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    Study on the apoptosis of human vascular smooth muscle cells induced by proteasome inhibitor MG132 and its mechanisms
    GUO Fang, QU Shun-lin, SUN Wen-qing, HE Hui, YANG Xiang-dong
    Chinese Journal of Clinical Pharmacology and Therapeutics    2009, 14 (5): 487-492.  
    Abstract104)      PDF (697KB)(750)       Save
    AIM:To study the effect of proteasome inhibitor MG132 on the expression of caspase 3 and the apoptosis in cultured human umbilical vascular smooth muscle cells. METHODS:Human umbilical vascular smooth muscle cells were treated with MG132 (2. 5, 5, 10 μmol/L) for 24 hours and for 48 hours. The apoptotic cells were determined by flow cytometric analysis. The levels of Ub, E1, E2, E3, 26S and caspase 3 mRNA expression were detected by reverse transcription- polymerase chain reaction (RT-PCR). The expression of caspase 3 protein was detected by immunocytochemistry. RESULTS: The results showed that the expressions of Ub, E1, E2, E3, 26S genes were decreased in treatment group and the apoptosis rates were increased obviously. MG132 could up-regulate the gene/protein expression of caspase 3. CONCLUSION: The results implicate that proteasome inhibitor MG132 could dose-dependently induce human umbilical vascular smooth muscle cells apoptosis, the apoptosis of human umbilical vascular smooth muscle cells induced by MG132 probably is relates to the decreases of Ub, E1, E2, E3 and 26S expressions and the increase of caspase 3 expression.
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    Analysis of metabolomic data: principal component analysis
    Jiye Aa
    Chinese Journal of Clinical Pharmacology and Therapeutics    2010, 15 (5): 481-489.  
    Abstract1012)      PDF (913KB)(3084)       Save
    Metabolomics has been widely applied to life science and showing a promising perspective. Conventional statistic analysis is not applicable to the large, multivariate dataset generated by high-throughput metabolomic tool, while it's of crucial importance to analyze and interpret the dataset. This article reviews the basic methods of principal components analysis(PCA) that is popular in metabolomics study, aiming at strengthening the fundamental knowledge of PCA and standardizing the methods and procedures for data analysis.
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    Effects of puerarin on blood lipid and expression of aorta laminin B1 mRNA in streptozotocin-induced diabetic rats
    LI Qiang-xiang, WANG Cai-yun, OU Yu-lan, HE Jin-lian, ZHU Fei-yue, ZHANG Zhuo, ZHONG Hui-ju
    Chinese Journal of Clinical Pharmacology and Therapeutics    2006, 11 (8): 883-887.  
    Abstract91)      PDF (334KB)(690)       Save
    AIM: To observe the effects of puerarin on blood lipid and expression of aorta laminin B1 mRNA in streptozotocin-induced diabetic rats.METHODS: Diabetic nephropathy rats were induced by intraperitoneal injection of STZ, and the experimental rats were divided into normal control group, model group, and puerarin group.During and after the treatment for 12 weeks, the general state, blood suger(BS) , triglyceride(TC) , cholesterol,low density lipoprotein(LDL-C) , high density lipoprotein(HDL-C) , glycosylated hemoglobin (HbA1c)and glycosylated low density lipoprotein(G-LDL) were detected.Aorta alteration of tissue morphology was observed by H.E staining, and the expressions of laminin B1 mRNA were determined by in situ hybridization analysis.RESULTS: Diabetes mellitus and aorta lesion occurred in the two model groups.Puerarin could improve the general state, decrease the level of triglyceride(P<0.05) ,serum cholesterol (P<0.05) , low density lipoprotein(P<0.05) , glycosylated hemoglobin(P<0.05) , and glycated low density lipoprotein(P<0.05) , and increase the level of high density lipoprotein(P<0.05).The expression of laminin B1 mRNA in the aorta were significantly inhibited by Puerarin (P<0.05).CONCLUSION: Puerarin have certain protective effects on aorta in rats.
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    Pharmacokinetics of single and multiple doses of Clofarabine for injection in patients with leukemia
    QIAN Zhong-lian, ZHAO Li-bo, LU Jin, ZHU Bao-ying, XU Jia, WANG Qian, FANG Yi, HUANG Jing
    Chinese Journal of Clinical Pharmacology and Therapeutics    2013, 18 (5): 537-544.  
    Abstract301)      PDF (850KB)(999)       Save
    AIM: To investigate the pharmacokinetics of Clofarabine for injection with a single and multiple dose administration in patients with acute leukemia.METHODS: 4 patients with acute leukemia received a single dose intravenous of 52 mg·m-2·d-1, and then they are repeatedly administrated with 52 mg·m-2·d-1 Clofarabine for 5 days.The concentrate of Clofarabine in plasma and urine were determined by HPLC-MS/MS.DAS pharmacokinetics software was used for data process and calculation of pharmacokinetic parameters.RESULTS: The main pharmacokinetic parameters of Clofarabine after single dose of 52 mg·m-2·d-1 Clofarabine for injection were as follows: Cmax(414±205) μg/L,tmax(3.0±1.4) h, t1/2z(4.4±2.0) h,AUC0-t(2475±659) μg·h·L-1, AUC0-∞(2566±606) μg·h·L-1, CLz(21.2±5.1) L·h-1·m-2, Vz(142±97) L/m, MRT0-t(6.3±2.2) h, Zeta(0.18±0.07) h-1, the 12 h cumulative urine excretion rate was (39.53±20.98)%, the main pharmacokinetic parameters of Clofarabine after 52 mg·m-2·d-1 for 5 days were as follows: Cmax(581±126) μg/L, tmax(2.0±0.8) h, t1/2z(6.4±3.1) h, AUC0-t(2451±349) μg·h·L-1, AUC0-∞(2603±409) μg·h·L-1, CLz(20.4±3.7) L·h-1·m-2, Vz(187±80) L/m, Zeta(0.13±0.05) h-1, MRT0-24 h(5.1±1.8) h, Css(102.14±14.53) μg/L,the accumulation coefficients R was (1.04±0.28), the fluctuation coefficients of plasma concentration DF was (576.26±226.89)%.CONCLUSION: No accumulation is detected when 52 mg·m-2·d-1 Clofarabine for injection has been administrated for 5 days, it was safe.
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    Studies on the metabolism and effect on the CYP450 of CH330331 in rat liver microsomes
    SUN Hai-yan, HE Fan, BI Hui-chang, HUANG Wen-lin, HUANG Min
    Chinese Journal of Clinical Pharmacology and Therapeutics    2010, 15 (6): 607-612.  
    Abstract88)      PDF (364KB)(636)       Save
    AIM: To study the metabolic kinetics of CH330331 in rat liver microsome, and its inhibition on CYP450 subtypes in the “cocktail” models. METHODS: The incubation parameters in rat liver microsome were optimized and were the Michaelis-Menten parameters Km and Vmax estimated the component of probe inhibitors in “cocktail” models were also confirmed and the effect of CH330331 on main subtypes of cytochrome P450 studied. RESULTS: The Km and Vmax of CH330331 were 18.96 μmol/L and 2.08 μmol/(min·mg protein), respectively. CH330331 had a weakly inhibition to the activity of CYP1A2, CYP2D6 and CYP2C9 but had no effect on CYP2C19, CYP2E1, and CYP3A4. CONCLUSION: CH330331 can increase the blood concentration of those drugs that are metabolized mainly by CYP1A2, CYP2D6 and CYP2C9.
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    Antithrombotic therapy in atrial fibrilation patients with coronary heart disease
    WU Mei-hua
    Chinese Journal of Clinical Pharmacology and Therapeutics    2012, 17 (8): 957-960.  
    Abstract312)      PDF (204KB)(738)       Save
    Antithrombotic therapy is a real challenge in atrial fibrilation patients with coronary heart disease, especially in patients undergoing coronary stenting on triple therapy, need to balance the risk of bleeding complications and the benefits of reducing atherothrombotic events.This article will focus on antithrombotic therapy in atrial fibrilation patients with coronary heart disease.
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    Development of moxifloxacin in treating community-acquired pneumonia
    ZHU Wen-jing, CUI Wei-hua, WANG Shao-hua, ZHANG Yuan-yuan, GAO Ji-jun
    Chinese Journal of Clinical Pharmacology and Therapeutics    2015, 20 (5): 597-600.  
    Abstract207)      PDF (194KB)(1108)       Save
    Community-acquired pneumonia(CAP), the inflammation of lung parenchyma, is one of the common infectious disease threaten human health. Moxifloxacin is the fourth-generation fluoroquinolone, usually used to treat CAP. Moxifloxacin holds extensive promise for clinical application because of the high antibacterial activity, low incidences of adverse effect and well tolerated. This article summarizes pharmacokinetics, pharmacodynamics and safety of Moxifloxacin to provide reference for its reasonable application.
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    Study on features of postantibiotic effects induced by six β-Lactams against Gram-negative bacilli
    Liang Yuxia1, Chen Qian, Wang Rui, Fang Yi, Liu Qingfeng
    Chinese Journal of Clinical Pharmacology and Therapeutics    1997, 2 (3): 186-189.  
    Abstract97)      PDF (163KB)(525)       Save
    Aim The postant ibio tic effects (PAEs) induced by Tienam (TIN), Carberin(CBN), Piperacillin (PIP), Mezloci llin (MZL), Cefope razone(CPZ)and Cefodizime (CDZM)against Escherichia coli and Pseudomonas aerug inosa were investigated.Methods PAEs were determined by spect rophotome tric method.Results PAEs induced by MZL, PIP, CPZ and CDZM against escherichia coli and Pseudomonas aerug inosa were rather short(<1h).No PAEs or negative PAEs were even found in the results of MZL against Esche richia coli.In genaral, β-lactam antibiotics induced very short PAEs against Gram-negative bacilli.However, PAEs (1~3h)induced by TIN and CBN were markedly longer than those by the other four β-latams.PAEs induced by CBN were significant longer than longer than that induced by TIN. PAEs induced by CBN and CBN were obviously concent ration-dependent.Conclusion The results suggested there were multiple mechanisms for PAEs induced by β-lactams.The features of TIN and CBN should be emphasized when they are individually used to define drug dosing intervals in clinic.
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    Pharmacokinetic interaction study between sorafenib and dapagliflozin in rats
    HE Xueru, LI Ying, MA Yinling, FU Yuhao, XUN Xuejiao, DONG Zhanjun
    Chinese Journal of Clinical Pharmacology and Therapeutics    2023, 28 (5): 498-507.   DOI: 10.12092/j.issn.1009-2501.2023.05.003
    Abstract241)      PDF (1822KB)(617)       Save
    AIM: To explore the pharmacokinetic interactions between sorafenib and dapagliflozin in rats and to provide some theoretical basis for the rational clinical use of the two drugs. METHODS: An ultra-performance liquid chromatography-tandem mass spectrometry (UPLC/MS/MS) method was developed for the simultaneous determination of sorafenib and dapagliflozin. Male SD rats were randomly divided into 5 groups (6 rats in each group), including 100 mg/kg sorafenib group, 0.5 mg/kg dapagliflozin group, 1 mg/kg dapagliflozin group, and 100 mg/kg sorafenib combined with 0.5 mg/kg dapagliflozin group and 100 mg/kg sorafenib combined with 1 mg/kg dapagliflozin group, for sorafenib and dapagliflozin drug interaction study. All samples were analyzed using a validated UPLC/MS/MS method, and the main pharmacokinetic parameters were calculated by compartment model. RESULTS: 1 mg/kg dapagliflozin increased the Cmax, AUC0-t and AUC0-∞ of sorafenib by 52.5%, 38.1% and 37.7%, respectively, and 0.5 mg/kg dapagliflozin increased the AUC0-t and AUC0-∞ of sorafenib by 36.3% and 36.3%. CONCLUSION: Pharmacokinetic interactions may exist between sorafenib and dapagliflozin, active surveillance for treatment and toxicity should be required when the two drugs combined together in clinical practice.
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    Effects of recombinant human insulin-like growth factor-Ι on the expression of matrix metalloproteinases and interstitial degradation of myocardial infarction rats
    WEI You-quan, CAO Heng
    Chinese Journal of Clinical Pharmacology and Therapeutics    2014, 19 (8): 866-871.  
    Abstract186)      PDF (394KB)(589)       Save
    AIM: To examine the effect of recombinant human insulin-like growth factor-I(rhIGF-I) on the expression of matrix metalloproteinases (MMPs) and interstitial degradation of myocardium in postinfarction rats. METHODS: Seven-week old male Sprague-Dawley (SD) rats were intraperitoneally injected with isoprenaline to establish myocardial infarction (MI) model. Forty-eight rats showed clear ECG evidence of infarction and were assigned randomly to IGF-I group (rhIGF-I 50 μg·kg-1·d-1, i.v.), Oct group (Octreotide 50 μg·kg-1·d-1, i.v.) or MI group (normal sodium 5 mL·kg-1·d-1, i.v.). Each group was divided into two subgroups (n=8, respectively) according to the treatment days, 2 or 14 days when the rats were sacrificed. Another 8 normal SD rats were selected as the control group. Transthoracic echocardiograms were performed to examine the thickness of anterior wall (LVAW) and posterior wall (LVPW) of left ventricle, left ventricular end-systolic diameter (LVESD), left ventricular end-diastolic diameter (LVEDD), and fractional shortening (FS) as well. The levels of MMP-2, MMP-9, TIMP-1 in myocardium were quantified with immunohistochemistry. Tissue homogenate myocardium hydroxyproline concentration was determined by pepsis method.RESULTS: Compared with the MI group, the expressions of MMP-2 and MMP-9 in rhIGF-I group were decreased, and the expression of TIMP-1 in the infarcted areas was increased;the degradation of myocardium collagen were decreased and the LVEDD and LVESD were decreased, the FS was increased; the expressions of MMP-2 and MMP-9 in Oct group were increased, the degradation of myocardium collagen was aggravated, the LVAW was decreased, the LVEDD, LVESD were increased, the FS was decreased.CONCLUSION: rhIGF-I administered to rats after MI is associated with decreased activities of MMPs, substantial increase of expression of TIMP-1, and leads to attenuate interstitial degradation of myocardium and may improve ventricular remodeling.
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    Progress in clinical application of topical anesthesia
    TAO Yijia, YANG Chun, LIU Cunming
    Chinese Journal of Clinical Pharmacology and Therapeutics    2023, 28 (5): 594-600.   DOI: 10.12092/j.issn.1009-2501.2023.05.015
    Abstract348)      PDF (614KB)(2836)       Save
    Topical anesthesia are being widely used in clinical diagnostic or therapeutic fields such as ophthalmology, ENT, dermatology, urology. It is defined as superficial loss of sensation in mucous membranes or skin, produced by direct application of penetrating local anesthetics. Topical anesthesia has the advantages of simple performance, high safety, quick recovery, which can effectively improve patient's satisfaction. In recent years, more and more attention has been paid to the concept of comfortable diagnosis and treatment. The new drugs and application methods of topical anesthesia are emerging constantly, special attention must be paid to their pharmacological characteristics and possible adverse reactions when using them. This article reviews the research progress of topical anesthesia in clinical application in order to provide reference for clinical practice.
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    Targeting multiple signaling pathways in LNCaP prostate cancer cell line by trichostatin A
    SUN Sheng-kun<, LIU Bing<, LI Xiu-shen<, HOU Chun-mei<, HONG Bao-fa2, YU Xiao-dan<
    Chinese Journal of Clinical Pharmacology and Therapeutics    2006, 11 (9): 1013-1016.  
    Abstract92)      PDF (290KB)(458)       Save
    AIM: To investigate the molecular mechanisms underlying the antitumor effect of trichostatin A (TSA) on LNCaP prostate cancer cells.METHODS: Colony formation analysis was performed to assay the effect of TSA on LNCaP colony forming ability.Western blotting was used to analyze protein acetylation standard as well as the expression of a panel of signaling molecules after TSA exposure.RESULTS: TSA inhibited the colony forming ability of LNCaP cells at a very low concentration.TSA exposure caused elevated acetylation of total cellular proteins as well as accumulation of acetylated-H3.In addition, signaling molecules which play key roles in prostate cancer such as AR, ErbB2, Raf-1,CDK4, and Akt were depleted by TSA in a dose and time-dependent manner.CONCLUSION: TSA exhibits significant antitumor activity against LNCaP cells by simultaneously interfering with multiple signaling pathways such as HER2/MAPK, AR, and PI-3K-AKT pathways.
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    Clinical application of carboprost tromethamine on prevention and treatment of postpartum hemorrhage in cesarean section
    LUO Yong-hong, HE Lian-zhi, SUN Yun-xia
    Chinese Journal of Clinical Pharmacology and Therapeutics    2012, 17 (3): 326-330.  
    Abstract485)      PDF (215KB)(568)       Save
    AIM: To investigate the clinical efficacy of carboprost tromethamine on the prevention and treatment for hemorrhage during cesarean section (CS) and postoperative hemorrhage. METHODS: From Feb. to Oct. 2011, 120 cases undergone CS with high risk of PPH were divided randomly into two groups. After delivery 250 μg carboprost tromethamine was injected on the uterine body in study group, while methyl-carboprost suppository 1.0 mg by sublingual was given immediately in control group,both on the basis of oxytocin intravenous drip. The intraoperative blood loss, postpartum bleeding in 2 h and 2-24 h and the rate of postpartum hemorrhage were compared between two groups. The changes of vital signs before and after the treatment in two groups were observed. RESULTS: There were statistically significant differences between two groups on intraoperative blood loss, postpartum hemorrhage in 2 h and 2-24 h (P<0.05); And the incidence rate of postpartum hemorrhage in study group was less than that in control group(P<0.05). There were no significant differences on the change of vital signs before and after treatment (P>0.05)CONCLUSION: It was effective, rapid and convenient to use carboprost tromethamine for the prevention and treatment in high hemorrhagic risk fators of PPH during CS with less adverse reaction.
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    Effects of the proliferation, migration and apoptosis of AHVAC-Ⅰ on gastric cancer MKN-28 cells
    HUANG Xiaomei, ZHI Hui, CHEN Hao, LU Linming, ZHU Xiaoqun, WANG Lizhen, ZHOU Jue, PANG Jinjin, XU Jinliang
    Chinese Journal of Clinical Pharmacology and Therapeutics    2024, 29 (3): 270-276.   DOI: 10.12092/j.issn.1009-2501.2024.03.004
    Abstract128)      PDF (1799KB)(377)       Save
    AIM: To investigate the effects of agkis-trodon halys venom anti-tumor component Ⅰ (AHVAC-Ⅰ) on the biological behavior of gastric cancer MKN-28 cells. METHODS: Gastric cancer MKN-28 cells were treated with the experimental concentrations (5, 10, 15 μg/mL) of AHAVC-Ⅰ for 24 h.Cell proliferation and toxicity assay (cell counting kit-8, CCK-8) was used to detect the inhibition rates of the cells in different concentrations of AHVAC-Ⅰ. The migration ability of the cells was evaluated by wound-healing and Transwell assay. The apoptosis were observed by laser confocal microscopy with annexin V-mCherry/DAPI double staining, and the apoptosis rates were analyzed by flow cytometry with annexin V-FITC/PI double fluorescence staining. The protein level of Caspease-3 was determined by Western blot. RESULTS: Compared with normal control group, the results of AHVAC-Ⅰ concentration groups showed that with the increase of AHVAC-Ⅰ concentration, the proliferative activity of MN-28 cells decreased gradually (P<0.01), the cell migration ability decreased gradually (P<0.01), and the cell apoptosis rate increased (P<0.05). The expression of apoptosis-related protein Caspease-3 was up-regulated (P<0.01). CONCLUSION: AHVAC-Ⅰ inhibits proliferation and migration of gastric cancer MSN-28 cells and induces apoptosis.
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    Effects of benazepril on pharmacokinetics of amlodipine in healthy volunteers
    HUANG Yi-ling, TIAN Lei, JIANG Juan-juan, HUA Lu, LIU Hong, LI Yi-shi
    Chinese Journal of Clinical Pharmacology and Therapeutics    2008, 13 (2): 174-178.  
    Abstract121)      PDF (212KB)(584)       Save
    AIM:To study the pharmacokinetics of amlodipine after coadministration of benazepril (10mg) plus amlodipine (5mg), or amlodipine (5mg) alone in healthy volunteers, and to evaluate the effects of pharmacokinetic interaction between amlodipine and benazepril.METHODS:Twelve male healthy volunteers were enrolled in a randomized two-way crossover study. An LC-MS-MS method was established for the determination of amlodipine in human plasma, and the data were analysed by WinNonLin software.RESULTS:The mean pharmacokinetic parameters of amlodipine after coadministration with benazepril plus amlodipine, or amlodipine alone were as follows:Cmax were (2.6 ±0.6) and (2.8 ±0.7) μg/L,AUC0 -144 were (99 ±39) and (109 ±26) μgL -1。h, t max were (5.8 ±1.3) and (5.3 ±1.0) h, t1/2 were (37 ±6) and (44 ±12) h, respectively.There were no significant differences in these parameters between coadministration of benazepril plus amlodipine and amlodipine administered alone (P >0.05 ).CONCLUSION:Coadministration with benazepril did not significantly affect the pharmacokinetics of amlodipine.
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    Effect of orange juice on talinolol pharmacokinetcs
    HE Shan
    Chinese Journal of Clinical Pharmacology and Therapeutics    2007, 12 (8): 953-956.  
    Abstract111)      PDF (170KB)(445)       Save
    AIM: To observe the effect of orange juice on the pharmacokinetics of p-glycoprotein (PGP) substrate drug talinolol. METHODS: 12 healthy adult men were enrolled in this clinical trial with a 2-phase randomized crossover design.In each phase the volunteers received placebo water or 200 mL orange juice 3 times daily for 3 consecutive days, on the fourth day, all subjects took 100 mg talinolol tablet after treated either with orange juice or placebo water one more time, blood samples were collected up to 36 hours with a 7-day washout period.Plasma talinolol were measured by HPLC.Pharmacokinetic parameters between orange juice and placebo water treatment groups were compared. RESULTS: Orange juice treatment reduce the plasma talinolol concentrations, decreases Cmax and AUC by 47.6% [(166±44) ng/mL versus (317±119) ng/mL] and 27%[(1783±494) ng·mL-1·h versus (2456±1048) ng·mL-1·h].The time to reach maximal talinolol concentration was markedly prolonged, 2.5 h (1.5-4 h) versus 4 h (2.5-6 h), there was no significant difference for half life of talinolol between the two groups(P> 0.05). CONCLUSION: The orange juice substantially reduces the absorption and the bioavailability of talinolol, to such a great extent of the orange juice-talinolol interaction, it is likely to have clinical importance, not only for talinolol, but also for those drugs which share the same transport protein.
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    Pharmacokinetic and pharmacodynamic interaction between irbesartan and hydrochlorothiazide in renal hypertensive rats
    HUANG Xiao-hui, HUANG Ji-han, CHEN Yun, QIU Fu-rong, LI Jun, SUN Rui-yuan
    Chinese Journal of Clinical Pharmacology and Therapeutics    2012, 17 (3): 294-301.  
    Abstract447)      PDF (494KB)(626)       Save
    AIM: Pharmacokinetic-pharmacodynamic (PK/PD) modeling was applied to investigate the pharmacokinetic and pharmacodynamic interaction between irbesartan and HCTZ in renal hypertensive rats at non-steady-state and steady-state. METHODS: The renal hypertensive rats were treated with oral irbesartan alone, or HCTZ alone, or the combination of irbesartan and HCTZ for 8 days. Systolic and diastolic blood pressure and plasma concentrations were measured after single- and multi- dosing and PK/PD parameters were analyzed. RESULTS: Irbesartan showed a two-compartment model pharmacokinetic profile. The concentration-time course of irbesartan was not changed by HCTZ, but irbesartan increased the peak plasma concentration and area under the curve of HCTZ at steady-state. Irbesartan plus HCTZ had greater blood pressure lowering action than irbesartan alone. HCTZ increased actions of irbesartan. Hysteresis phenomenon was found between effect and plasma concentrations of irbesartan after a single dose. However, hysteresis phenomenon disappeared at steady state with more rapid realization of maximum concentration and effects. The relationship between effects and effect-compartment concentrations of the drugs was represented by a sigmoid Emax model. CONCLUSION: The results suggest synergistic pharmacodynamic interaction between irbesartan and HCTZ in renal hypertensive rats and some differences of PK/PD properties between irbesartan and irbesartan/HCTZ combinations at non-steady state and steady state. These comparisons are likely to be clinically significant.
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    Effect of Heparin on heparanase mRNA expression and invasion of human hepatoma carcinoma cells in vitro
    CHEN Xiao-peng, LIU Ying-bin, SHI Liang-hui, PAN Yi-long, RUI Jing
    Chinese Journal of Clinical Pharmacology and Therapeutics    2006, 11 (7): 810-813.  
    Abstract96)      PDF (269KB)(392)       Save
    AIM: To explore the effect of Heparin on heparanase (HPA) mRNA expression and invasion of human hepatoma carcinoma cells(HCC) in vitro.METHODS: Human liver carcinoma cells, BEL-7404, were transfected with a full-length human HPA cDNA using a pcDNA3 expression plasmid, and different dose of Heparin was added when the cells were cultured.The invasiveness of transfected BEL-7404 was measured by the Matrigel invasion assays, and the HPA mRNA expression was observed by using RT-PCR.RESULTS: The HPA mRNA expression could not be detected in BEL-7404 cells(HCC group) and HCC transfected with a control pcDNA3 plasmid lacking the HPA cDNA insert (pcDNA3 group) while the HPA expression was positive in HPAtransfected HCC (pcDNA3-HPA group).The number of membrane-permeating cells in pcDNA3-HPA group(27.00±4.30) was significantly more than that in the other groups (11.67±2.52 for HCC group and 9.67±2.89 for pcDNA3 group ) (P<0.01).No obvious changes inHPA expression and cell invasiveness were observed in both HCC group and pcDNA3 group after Heparin was added.The membrane-permeating cells in pcDNA3-HPA group gradually decreased along with the increase in the dose of Heparin, and the further decrease was no longer found when added Heparin exceeded a certain quantity.The HPA expression was positive all the time in pcDNA3-HPA group.CONCLUSION: Within a certain dose range, Heparin can inhabit the invasive ability of HPA gene-transfected HCC, but does not influence the HPA mRNA expression.
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    Application of chitosan nanoparticle served as drug delivery system for cancer therapy#br#
    SUN Rensong, ZHANG Jianbin, FANG Jiani, LYU Xia, TANG Zeyao, TIAN Yan
    Chinese Journal of Clinical Pharmacology and Therapeutics    2021, 26 (1): 65-75.   DOI: 10.12092/j.issn.1009-2501.2021.01.009
    Abstract832)      PDF (801KB)(1261)       Save
    Cancer is one of the malignant diseases threatening human. In recent years, nanotechnology is becoming the hope the cancer treatment, as it can take the drugs targeting to tumor sites, with enhanced efficacy and reduced toxicity. Chitosan is the only alkaline polysaccharide in nature with good biocompatibility and biodegradability. Moreover, chitosan has many reaction sites to make derivatives with different properties. Chitosan and its derivatives are widely used for drug delivery systems and tissue engineering scaffolds. Hence, they are valuable in the field of biomedicine. In this paper, the recent advances chitosan nanoparticles as drug delivery system for delivering anticancer drugs are reviewed, especially the advances of the preparation, passive targeting, active targeting, and stimuli-responsive drug delivery systems of chitosan nanoparticles. 
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    Effects of rosiglitazone coadministration with compound sulfamethoxazole on the pharmacokinetics
    HE Jun , DUAN Li-fang , ZHANG Wei , LI Zhi , FAN Lan , SHEN Jie , ZHOU Hong-hao
    Chinese Journal of Clinical Pharmacology and Therapeutics    2009, 14 (5): 531-535.  
    Abstract103)      PDF (327KB)(382)       Save
    AIM:To investigate the effect of compound sulfamethoxazole on the rosiglitazone pharmacokinetics in normal Chinese subjects and assess the safety when they are coadministrated in clinic. METHODS: Ten male healthy volunteers completed a randomized, two-period, double-blind crossover study. Volunteers received single dose rosiglitazone (4 mg)in the presence and absence of compound sulfamethoxazole 1g given twice daily for 4. 5 days. The plasma drug concentrations were determined at each time point after oral rosiglitazone. The related pharmacokinetical parameters in vivo were computed. The concentrations of rosiglitazone and N-demethylrosiglitazone were assessed by HPLC-MS/MS. RESULTS:The Cmax and tmaxof rosiglitazone and N-demethylrosiglitazone were not changed by compound sulfamethoxazole treatment, respectively(P >0. 05).But the AUC0-48 of rosiglitazone was increased by 40% (P =0. 000)from (6768 ±900)ng·mL-1·h to (9485 ±1638)ng·mL-1·h, and the tmaxwas increased by 44% (P =0. 007)from (4. 4 ±0. 8)to (6. 1 ±1. 2)h. The AUC0-48 of biotransformation rate of N-demethylrosiglitazone/rosiglitazone was decreased to 59. 8% (P =0. 001).CONCLUSION: Compound sulfamethoxazole decreases the rosiglitazone biotransformation rate and increases the plasma rosiglitazone concentrations in healthy volunteers when they are co-administrated.
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    Progress in research and evaluation on drug-plasma protein binding in pharmacology
    GUO Bin, LI Chuan
    Chinese Journal of Clinical Pharmacology and Therapeutics    2005, 10 (3): 241-253.  
    Abstract500)      PDF (406KB)(3065)       Save
    Drug-protein binding changes involved in numerous factors in vivo may cause changes of pharmacokinetic parameters.The tendency gained from large numbers of articles overemphasized the clinical importance of these changes.However, theoretic analysis and review of available literature data indicated that changes in plasma protein binding are usually of no principle pharmacodynamic implication.And they have little effect on the clinical exposure of a patient to a drug in a practical sense. The progress is reviewed in research and current opinions on drug-plasma protein binding in pharmacological basis for pharmacokinetic consequence and clinical relevance in this article.
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    Network pharmacology-molecular docking analysis and experimental validation to explore the protective mechanism of Mongolian medicine Gaoyou on renal function
    Celimuge, Hudeligen, XU Liang
    Chinese Journal of Clinical Pharmacology and Therapeutics    2024, 29 (9): 968-978.   DOI: 10.12092/j.issn.1009-2501.2024.09.002
    Abstract156)      PDF (2207KB)(379)       Save
    AIM: To explore the protective mechanism of Mongolian medicine Gaoyou on renal function through network pharmacology molecular docking and animal experiments. METHODS: The effective active components and targets of Gao you acting on acute kidney injury (AKI) and the related targets of AKI disease were obtained by using the relevant database of traditional Chinese medicine. The targets and components were mutually constructed to act on the network, and the signal pathways of drugs and diseases were enriched and analyzed. And the molecular docking validation study was carried out on the pharmacodynamic components with high moderate value in the network and the core action target. On this basis, after establishing the rat model of acute renal injury and giving Gaoyou intervention, the contents of creatinine (CR), urea nitrogen (BUN) and tumor necrosis factor-A (TNF-α), Kidney damage molecule-1 (Kim-1), cystatin C (Cys-C), neutrophil gelatinase related lipid transporter (NGAL) in serum of rats were detected, and renal tissue sections were observed with HE staining to verify the protective effect of Mongolian medicine Gaoyou on renal function of rats with acute renal injury. The predicted signal pathway was verified by Western blot. RESULTS: 40 key targets were obtained by network pharmacology and molecular docking analysis. KEGG and go enrichment analysis were carried out on the key targets. ALB, AKT1, VEGFA, IL-6, CASP3 and other key targets were predicted, and cancer signal pathway, TNF signal pathway, PI3K/AKT signal pathway and other key pathways were predicted. The results of molecular docking showed that the main active components of Gaoyou had good binding activity with related targets. The results of animal experiments showed that Gao you had a good protective effect on renal function, and Cr and BUN were significantly lower than those in the model group (P<0.05). The content of TNF-α decreased significantly (P<0.05). Kim-1, Cys-C and NGAL decreased significantly (P<0.05). HE staining showed that Gao can obviously improve the pathological state of acute renal damage. The expression of AKT1, p-AKT1 and CASP3 in renal tissue of rats with acute renal injury increased (P<0.05). Compared with the model group, the expression of AKT1, p-AKT1 and CASP3 in renal tissue of rats in Gaoyou group decreased significantly (P<0.05). CONCLUSION: Gaoyou can protect the renal function of rats with renal injury through multiple pathways such as anti-inflammatory, antioxidant, antithrombotic, anti apoptotic and so on through the characteristics of multi-component, multi target. Intervention of PKA3/AKT signal pathway and apoptosis factor may be one of its main mechanisms.
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    Clinical observation of nebulized budesonide and oral montelukast in the treatment of cough variant asthma
    JIA Li-hong ,YAN Juan-juan
    Chinese Journal of Clinical Pharmacology and Therapeutics    2012, 17 (7): 816-820.  
    Abstract461)      PDF (261KB)(735)       Save
    AIM: To compare the therapy effect of inhalation of budesonide suspension with oral montelukast in cough variant asthma ( CVA ) of children.. METHODS: 118 cases of CVA were divided into group A(n=40) , who were used air compression pump inhalation of budesonide suspension; group B(n=40), who were taken orally montelukast; group C(n=38), who were given loratadine by oral administration .Each group of children were done observation diary every day, recorded the cough,asthma and medication from day to night, followed up once a week in the treatment of 4 weeks,followed up 1-2 times once month after symptom controlled, telephone followed up during the period.If appeared asthma, outpatient was received follow-up. During the follow-up period, three groups were recorded respectively cough symptoms in day and night after treatment with 1, 2, 3, 4, 8, 12 week and done total scores.After 6 months of treatment, we assessed the control condition of asthma. Continue to follow-up 18 months, we observed the recurrence of patients within 2 years and the numbers of wheezing episode and changed into typical asthma (CA) of three groups within 2 years, and recorded the adverse reaction during the treatment. RESULTS: The valid control rates of three groups were 97.5%, 95%, 18.4%, respectively. Compared with group C, the efficacy had significant difference in group A,group B (χ2=16.004, P<0.05). There was no significant difference between group A and group B (χ2=1.946, P>0.05). Compared with before treatment,the total scores was decreased in the treatment of 1, 2, 3, 4 week in group A, group B; In the treatment of 2, 3 week, cough score of group A was decreased obviously than that in group B, the difference was statistically significant (P<0.05); Three groups after treatment, the number of CVA recurrence and wheezing in group A,B was less than that in group C , and relapse rate of group A was 7.5%, wheezing ratio was 10%, while in group B were 25%, 35% (χ2=8.467, P<0.05). CONCLUSION: Compare with take orally montelukast, compress aerosol inhalation budesonide can anesis clinical symptoms better and faster, reduce the recurrence of CVA, effective prevent into typical asthma, and the long-term efficacy is superior to oral montelukast.
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    Mistletoe induces apoptosis by down-regulating the constitutive activation of nuclear factor-κB in HCT116 cells
    LIN Lei, YE Meng, WANG Shao-ming, NI Shu-min, WU Xiao
    Chinese Journal of Clinical Pharmacology and Therapeutics    2008, 13 (7): 730-734.  
    Abstract104)      PDF (271KB)(442)       Save
    AIM: To investigate the role of NF-κB in apoptosis induced by mistletoe in human colon cancer HCT116 cells.METHODS: The cell growth inhibiting was measured by MTT assay, the cell apoptosis was observed by the agarose gel electrophoresis.The protein expression was detected by Western Blotting. DIG-EMSA was conducted to detemine the DNA-binding activation of NF-κB.RESULTS: Mistletoe had a remarkable growth inhibitory action on HCT116 cells. After exposed to mistletoe, HCT116 cells presented some morphologic features of apoptosis including cell shrinkage, nuclear condensation and DNA fragmentation.NF-κB was inhibited in cancer cells treated with mistletoe.Mistletoe may potentiate the cytotoxic effects of chemotherapeutic agents such as HCPT.CONCLUSION: Mistletoe may induce apoptosis in HCT116 cell line.Inhibitory action of NF-κB may play a significant role in apoptosis induced by mistletoe.
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    Research progress in the treatment of depression with monome of Chinese herb, drug pairs, compound prescriptions and Chinese patent drugs
    CHEN Ying, YUAN Yonggui
    Chinese Journal of Clinical Pharmacology and Therapeutics    2021, 26 (5): 586-593.   DOI: 10.12092/j.issn.1009-2501.2021.05.016
    Abstract1360)      PDF (536KB)(2096)       Save
    Depression is a relatively common psychosomatic disease in clinical practice. It is mainly characterized by significant and lasting depression. It generally manifests as depression, loss of interest, impaired cognitive function, etc. Some patients are accompanied by somatization symptoms such as insomnia or lethargy, Loss of appetite, fatigue, loss of libido, etc. In severe cases, self-injury or even suicide may occur. According to research, depression has become the third leading cause of disability and death. At present, the pathogenesis of depression has not been definitively concluded, but a large number of studies have shown that it is related to biochemical, neuroendocrine, and neuroimmunological factors. At present, selective 5-HT reuptake inhibitors are routinely used in clinical treatment, such as sertraline, citalopram, Prozac, etc., but they often have slow onset and obvious side effects, making it difficult to achieve satisfactory therapeutic effects. Traditional Chinese medicine has gradually begun to be accepted by doctors and patients in the treatment of refractory diseases due to its multi-component and multi-target characteristics. This article mainly discusses the research progress of Chinese herbal extracts, Chinese herbal medicine pairs, Chinese herbal compound prescriptions, and Chinese patent medicines in the treatment of depression, and provides references for the clinical application of Chinese medicines in the treatment of depression.
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    Clinical trials simulation in drug development
    HUANG Ji-han, HUANG Xiao-hui, LI Lu-jin, WANG Qin, WANG Kun, ZHENG Qing-shan
    Chinese Journal of Clinical Pharmacology and Therapeutics    2010, 15 (6): 691-699.  
    Abstract127)      PDF (412KB)(615)       Save
    Clinical trial simulation is playing more and more important role in new drug development, making the drug development more efficient and informative. Clinical trial simulation can be viewed as the abstraction of the clinical trial process. It is used to investigate assumptions and to influence trial design in order to maximize the amount of information gained in drug development. Simulation can be used for modeling variability, estimating the impact of operational factors, evaluating assumptions, comparing trial designs, discriminating between competing drugs. In this review, we describe the motivations and history, general methodology and some examples of clinical trial simulation, including a brief description of current software available for performing such simulations, and finally our view of the current and future impact and directions for this powerful technology in drug development. Simulation is applicable to many areas of the clinical trial process. The focus here centers on the use of simulation with models based upon the pharmacokinetic-pharmacodynamic relationship that reflect the disposition and effect of drugs as observed in clinical trials.
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    Discussions in pharmacological action and the development in clinical application of puer arin
    YAO Dan, DING Xuan-sheng
    Chinese Journal of Clinical Pharmacology and Therapeutics    2008, 13 (4): 468-474.  
    Abstract325)      PDF (237KB)(1587)       Save
    As a saft and effective traditional Chinese medicine’s parenteral in jection, puerarin, whose molecular formula is 4,7-dihydroxy- 8β-D glucose isoflavone, has comprehensive and extensive phammaco logical action, and is generally used for treatment of cardiovascu lar and cerebrov ascular system diseases such as arhythmia, myocardial ischemia and hypertension.It has an extensive deve lopment perspective. The recent research in the mechanism of phamacological action and clinical application W ere review ed.
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    Effect of China-produced enalapril on long-term life quality of patients with dilated cardimyopathy and severecardiac dysfunction
    PENG Ying-Xin, HUANG Xi-Zheng, WANG Zhen-Qi, ZHANG De-Lan, YANG Su-Jie
    Chinese Journal of Clinical Pharmacology and Therapeutics    1998, 3 (2): 103-104.  
    Abstract80)      PDF (134KB)(332)       Save
    Aim and Metheds Theinfluence oforal enalapril on long-term quality of life was obser vedin 41 patients with dila ted cardiomyopathy and severecardiac dy sfunction (N YHA class Ⅲ-Ⅳ, left ventricularejective f raction<30 %), Theoral enalapril(10 ~ 40 mg/d ay)was give n for 24 months in addition to digitalis, diure tic drog and vasodilators (nitraes mainly).Results Follow-up rate was 95.1 %.Themaximal six-minute-walking distance was increased by 43.0 % (P<0.01)and exercisetolerance and t imewere increased by 73.1% and 61.4%, respectively (both P<0.001)and left ventriclesystolic parameters were improvedinvarying deg rees.Conclusion Thelife quality of patients with cardiomyopathy and severecardiac dysfunction could be greatly improved by administration of enalapril.
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    Research advancement of heartleaf houttuynia herb on antibacterial action
    LI Juan, SHAO Hui, ZHONG Zheng-ling, CHU Ji-ru, XIE Hai-tang
    Chinese Journal of Clinical Pharmacology and Therapeutics    2012, 17 (12): 1427-1432.  
    Abstract477)      PDF (249KB)(2773)       Save
    Heartleaf houttuynia herb has many pharmacologic actions especially antibacterial action. This review describes the research advancement of heartleaf houttuynia herb on antibacterial action from three aspects including the whole antibacterial action evaluation, special antibacterial action, and the trouble in clinic and the study direction. This paper provides a review for the next research.
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    Progress on the pathological mechanism and treatment of frostbite 
    ZHANG Li, LIN Xingyao, SHANG Yun, WANG Qiang
    Chinese Journal of Clinical Pharmacology and Therapeutics    2023, 28 (3): 347-354.   DOI: 10.12092/j.issn.1009-2501.2023.03.014
    Abstract400)      PDF (808KB)(1436)       Save
    Frostbite is a tissue injury that occurs when the body is exposed to extreme cold. Its path-ological mechanism is complex and has not been ful-ly elucidated. In high cold and high altitude areas, outdoor sports people have a high risk of injury, and severe frostbite has high disability and mortality. Ex-ploring the pathological mechanism of frostbite is helpful to determine the treatment methods and timing. At present, the clinical treatment of frostbite is mainly symptomatic treatment, such as drug treatment and surgical treatment, but the curative effect can not meet the clinical needs. Therefore, it is of great significance to seek more efficient drugs or treatment methods. This article reviews the rele-vant research progress in pathophysiological mecha-nism, clinical treatment, cellular and molecular path-ways of frostbite in recent years, in order to provide new ideas for future research and clinical treatment. 
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    Exploring the mechanism of Xin Mai Jia in inhibiting hypertensive cardiac hypertrophy based on network pharmacology and animal experiments
    LEI Chengjing, YU Miao, LI Yange, TANG Xiaoguang, ZHAO Fanrong, ZHU Tiantian
    Chinese Journal of Clinical Pharmacology and Therapeutics    2025, 30 (1): 32-41.   DOI: 10.12092/j.issn.1009-2501.2025.01.004
    Abstract48)      PDF (4635KB)(205)       Save
    AIM: To exploring the mechanism of Xin Mai Jia (XMJ) in inhibiting hypertensive cardiac hypertrophy through network pharmacology and animal experiments. METHODS: Retrieving the active ingredients and target points of XMJ by searching the TCMSP database and related literature reports; using the Gene Cards, OMIM, and Drug Bank databases to screen targets for hypertensive cardiac hypertrophy; constructing a network of traditional Chinese medicine-active ingredients-potential targets and a protein-protein interaction (PPI) network; using DAVID software for target gene ontology (GO) functional enrichment analysis and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway enrichment analysis; using Auto Dock software for molecular docking. A spontaneously hypertensive rat (SHR) model was established, and hematoxylin-eosin (HE) staining was used to detect the morphology of cardiac tissue and cellular hypertrophy, Masson staining was used to detect collagen deposition in cardiac tissue, and Western blot to detect the expression of heat shock protein (HSP90AA1), mammalian target of rapamycin (mTOR), peroxisome proliferator-activated receptor γ (PPARG), and tumor necrosis factor (TNF-α) in cardiac tissue. RESULTS: A total of 56 potential active ingredients were identified in XMJ, and 5,492 targets related to hypertensive cardiac hypertrophy were obtained. The targets in the core network were ranked according to their Degree values, and four main targets were selected: HSP90AA1, mTOR, PPARG, and TNF-α. The results of HE staining showed that compared with the normal group, the average area of cardiomyocytes in the SHR group increased significantly (P<0.05), while there was no significant change in the XMJ group. The hypertrophy in the SHR+XMJ group was significantly alleviated (P<0.05). The results of Masson staining showed that compared with the normal group, the levels of interstitial fibrosis and perivascular fibrosis in the SHR group rats increased significantly (P<0.01), and XMJ could significantly reduce the fibrosis levels in the SHR group rats (P<0.01). The results of Western blot showed that compared with the normal group rats, the expression of HSP90AA1 and PPARG in the myocardial tissue of SHR group rats was downregulated, mTOR phosphorylation was downregulated, and TNF-α was significantly upregulated (P<0.01). In the SHR+XMJ group, the expression of HSP90AA1, PPARG, and TNF-α in the myocardial tissue of rats returned to normal levels, and mTOR phosphorylation returned to normal levels. In the XMJ group, there were no significant changes in the above indicators compared with the normal group rats. CONCLUSION: The mechanism underlying the inhibitory effect of XMJ on myocardial cell hypertrophy in hypertension involves a comprehensive action through multiple components, multiple targets, and multiple pathways.
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    Relative bioavailablity of cefacloreffervescent tablets in human volunteers
    QIU Fu-Rong, JI Jin-Mei, CHENG Bo, ZENG Zhao-Hong, SUN Hua, MAO Guo-Guang
    Chinese Journal of Clinical Pharmacology and Therapeutics    2000, 5 (2): 142-144.  
    Abstract101)      PDF (132KB)(288)       Save
    Aim To study relative bioavailablity of cefacloreffervescent tablets in healthy volunteers.Methods According to the crossover design, Avolunteers wereeach orally g iven a sing le does of the 0.75 g cefacloreffervescent tablets and cefaclor capsules with an interval of 5 days between the twoformulations.The plasma concentrations of the drug weredetermined by RP-HPLC.Pharmacokinetic parameters wereobtained by A TPK programe, and calculated on the basis of open sing le compartment model.Results After a single oral dose, the peak levels in plasma averaged Cmax(31.27±5.81) μg·ml-1 and(30.56±5.25) μg·ml-1 at (0.58±0.12) h and(0.73±0.17) h and AUC0~4(35.48±4.65) μg·h·ml-1 and (35.89±2.90) μg·h·ml-1 for tablet and capsule, respectively.Conclusion Theresult show s that twoformulations arebioequivalence.
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    Evaluation and calculation of the accumulation index in clinical pharmacokinetics
    LI Xian-xing, LI Lu-jin, XU Ling, ZHENG Qing-shan
    Chinese Journal of Clinical Pharmacology and Therapeutics    2013, 18 (1): 34-38.  
    Abstract1579)      PDF (608KB)(3615)       Save
    AIM: To analyze and evaluate the accumulation index (Rac) in clinical pharmacokinetics of multiple dosing administrations in order to obtain one reasonable method. METHODS: The plasma concentration-time data of arteether was simulated for 1000 subjects in multiple doses administration. The 20-40 subjects were sampled for 1000 time by the Boostrap method and values of Rac were calculated by the AUC, Cmax, Ctrough and model. The values of Rac were evaluated by their distributions. RESULTS: The AUC and Cmax method were more stable than the Ctrough and model method. If the efficacy or toxicity was related with the concentration, it was appropriate to use the Cmax method, and if the efficacy or toxicity was related with the time, it was appropriate to use the AUC method. CONCLUSION: The drug accumulation is related with effectiveness and safety, and the reasonable choice of Rac calculation method should be based on drug and data characteristics.
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    Quantitative evaluation of pharmacodynamic interactions on diaphoretic effects among the components of Mao-to in rats
    XIONG Qian, ZHANG Mi, ZHENG Qing-shan
    Chinese Journal of Clinical Pharmacology and Therapeutics    2011, 16 (7): 763-767.  
    Abstract702)      PDF (329KB)(539)       Save
    AIM: To analyze pharmacodynamic interaction on diaphoretic effects among the components from Mao-to for finding an optimal combination.METHODS: According to the four components that included in Mao-to, an orthogonal design with 1-level = used and 0-level = not used, was selected in L14(24) and a mathematical model was built up with the nonlinear mixed effect model (NONMEM) for rat experiment. Vacuole incidence of axillary sweat gland was determined to evaluate the diaphoretic effect. The importance and effectiveness of each component were analyzed in combinations and the bias was evaluated by some charts.RESULTS: The prediction model showed that it would be Cassia Twig (B), Ephedra (A), Apricot (C), and Liquorice (D) in order by the importance and the best combination is A plus B, while the worst is C combined with D.CONCLUSION: Ephedra and Cassia Twig in combination have significant diaphoretic effect in rats, and the combination will show better effect in comparison with any single component.
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    Effects of Ginkgo biloba extract on action potential and L-type calcium channel in guinea pig's ventricular myocytes
    ZHANG Xu-Guo, WANG Jia-Ning1, LI Jian-Jun2, LIU Zhong-Wu3, HUANG Chong-Xing2
    Chinese Journal of Clinical Pharmacology and Therapeutics    2004, 9 (3): 345-349.  
    Abstract96)      PDF (203KB)(588)       Save
    AIM: To study the effects of Ginkgo biloba extract (EGB)on action potential (AP)and L-type calcium channel in isolated guinea pig's ventricular myocytes. METHODS: AP was recorded by current-clamp mode and ICa-L was recorded by voltage-clamp mode using whole patch clamp technique.RESULTS: Action potential duration of repolarization 90 %(APD90)was shortened by 13 %, 23 % at the dilution of EGB 1 ∶800, and 1 ∶ 200, respectively (P <0.05).L-type calcium current (ICa-L)was inhibited by EGB significantly in a concentration-dependent manner.Peak ICa-L was reduced by 15 %at the dilution of EGB 1 ∶800 and 42 %at 1 ∶200, respectively(P <0.05).I-V relationship and the voltage of peak current did not change significantly.CONCLUSION: EGB can shorten APD and inhibit ICa-L in a concentration-dependent manner, which may be one of critical basis on antiarrhythmia.
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    Effect of bufalin on the proliferation and apoptosis of human bladder cancer T24 cells
    HUANG Hou-bao, XIA Dong-dong, SHEN Qun-shan, CHEN Qing-shui, WANG Xiao, QIU Teng
    Chinese Journal of Clinical Pharmacology and Therapeutics    2014, 19 (7): 733-737.  
    Abstract234)      PDF (1203KB)(516)       Save
    AIM: To investigate the effect of bufalin on the proliferation of human bladder cancer T24 cells and explore the underlying anticancer mechanisms of bufalin. METHODS: The proliferation-inhibiting effect of bufalin on T24 cells was measured by methyl thiazole tetrazolium (MTT)colorimetric assay; the cell cycle distribution and apoptosis were detected by flow cytometry ( FCM ); the expression of CyclinD1 was detected by RT-PCR.RESULTS:Bufalin inhibited the proliferation of T24 cells in a time- and dose-dependent manner; bufalin could induce apoptosis of T24 cell; exposure of T24 cells to 20 nmol/L of bufalin led to significant induction of G0/G1 growth arrest at both 12 h (69.76%) and 24 h (88.14%),compared with negative control cells (36.42%).The mRNA levels of CyclinD1 in T24 cells was markedly decreased after treatment with bufalin.CONCLUSION: Bufalin could inhibit the proliferation and induce apoptosis of T24 cells. Bufalin could induce T24 G0/G1 growth arrest and decrease the mRNA levels of CyclinD1.
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    Study on pharmacokinetics of rosuvastatin and its drug interactions with other drugs
    WEN Jin-hua, XIONG Yu-qing
    Chinese Journal of Clinical Pharmacology and Therapeutics    2011, 16 (11): 1309-1314.  
    Abstract572)      PDF (261KB)(2089)       Save
    Rosuvastatin, a new generation of statins , has better liver selectivity, less metabolism and long elimination half-life.It has more lipid-lowering effect and a wide range prospects of clinical applications. Moreover, rosuvastatin has good tolerability and the incidence of adverse reactions was similar to other kind of statins. In this paper, rosuvastatin pharmacokinetics and pharmacokinetic interactions with other drugs are reviewed. In order to lay down a solid theory foundation for the guidance in clinical usage of Rosuvastatin, ensure the safety and effectiveness of clinical usage, achieving individualized therapy in its true sense.
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    Research advance on the characteristics and application of CYP450 metabolic enzymes
    LI Xiao-yu, LIU Gao-lin
    Chinese Journal of Clinical Pharmacology and Therapeutics    2008, 13 (8): 942-946.  
    Abstract320)      PDF (177KB)(1770)       Save
    Cytochrome P450 is an important kind of enzymes for the metabolism of drug and other endoor xeno-biotics.Classification of metabolic enzymes, molecular biological characteristic of CYP3A4, CYP2D6, CYP2C9, CYP2C19, CYP2E1, CYP1A2 and CYP2A6were described in this review.Influence of traditional Chinese medicine (TCM)on metabolic enzyme and its application in clinical drug therapeutics and drug development were also reviewed in this article.
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    Membrane proteins and membrane proteomics
    LIANG Yan, KAN Hong-wei, YANG Shi-you
    Chinese Journal of Clinical Pharmacology and Therapeutics    2009, 14 (11): 1313-1320.  
    Abstract168)      PDF (259KB)(1096)       Save
    A membrane protein is a protein molecule that is attached to, or integrated into the membrane of a cell or an organelle.As the membrane protein is a good target for drugs, more than 80 % of the drugs on the present market take the effect on the membrane protein.Therefore, it is significant to study the membrane proteins.However, the traditional study on membrane proteomics is obstructed by the difficulties in solubilizing, separating, and identifying membrane proteins.This review summarizes the structure of membrane proteins, the significant role of the membrane proteins on the cell physiology and the human diseases, the potential of the membrane proteins to be the target for drugs and the techniques of the research on the membrane proteomics.
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    Sinomenine inhibits oxidative stress and pulmonary fibrosis by activating the Keap1/Nrf2 signaling pathway
    LIU Lijing, QIAN Hong, MENG Qingxin, ZHANG Xiang, HE Bin, HE Jianbin, WEI Yingmin
    Chinese Journal of Clinical Pharmacology and Therapeutics    2023, 28 (9): 979-987.   DOI: 10.12092/j.issn.1009-2501.2023.09.003
    Abstract287)      PDF (2016KB)(357)       Save
    AIM: To explore the protective effects of sinomenine (SIN) on oxidative stress and pulmonary fibrosis and its relationship with the Kelch-like ECH-associated protein 1 (Keap1)/nuclear factor erythroid 2-related factor 2 (Nrf2) signaling pathway. METHODS: MRC-5 cells were treated with hydrogen peroxide (H2O2) to establish the oxidative stress injury model, followed by administration with SIN. Cell viability was detected using the CCK-8 method. The biochemical kits were employed to measure malondialdehyde (MDA) content and superoxide dismutase (SOD), glutathione peroxidase (GSH-Px) and catalase (CAT) activities. The protein expression of Keap1 and Nrf2 was examined by western blot. Thirty SD rats were randomly divided into control group, bleomycin A5 (BLM) group and BLM+SIN group, with 10 animals in each group. Bleomycin A5 were intratracheally administered to the rats in BLM group and BLM+SIN group to establish the pulmonary fibrosis model. The rats in control group received the same volume of 9 g/L sodium chloride solution. The second day after model construction, the rats in BLM+SIN group were gavaged with SIN, while the rats in the other two groups were treated with 9 g/L sodium chloride solution. On day 28, all rats were sacrificed. Pulmonary tissue was isolated, and HE and Masson staining was performed to observe the pathological changes. The MDA content and SOD, GSH-Px and CAT activities in pulmonary tissue were evaluated. Western blot was used to assay pulmonary tissues Keap1 and Nrf2 protein expression. RESULTS: When compared with H2O2 group, SIN treatment increased cell viability, decreased MDA content, elevated SOD, GSH-Px and CAT activities, down-regulated Keap1 expression, and promoted nuclear translocation of Nrf2 in MRC-5 cells. In comparison with BLM group, administration of SIN decreased alveolitis and pulmonary fibrosis pathological changes and scores as well as pulmonary tissue MDA content, enhanced pulmonary tissues SOD, GSH-Px and CAT activities, down-regulated pulmonary tissues Keap1 expression, and raised Nrf2 levels in the nucleus. CONCLUSION: SIN alleviates oxidative stress and pulmonary fibrosis possibly by activating the Keap1/Nrf2 signaling pathway.
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