Table of Content

Volume 19 Issue 2
26 February 2014

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Apoptosis of RAW264.7 macrophages induced by chloral hydrate and its mechanisms

PAN Qing-jun, ZHU Xue-zhi, LIU Yuan

2014, 19(2):  121-126. 

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AIM: To investigate the effect of chloral hydrate treatment on the apoptosis of RAW264.7 macrophages and the mechanisms of apoptosis.METHODS: To treat RAW264.7 macrophages by chloral hydrate with different concentrations and different times, then to observe the morphological changes. Also, Annexin V-FITC/PI double staining assay, Hochest 33258 and and DNA ladder assay were used to detect the apoptosis, and the expression of Fas/FasL.RESULTS: After treatment with chloral hydrate, the morphology of RAW264.7 macrophages changed from fusiform to round, and suspension at last. Annexin V-FITC/PI double staining assay showed RAW264.7 macrophages were from early to late apoptosis after chloral hydrate treatment. Hochest 33258 and and DNA ladder assay showed chloral hydrate treatment can induced the apoptosis of RAW264.7 macrophages. Also, the apoptotic RAW264.7 macrophages expressed higher levels of Fas, but did not express FasL.CONCLUSION: Chloral hydrate treatment could induce RAW264.7 macrophages apoptosis via the Fas/FasL pathway.

Effects of salvia miltiorrhiza and electroacupuncture on the expressions of glial fibrilliary acidic protein and iNOS in rats with cerebral ischemia-reperfusion injury

ZHANG Ye-gui, ZHAO Jian, DING Yan-xia, HOU Liang-qin

2014, 19(2):  127-132. 

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AIM: To observe the effects of salvia miltiorrhiza(SM) and electroacupuncture (EA) on the expressions of glial fibrilliary acidic protein (GFAP) and iNOS in rats after focal cerebral ischemia-reperfusion.METHODS: 60 Sprague-Dawley rats were randomized into the sham opration, model, SM, EA, and SM+EA groups. The models rats received intraluminal middle cerebral artery occlusion(MCAO) with a nylon monofilament suture. SM injection at 5 g/kg were injected into abdominal cavity in the SM group, EA(2-15Hz, dilatational wave) at Baihui and Dazhui was performed to rats in the EA group, lasting for 30 min, SM+EA group was treated with both SM abdominal cavity injection and electroacupuncture therapy, once a day for 4 days.To observe the neurologic impairment score in each group, and the water content of brain tissue was determined by weighing. HE staining was performed to display the pathological changes of the brain tissues, and the expressions of GFAP and iNOS in striatum were detected by immunohistochemical method.RESULTS: The neurologic impairment score and water content of brain tissue in model group were significantly increased compared with sham operation group(P<0.01).Compared with model group, the neurologic impairment score and water content of brain tissue in SM group, EA group and SM+EA group were significantly decreased (P<0.05,P<0.01), and the score and water content in SM+EA group was obviously lower than those of the SM group and the EA group(P<0.05, P<0.01). The pathological changes of the brain tissues of four group rats were consistent with the above result. The expression of GFAP and iNOS in model group was obviously increased compared with sham operation group(P<0.01).Compared with model group, the expression of GFAP and iNOS in SM group, EA group and SM+EA group were significantly decreased (P<0.05, P<0.01). The expression of GFAP and iNOS in SM+EA group was obviously lower than those of the SM group and the EA group (P<0.05, P<0.01).CONCLUSION: SM and EA has a neuroprotective activity in cerebral ischemia-reperfusion neuronal injury, which is probably related to inhibit the excessive activation of astrocytes, decrease the expression of iNOS, besides, the effects of SM combined with EA was higher than the SM group or the EA group.

Atorvastatin ameliorates aortic YKL-40 level in diabetic rats fed with an atherogenic diet

ZHENG Jian-lei, CHEN Qiu-jing, LU Lin, ZHANG Qi, ZHANG Rui-yan, SHEN Wei-feng

2014, 19(2):  133-138. 

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AIM: To investigate the effects of atorvastatin on expression of the pro-inflammatory cytokine, YKL-40, in the aortic intima of diabetic rats fed with an atherogenic diet.METHODS: Male Sprague-Dawley (SD) rats were randomly divided into five groups: control, atherogenic diet, atherogenic diet + atorvastatin, diabetes mellitus+atherogenic diet, and diabetes mellitus + atherogenic diet + atorvastatin (n=9, in each group). Aortic atherosclerosis was induced by a single dose of vitamin D3, followed by a fatty diet. Diabetic model was established using intraperitoneal injection of streptozotocin (STZ). Serum levels of fasting blood glucose (FBG), HbA1c, triglyceride (TG) and total cholesterol (TC) were determined. The mRNA level and protein expression of YKL-40 in the aortic intima were measured after treatment with atorvastatin (20 mg/kg) for 8 weeks.RESULTS: FBG, HbA1c, and TG were higher in diabetic rats with atherogenic diet than controls (all P<0.01) and rats with single atherogenic diet (all P<0.05). Real-time PCR and immunohistochemistry revealed that mRNA level and protein expression of YKL-40 were significantly elevated in the aortic intima of diabetic rats with atherogenic diet (all P<0.01 vs controls and rats with single atherogenic diet), which were significantly decreased after treatment with atorvastatin for 8 weeks (all P<0.01).CONCLUSION: Atorvastatin significantly suppresses aortic YKL-40 expression in STZ-induced diabetic rats with atherogenic diet, suggesting that this agent may be beneficial in reducing the pathological effect of YKL-40 in the formation of atherosclerosis.

Reversal of human hepatic cancer multidrug resistance is induced by AstragalosideⅡ in BEL-7402/FU cells

WANG Pei-pei, XU Du-juan, HUANG Can, XU Wen-ke, LUAN Jia-jie

2014, 19(2):  139-144. 

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AIM: To investigate the effect of AstragalosideⅡ on the reversal of multidrug resistance in human hepatic cancer cells.METHODS: Susceptibility of chemotherapy drugs and relative reversal fold was evaluated by MTT. The mRNA level of MDR1 gene was detected by RT-PCR and the P-glycoprotein expression was detected by immunocytochemistry method. Intracellular Rhodamine123 accumulation was determined by flowcytometry.RESULTS: BEL-7402/FU cells showed resistance to three chemotherapy drugs 5-fluorouracil, Adriamycin and Mitomycin, their resistance index were 19.64, 1.98, 1.92. Astragaloside Ⅱ(0.04, 0.08 mg/mL) relative reversal fold were 1.49, 1.81 to 5-fluorouracil. Astragaloside Ⅱ(0.08 mg/mL, 0.16 mg/mL) could downregulate the expression of MDR1 mRNA and P-glycoprotein, increase the intracellular Rhodamine123 fluorescence.CONCLUSION: Astragaloside Ⅱ could reverse the drug resistance of Bel-7402/FU cells via regulating down the expression of MDR1 mRNA, inhibit the expression and function of P-glycoprotein.

Telithromycin suppresses nontypeable Haemophilus influenzae-induced MUC5AC expression via inhibition of activator protein-1 signaling

YANG Fan, LI Jian, GU Bin, ZHAO Wen-jian, YANG Zhi-ying

2014, 19(2):  145-149. 

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AIM: To investigate the effect of Telithromycin on nontypeable Haemophilus influenza (NTHi)-induced mucus MUC5AC expression in airway epithelial cells and underlying molecule mechanism.METHODS: Cultured NCI-H292 cells were pre-incubated with 10 mg/L of Telithromycin for 6 h, and then NTHi was added in different concentrations for 3-9 h. MUC5AC gene mRNA level and mucin protein expression were quantified by real time PCR and ELISA, respectively; DNA-binding activities of NF-κB and activator protein-1 (AP-1) were detected by ELISA.RESULTS: NTHi significantly increased MUC5AC gene and protein expression in NCI-H292 cells, and it could activate NF-κB and AP-1. Telithromycin significantly attenuated NTHi-induced MUC5AC mRNA and protein expression, and inhibit AP-1 activation as well, but not NF-κB.CONCLUSION: Telithromycin can attenuate NTHi-induced mucus expression via inhibition of AP-1 but not NF-κB.

Distribution of aminophylline after aerosol inhalation in beagles

TANG Zhi-hua, WANG Wei, DING Jie-wei

2014, 19(2):  150-155. 

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AIM: To investigate the tissue distribution and pharmacokinetics of aminophylline after aerosol inhalation in beagles.METHODS: HPLC was used to determine the concentration of theophylline in different tissues and plasma of the beagles. The tissue distribution of theophylline after aerosol inhaling was compared to intravenous infusing aminophylline. Plasma concentrations at different time after aerosol inhalation were compared with intravenous infusion.RESULTS: The theophylline concentrations in trachea after aerosol inhalation at 0.25 and 0.5 h were higher obviously than that of intravenous infusion administration group (0.25 h, P<0.01; 0.5 h, P<0.05). At 0.25, 0.5, 1 and 2 h, the theophylline concentrations in other tissues were decreased obviously. The absolute bioavailability of aminophylline after aerosol inhalation was 24.52%.CONCLUSION: After aerosol inhaling aminophylline, the theophylline is retained mostly in trachea. At the same time, the theophylline concentrations in other tissues are decreased obviously. The administration route of aerosol inhaling aminophylline can raise the therapeutic index and reduce adverse effects dramatically

Gender difference of limonin metabolism in rat liver microsomes

WANG Jun-qing, CHEN Ai-ying, DONG Wen-bin, CHENG Min, ZHENG Gao-li

2014, 19(2):  156-161. 

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AIM: To study the gender difference of limonin metabolism and the effects of selective CYP450 inhibitors on the metabolism of limonin in rat liver microsomes.METHODS: Limonin was incubated in rat liver microsomes, the enzyme kinetics parameters were studied; the metabolism of gender differences of limonin in male and female rat liver microsomes were compared; four kinds of CYP450 subtype specificity inhibitors were incubated with liver microsomes, the metabolic inhibition of inhibitors of limonin were calculated.RESULTS: The optimal incubation time was 30 min and the optimal enzyme concentration was 2.0 mg/mL. Km of limonin in female and male rat liver microsomes are (12±3) and (16±4) μg/mL and V_max are (49±6) and (93±14) ng·min^-1·mg^-1. The metabolic percentage are (33.9±4.7)% and (53.8±2.8)% and metabolic rate are(4.46±0.62)and (7.08±0.37) ng·min^-1·mg^-1 respectively in famle and male rat liver microsomes. Inparticularly Ketoconazole(Ket) and Cimetidine (Cime) had significant inhibitory effects on the metabolism of limonin. It was further found that α-Naphthoflavone (α-Naph) and Quinidine (Quin) had little effects on the metabolism of limonin.CONCLUSION: The gender difference of limonin metabolism in rat liver microsomes has been investigated in this study, and the CYP3A2 and CYP2C11 may be the main reason for the sex difference.

Effects of Huanglian-Jie-Du-Tang on learning and memory in aging mice

YE Qiao-hong, CHEN Shan-shan, LI Sheng-jian, YE Yi-lu, ZHANG Qi, YU Yue-ping, WANG Jue

2014, 19(2):  162-165. 

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AIM: To investigate the potential anti-aging effect of Huanglian-Jie-Du-Tang (HJDT) and explore the mechanism in mice.METHODS: The ICR mice were divided into normal control group, aging model group and HJDT treated group (1, 2, 4, and 8 g/kg). Aging mice were induced by subcutaneously injection with D-galactose. The spontaneous activity and the learning and memory ability were evaluated by a locomotor test and step down test. The SOD activity and the MDA level were measured by xanthine oxidase method and thiobarbituric acid method.RESULTS: Compared with the normal control group, the learning and memory ability and the MDA level decreased and the SOD activity increased in aging mice, which were markedly reversed by HJDT (2 and 4 g/kg). But there was no significant effect of HJDT (1 and 8 g/kg).CONCLUSION: HJDT ameliorates learning and memory impairment in D-galactose-induced aging mice through its potent antioxidant activities.

Studies on absorption kinetics of gambogenic acid in rat's intestines

CHEN Jin-pei, WANG Shan-shan, WANG Dian-lei, YANG Li-li, WANG Chen-yin, TAO Xiu-hua, CAO Yin, WANG Shu-jun, CHEN Ya-jun

2014, 19(2):  166-170. 

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AIM: To investigate the absorption kinetic characteristics of Gambogenic acid at different intestine segments in rats and provide reliable biopharmaceutics basis of novel drug delivery systems of Gambogenic acid.METHODS: The rat intestinal absorption model was established to investigate the influence of different concentrations (3.0,10.0,30 μg/mL) and intestine segments on the intestinal absorption of GNA. Gambogenic acid concentration was measured by the RP-HPLC.RESULTS: Within the range from 3.0-30.0 μg/mL, the absorption rate and the quality concentration of Gambogenic acid had a linear relation. The permeability coefficient of Gambogenic acid at colon, ileum, jejunum, duodenum were(0.03944±0.00158), (0.04012±0.00103), (0.04104±0.00124) ,(0.08620±0.00272) h^-1,respectively.CONCLUSION: The absorption of Gambogenic acid conforms to passive diffusion mechanism and first-order kinetics. Gambogenic acid could be absorbed in whole intestinal segments, so it is feasible for Gambogenic acid to be designed as a controlled-release formulation.

Pharmacokinetics of nuciferine in rats

GU Sheng-ying, ZHU Guan-hua, KANG Lei, LI Xiao-yu, LIU Gao-lin

2014, 19(2):  171-175. 

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AIM: To study the pharmacokinetics of nuciferine after intravenous administration in rats using high performance liquid chromatogram (HPLC).METHODS: Nuciferine was administered by intravenous injection in rats and plasma was collected from fundus oculi venous plexus. Liquid-liquid extract procedure was employed for the extraction of nuciferine in rat plasma. The concentrations of nuciferine in plasma were measured by using HPLC method and the pharmacokinetic parameters were calculated by DAS.RESULTS: The main pharmacokinetic parameters of nuciferine after intravenous injection were as follows: t_1/2 was (1.73±0.58) h, V was (5.03±0.24) L/kg, CL was (4.23±0.78) L·h^-1·kg^-1, AUC_0-inf was (2.35±0.46) mg·L^-1·h, MRT was (1.51±0.31) h.CONCLUSION: The HPLC method for the determination of nuciferine in rat plasma is sensitive, stable and rapid, which is successfully employed for the pharmacokinetic study of nuciferine in rats. After intravenous injection in a dose of 100 mg/kg, intensity distribution of nuciferine in plasma and a high elimination rate are investigated.

PK-PD study on gemifloxacin mesylate against common pathogenic bacteria in urinary tract

REN Bin, LIAO Kang, LI Rui-ming, FU Xiao-hua, YE Yi-fang, HONG Xiao-dan

2014, 19(2):  176-179. 

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AIM: To carry out PK/PD study of gemifloxacin mesylate against common pathogenic bacteria in urinary tract.METHODS: MIC (minimum inhibitory concentration) and MBC (minimum bactericidal concentration) of gemifloxacin against common pathogenic bacteria in urinary tract were determined. Urine concentration of healthy subjects after oral administration of gemifloxacin mesylate tablets (320 mg) was determined and then C_max/MIC₉₀ and AUC_{24 h}/MIC₉₀ were calculated.RESULTS: Gemifloxacin had lower sensitivity to common pathogenic bacteria in urinary tract. Urinary peak concentration (C_max) of gemifloxacin was(144±124) μg/mL and the area under urine concentration-time curve (AUC_{24 h}) was(1368±671) μg·mL^-1·h after orally administered gemifloxacin mesylate tablets (320 mg) to healthy subjects. C_max/MIC₉₀ of gemifloxacin in urine against Escherichia coli, Pseudomonas aeruginosa and Enterococcus faecalis was 2.9-5.8 and AUC_{24 h}/MIC₉₀ was more than 30, whereas AUC_{24 h}/MIC₉₀ of gemifloxacin against Klebsiella pneumoniae and Enrerococcus feces was 19.25.CONCLUSION: Gemifloxacin could effectively remove Escherichia coli, Pseudomonas aeruginosa and Enterococcus faecalis infected in urinary tract, and avoid resistance. Gemifloxacin could inhibit growth of Klebsiella pneumoniae and Enterococcus feces.

Comparison of curative effect and clinical influence factors of risperidone and olanzapine in the treatment of acute phrase of schizophrenia

NI Ping, LV Hai-long, GUO Xiao-feng, ZHANG Li-li, XU Lin-yong

2014, 19(2):  182-185. 

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AIM: To compare the curative effect and clinical influence factors of risperidone and olanzapine in the treatment of the acute phrase of schizophrenia.METHODS: 27 cases were treated with risperidone in a regimen of 2-6 mg/d.26 cases were treated with olanzapine in a regimen of 10-20 mg/d.Positive and Negative Syndrome Scale(PANSS) were used to measure the efficacy for 6 weeks.The patient's gender, age, duration before treatment and accurately record the patient's drug use were collected during treatment. RESULTS: The response rate at the end of 6 weeks of risperidone and olanzapine both were 84.6%. The general pathological symptoms and positive symptoms, the curative effects of olanzapine is better than those of risperidone(P<0.05). Risperidone and olanzapine curative effects in the treatment of the acute phrase of schizophrenia were increased with the extension of the treatment time(P<0.05). The treatment time had no interactions with risperidone and olanzapine(P>0.05). Treatment time, duration, dose, affected the efficacy of risperidone(P<0.05), treatment time affected the efficacy of olanzapine(P<0.05).CONCLUSION: The curative effect between olanzapine and risperidone has no difference,but the stablity of olanzapine is better than it of risperidone in the treatment of the acute phrase of schizophrenia.

Study of paroxetine and venlafaxine on the short-term effect and memory function in the recurrent depression

WEN Sheng-lin, CHENG Min-feng, WANG Hou-liang

2014, 19(2):  186-189. 

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AIM: To compare the short-term effects of paroxetine and venlafaxine on memory function in the patients with recurrent depression.METHODS: Using randomized study, recurrent depression patients were divided into paroxetine and venlafaxine group respectively for six weeks treatment. The doses were 20-60 mg/d and 150-225 mg/d respectively. All subjects were tested by Wechsler Memory Scale - revised in China and Hamilton Depression Scale-24.RESULTS: There was no difference between two groups about the effective rate (76.67% vs 70%,P＞0.05). The scores of short-term memory and memory quotient after 6 weeks treatment in venlafaxine group were higher than those in paroxetine group (P<0.05).CONCLUSION: The paroxetine has the same short-term effect as the venlafaxine in the patients with recurrent depression. Venlafaxine has more effect on short-term memory and memory quotient than paroxetine does.

Effect of lornoxicam on efficacy of PCSA with sufentanil in elderly patients after total hip replacement

YANG Yun-li, WEI Hu-ming, ZHANG Cheng-hua, HE Yan-fen, LU Cheng-rui

2014, 19(2):  190-195. 

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AIM: To evaluate the effect of lornoxicam on efficacy of PCSA with sufentanil after total hip replacement in elderly patients.METHODS: One hundred and twenty five ASA Ⅱ-Ⅲ patients aged 70-90 yrs after total hip replacement performed under general anesthesia were randomly divided into 5 groups(n=25 each)according to the composition of PCSA solution: group S₁L(sufentanil 0.4 μg·kg^-1·d^-1+ lornoxicam 32 mg ),group S₂L(sufentanil 0.6 μg·kg^-1·d^-1+ lornoxicam 32 mg),group S₁(sufentanil 0.4 μg·kg^-1·d^-1), group S₂( sufentanil 0.6 μg·kg^-1·d^-1)and group S₃(sufentanil 0.8 μg·kg^-1·d^-1).In the five groups ,the drugs were diluted 100 mL of normal saline , a loading dose of 2 mL was given at the end of operation.The PCSA setting was as follows: background infusion at 2 mL/h, a bolus dose of 0.5 mL, lockout interval 15 min. The number of deliveries (D₁) and the number of effective deliveries(D₂), total satisfactory degree (TSD), SpO₂, respiratory rate (RR), mean arterial pressure (MAP) and heart rate(HR), Visual analogue scale (VAS) and Ramsay sedation score (RSS) were recorded at 2, 4, 8, 12, 24 and 48 h after after loading dose of sufentanil. The adverse effects during analgesia period such as nausea and respiratory depression, vimiting, pruritis, somnolence were also recorded.RESULTS: The vilal signs was no significant change in four groups. During analgesia period the VAS, D₁, D₂ and TSD was significantly lower in group S₂L than group S₁L,S₁ and group S₂(P<0.05), no significant change as compared with group S₃. RSS was significantly higher group S₂L than group S₁L and group S₂(P<0.05).The percentage of vomiting, nausea, somnolence was significantly lower in group S₂L than group S₃(P<0.05).CONCLUSION: Lornoxicam can improve the efficacy of PCSA with sufentanil in elderly patients after total hip replacement with no significant adverse effect.

Small dose of tacrolimus combined with hormone in the treatment of refractory nephrotic syndrome

PENG Jian-yun, XU Wei-hai, ZHANG Xiao-ru, LAN Le-jian, GUI Zhi-hong, XIANG Mei-juan

2014, 19(2):  196-199. 

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AIM: To observe the clinical efficacy and safety of small dose of tacrolimus (TAC) combined with hormone in the treatment of refractory nephrotic syndrome (RNS).METHODS: 20 cases of prospective study of refractory nephrotic syndrome patients, when the study began hormone dosage adjustment to 0.5 mg·kg^-1·d^-1, for 8 weeks and gradually reduced, while taking a low dose of TAC, according to TAC serum concentration and clinical efficacy of adjusting dosage, regular follow-up liver function, 24 hour urinary protein, blood plasma TAC concentration and other biochemical indexes, and record adverse reactions.RESULTS: After second weeks to reduce proteinuria patients, plasma albumin level began to be recovered, there was statistically significant difference (P<0.05) before and after. 20 patients had different degree of ease in small dose of TAC combined with corticosteroid therapy, 5 cases in remission stage drug reduction process, TAC to add weight to the original dose relieved in 2 cases, the other 3 cases without response, including 1 cases of death;In 2 cases of infection recurrence, TAC amount does not relieve, 13 patients in remission was 9 months, TAC dose reduction is still in follow-up.Complete remission rate was 75%, the mortality rate was 5%, the relapse rate was 20%.CONCLUSION: Low dose of TAC combined with hormone can make the refractory nephrotic syndrome patients were relieved quickly, recurrence and treatment effect is related to the pathologic type, the less adverse reaction, good safety, and provides a new method for the treatment.

Effects of food on Cytochrome P450 drug metabolic enzymes

ZHANG Ran-ran, YANG Guo-ping, JING Ning-ning, HUANG Jie, HUANG Lu, WANG Yan

2014, 19(2):  200-205. 

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Cytochrome P450 (CYP450) enzymes play important roles in the biological oxidation process of many endogenous and exogenous moleculars, especially in drug metabolism. The great individual variations of the CYP450 enzymes among human subjects have been showed. In addition to the genetic factors, food and other environmental factors may also affect the activity and expression of CYP450 enzymes, which ultimately lead to the increased possibility of adverse reactions or toxicity. This review article summarizes the recent literatures with interests in the effects of food on cytochrome P450.

The influence of the drug on the fetus of diagnosis and treatment of breast cancer during pregnancy

DU Xiang-hui, JI Yong-lin, WANG Xiao-jia

2014, 19(2):  206-213. 

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Breast cancer is the most common malignant tumor for women. In China, breast cancer during pregnancy accounts for about 1.5%-8.2% of all breast cancer,≤35 years old fertile period breast cancer accounts for about 5%-20%. Breast cancer during pregnancy does not make a diagnosis and give treatment in time, illness will progress and even life-threatening; But the diagnosis and treatment of breast cancer drugs will be affect fetal health. Imaging contrast agents, radioactive isotope, sentinel lymph node tracer, anesthesia drugs, cytotoxic chemotherapy, endocrine therapy, targeted and other biological treatment for breast cancer during pregnancy was reviewed in this paper.Hope oncology department, gynecology, pediatrics physicians in the diagnosis and treatment of breast cancer drug effects on the fetus during pregnancy have a better understanding on the matter.To better solve the clinical actual problems such as breast cancer during pregnancy and lactation,to better guide the medical personnel processing.

Progress in pharmacokinetics, pharmacodynamics and pharmacogenetics of the antiplatelet drug ticagrelor

LI Mu-peng, XIONG Yan, CHEN Xiao-ping

2014, 19(2):  214-222. 

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Ticagrelor is a recently approved oral antiplatelet agent that belongs to a new chemical class, the cyclopentyltriazolopyrimidines (CPTP). Ticagrelor is rapidly absorbed, with a median time to maximum concentration of 1.5 hours. The new drug possesses advantages compared with other P2Y12 receptor antagonists such as clopidogrel and prasugrel in that it acts more quickly with no necessity of metabolic activation, bonds to P2Y12 receptor reversibly and therefore the platelet function can recover rapidly after drug withdrawal. Furthermore, ticagrelor may confer additional pharmacological effect via inhibition of non-platelet P2Y12 receptors. The pharmacokinetic characteristics of ticagrelor are not influenced by age, gender, diet, or clopidogrel responsiveness. Ticagrelor is primarily metabolized by cytochrome P450 (CYP) 3A4, rapidly produces plasma concentration-dependent IPA and can overcome non-responsiveness in patients previously treated with clopidogrel. What's more, CYP2C19 and ABCB1 genotypes show no effects on the pharmacodynamic profile of ticagrelor. This review summarized recent progress in pharmacokinetics, pharmacodynamics and pharmacogenetics of ticagrelor.

Survey on anticoagulant therapy in pregnant women with cardiovascular disease

XIONG Qin-mei, HONG Kui

2014, 19(2):  223-227. 

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In recent years, extensive application of anticoagulation drugs benefits more and more patients suffering from thromboembolic events. However, the anticoagulants have benefits and risks, which like a double-edged sword. How to balance the prevention of thromboembolism and the bleeding problems and optimize the treatments might be a serious problem for clinical physicians. Considering the women with pregnancy, anticoagulant therapy is a complex and challenging problem. According to the latest guidelines and recent studies on pregnant women with anticoagulant therapy, this review summarized anticoagulant therapies for the pregnant women with cardiovascular diseases, which includes the hypercoagulable states of pregnant women, the main types of anticoagulant drugs and clinical application.

The development of the SELEX technology and its application in clinical treatment

LONG Yu-peng, REN Jun

2014, 19(2):  228-232. 

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Based on the three-dimensional structure of oligonucleotide ligands, systematic evolution of ligands by exponential enrichment (SELEX) technology can screen for efficient and specific oligonucleotide aptamer to combine with molecular targets. Due to its high affinity, strong specificity, low immunogenicity, short filtering cycle and wide range of application, the ligands have several advantages and potential for new drugs in clinical diagnosis and treatment. In this article the application of oligonucleotide aptamer in the clinical treatment are reviewed from several aspects such as the development of the SELEX technology, modification of ligands, the advantages of clinical treatment, functions of ligands as target protein blocking agents and targeted drug delivery carrier.

Research progress of aspirin resistance in diabetic statue

XIE Hao, ZHU Yu-mei, HAO Hai-ping, ZHENG Xiao, MA Si-jing, WANG Guang-ji

2014, 19(2):  233-240. 

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Aspirin is the “gold standard” of antiplatelet therapy. It plays a very important role in the prevention of cardiovascular disease. However, not all the patients can respond a consistent anti-aggregation effect after they take aspirin. Clinically, this phenomenon that therapeutic dose of aspirin can not prevent the cardiovascular events is called “aspirin resistance (AR)”. A considerable portion of aspirin resistance patients also have diabetes or insulin resistance. Many diabetic patients take aspirin for primary prevention of cardiovascular disease, but the benefit is low. Aspirin can reduce the risk of cardiovascular events by 41% in non-diabetic patients. But the risk reduction in the subgroup with diabetes was only 10%.Although diabetes has been recognised as a high risk factor of aspirin resistance, the mechanism under the high diabetic prevalence in aspirin resistance patients is unclear. This paper will review the mechanisms of aspirin resistance in diabetic statue and explore methods to reverse it.