Table of Content

Volume 11 Issue 5
26 May 2006

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Review on endothelial dysfunction in atherosclerosis and drug therapy

HU Zhe-yi, WANG Qiu-juan, DING Xuan-sheng

2006, 11(5):  481-484. 

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Endothelial dysfunction plays a crucial role in the development of arteriosclerosis (AS).Accu-mulating evidence suggests that endothelial dysfunction is an initiating event in the etiology of arteriosclerosis.This article reviewed the relationship between endothelial dys-function and atherosclerosis, and the effects of therapeutic drugs especially statins on endothelial dysfunction.

Effects of N-n-butyl haloperidol iodide on intracellular calcium in rat car-diomyocytes

HUANG Zhan-qin, SHI Gang-gang, GAO Fen-fei, ZHOU Yan-qiong, ZHANG Yan-mei, LIU Xin-ping

2006, 11(5):  485-490. 

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AIM: To investigate the effects of N-n-benzyl haloperidol iodide (F₂) on intracellular calcium ([ Ca²⁺ ]_i) in rat cardiomyocytes.METHODS: Cardio-myocytes were loadedwith Fluo3-AM, a calcium sensitive fluorescent dye, and the[ Ca²⁺ ]_i was determined by the use of laser scanning confocal microscope (LSCM).RESULTS:In the Tyrode' s solution with Ca²⁺ at the con-centration of 1.8 mmol·L^-1, 60 mmol·L^-1 KCl induced a rapid increase of intracellular calcium fluorescence in-tensity (FI).The FI was increased from the basic value (1.0) to 1.84±0.35 (P<0.01, n =50).With prein-cubation of cardiomyocytes with F₂ 0.1, 1, 10 μmol·L^-1, the FI elevation was inhibited in a concentra-tion-dependent manner.The calculated IC₅₀ was 1.61 μmol·L^-1.F₂ also reduced the FI elevated by 60 mmol·L^-1 KCl in a concentration dependent manner.The FI was decreased by 0.1、1、10μmol·L^-1 F₂ from 1.92± 0.42(n =50) to 1.88 ±0.39(P >0.05, n =50), 1.31 ±0.36(P<0.01, n =50), 1.09 ±0.05(P<0.01, n =50), respectively.The calculated IC₅₀ was 1.78 μmol·L^-1.F₂ had no effects of on[ Ca²⁺ ]_i in the resting state, and had no effects on intracellular calcium release induced by caffeine and inositol-1, 4, 5-trisphosphate. CONCLUSION: F₂ reduces[ Ca²⁺ ]_i.via inhibition of voltage dependent calcium channel, which is possibly in-volved in the mechanism of its protective effects on myo-cardial ischemia reperfusion injury.

A new method for determination of kaempferol-3-O-rutinoside in plasma: application to pharmacokinetic study in Sprague-Dawley rats

LIANG Shi-piao, LIU Fei, DU Fei-fei, NIU Wei, SUN Yan, LI Chuan, GUO Mei-li

2006, 11(5):  491-496. 

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AIM: To develop a sensitive and reliable method for determination of kaempferol-3-O-rutinoside (NFR) in plasma.METHODS: The optimal ionization and fragmentation conditions, aswell as liquid chromato-graphic ones, to detect kaempferol-3-O-rutinoside were identified.Effective sample clean-up method for recover-ing the analyte from plasma was also studied.The newly developed analytical methodwas evaluated in terms of ac-curacy, precison, selectivity, sensitivity, and stability, which was further demonstrated its applicability in a pilot plasma pharmacokinetics study in Sprague-Dawley rats re-ceiving an intravenous dose of NFR at 30 mg·kg^-1.RESULTS: Positive ion electrospray ionization was found to effeciently generate precursor protonated moleculesof both the analyte and the internal standard (IS, l-Stepholidine) which was optimized and used to produce their character-istic and abundant fragment ions for MS/MS analysis in selected reaction monitoring mode with precursor-to-prod-uct ion transitions m/z 595→287 for NFR and m/z 328 →178 for IS.The chromatographic retention times were 2.3 and 2.2 min for NFR and IS, respectively.Liquid-liquid extraction using ethyl acetate provided good recov-ery for both the analyte and IS from HCl-acidified rat plasma samples demonstrating 58.5% -70.1% and 72.5% recovery, respectively.NFR and IS were stable during the whole process of the bioassay.Good linearity was achieved for regresion of NFR IS peak area ratio to nominal plasma concentration of the analyte demonstrating r value equal to 0.9999 (n =6×5), when the concen-trationwas between 0.192 and 600 ng·ml^-1.The within-run acurracy and presicion of the analytical method were quite good for plasma NFR, i.e., 92%-107% and 1.0%-5.7%, respectively and the between-run data were 94%-99 %and 1.5%-8.4%, respectively.The lower limit of quantification (LLOQ) of the method was 0.192 ng·ml^-1.Following a single intravenous dose of NFR at 30 mg·kg^-1 to Sprague-Dawley rats, NFRexhib-ited the elimination half-life (T_1/2) 1.27 h and mean res-ident time (MRT) 0.32 h.The clearance (CL) and dis-tribution volume at stable status (V_SS) of NFRwere 2.73 L·h·kg^-1 and 0.92 L·kg^-1, respectively.CONCLUSION: The first analytical method based on LC-MS/MS, providing simple, robust, sensitive, and rapid measure-ment of NFR in plasma, is presented in this communica-tion, which will prove useful for the future preclinical pharmacokinetic evaluation of NFR.

Compare effects of total intravenous anesthesia and balanced anesthesia on stress response on suspensive laryngoscope vocal cords surgery

MAN Yuan-yuan, JIANG Yu-ge, XU Long-he, ZHANG Hong

2006, 11(5):  497-500. 

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AIM: To compare the effects of total in-travenous anesthesia and balanced anesthesia on stress re-sponse on suspensive laryngoscope vocal cords surgery. METHODS: Thirty patients undergone microlaryngeal surgery were randomly divided into two groups(n =15). Analgesia and amnesia slow inductionwas used in all pa-tienswith nosal incubation.During maintenance of anes-thesia, propofol, remifentanil and scopolamine were used in total intravenous anesthesia group(group TIVA);fenta-nyl, scopolamine and isoflurane were used in balanced anesthesia group(group BAL).Record the data of each group, including base data, after induction, end of tra-cheal intubation, 3 min after intubation, setting the sus-pensive laryngosopy, 3 min after setting the suspensive la-ryngosopy, removing the trachea, MAP, HR of each time, the time of recovery.The blood concentrations of epinephrine (E), noradrenalin(NE), cortisol, IL-6 were measured at each time point of base data, end of tracheal intubation, setting the suspensive laryngosopy, 3 min af-ter setting the suspensive laryngosopy.RESULTS: There is no significant difference of HR, MAP, blood concen-tration of E, NE, cortisol, IL-6 at end of tracheal intuba-tion compared with base data.AT setting the suspensive laryngosopy, 3 min after setting the suspensive laryngos-opy, HR, MAP, blood concentrations of E, NE, corti-sol, IL-6 in group BAL were all higher than that of base data, and were also higher than group TIVA at the same time.The recovery time of group TIVA was shorter than that of group BAL.CONCLUSION: Analgesia and am-nesia slow induction with nosal intubaion and maintenance with remifentanil, propofol can inhibit sudden change of hemodynamics and stress response of intubation and set-ting the suspensive laryngoscope, with quicker recovery. It is an ideal anesthesia method for suspensive laryngo-scope vocal cords surgery.

Comparison of blocking effect of ropivacaine and bupivacaine on sodium channels of rat dosal root ganglia

XU Long-he, JIANG Yu-ge, FENG Ze-guo, ZHANG Hong

2006, 11(5):  501-504. 

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AIM: To compare the blocking effect of ropivacaine and bupivacaine on sodium channels of rat dosal root ganglia(DRG) using whole cell recording tech-nique.METHODS: Rat DRG neuronswere enzymatical-ly isolated, tetrodotoxin-sensitive(TTX-s) and tetrodotox-in-resistant (TTX-r) sodium currents of DRGwere record-ed by whole cell recording.Drugs were given in bath solu-tion.The concentrations of ropivacaine were 10, 30, 100, 1 000 μmol·L^-1 and bupivacaine were 10, 30, 100, 300 μmol·L^-1.The recording number in each dose groupwas six.RESULTS: CsCl in extracellular fluid and TEA in intracellular fluid were used to block the potassium chan-nels.Sodium currentswere recordedwhen the holding po-tential was -70 mV and a serials of pulse with step 10 mV and duration 70 mswas given.TTX-s sodium channel was recorded in 80.1%large DRG cells and TTX-r sodi-um channel was recorded in 92.4% medium and small DRG cells, of which 56.3% cells had no response to 1 μmol·L^-1 TTX.The half-maximal blocking concentra-tions of ropivacaine on TTX-r sodium channel was 65.7± 6.1 μmol·L^-1, which wasmuch lower than that on TTX-s sodium channel 246.8±11.2 μmol·L^-1 (P<0.01); The half-maximal blocking concentrations of bupivacaine on TTX-r and TTX-s sodium channel was essentially the same (27.2±6.2 μmol·L^-1 vs 29.5±2.9 μmol·L^-1, P >0.05).CONCLUSION: Ropivacaine preferentially blocks TTX-r sodium channel.Selective blocking of TTX-r and TTX-s sodium channel was one of the reasons of se-peration of sensation and motion when it is used in epi-dural anesthesia.

Colon-targeted delivery system of dexamethasone-angelica sinensis po-lysaccharides prodrug in rats

LIU Xin-you, ZHOU Si-yuan, CHENG Jian-feng, RAN Yu-hua, TENG Zeng-hui, YANG Run-tao, YANG Xi, MEI Qi-bing

2006, 11(5):  505-509. 

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AIM: To explore the transport and deliv-ery of active drug from dexamethasone-angelica sinensis polysaccharides prodrug in the gastrointestinal tract of rats.METHODS: Dexamethasone and the prodrug were orally administered to rats at the dose of 1.96 mg·kg^-1 (calculated by carried dexamethasone).The drugs in the plasma and contents of different parts of the rats' gastroi-ntestinal tract were determined by high performance liquid chromatography (HPLC).RESULTS: Dexamethasone carried by the prodrug wasmainly released in the contents andmucosa of cecum and colon after oral administration of the prodrug.The absorption of released dexamethasone was reduced significantly.The peak time, peak concen-tration and AUC were 7.2 h, 42 μg·L^-1 and 334 μg·h·L^-1, respectively.However, free dexamethasone was found mainly in the contents and mucosa of the stom-ach, proximal and distal small intestine after oral admin-istration.The peak time, peak concentration and AUC were 2.2 h, 2 120 μg·L^-1 and 11 875 μg·h·L^-1, re-spectively.CONCLUSION: Dexamethasone can be spe-cifically delivered to the cecum and colon by using dexam-ethasone-angelica sinensis polysaccharides prodrug.The absorption of dexamethasone was reduced significantly and the drug concentration in colon was increased significant-ly.The prodrug has a potential in the treatment of colitis.

Experimental studies and evaluation on safety of compound aluminum sulfate injection

XU Feng-hua, FU Wei-jun, ZHANG Zhi-ping, WANG Xiao-xiong

2006, 11(5):  510-514. 

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AIM: To study the in situ stimulation ef-fect of compound aluminum sulfate injection after i.m. in rabbit quadriceps and dog bladder.The absorption of aluminum and the healing of the bladder wall were also studied to give an evaluation on the safety of the com-pound injection.METHODS: Compound aluminum sul-fate injection was i.m.injected into quadriceps of the rabbits.The in situ stimulation effect was observed mac-rographically.Blood samples were collected at different time after i.m.injection.Aluminum concentrationswere determined by ICP-MS assay and simulated with DAS software.Tissue necrosis as well as the healing of the bladder wall were observed macrographically or pathologi-cally after the injection was given into dog bladder.RESULTS: Severe stimulation was observed after intra quad-riceps injection, however, there was no obvious elevation of blood aluminum concentration.The average AUC_0-24 was 2.93±1.82 mg·h·L^-1 (n =5), corresponding to a relative bioavailability of about 2.77%.Injecting in bladder muscle necrotized the bladder wall in situ, but fi-broblast generated and took place of the necrotized mem-brane and muscle four weeks after injection.There was no bleeding or perforation on the bladder wall.CONCLU-SION: Caused compound aluminum sulfate injection in situ necrosis which healed up in 4 weeks.Aluminum ab-sorption is very low after injection, giving a further expla-nation to the safety of the compound injection.

Protective effects of platelet factor 4 on bone marrow of mice with radi-ation injury and its mechanism

WANG Hai-tao, YANG Lan, TIAN Qiong, HAN Xiao-xia, GAO Ying, WANG Xin

2006, 11(5):  515-518. 

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AIM: To study the protective effects of platelet factor 4(PF4) on the bone marrow cellsof the ra-diation injury mice and to do some preliminary studies for its mechanism.METHODS: BALB/c male mice were randomly divided into three groups:exposure group, pro-tection group with PF4 and control group.The mice of protection group were injected PF4 (40 μg·kg^-1) into abdominal cavity twice at 26 h and 20 h before irradiation of 4 Gy⁶⁰Co-γray.The cell cycle of bone marrow cells was determinedwith flow cytometry on d 1、2、4、8 after ir-radiation.The expression level of p21 in BMSCswere de-tected with immunohistochemistry.RESULTS: The cells on G₀ +G₁ phase of exposure group on d 1、2 and of pro-tection group on d 1 were significantly higher than that of control group, the difference between exposure group and protection group is notable at every time point (P<0.05), while the difference between protection group on d 2、8 and exposure group on the same day was not signifi-cant(P >0.05).On d 2、4 after irradiation, the expres-sion of p21 in BMSCs of protection group was up-regulat-ed compared with that of exposure group.On d8 the result was opposite.CONCLUSION: PF4 has obvious protec-tive effects on the bone marrow of the radiation injury mice by controlling cell cycle and recovering its hemato-poietic function as early as possible.The high expression of p21maybe has a certain effect on the protective mecha-nism.

Effects of ketamine on expression of nitric oxide synthase in medial septal nuclei and vertical diagonal band of rats

WU feng, XIONG Ke-ren

2006, 11(5):  519-523. 

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AIM: To explore the effects in different dosage of ketamine on the expression of nitric oxide syn-thase (NOS)in medial septal nuclei (MS)and vertical diagonal band (VDB)of rats.METHODS: 40 SD rats were randomized into normal control group, normal saline (NS)group, low, middle and high dosage of ketamine (25,50, 100 mg·kg^-1, ip)group.Each group was main-tained intraperitoneally by given daily dosage once a day for a period up to 7 days.That was done at 21∶00 hour each night, and by 2 h of the last administration, poured, fixed and slicedwere carried out.Method of nic-otinamide adenosine dinucleotide phosphate diaphorase (NADPH-d)was used to show the expression of NOS in MS andVDB parsdorsalis and ventro.RESULTS: Com-pared with normal control and NS group, the number of NOS positive neurons were decreased inMS andVDB pars dorsalis and ventro in ketamine groups.There were statis-tical meaing in different-dosage groups of ketamine(P<0.05 or P<0.01).Cell-dyeing became lighten, and cel-luar average optical density value wasincreased inMS and VDB pars dorsalis and ventro in each administered ket-amine groups, There were statistical meaing in high and low dosage of ketamine(P<0.01).CONCLUSION: Ketamine can reduce the expression of NOS in MS and VDB by dosage dependence, which suggests that anesthe-sia effect of ketamine has possible correlation with neuro-pathic side effect.

Effects of hirudo and earthworm liquor extract on syndecan-1 in rats with experimental cerebral ischemia reperfusion

LUO Hai-yan, HU Chang-lin

2006, 11(5):  524-527. 

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AIM: To investigate the effect of hirudo and earthworm liquor extract on the expression of synde-can-1 in focal cerebral ischemia reperfusion rats and the relationship between syndecan-1 expression and cellists underlying antiinflammatory mechanism.METHODS: The MCAO modelsof rats were built with the intraluminal filament occlusion.Rats' brains were cut at the levels of the hippocampus as the templates.Immunohistochemistry staining and HE staining were used to facilitate the obser-vation of the distribution and the quantities of cells with expression of syndecan-1 and the pathological change of MCAO ischemia 2 h reperfusion 4, 24, 72 h and 7 d with hirudo and earthworm liquor extract or saline treatment, respectively.RESULTS: Hirudo and earthworm liquor extract could upregulate the expression of syndecan-1 on ischemia/reperfusion in rats' brains, especially at 72 h. The numbers of syndecan-1 cells got peak, hirudo and earthworm extract liquor could downregulate polynucle-ation inflammatory cells at 24 and 72 h.The expression of inflammatory cells in both hirudo and earthworm liquor extract group and saline group at 4 h was not significant. Hirudo and earthworm extract liquor downregulated the monocytic inflammation cells infiltration at 7 d.CONCLUSION: Hirudo and earthworm liquor extract can up-regulate the expression of syndecan-1on ischemia reperfu-sion in rats' brains.The upregulation of syndecan-1 can decrease inflammatory cell infiltrate.

Effects of hydrochlorothiazide and indapamide on left ventricular hyper-trophy and eNOS expression in spontaneous hypertensive rats

HE Yan, ZHONG Guo-qiang, WANG Yan, TOU Rong-hui, WANG Dao-wen

2006, 11(5):  528-531. 

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AIM: To investigate the effects of hydro-chlorothiazide and indapamide on cardiac remodeling and the expression of endothelial nitric oxide synthase (eNOS) in spontaneous hypertensive rats (SHR).METHODS: Fifteen female SHRs were randomly divided into 3 groups (n =5):control group, hydrochlorothiazide(HCTZ, 10 mg·kg^-1 ·d^-1)group and indapamide (IND, 0.625 mg·kg^-1 ·d^-1)group.Systolic blood pressure (SBP)of the rats in each group was measured at pretreatment and each week during the study.Four weeks later, rats were sacrificed and the ratio of heart weight to body weight was calculated, collagen deposition in the heart was deter-mined histochemically using Sirius red staining, and eNOS protein expression of the heart was determined by Western blot.RESULTS: Both HCTZ and IND reduced the SBP of SHRs significantly (P<0.05).The drug group showed normal myocardium structure as compared with control rats which showed myocardium cell hypertro-phy, derangement, interstitial proliferation and mass col-lagen deposition.HCTZ and IND increased the eNOS ex-pression significantly.CONCLUSION: Both HCTZ and IND can protect the heart by reversing cardiac remodel-ing, upregulate the eNOS expression and reduce collagen deposition.

Effect of liquorice on airway inflammation and Th₁/Th₂ imbalance in mouse model

LV Xiao-hua, WU Tie, WANG Hui, QIN Dong-yun

2006, 11(5):  532-534. 

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AIM: To explore the effect of liquorice on airway inflammation and Th₁/Th₂ imbalance in chronic asthma.METHODS: The chronic asthma model was es-tablished by intraperitoneal ovalbumin.The effect of liquorice on mice model of chronic bronchial asthma was observed, and the levels of serum IFN-γand IL-4 were tested by ELISA.RESULTS: Decreasing inflammatary cells infiltration in pulmonary tissue slices of tiny bronchi-al wall together with increasing serum IFN-γand decreas-ing serum IL-4 levels.CONCLUSION: Liquorice can adjust Th₁/Th₂ imbalance and inhibit the airway inflam-mation.

Effects of fenofibrate on proliferation and apoptosis induced by lysophos-phatidylcholine in cultured human umbilical vein endothelial cells

SUN Guo-ju, XIE Xiu-mei, XING Ying, YANG Tian-lun, YU Guo-long

2006, 11(5):  535-539. 

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AIM: To investigate the effect of fenofi-brate on proliferation and apoptosis induced by lysophos-phatidylcholine(LPC) in cultured human umbilical vein endothelial cells (HUVECs) and itsmechanism.METHODS: HUVECs were cultured in vitro.The study was designated to 5 groups:normal control;group LPC;low-concentration fenofibrate(10 μmol·L^-1) group;middle-concentration fenofibrate (50μmol·L^-1) group;high-con-centration fenofibrate(100 μmol·L^-1) group.Proliferation and apoptosis of HUVECs were evaluated by MTT assay, flow cytometry (FCM) and fluorescence microscopy.The expression of XIAP proteinwas examined by immunohisto-chemistry method.RESULTS: Compared with control group, LPC could inhibit the growth and induce apoptosis of HUVECs, and decrease the expression of XIAP protein in HUVECs.Fenofibrate could increase the growth and decrease the apoptosis of HUVECs, and enhance the ex-pression of XIAP protein in HUVECs.CONCLUSION: Fenofibrate can improve proliferation and apoptosis in-duced by lysophosphatidylcholine in HUVECs by enhanc-ing expression of XIAP protein.

Effects of proliferation inhibition and apoptosis of resveratrol trinicotinate on HepG2 cells and its mechanism

FAN Hui-ting, XIONG Xiao-yun, CAO Wei, GAO Zhong-bao, LI Xiao-qiang, JIA Min, MEI Qi-bing

2006, 11(5):  540-544. 

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AIM: To study the effects of resveratrol trinocotinate(ResT), a structure modification compound on the basis of resveratrol, on proliferation inhibition and apoptosis in HepG2 cell line.METHODS: HepG2 cell were cultivated with different concentration of ResT at the different time in vitro.The proliferation inhibition was measured by MTT assay.Hochest staining method was used to determine the apoptosis, and then FCM was used to analyzed the cell cycle distribution and apoptosis rate, Colorimetric assay wasemployed to detect the activation of Caspase-3.RESULTS: ResT caused growth inhibition in a time and dose-dependent manner.After treatment with ResT for 24 h, some cells appeared apoptotic characteris-tics.The flow cytometric profiles revealed that ResT in-duced cell into G₁ -phase and cells in S-phase were de-creased, Apoptotic peaks were observed in the cell cycle analysis.The apoptosis rates were 8.7%, 21.1% and 32.7% respectively after treatment for 12, 24, 48 h. Caspase-3was also activated.CONCLUSION: Induction of apoptosis and G₁ -phase cell cycle arrest may be respon-sible for the growth inhibition effect of ResT in HepG2 cell.

Effect of three extracts of Fufang Dihuang decoction on relaxation of mes-entery artery in streptozotocin-induced diabetic rats

LIU Hao-ran, XIA Hui-jing, DAI De-zai

2006, 11(5):  545-549. 

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AIM: To investigate the effects of three extracts of Fufang Dihuang decoction on the relaxation of mesentery artery in streptozotocin(STZ)-induced diabetic rats.METHODS: Diabetic rat model was induced by i. p injection STZ at a dosage of 60 mg·kg^-1.30 d later, 95%ethanol, 70%ethanol or water extract of Radix Re-hmanniae was p.o administrated for 30 d at the dosage of 107.8, 154.7 and 56.8 mg·kg^-1, respectively.On the 60th day, the responses of mesentery artery were deter-mined in the absence or presence of L-argine (L-Arg), N-Nitro-L-argine (NLA) and Indomethacin (Ind).RESULTS: The relaxation of mesentery artery of diabetic rat was diminished compared with the normal control.The basal release of NO and the L-argine-induced release of NO decreased 64.6%, 77.6% respectively in diabetic group compared with the normal control, with the de-creased proportion of NO in the endothelium dependent relaxation.95% and 70 %ethanol extract of Fufang Di-huang decoction ameliorated the impaired release of NO in rat' s mesentery artery.CONCLUSION: Abnormal re-laxation of mesentery artery in diabetic rat may be due to the decreased releasing of NO.The extracts of Fufang Di-huang decoction can protect the endothelium cells and im-prove the relaxation of mesentery artery, among them 70%ethanol extract exert the best potency, followed by 95%ethanol extract.And the water extract has a poor ef-fect.

Effects of Zhengan Xifeng decoction on angiotensin and endothelin of spontaneously hypertensive rats

MENG Yun-hui, WU Yan-xia, TU Xin, TU Jin-wen

2006, 11(5):  550-553. 

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AIM: To observe the effects of Zhengan Xifeng decoction on blood pressure, concentrations of an-giotensin II and endothelin in the plasma, myocardium and brain of spontaneously hypertensive rats (SHR). METHODS: Twenty-four male SHR of fourteen weeks old were divided into three groups at random:SHR group, Zhengan Xifeng decoction group, enalapril group, compared with control group with eight congeneric male Wistar-Kyoto(WKY).After eight weeks, rat blood pres-sure was measured by a sixteen leads physiologic record system.Concentrations of angiotensin and endothelin in plasma, myocardium and brain were detected by radioim-munoassay.RESULTS: Compared with the control group, blood pressure of SHR was elevated while concen-trations of angiotensin in plasma, myocardium and endo-thelin in rat brain were increased significently.Zhengan Xifeng decoction could decrease the concentrations of an-giotensin in plasma, myocardium and endothelin in brain. CONCLUSION: Zhengan Xifeng decoction can protect the myocardium and brain by reducing the release of vaso-constricting materia to prevent complications of hyperten-sion.

Inhibition of multidrug-resistant tumor cells induced by fraction CⅡ from naja naja atra venom

ZUO Chang-qing, LIN Zhen-tao, KONG Tian-han, WU Tie

2006, 11(5):  554-557. 

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AIM:To investigate the inhibition of frac-tion C Ⅱ from naja naja actra venom(FC ⅡNNAV)on multidrug-resistant tumor cell lines KBv200 and K562 A02.METHODS: Cytotoxicities of FC ⅡNNAV on KB、 KBv200、K562 and K562/A02 cells were measured by MTT assay.And the apoptosis induced by FC ⅡNNAV on K562/A02 cells were observed by DNA Ladder and flow cytometry (FCM).RESULTS: FC ⅡNNAV had the in-hibitory effects on KB 、KBv200、K562 and K562/A02 cells.The IC₅₀ were 0.87 ±0.15、1.07 ±0.08、0.67 ± 0.11 and 0.75±0.01 μg·ml^-1, respectively.It was obvi-ous that FC ⅡNNAV could induce cell apoptosis of K562 A02.CONCLUSION: FCⅡNNAV has the inhibitory ef-fect on KB、KBv200、K562 and K562/A02 cells.FC Ⅱ NNAV can induce apoptosis on multidrug-resistant tumor cell, which may be one of mechanisms for circumventing tumor multidrug-resistant.

Bioequivalence of lansoprazole enterosoluble tablets and capsules in healthy volunteers

LI Jian-chun, HU Qi-sheng, GAO Shu, JIANG Zhi-wen

2006, 11(5):  558-561. 

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AIM: To investigate the bioequivalence of lansoprazole enterosoluble tablets and capsules in Chi-nese healthy volunteers.METHODS: Twenty volunteers were randomly divided into two groups (test and refer-ence), with double cross over design.The concentration of lansoprazole in serum was determined by HPLC and pharmacokinetic parameters were calculatedwith DAS 2.0 practical pharmacokinetics program.RESULTS: The pharmacokinetic parameters of lansoprazole enterosoluble tablets and capsules were as follows:t_1/2 were 1.808 ± 1.031 and 1.341 ±0.498 h, C_max were 0.764 ±0.385 and 0.902 ±0.369 μg·ml^-1, T_max were 3.639 ±0.744 and 2.500±1.000 h, AUC 0-10h were 3.024±1.941 and 3.098±1.742 μg·h·ml^-1。 The relative bioavalibility of lansoprazole enterosoluble tablets was 109.57% ± 59.48%. CONCLUSION: The statistical analysis showed that the test and reference preparation were bio-equivalent.

Effects of propofol and isoflurane on general brain ischemia-reperfusion injury in rats

WANG Shi-lei, WANG Shi-duan, LI Yu, LIU Chuang-sheng, PAN Wei-ming, ZHANG Lin

2006, 11(5):  562-564. 

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AIM: To explore the effects of propofol and isoflurane on total cerebral ischemia-reperfusion inju-ry of rats.METHODS: Male SD rats were randomly di-vided into two grougs (n =14), which were respectively anesthetized with propofol and isoflurane under mechani-cal ventilation.Global cerebral ischemia was induced by occlusions of bilateral common carotid and vertebral arter-ies (four vessels).Each group was divided into two sub-groups according to reperfusion time:30 min for detecting MDA and SOD in brain tissues and 3 d for detecting sur-vived CA1 Cells of hippocampus.RESULTS: The cont-ents of MDA was more after 30 min reperfusion in isoflu-rane group than that in propofol group (P<0.01), whereas the activities of SOD was higher in propofol group than that in isoflurane group(P<0.01).There were more survived neurons in CA1 after 3 day reperfusion in propofol group than in isoflurane group(P<0.05). CONCLUSION: Propofol has stronger protection effect in general brain ischemia-reperfusion injury, the mecha-nism is associated with the activity of oxide free radical.

Effects of xy9902 a centchroman derivative on proliferation of MCF-7 cells

HOU Jin, XIONG Xiao-yun, MI Man, WANG Jie-pin, LIU Li, MEI Qi-bing

2006, 11(5):  565-568. 

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AIM: To investigate the effects of xy9902 on the proliferation in MCF-7 cells and its mechanism. METHODS: Effects of xy9902 on the proliferation of MCF-7 cellswere determined by MTT measurement.Cell cycle was examined by flow cytometry.Competitive estro-gen-receptor binding assay was used to investigate the af-finity of xy9902 to ER.RESULTS: xy9902 induced cell proliferation of MCF-7 cells at a lower concentration with an increase of the number of cells in S phase.On the contrary, inhibited cell proliferation at higher concentra-tionswith a decrease of the number of cells in S phase. Tamoxifen could block the stimulation of proliferation ef-fect of MCF-7 induced by xy9902.The relative binding affinity of xy9906 for ERαand ERβ showed an IC₅₀ of 8.45 ×10^-6 and 1.66 ×10^-6 mol·L^-1 respectively. CONCLUSION: xy9902 directly stimulates cell prolifer-ation of MCF-7 cells through ligand-receptor binding at a low concentrations and inhibits cell proliferation at high concentrations.

A simple method for determining content of nicotine in blood of rats ex-posed in burning cigarette smoke or nicotine fog

CHEN Yan, YUAN Shou-jun, LI Zheng-qiang, TIAN Zeng-yue, XU Lan-ping

2006, 11(5):  569-573. 

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AIM: To investigate the method of mea-suring the content of nicotine in the blood of rats exposed in burning cigarette smoke or nicotine fog.METHODS: The potassium cyanide-barbituric acid method for deter-mining cotinine, the metabolite of nicotine, in the urine of rats was evaluated.The nicotine solutions of various concentrations were infused to rats through tail vein with stable rate for one hour to make the standard curve of nic-otine in the blood of rats.Then, the total urine of 60 h was collected and the content of cotinine in the urine was measured as the output of nicotine from rats.The standard curve was established between the standard control of nic-otine and the output of cotinine.The ratswere exposed to the box filled with burning cigarette smoke or nicotine fog for 1 h, the total urine of 60 h was collected and the cont-ent of cotinine in the urine was measured, and the ab-sorbed content of cotinine in the blood of rats was calcu-lated according to standard curve equation, respectively. RESULTS: The standard control of nicotine and the out-put of nicotine in rat had a well linear relation, and the absorbed content of nicotine in the blood of rats could be estimated according to the output of the cotinine.CONCLUSION: The potassium cyanide-barbituric acid meth-od for determining cotinine in rat urine is consistent with the pharmacokinetical research.

Regulatory effect of puerarin on lipid profile in hypercholesterolemic rats

YAN Li-ping, CHEN Shun-hong, CHEN Wei-min, CHEN Shi-lin, MA Xiao-jun, XU Hong-xi

2006, 11(5):  574-577. 

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AIM: To investigate the regulatory effect of puerarin on lipid profile in diet-induced hypercholester-olemic rats and elucidate the mechanisms involved. METHODS: SD rats were randomly divided into the control group, hypercholesterolemia group and puerarin-treated group.The hypercholesterolemia group and puera-rin-treated group were given diet rich in cholesterol.In the meantime, the puerarin-treated group was orally ad-ministrated with puerarin (300 mg·kg^-1 ·d^-1).The lipid profile was investigated by the content of serum TC, TG, HDL-c and LDL-c.The mRNA levels of 7α-hydroxylase (CYP7A1), 3-hydroxy-3-methylglutaryl-CoA reductase (HMGR)and lanosterol 14α-demethylase (CYP51)were analyzed by real time RT-PCR.RESULTS: Puerarin markedly attenuated the increased serum total cholesterol induced by hypercholesterolemic diet.It caused a signifi-cant reduction in the atherogenic index.Expression of mRNA of CYP7A1 was significantly enhanced but not for those of HMGRand CYP51.CONCLUSION: These da-ta indicate that puerarin can reduce the atherogenic prop-erties of dietary cholesterol in rats.Its hypocholester-olemic function may be due to promoting the conversion of cholesterol into bile acids.

Determination of cefathiamidine in dogs HPLC and its pharmacokinetics

LU Cheng-yu, XU Wei-ming, CHEN Fang, ZHANG Xiao-na, WU Tie

2006, 11(5):  578-581. 

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AIM: To develop a method for the determination of cefathiamidine in dog plasma and to study the pharmacokinetic characters following intravenous injection of cefathiamidine at varied doses (31.5, 63.0, 126. mg·kg^-1 ) in dogs.METHODS: The concentrations of cefathiamidine in the plasma of dogs were determined by RT-HPLC.The determination has been performed on C₁₈ column(Hypersil, 250 mm×4.0 mm, 5 μm ) with acetonitrile :phosphatic buffer (20 ∶80, v v ) as mobile phase.RESULTS: The method has good linearity between 0.2 -50.0 μg·ml^-1 (r >0.999) with a limit of quantitation of 0.2 μg·ml^-1.Recovery varied from 93.27 % -102.18 %.Pharmacokinetics of cefathiamidine could be described by the two compartment open models.The main pharmacokinetic parameters of cefathiamidine were as follows :T1/2αwere 0.11 ±0.05, 0.13 ± 0.03, 0.10 ±0.03 h;T1/2β were 1.01 ±0.29, 0.84 ± 0.17, 1.08 ±0.31 h;AUC were 14.3 ±1.2, 27.3 ± 7.7, 74.4 ±21.2 mg·L^-1·h.CONCLUSION: The method can be used in pharmacokinetics of cefathiamidine and provided evidence for clinical application.

Influence of Yinxingdamo injection and Shuxuening injection on hemorhe-ology and plasma levels of superoxide dismutase, malondialdehyde and ni-trogen monoxidum in aged rats

LU Hua, LUAN Jia-jie, SONG Jian-guo

2006, 11(5):  582-585. 

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AIM: To compare Yinxingdamo injection with Shuxuening injection on hemorheology and plasma levels of superoxide dismutase (SOD), malondialdehyde (MDA) and nitrogen monoxidum (NO) in aged rats. METHODS: 24 aged rats were randomly divided into 4 groups:control, Yinxingdamo group, Shuxuening group and dipyridamole group.The ratswere givenNS, Yinxing-damo injection, Shuxuening injection and dipyridamole, respectively.The administration dosages were 2 ml·kg^-1, once everyday for 7 d successively.Another six normal young rats were arrayed into normal control.Hemorheolo-gy and plasma levels of SOD, MDA and NO were mea-sured.RESULTS: After intraperitoneal injection of Yinxingdamo for 7 days, the level of SOD in plasma of aged rats increased (P<0.05) and the level of MDA de-creased (P<0.01), the whole blood viscosity (at high shear rate) and contents of fibrinogen decreased (P<0.05) compared with those of control group.The level of SOD in plasma of aged rats increased obviously (P<0.05), the whole blood viscosity (at high or lower shear rate) and content of fibrinogen decreased (P<0.05) in Shuxuening group compared with those in control group. After intraperitoneal injection of dipyridamole injection, content of fibrinogen decreased (P<0.01) and index of red blood cell deformation increased (P<0.05) com-pared with those of control group.Plasma NO contents showed a tendency to decrease, but there was no signifi-cant statistical difference between either two groups. There was also no obvious difference on hemorheology and levels of SOD, MDA andNO in plasma between Yinxing-damo group and Shuxuening group (P >0.05).CONCLUSION: Changes of hemorheology in aged rats can be improved with Yinxingdamo or Shuxuening, the level of SOD increases and the level of MDA decreases.The re-sults suggest that the two drugs have effects of anti-aging, anti-oxidation, dilating coronary vessels and cerebral ves-sels and improving the symptom of cerebral ischemia, which may be the pharmacological foundation of prevent-ing and treating high-incidence diseases among aged peo-ple of these two drugs.

Study on absorption and distribution of oxybutynin oral tablet and transdermal gel in rats

WEN Qing, FENG Kun, GUO Rui-chen

2006, 11(5):  586-589. 

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AIM: To study the absorption and distri-bution characteristics of oxybutynin (OXY) oral tablet and transdermal gel.METHODS: A single dose of 0.1 g OXY transdermal gel (2mg OXY) was applied to abdom-inal area about 4 cm² and 0.5mg immediate-release tablet was orally given to 48 rats in a randomized, open-label, control design test.The plasma, bladder and liver tissue were collected, disposed and analyzed and OXY pharma-cokinetic parameters were calculated and evaluated.RESULTS: The C_max of OXY transdermal gel and oral table-ts in bladder are approximately 800 and 70 times higher than those in plasma.The plasma half life of OXY gel de-layed 5.99 h, tablets 2.18 h.CONCLUSION: OXY gel show better pharmacokinetic properties, characterized with long half life and high target organ concentrations than those of tablets.

Prophylactic and therapeutic effects of Mugua Pill on adjuvant-induced arthritis in rats

BING Fei-hong, ZHANG Guo-bin, DENG Cheng-zhi, SU Yan-qi

2006, 11(5):  590-592. 

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AIM: To investigate the prophylactic and therapeutic effects of MuGua Pill on Freund' s adjuvant-induced arthritis in rats.METHODS: The rat adjuvant-induced arthritis model was established, and the effect of MuGua Pill in the rats were studied.RESULTS: The medicine aimed at primary prevention could obviously control local inflammation, re-swell on d 8 and another paw swelling.The medicine aimed at the secondary pre-vention could control paw swelling and relieve the inflam-mation on limb and tail.CONCLUSION: MuGua Pill has significant prophylactic and therapeutic effects on ad-juvant-induced arthritis in rats.

Therapeutic effect of treatment with surgery and mifepristone in patients with endometriosis

ZHANG Hui-zhen

2006, 11(5):  593-595. 

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AIM: To evaluate the therapeutic effect of treatment with surgery and mifepristone in patients with endometriosis.METHODS: The medical records of 126 endometriosis patients undergoing surgical operation were analyzed retrospectively.There were 28 cases in stage Ⅰ or Ⅱ, 73 cases in stage Ⅲ, and 25 cases in stage Ⅳ. Conservative surgery was performed in 96 cases and semi-conservative surgery in 30 cases.Postoperation, 92 cases continued taking 10 mg·d^-1 of mifepristone for 6 months and 34 cases did not.All patients received 3 to 5 years follow up.RESULTS: The complete remission (CR) rate in mifepristone group was 77.2%, partial remission (PR) rate was22.8%, and recurrence rate was16.3%. The CR of controls was 52.9%, PR was 47.1%, and recurrence rate was 32.4%.There was significant differ-ence between two groups (P<0.05).The side effect of mifepristone occurred in 17.4% of all patients, but it eliminated the remained lesions in 89.1%of all patients. The levels of estradiol, progestin and CA125 in serum from pretreatment or recurrent patients were significantly higher than the patientswith posttreatment of mifepristone (P<0.05).CONCLUSION: Surgery is the principal method for treating endometriosis.Taking mifepristone can improve the prognosis, and decrease the recurrence rate, and maintain the serum markers at normal levels.

Application of SAS window in randomization of multi-center clinical trial

CAO Bo, ZOU Jian-dong

2006, 11(5):  596-600. 

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To meet the needs of randomization in multi-center clinical trial, a window in SAS by using the macro and %window program was designed.The results can be obtained automatically when the necessary parame-ters for randomization are filled in the right positions.The method has commonly usage.