Table of Content

Volume 15 Issue 7
26 July 2010

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Protective effects of icariin on cerebral mitochondria function in SAMP8 mice

WU Man-gang, HE Xiao-li, LIU Dong-hua, QIANG Gui-fen, SHI Li-li, LI Xiao-xiu, ZU Mian, BI Ming-gang, DU Guan-hua

2010, 15(7):  721-726. 

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AIM: To investigate the protective effects of icariin (ICA) on cerebral mitochondria in senescence accelerated mice (SAM).METHODS: The 8-month-old senescence-accelerated mouse prone /8(SAMP8) mice were divided into SAMP8 group, Donepezil Hydrochloride (DON)-treated SAMP8 group (1 mg/kg), Piracetam (PIR)-treated SAMP8 group (200 mg/kg) and ICA-treated SAMP8 groups (75 mg/kg and 150 mg/kg). The age-matched senescence-accelerated mouse resistance 1( SAMR1) mice served as control. After treatment for 30 d, the cerebral mitochondria were isolated. The ATP production, reactive oxygen species (ROS) level, oxidative phosphorylation parameters and mitochondrial permeability transition pore (MPTP) were detected to evaluate the function of mitochondria in SAM mice.RESULTS: Respiratory control index, ADP/O ratio, State Ⅲ respiration and oxidative phosphorylation rate (OPR) were significantly lower in SAMP8 than those in SAMR1(P<0.05). State Ⅳ respiration did not significantly change in SAMP8 compared with that in SAMR1. At the same time, the loss of mitochondrial membrane potential(MMP), the decreased of ATP content, the increase of mitochondrial swelling degree and the increased level of ROS were also observed in SAMP8 brain mitochondria. ICA at the dosage of 75 mg/kg and 150 mg/kg significantly improved oxidative phosphorylation process, mitochondria swelling degree, MMP and other biochemical functions.CONCLUSION: ICA has a protective effect on cerebral mitochondrial impairment in SAMP8 mice.

Comparison of the inhibitory effect on HBV replication by siRNA and lamivudine in HepG2.2.15 cells

LI Gui-qiu, CHEN Shu-lan, CUI Lan-ying, ZHAO Jin-ying, LUO Wen-tao, LU Juan

2010, 15(7):  727-731. 

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AIM: To compare the inhibitory effect of inhibition of siRNA and lamivudine on hepatitis B virus replication and expression in HepG2.2.15 cells.METHODS: Recombinant plasmid psil-HBV was constructed and transfected into HepG2.2.15 cells. The transfected cells were harvested at 48,72 and 96 h. The concentration of HBeAg and HBsAg was determined using ELISA method. HBV DNA replication was examined by real time PCR, and the level of HBV mRNA was measured by reserved transcribed PCR.RESULTS: siRNA effectively inhibited the expressing and replication of HBV at the levels of HBsAg, HBV DNA and mRNA(P<0.05). Lamivudine had only inhibitory effect on viral DNA synthesis.CONCLUSION: The anti-HBV effect of HepG2.2.15 cells treated by siRNA is totally differently and more effective from that seen with lamivudine in HepG2.2.15 cells.

Effect of tirofiban on the plasma inflammatory factors of P-selectin,IL-6 and IL-1β in vitro

XIE Shuang-feng, YIN Song-mei, NIE Da-nian, LI Yi-qing, XIAO Jie, MA Li-ping, WANG Xiu-ju, WANG Jing-feng

2010, 15(7):  732-736. 

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AIM: To explore the anti-inflammatory effects of tirofiban in vitro, and to provide the theoretical basis for properly using the GP Ⅱb/Ⅲa receptor antagonists.METHODS: The platelets in the blood samples were activated in vitro with adenosine diphosphate (ADP) or thrombin respectively. Tirofiban was added to each sample in 20%, 50% or 80% inhibiting concentrations. Then the mixed liquor was incubated in 37 ℃ for 30 minutes. After centrifugation, the samples were divided to supernatants and sediments. The P-selectin, interleukin-6 (IL-6) and interleukin-1β (IL-1β) of were detected by enzyme linked immunosorbent assay (ELISA).RESULTS: ADP (final concentration: 10 μmol/L) could induce the production of P-selectin, that could be inhibited by tirofiban in concentrations higher than 31.25 μmol/L (IC₂₀). ADP had no effect on the production of IL-6 or IL-1β. Thrombin (final concentration: 0.03 U/L) could induce the production of P-selectin, IL-6 and IL-1β, those could be inhibited by tirofiban in concentrations higher than 156.25 μmol/L (IC₅₀). Tirofiban without ADP or thrombin had no effect on the production of P-selectin, IL-6 or IL-1β.CONCLUSION: Tirofiban in concentration higher than IC₅₀ could inhibit the production of P-selectin and inflammatory factors induced by thrombin. Tirofiban in full dosage could inhibit the activation of platelet and decrease the production of inflammatory factors at the same time in vitro.

Protective effect of MIF siRNA mediated by lipid microbubbles on acute lung injury in mice

JIANG Yong-nan, MO Hong-ying, CHEN Jian-hai

2010, 15(7):  737-741. 

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AIM: To investigate the protective effect of MIF siRNA mediated by ultrasound lipid microbubbles gene transfer system and evaluate the efficacy of this gene transfer system.METHODS: The model of acute lung injury was induced by LPS in mice which were randomly divided into 4 groups: normal control group (Con), LPS stimulation (LPS), LPS + PC + MIF siRNA treatment group (PC + MIF siRNA), LPS + WP + MIF siRNA treatment group (WP + MIF siRNA). The MIF siRNA was transfected by microbubbles ultrasound. These methods including EMSA, Western-Blot, ELISA and HE stained for histopathological examination were used to observe the expressions of NF-κB and IκB-α, to detect the levels of inflammatory mediators of TNF-α, IL-1β, IL-6, and to assess the pathological changes.RESULTS: MIF siRNA was carried and transferred by WP + MIF siRNA which up-regulated the expression of IκB-α in cytoplasm and significantly inhibited the expression of NF-κB in nucleus, then inhibited the levels of inflammatory mediators of TNF-α, IL-1β, IL -6 and improved the pathological changes. But the PC+ MIF siRNA treatment group has no any improvement on acute lung injury in mice.CONCLUSION: MIF siRNA can be effectively transferred by lipid microbubbles gene transfer system and have protective effect on acute lung injury in mice.

Effect of Urotensin II on the apoptosis of human lung adenocarcinoma A549 cells and the underlying mechanism

ZHOU Cheng-hua, SONG Zheng, XING Shu-hua, WU Yu-qing, ZHENG Jun-nian, PEI Dong-shang

2010, 15(7):  742-746. 

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AIM: To explore the effect of Urotensin II on the apoptosis of human lung adenocarcinoma A549 cells and its underlying mechnism. METHODS: A549 cells were divided into three groups: Control group, Cisplatin group (25 μg/mL)and Urotensin II+Cisplatin group(10^-7 mol/L U-Ⅱ+ 25 μg/mL cisplatin). The effect of Urotensin II on the apoptosis of A549 cells was determined by TUNEL method. The expressions of Bcl-2 and Bax were detected by immunocytochemistry. RESULTS: Comparing with Control group, the apoptotic rate and the expression of Bax were increased, while the expression of Bcl-2 was decreased in Cisplatin group(P<0.01). Urotensin II significantly inhibited Cisplatin-induced apoptosis of A549 cells and antagonized Cisplatin-induced down-regulation of Bcl-2 and up-regulation of Bax(P<0.01). CONCLUSION: Urotensin II inhibits the apoptosis of human lung adenocarcinoma A549 cells by up-regulating the expression of Bcl-2 and down-regulating the expression of Bax.

Effects of proteasome inhibitor MG-132 on cardiac function and expressions of Hsp70 and CHIP in myocardial infarction rats

ZHANG Xin-min, DAI Cui-lian, TANG Ji-fei, YANG Peng-lin

2010, 15(7):  747-752. 

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AIM: The study was designed to examine the effect of proteasome inhibitor MG-132 on cardiac structure and function in myocardial infarction rats, and to investigate its mechanism. METHODS: The myocardial infarction model was established by ligating rat's left anterior descending coronary artery. Proteasome inhibitor MG-132 was administered in a dose of 0.75 mg·kg^-1·d^-1 for 7 days. The myocardial pathological change, infraction volume, hemodynamics and brian natriuretic peptide were measured to evaluate the cardiac function; realtime PCR and Western blotting were applied to measure the mRNA and protein expressions of Hsp70 and CHIP. RESULTS: MG-132 decreased the levels of myocardial infraction volume, left ventricular end diastolic presssure and serum BNP (P<0.05). Meanwhile, MG-132 markedly elevated the mRNA and protein levels of Hsp70 and CHIP (P<0.05). CONCLUSION: MG-132 protects myocardium against acute myocardial ischemia injury by inducing CHIP and Hsp70 expression.

Effects of crocetin on the proliferation and differentiation of 3T3-L1 preadipocyte

ZHANG Xiao-ming, QIAN Zhi-yu, JI Hui, YANG Li-na, YANG Ru-hui, SONG Lei

2010, 15(7):  753-757. 

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AIM: To observe the effect of crocetin on proliferation and differentiation of 3T3-L1 preadipocyte, and to investigate the possible mechanism involved. METHODS: The 3T3-L1 cells were pretreated with crocetin, while, the MTT method was used to detect the proliferation of the cells, oil red O staining method and spectrophotography were applied to analyze the degree of differentiation. The expression of AMP-activated protein kinase(AMPK)mRNA, which was called as the energy regulator of cell, was detected by reverse transcription PCR (RT-PCR), and the protein level of p-AMPK was determined by western blot. RESULTS: High and middle dose crocetin(10^-5, 10^-6 mol/L) could significantly inhibit the proliferation and differentiation of 3T3-L1 cell(P＜0.01); also, the low dose croctin(10^-7 mol/L) could inhibit its proliferation and differentiation(P＜0.05); croctin could incease the expression of AMPK mRNA and the protein level of p-AMPK(P＜0.05). CONCLUSION: Crocetin inhibit the proliferation and differentiation of 3T3-L1 cell possibly by influence AMPK.

Improvement effect of salvianolate on small intestinal mucosal barrier in cirrhotic rats

YANG Dan-hong, YE Zai-yuan, HE Xu-jun, ZHANG Qin, ZHOU Wei-ming, XU Wen-juan, LV Huo-xiang

2010, 15(7):  758-763. 

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AIM: To investigate the effect of salvianolate on small intestinal mucosal barrier in rats with CCl₄-induced liver cirrhosis.METHODS: Cirrhosis was induced in rats using CCl₄ (0.3 mL/kg ). Rats were divided randomly into four groups:untreatmeat, low-dose salvianolate(12 mg/kg), medium-dose salvianolate(24 mg/kg), and high-dose salvianolate(48 mg/kg). They were all treated for 2 weeks.Another 10 healthy rats were enrolled as normal control. Mortality of cirrhotic rats in each group were evaluated after treatment. Serum samples were collected from the portal vein for the detection of endotoxin. Tissue samples from the ileocecum were observed under light microscopy for morphological changes.A contrasting study on the expression of secretary immunoglobulin A(sIgA) were performed in each group by immunohistochemical staining method.RESULTS: The mortality of cirrhotic rats in the untreatmeat group was 42.86%. No cirrhotic rat died in the high-dose salvianolate group. The serum endotoxin level was highter in the untreatmeat group than that in salvianolate group(P<0.05). Intestinal mucosal and villous atrophy were observed in the untreatmeat group, with necrosis and shedding of the intestinal mucosal epithelium. These pathological changes were reversed in the salvianolate-treated groups.The expression of sIgA in intestinal mucosa were reduced obviously in the untreatmeat group, in compared with those in the salvianolate-treated groups and healthy rats group. The integral optical density of immunohistochemical staining image in untreatmeat group was obviously lower than that in high-dose salvianolate-treated group (P<0.01). CONCLUSION: Salvianolate is helpful for reducing endotoxin level,ameliorating injury of intestinal mucosa,enhancing immune function of intestinal mucosa in rats with CCl₄ induced cirrhosis,and therefore improving the barrier function of intestinal mucosa.

Inhibitory action of crocetin on the expression of E-selectin in bovine endothelial cells induced by advanced glycation end products

XIANG Min, ZHOU Cheng-hua, QIAN Zhi-yu

2010, 15(7):  764-769. 

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AIM: To study the inhibitory effect of crocetin on the expression of E-selectin in bovine endothelial cells (BECs) induced by advanced glycation end products (AGEs).METHODS: Neutrophils and monocytes were separated and purified from the whole blood of new-born calf. The adhesion of neutrophils/ monocytes to endothelial cells was assayed by Fuhong staining method. Cell-based ELISA and sABC immunocytochemistry were adopted to analyze the expression of E-selectin.RESULTS: AGEs(100 μg/mL)could increase the adhesion of neutrophils/monocytes to endothelial cells(P<0.01 vs control). However, after pre-incubation the BECs with crocetin(1,0.1,0.01 μmol/L) for 12 h before exposure to AGEs (100 mg/mL), the above adhesion rate decreased significantly in a dose-dependent manner( P<0.05 or 0.01 vs AGEs group). Cell-based ELISA results demonstrated that the expression of E-selectin elevated in BECs treated by AGEs within 4 h, then decreased and regained to the normal level at 8 h, while the protein expression of E-selectin was suppressed by crocetin. sABC immunocytochemistry also confirmed that crocetin could decrease the level of E-selectin.CONCLUSION: These results demonstrate that crocetin could inhibit E-selectin over-expression in BECs exposed to AGEs and then down-regulate the adhesion of neutrophils/monocytes to endothelial cells, which is one of the possible mechanisms for crocetin to attenuate diabetic vascular complications.

Effect of nebivolol on circle and aortic renin-angiotensin system in spontaneously hypertensive rats

WANG Yan, ZHANG Ming-sheng, LIU Yu, CHEN Min

2010, 15(7):  770-774. 

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AIM: To study the effect of nevilolol on circle and aortic renin-angiotensin system (RAS) in spontaneously hypertensive rats (SHR).METHODS: SHR and age-matched Wistar-Kyoto (WKY) rats were randomly divided into 4 groups: (1) Nebivolol group(n=6): SHR were treated with nebivolol(5 mg·kg^-1·d^-1, i.g.); (2) Captopril group (n=6): SHR were treated with captopril (15 mg·kg^-1·d^-1, i.g.); (3) SHR control group (n=6): SHR were treated with vehicle once daily, i.g.; (4) WKY control group (n=6): WKY were treated with vehicle once daily, i.g. The therapy was continued for 8 weeks. At the end of this study, animals were anesthetized with 3% sodium pentobarbital (30 mg/kg, i.p.). Plasma renin activity (PRA) was measured. Plasma and aortic nitric oxide (NO), angiotensin Ⅱ(AngⅡ), NO/AngⅡ and angiotnesin converting enzyme(ACE ) activity were also measured.RESULTS: Compared with WKY, the levels of NO, NO/AngⅡin plasma and aortic were lowered, while the level of AngⅡ was increased in SHR. ACE activity in aorta form SHR were increased than those in WKY, but plasma ACE activity was reduced. There was no difference in PRA between SHR and WKY. Nebivolol did not affect plasma AngⅡand ACE activity. But nebivolol reduced aortic AngⅡ concentration and inhibited aortic ACE activity. Nebivolol could increase the levels of plasma and aortic NO and NO/AngⅡ in SHR.CONCLUSION: The antihypertensive effect of nebivolol in SHR is accompanied by the inhibition of RAS.

Effects of Danshen Injection on the activity of rabbit CYP1A2, CYP2D6 and CYP3A4 in vivo

LIU Gao-feng, ZHEN Li-mian, HUANG Li-jun

2010, 15(7):  775-780. 

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AIM: To evaluate the effects of Danshen Injection on rabbit cytochrome P450 (CYP450) activity by Cocktail probe drugs.METHODS: Male rabbits were randomly divided into three test groups and one control group. The test groups were treated with Danshen Injection (i.v.) at three dosages (low, midst and high dosage), and the control group was treated with physiological saline. The plasma concentrations of probe drugs(caffeine,metoprolol and dapsone) were determined by HPLC. Effects of Danshen Injection on CYP450 activity were observed by comparing the concentration-time curves and pharmacokinetic parameters of probe drugs. RESULTS: The three dosages of Danshen Injection inhibited the CYP2D6 activity(P＜0.05, or P＜0.01), but had no effects on the activities of CYP1A2 and CYP3A4. CONCLUSION: Danshen Injection can inhibit CYP2D6 activity in rabbit, but has no effect on CYP1A2 and CYP3A4. When Danshen Injection is used in clinic, attention should be paid to the inhibition effect on CYP2D6 to avoid CYP2D6-mediated drug interaction, and to promote safe and rational drug use.

Effect of puerarin on contents of MCP-1, TNF-ɑ and pulmonary ultrastructure after thrombolytic therapy in rabbits with acute pulmonary embolism

JIANG Qin-hua, CHEN Yan-fan, XU Xian-rong, XU Wen, LI Guo-ping, WANG Liang-xing, CHEN Shao-xian

2010, 15(7):  781-785. 

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AIM: To observe the effect of puerarin on the contents of MCP-1,TNF-ɑ and pulmonary ultrastructure after thrombolytic therapy in acute pulmonary thromboembolism.METHODS: Twenty-four Japanese rabbits were randomly divided into sham operation group, thrombolysis-only group, and puerarin group.Acute pulmonary thromboembolism models of rabbits were established with injection of autologous blood clots through the right heart catheters. Haemodynamic monitoring was performed by introducing heart catheter through right jugular vein. These rabbits were sacrificed at 4 h after thrombolysis, the lung was removed and the ratio of wet to dry of lung tissue weight (W/D) was detected. The contents of MCP-l and TNF-α were also investigated with ELISA. The myeloperoxidase (MPO) activities of lung tissue were detected with colorimetry. The ultrastructure of lung tissue was observed by electronic microscope.RESULTS: The pulmonary arterial mean pressure (mPAP) was decreased immediately at 1 h after thrombolysis both in thrombolysis-only group and puerarin group (P<0.01), the mPAP in puerarin group were significantly lower than those in thrombolysis-only group at 1 h after thrombolysis(P<0.05); The contents of MCP-l and TNF-α, the value of W/D and the MPO activity of lung tissue were significantly increased in thrombolysis-only group and puerarin group than those of sham operation group; The histopathologic analysis showed the injuries of vascular endothelial cells and alveolar cells in thrombolysis-only group were more severe than those in puerarin group.CONCLUSION: Chinese herb puerarin can protect lung against reperfusion injury after thrompolytic therapy in acute pulmonary thrombembolism which may associate with the action of inhibiting inflammation reaction by reducing the contents of MCP-1 and TNF-α.

Evaluation of promoting effects of transdermal enhancers with principle components analysis method

CHEN Yan-fen, WANG Tong-ren, WANG Hui, LIANG Qing

2010, 15(7):  788-793. 

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AIM: To evaluate the promoting effects of several transdermal enhancers with principle components analysis method.METHODS: Using 5-fluorouracil(5-Fu)as model drug,the promoting effects of caryophyllus oil, agastache rugosus oil, chaste oil, azone, menthol crystal, oleic acid and camphor were detected by transdermal absorption experimentation in rabbit skin in vitro, indexes such as cumulative permeation quantity, penetrating rates, enhancement ratio and lag time were calculated, finally the principle components analysis method was used to evaluate the promoting effects of those transdermal enhancers.RESULTS: Oleic acid, caryopyllus oil, menthol crystal, agastache rugosus oil, azone and chaste oil all promoted 5-Fu through the skin, and the effects of these transdermal enhancers increased in sequence,2% chaste oil occupied the strongest position. Azone, caryopyllus oil, camphor, agastache rugosus oil, oleic acid, menthol crystal and chaste oil all showed the deposit effect, and those enhanced in sequence, too.CONCLUSION: The method of principle components analysis could evaluate the promoting effects of transdermal enhancers objectively and synthesizly.

Evaluation of sustained-release effect on Compound Danshen Skeleton Sustained-Release Tablet by pharmacodynamics method

XU Guo-liang, TANG Xi-lan, SHAN Yi-min, ZHANG Qi-yun, ZHENG Qin, YANG Ming

2010, 15(7):  794-797. 

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AIM: To evaluate the sustained-release effect on Compound Danshen Skeleton Sustained-Release Tablet (CDSRT) by pharmacodynamics method.METHODS: By reference to Compound Danshen Tablet(CDT), Sprague-Dawley rats had been administrated with CDT and CDSRT with the content of crude drugs 2911.14 mg/kg. The medicated serum of CDT and CDSRT were prepared at the time of 0.25,0.5,0.75,1,2,4,8,12 h after single oral administration. The medicated serums were added to myocardial cells respectively. The protective effects of CDT and CDSRT on hypoxia/reoxygenation and the sustained-release effect of CDSRT were evaluated.RESULTS: Compared with the H/R model group, the medicated serum of CDT 4,8 h and CDSRT 2,4,8,12 h had apparent protective effects against proliferation inhibition caused by hypoxia/reoxygenation(H/R) induced injury in myocardial cells. The present half-life t_1/2(ka) of CDT and CDSRT were 2.655 h and 0.719 h. The peak times of effective action were 5.213 h and 2.957 h. And the elimination half-life t_1/2(ke) were 4.953 h and 10.166 h respectively. Compared with CDT, CDSRT had a higher speed of the effect present and the peak time of effective action and a lower speed of sustained-release.CONCLUSION: CDSRT has a certain sustained-release function as t_1/2(ke) longer than that of CDT. Pharmacodynamics method is a feasible method for the evaluation of CDSRT sustained-release effect.

Auto statistical report for trough/peak ratio index in the evaluation of ambulatory blood pressure monitoring by SAS software

XU Lin-yong, ZHANG Wei, ZENG Fang, FU Chen-chao, ZHAO Li, ZHAO Xiao-hua, SUN Zhen-qiu

2010, 15(7):  798-802. 

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AIM: To develop an efficient SAS macros to automatically output table of statistical analysis report for trough: peak ratio index. METHODS: Applying SAS functions such as int, floor and SAS procedure such as proc mean /ttest, wilcoxon.RESULTS: Some SAS Macros were made including data management and transform, creating variables and outputing statistical analysis report tables.CONCLUSION: The SAS Macros are useful to output statistical analysis report tables and improve the efficiency for clinical trial evaluation.

Clinical study on efficacy and security of fixed-dose glipizide/metformin on type 2 diabetes mellitus(DM)

YAO Lu, LV Xiao-feng, JI Xin, ZHANG Jian-li

2010, 15(7):  803-808. 

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AIM: To evaluate the effect and safety of fixed-dose glipizide/metformintablets on type 2 diabetes. METHODS: This was a double blind randomized 12-week clinical observation on multiple centers comparing the blood glucose lowering effect and safety between fixed-dose glipizide/metformin tablets and glipizide co-administered with metformin.RESULTS: The cohort consisted of 116 patients who received glipizide/metformin tablets and 118 taking glipizide and 118 taking metformin. The levels of glycosylated hemoglobin (HbA1c)were (5.5±1.3)%,(6.0±1.4)% and (6.1±1.5)%,the levels of fasting blood glucose (FBG) were (7.3±1.8),(7.9±2.3) and (8.2±2.4)mmol/L and the levels of 2 hours postprandial blood glucose (PBG 2 h) were (11.0±4.0),(12.2±4.2) and (12.5±4.5)mmol/L, in glipizide/metformin group, metformin group, glipizide group, after 12-week therapy. The level of 2 hours postprandial insulin was increased,but the fasting insulin level was significantly changed. The levels of TG were decreased in glipizide/metformin and metformin groups,and that in the glipizide group was increased . There were no statistical difference of the rates of side effect in three groups.CONCLUSION: Fixed-dose glipizide/metformin is a convenient, effective and safe blood glucose lowering drug for diabetic patients.

A rapid and sensitive LC-MS/MS method for determination of valsartan in human plasma

LI Ling, TAN Zhi-rong, CHEN Yao, ZHOU Gan, GUO Dong, YAN Jin, YANG Guo-ping, OUYANG Dong-sheng

2010, 15(7):  809-813. 

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AIM: To establish a rapid and sensitive LC-MS/MS method for determination of valsartan in human plasma.METHODS: The prepared analytes were separated on an ODS column using mobile phase of acetonitrile and 1‰ methanoic acid (70∶30). Valsartan and irbesartan were detected by multiple reaction monitoring (MRM) mode after ionized by ESI source. The transitions of m/z436.3→235.2 and m/z 429.4→207.2 were used to quantify valsartan and irbesartan, respectively.RESULTS: The method was linear in the range of 24.2-3100.0 μg/L for valsartan. The intra-day mean precision and inter-day mean accuracy precision was not more than 15%.CONCLUSION: The method is rapid and sensitive, and it's adaptive for clinic pharmacokinetic evaluation of valsartan.

Research advance on P-glycoprotein inhibitors and the structure-activity relationship

WEN Xiao-zhou, ZHOU Fang, WU Xiao-lan, WANG Guang-ji

2010, 15(7):  814-820. 

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P-glycoprotein (P-gp) is an important ATP-dependent transmembrane transporter, which can pump out a large number of structural and functional diverse compounds. P-gp plays a prominent role in physiological and pathological functions. It is not only crucial to drug disposition, but also one of the main causes of multidrug resistance (MDR). Therefore, developing P-gp inhibitors is significant to researches on modulation of drug pharmacokinetics and reversion of multidrug resistance. In this paper, we summarize studies on structure-activity relationship of P-gp inhibitors, which will give us important information for screening and synthesizing desirable P-gp inhibitors in the future.

Advances of desloratadine in clinic treatment of allergic diseases

LIU Wei

2010, 15(7):  821-826. 

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Desloratadine is a new H₁-histamine antagonist which have potent, rapid and continuous anti-allergic effect. In additional, it possesses unique anti-inflammatory properties and mechanism. Many recent clinic studies had confirmed a good prospect of desloratadine in clinic treatment of allergic diseases.

Advances in study of fluorouracil for implantation and its clinical application in adenocarcinoma

ZAN Pei-xia, YAN Shi-jie

2010, 15(7):  827-831. 

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Fluorouracil for implantation is a new implanting sustained release preparation, and it is the first tumor therapy controlled release implantation that has been ratified by SFDA.5-fluorouracil is the main component of fluorouracil for implantation. Fluorouracil for implantation can elevate the local drug concentration,extend the time of effective drug concentration,reduce the general toxic and side-effect. The article contains fluorouracil for implantation pharmacokinetics, pharmacologic and apply to adenocarcinoma.

Clinical application advancement of pulmonary surfactant

XU Guo-cheng, LI Zhi-qi

2010, 15(7):  832-835. 

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Pulmonary surfactant is a type of a phospholipid - protein complexes synthesized by II alveolar epithelial cells. It has many functions as decreasing alveolar surface tension to maintain alveolar stability, reducing alveolar fluid extravasation in the prevention of pulmonary edema, promoting the clearance of inlet ability, inhibiting bronchoconstriction and increasing the pulmonary immune function, reducing the inflammation and improving the lung anti-infection. The natural and synthetic surfactant preparations have some therapeutic effects on the clinical treatment of primary pulmonary surfactant deficiency disease and various secondary pulmonary surfactant-related diseases through tracheal injection or inhalation.

Pharmacological mechanism of propofol and its new clinical usage

LIU Qiang, HONG Jiang, LI Xiao-yu

2010, 15(7):  836-840. 

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Propofol is a short-acting intravenous anaesthetic agent which has the advantages of minimal side effects, controllable anaesthetic state, quick onset and rapid emergence from general anaesthesia.Apart from these anaesthetic advantages, it also has some non-anaesthetic effects. It has been found that propofol can protect heart, kidney and liver from ischemia-reperfusion injury. It has neuro-protective effects, immunomodulatory activity, antiemetic effects, antinociceptive actions and amnesic effects. It is obvious that these nonanaesthetic effects that propofol exerts can substantially change the daily use of propofol and may expand its pharmacological and clinical use. Advances in pharmacological mechanism and new clinical of propofol in recent years were summarized in this paper.