Kang HE ; Yan XIE ; Rong HAN ; Zheng Hong QIN ; Lu Jia ZHU
Biomedical and Environmental Sciences 2012;25(6):630-638
OBJECTIVETo study the protective effects of naja naja atra venom (NNAV) in a rat model of diabetic nephropathy (DN).
METHODSThe rat diabetes model was induced by intraperitoneal injection of streptozotocin (STZ). Thirty-two model rats were randomly divided into one DN group (n=8) and three treatment groups (n=8 each) that received NNAV at doses of 30, 90, or 270 μg/(kg·day) via oral gavage, another eight rats as normal controls. After 12 weeks, all rats were sacrificed and the changes in serum and urine biological index levels were determined by colorimetric assay. Microalbumin (mALB), N-acetyl-β- glucosaminidase (NAG) and cystatin C (CysC) concentrations were measured by ELISA. Renal tissues were sliced for pathological and immunohistochemical observations.
RESULTSComparied with the DN group, serum glucose was decreased by 31.04%, total cholesterol 21.96%, triglyceride 23.78%, serum creatinine 19.83%, blood urea nitrogen 31.28%, urinary protein excretion 45.42%, mALB 10.42%, NAG 20.65%, CysC 19.57%, whereas albumin increased by 5.55%, high-density lipoprotein-cholesterol 59.09%, creatinine clearance 19.05% in the treatment group by NNAV administration at dose of 90 μg/(kg·day). NNAV also reduced the levels of malondialdehyde in serum (22.56%) and kidney tissue (9.79%), and increased superoxide dismutase concentration in serum (15%) and decreased it in renal tissue (8.85%). In addition, under light microscopy kidney structure was improved and glomerular hypertrophy decreased by 8.29%. As shown by immunohistochemistry, NNAV inhibited transforming growth factor-β1 by 6.70% and nuclear actor-κB by 5.15%.
CONCLUSIONNNAV improves biological indexes in DN, and it may exert renoprotective effects in rats with STZ-induced diabetes.
Animals ; Body Weight ; Diabetes Mellitus, Experimental ; complications ; Diabetic Nephropathies ; drug therapy ; pathology ; Dose-Response Relationship, Drug ; Elapid Venoms ; administration & dosage ; pharmacology ; Elapidae ; physiology ; Kidney ; drug effects ; pathology ; Male ; Malondialdehyde ; Organ Size ; Rats ; Rats, Wistar ; Superoxide Dismutase