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    药物研究
  • 药物研究
    Development of Paeonol Purity Reference Material and Method of Valuation
    XU Weisheng;YANG Dezhi;ZHANG Li;YANG Ning;MA Chen;LU Yang
    2011, 30(02): 143-148.
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    ObjectiveTo develop the paeonol purity reference material which has measurement traceability and high accuracy, and establish an effective method of valuation. MethodsThe paeonol purity reference material was studied on the basis of National Standard Material technical specification requirements. The homogeneity and stability test were measured by HPLC. The purity and uncertainty evaluation of the substance was measured by the peak area normalization method of HPLC and coulometry method. ResultsThe paeonol purity reference material developed in this study conforms to the technical requirements of national primary standard reference material. The purity value and uncertainty evaluation of paeonol was （99.87±0.35）% (k = 2, P= 0.95). ConclusionThe method established in our study was proved to be rapid, accurate and reliable, and was successfully applied to the purity value and uncertainty evaluation of paeonol purity reference material. It can provide the characteristic value transfer function.
  • 药物研究
    Purification of Pharmacological Active Parts in Smilax china L.
    HU Liling;LIAO Jing;YU Lixiu;HUA Xiaoli;CHEN Dongsheng
    2011, 30(02): 148-152.
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    ObjectiveTo find out the best process for purification of pharmacological active parts from Smilax china L. with macroporous adsorptive resins and biochemical integrity. MethodsD101 macroporous adsorptive resin was used to purify compounds and the corresponding chromatogram maps were set up with DADHPLC according to the content of total steroidal saponins. ResultsThe best procedure was that eluted the compounds with distilled water and 3BV 30% ethanol to eliminate the impurities, collected the 4BV 70% ethanol eluent to gain the steroid saponins and wash the resin with 95% ethanol at last. ConclusionThe purified substances obtained from this process are with high purity and good biochemical integrity.
  • 药物研究
    Effects of Recombinant Human Erythropoietin on Apoptosis and Mitofusin 2 Protein Expression in Rat Myocardium after Acute Myocardial Infarction
    SUN Yu;TU Zhiye;MI Tao;WANG Ying;ZHAO Jinping;CAO Wenjing;CHEN Lili;GUO Xiaomei
    2011, 30(02): 152-157.
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    ObjectiveTo investigate the effects of recombinant human erythropoietin (rHuEPO) at different doses on myocardial apoptosis and Mfn2 protein expression in rats with myocardial infarction. MethodsA total of 64 adult SpragueDawley rats were used and divided randomly into 4 groups: myocardial infarction (MI) rats, which were treated with 5 000 U•kg-1 loading dose followed by a maintenance dose of 1 500 U•kg-1 for 1 week of rHuEPO (MITH) ( high dose ), and low dose of MITL(a loading dose followed by a maintenance dose of 750 U•kg-1 for 1 week), respectively, and sham eperated rats. Twentyfour hours and 2 weeks after operation, myocardial apoptosis was assessed by in situ terminal deoxynucleotidyl transferase(TdT)dUTP nickend labeling (TUNEL staining) and Mfn2 protein expression was measured with immunohistochemistry staining. ResultsTwentyfour hours after operation, apoptosis index (AI) in sham operated, MI, MITH and MITL rats was 0, （60.99±5.28）,（36.97±2.68） and （38.10±3.41）, respectively; mean optical density (MOD) of Mfn2 protein in four groups was （0.080 6±0.0134）, （0.295 2±0.024 9）, （0.125 3±0.020 9） and （0.120 2±0.019 7）, respectively. Two weeks after operation, AI in sham operated, MI, MITH and MITL rats was 0, （50.08±8.00）, （26.54±2.97） and （24.16±3.74）; MOD of Mfn2 protein in four groups was （0.095 3±0.007 3）, （0.247 3±0.019 1）, （0.146 1±0.012 6） and （0.154 2±0.010 6）. Twentyfour hours and 2 weeks after operation, AI and Mfn2 protein expression in MI rats were remarkably increased in comparison with sham rats (P＜0.05), and those in MITH rats were significantly decreased in comparison with MI rats (P＜0.05). There was no significant difference in apoptosis and Mfn2 protein expression between MITH group and MITL group (P＞0.05). ConclusionImmediately loading dose followed by a maintenance (one week) lower dose of rHuEPO can significantly reduce apoptosis and mitofusin 2 protein expression in rat myocardium after acute myocardial infarction. No significant difference in the effects by rHuEPO on Mfn2 protein expression and apoptosis was observed between high and low dose maintenance treatments.
  • 药物研究
    The Antiangiogenesis Activity of Fraction K Purified from Guangxi Agkitrodon Acutus Venom
    LI Yingxin;LI Jianjun;ZHOU Xianli;LEI Danqing
    2011, 30(02): 157-160.
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    ObjectiveTo study the antiangiogenesis effect of fraction K from Guangxi Agkitrodon Acutus venom. MethodsThe inhibitory effects of fraction K against endothelial cell line ECV304 in vitro was measured by MTT, adhesion of ECV304 cells to fibronectin（FN）cell by fraction K was observed. The antiangiogenesis effect in vivo was evaluated by chick embryo chorioallantoic membrane （CAM）assay. ResultsThe proliferation of endothelial cell line ECV304 was inhibited significantly by fraction K in a time and dose dependent manner. Fraction K also inhibited endothelial cell adhesion to FN and tubule formation in CAM. ConclusionFraction K has an antiangiogenesis activity.
  • 药物研究
    Effect of Diterpenoid Curcumrinol C from Ether Extract of Curcuma Wenyujin on Proliferation of Human Colon Cancer Cells SW620
    JIN Haifeng;LV Bin;CHEN Zhe;ZHANG Shuo;MA Zhongjun
    2011, 30(02): 160-163.
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    ObjectiveTo investigate the effect of diterpenoid curcumrinol C from ether extract of curcuma wenyujin (compound C) on cell growth, apoptosis and cell cycle of human colon cancer cell line SW620 in vitro. MethodsThe human colon carcinoma cell SW620 were cultured and treated with the compound C at different concentrations compared with cisplatin(DDP) . MTT assay was used to test dynamically the cell growth inhibiting effect of curcumrinol C. Apoptosis induction (AnnexinVFITC/PI) and modulation of DNA cell cycle was detected by flow cytometry (FCM). ResultsIC50 value of the compound C and DDP were 24.16 and 45.80 μg•mL1, respectively. It was shown that the compound C at a low dose had similar effects to the positive control, obvious difference was developed in compound C at 30，50， 70 μg•mL1（P＜0.05）. The compound C induced SW620 cells apoptosis in a dose and time dependent manner, with inhibition percentage of 33.55% at the dose of 70 μg•mL1 for 48 h by FCM.The cell cycle was arrested at phase G1 treated by compound C and the ratio of cancer cells at phase S and G2/M was dropped. ConclusionThe compound C induces cell line SW620 apoptosis, blocks cell cycle and inhibits cell proliferation, which is one of the active antitumor components in curcuma wenyujin .
  • 药物研究
    Comparing Study of the Effects of Smilax sieboldii Miq., Clematis chinensis Osbeck. and C. hexapetela Pall on Cellular Immunity and Humoral Immunity
    SHI Qiang
    2011, 30(02): 163-166.
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    ObjectiveTo compare the effects of Smilax sieboldii Miq., Clematis chinensis Osbeck.and C. hexapetela Pall on cellular and humoral immunity, and further determine the feasibility of Smilax sieboldii Miq. to be used as a drug. MethodsThree cellular immune indexes including the formation rate of erythrocyte rosette, amount of T cell subsets and effects on delayed type hypersensitivity; two humoral immnue ones including the number of plaque forming cell (PFC) and amount of serum hemolysin were compared. ResultsAll of Smilax sieboldii Miq., Clematis chinensis Osbeck. and C. hexapetela Pall decoction were able to inhibit the activity of Tlymphocyte and reduce the humoral immune function. ConclusionSmilax sieboldii Miq.can be used equivalently as Clematis chinensis Osbeck. for the treatment of rheumatism.
  • 药物研究
    Effect of CES2 in Rat Liver and Intestines on the Site-specific Metabolism of Irinotecan
    LIU Dong;ZHANG Chengliang;XIANG Daochun;XU Yanjiao
    2011, 30(02): 166-170.
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    ObjectiveTo investigate the expression of carboxylesterases isoenzymes(CES2)in rat liver and intestines，and study its hydrolytic activity to irinotecan (CPT11). MethodsCPT11 was incubated with S9 fractions of rat liver and intestinal tissues and the sitespecific hydrolytic activity of CES2 was determined by the formation rate of metabolite SN38. Furthermore，the mRNA expression of CES2 was detected by realtime fluorescent quantitative reverse transcriptionpolymerase chain reaction (RTPCR). ResultsThe results obtained from the formation of SN38 showed a sitespecific degradation in rat liver and intestine homogenates. Hydrolysis of CPT11 in homogenates from intestine homogenates was low compared to that from liver homogenates. Segmental difference in intestine was observed in the degradation of CPT11as: duodenum＞jejunum＞ileum＞colon. The mRNA expression levels for the CES2 isozymes AB010635 and AY034877 also indicated that rat liver possessed much higher CES2 activity than intestines，with a gradual decrease of CES2 activity existed along the intestine. ConclusionCPT11 undergoes conversion to its metabolite in rat liver and intestine S9 fractions，and there is tissue variability in the extent of SN38 formation，which is associated with the sitespecific distribution of CES2 in these tissues. The results provide a basis for the strategies preventing side effects of CPT11 via CESs inhibition.
  • 药物研究
    Effects of LNMMA on Albumin Permeability of Isolated Rat Glomeruli
    ZOU Minshu;YU Jian;NIE Guoming;HE Weixun
    2011, 30(02): 170-173.
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    ObjectiveTo investigate the effect and potential mechanism of nitric oxide (NO) synthase inhibitior on albumin permeability (Palb) of isolated rat glomeruli. MethodsGlomeruli of normal male SpragueDawley rats was isolated with the standard sieve. Palb was calculated by measuring the volume change of isolated glomeruli by using videomicroscopy. Isolated rat glomeruli were incubated with various concentrations of NGmonomethylLarginine (LNMMA) (0.5, 1.0, 2.0 mmol•L-1) for 30 min, with 2.0 mmol•L-1 LNMMA for 15, 30, 45 min, respectively. Glomeruli were incubated with 2.0 mmol•L-1 LNMMA and 500 μmol•L-1 DETA NONOate for 45 min. Glomeruli were incubated with 2.0 mmol•L-1 LNMMA and 5 mmol•L-1 superoxide dismutase (SOD) for 45 min, and were observed for the change of Palb under different conditions. Results0.5 mmol•L-1 LNMMA had no obvious effect on Palb, whereas 1.0 mmol•L-1, 2.0 mmol•L-1 LNMMA casused a significant increase of Palb as compared to that of control group (P＜0.01). The effect of 2.0 mmol•L-1 of LNMMA on Palb increased further than that of 1.0 mmol•L-1. A significant increase in Palb was observed at concentration of 2.0 mmol•L-1 LNMMA incubated with glomeruli for 15, 30, 45 min (vs control, P＜0.01), respectively with incubated time lasting, Palb increased gradually. The maximal of Palb was obtained by incubation for 45 min . The increase of Palb was blocked in rat glomeruli with LNMMA and DETA NONOate for 45 min. Palb in rat glomeruli was not affected with 2.0 mmol•L-1 LNMMA and SOD. ConclusionNO is a regulatory factor in glomerular permeability to albumin, depletion of which resulting in an increase in Palb. The bioavailability of superoxide may be involved in the increases of Palb by NO synthase inhibitior.
  • 药物研究
    Effect of Domestic Cordycepin on NB4 Leukemia Cell Proliferation and Apoptosis
    WANG Yan;XIA Jun;ZHUO Guangchao;ZHU Hua
    2011, 30(02): 173-176.
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    ObjectiveTo investigate the effect of cordycepin on NB4 leukemia cell proliferation and apoptosis in vitro.MethodsNB4 cells were incubated with cordycepin （0.5, 1.0, 1.5, 2.0 mg•mL-1）. The cells growth was tested by cell counting and MTT assay after coculturing for 24，48，72 h. The apoptosis of NB4 cell was detected by cell morphology analysis, Hoechst 33258 fluorescence staining, DNA diploid content test and mitochondrial membrane protein assay. ResultsDifferent concentrations of cordycepin obviously inhibited the growth of NB4 cells in a time and dose dependent manner compared with the control. Apoptosis was significantly induced by different concentrations of cordycepin. ConclusionNB4 cells growth inhibition and apoptosis could obviously induced by cordycepin in vitro.
  • 药物研究
    Effects of Oleanolic Acid on Proliferation and Apoptosis of Human Colon Cancer LoVo Cell
    WU Zhen;WANG Qibin;CHEN Yongshun;TONG Qiang
    2011, 30(02): 176-180.
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    ObjectiveTo study the effects of oleanolic acid（OA） on proliferation and apoptosis of colon cancer LoVo cell lines in vitro. MethodsThe human colon cancer LoVo cells were treated with 2.00～32.00 mg•L1 OA for 12～96 h. The influence of OA on proliferation of LoVo cell in vitro was detected with MTT method. Cell apoptosis rate was determined by flow cytometry, and protein expressions of Bcl2, Bax, p53 and Caspase3 were investingated by Western blot analysis. The apoptosis was observed by electron microscopy. ResultsOA inhibited the proliferation of LoVo cells in a dose and time dependent way. It significantly induced apoptosis of LoVo cells and blocked cells at G2/M phase. The apoptosis rates were 10.32%～14.24% (P＜0.05) after 48 hours.With the increase of concentrateion of OA, the expressions of Bax, p53 and Caspase3 were increased, while the level Bcl2 protein was decreased. ConclusionOA induces apoptosis of colon cancer LoVo cell lines, which may be related to inhibition of Bcl2 and promotion overexpressing of Bax, p53 and Caspase3.
  • 药物研究
    Effects of Metoprolol on Left Ventricular Remodeling after Acute Myocardial Infarction
    WANG WeiNa;ZHAO Liangping;LI Bing
    2011, 30(02): 180-183.
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    ObjectiveTo investigate the effects and mechanism of metoprolol on left ventricular remodeling (LVR) after acute myocardial infarction(AMI) in rats. MethodsThe Wistar rats were randomly assigned to three groups: AMI control (n=9), metoprolol treatment (n=9) and shamoperated group (n=9). The rats of AMI control and metoprolol treatment were ligated in the left anterior descending coronary artery; the shamoperated rats were not ligated. The metoprolol group was given with metoprolol 10 mg•kg1•d1 , and the other two groups with the same dose of 0.9% natrium chloride. Four weeks later, the left ventricular enddiastolic dimension (LVDD), left ventricular enddiastolic volume (LEDV), left ventricular mass index (LVMI),ejection fraction (EF) and fractional shortening (FS) of each rat was detected by echocardiogram. Myocardial cell and interstitial tissue were observed by HE stain. ResultsCompared with those in the shamoperated group, the LVDD,LEDV and LVMI in AMI group were all significantly increased(P＜0.05). The parameters in AMI including EF and FS were all significantly alleviated (P＜0.05). Meanwhile, cardiac myocyte hypertrophy was found by HE stain. However, in metoprolol group, the EF and FS were improved in comparison to those in AMI group. ConclusionMetoprolol had a therapeutic effect on LVR after AMI，the mechanism of which should be associated with inhibiting sympathetic nerve hyperplasia and reforming anomalies of neuroendocrine and hemodynamics.
  • 药物研究
    Effects and Mechanism of Trimetazidine on Oxidative Stress in Rats with Chronic Heart Failure
    LI Jie
    2011, 30(02): 183-187.
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    ObjectiveTo investigate the effects of trimetazidine on the injury of oxidative stress in rats with chronic heart failure (CHF). MethodsMale SD rats were randomly divided into blank control, model, low trimetazidine treated and high trimetazidine treated groups. Rats except for the blank control were abdominal aortic constricted. Four weeks later, echocardiography, real time PCR, serological and myocardial pathological examination were performed, SOD in myocardium was determined. ResultsCompared with the model rats, both LVPW and LVD of the rats in high dose of trimetazidine treated group were raised. The microscopic and electron microscopic examination showed that the myocardial injury in high dose of trimetazidine treated group were ameliorated compared with those in the model. The level of SOD showed significant difference among groups（P＜0.05）. ConclusionTrimetazidine can improve antioxidance, pathological change and ultrastructure of myocardium and enhance the cardiac function in rats with heart failure.
  • 药物研究
    Effects of Nonephedrine Alkaloids of Ephedra sinica Stapf on Cholesterol in Mice
    WANG Jianjun;ZHOU Yunyun;FAN Yanbo
    2011, 30(02): 187-190.
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    ObjectiveTo investigate the effects of nonephedrine alkaloids on cholesterol in mice. MethodsMice were randomly divided into 5 groups: blank control group, model control group, positive control group, ephedra alkaloids group, nonephedrine alkaloids group. The mice except for blanks were fed with high fat diet for three weeks, resulting in a mouse model of hyperlipidemia. Intragastric administration of 6.7 mg•kg1simvastatin, 2 g•mL1 ephedra alkaloids and nonephedrine alkaloids was given continuously for 4 weeks, respectively, body weights were recorded weekly. Serum TC, TG, HDLC levels, and organ coefficient were determined. ResultsAfter 4 weeks’ administration .compared with the model control, nonephedrine alkaloids significantly reduced TC, TG levels in mice, increased HDLC levels; nonephedrine alkaloids reduced mouse liver, spleen, renal and epididymis fat coefficient at different degrees. ConclusionThe traditional Chinese medicine nonephedrine alkaloids in Ephedra sinica Stapf shows antagonistic effects on hyperlipidemia.
  • 药物研究
    Studies on Purificating Process of the Total Flavonoids of Polygonum Bistorta L.
    WANG Guiling;FANG Jianqiang;ZHAO Xuemei;WANG Song
    2011, 30(02): 190-193.
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    ObjectiveTo provide a reference to further development and ulitization of the total flavanoids of Polygonum bistorta L. . MethodsBy the static and dynamic adsorption experiments, six types of macroporous adsorption resins（D101,HPD100,HPD400,HPD500,HPD600,AB8） were evaluated and compared for the absorption and disaborption to find the optimum condition for the total flavanoids purification, and Rutin was used for the reference substance, 10%AlCl3 for the color reagent to determine the content of the total flavanoids of Polygonum bistorta L by UV-spectrophotometric method. ResultsThe HPD400 macroporous adsorption resin possessed optimum adsorption and elution parameters. The best technological conditions were adding 9.28 mg•mL-1 of sample with pH 3.0, being eluted with 2.9 multiple column volume of distilled water, 4.3 multiple column volume of 55% ethanol. The purified flavoniods was about 45% of total unpurified flavoniods. ConclusionThe HPD400 macroporous adsorption resin fits for purifying flavoniods from Polygonum bistorta L. . This method was simple, practicable and effective.
  • 药物研究
    Pharmacodynamic Study on Supercritical CO2 Extract from Fructus Litseae
    TANG Jie;WAN Jin;SHI Chunyang
    2011, 30(02): 193-196.
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    ObjectiveTo extract the volatile components from Fructus Litseae with a supercritical CO2 extraction technique and observe its pharmacodynamic activity. MethodsThe sensitivity of extracts from Fructus Litseae against Staphylococcus aureus and Pseudomonas aeruginosa was determined with an agar diffusion method. Its antiinflammation effect was studied by measuring capillary permeability induced by intraperitoneal injection with acetic acid, swelling of the pinna in mice induced by xylene. Its analgesia effect was investigated in the murine pain models induced by chemical and physical stimulations. ResultsThe bacteriostasis activity of the supercritical CO2 extracts from Fructus Litseae in vitro was confirmed. The extracts significantly inhibited two experimental animal inflammatory models and alleviated pain induced by acetic acid and fever. ConclusionIt is preferable and reasonable to extract volatile components from Fructus Litseae, the extract of which is shown to have remarkable activity.
  • 药物研究
    Overexpession of SATB1 Promotes Hepatoma Cell HepG2 Proliferation
    2011, 30(02): 196-199.
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    ObjectiveTo detect the effect of SATB1 on cell proliferation of hepatoma cell HepG2 . MethodsThe HepG2 cells were overexpessed SATB1 by being transfected with plasmids encoding for whole length of SATB1 gene, the mRNA and protein levels were measured by semiquantitative RTPCR and Western blot analysis. The cell proliferation was determined by MTT assay, cell cycle distribution was detected by flow cytometry. ResultsAfter SATB1 overexpressing, compared with the blank and control groups, SATB1mRNA and protein were increased significantly in HepG2, and cell growth was promoted, cell number in G0/G1 phase was decreased and that in S and G2/M phase was increased. ConclusionThe results showed that SATB1 overexpression promoted cell proliferation in HepG2 cell lines, and the mechanism of which may be associated with promoting DNA replication and transcription in cell phase.
  • 药物研究
    The Study of Adsorptive Properties of TSG from Polygonum Multiflorum Thunb. with Different Types of Macroporous Absorption Resin
    CAO Cheng;WANG Shuling;CHEN Fenglian;ZENG Yuaner;JIANG Danna
    2011, 30(02): 202-204.
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    ObjectiveTo optimize the macroporous adsorption resin for purification of water extract of Polygonum multiflorum Thunb.MethodsThe retention rate of 2, 3, 5, 4’ tetrahedroxystilbene2 OβDglucoside was used as the evaluation indicator, content of 2, 3, 5, 4’ tetrahedroxystilbene2 OβDglucoside from water extacts and eluents of Polygonum multiflorum Thunb. were determined by HPLC. Through the adsorption rate，elution rate and absorption efficiency to optimize the macroporous adsorption resin for purification of water extracts from Polygonum multiflorum Thunb. and study the adsorption equilibrium time of D101 macroporous absorption resin. ResultsDifferent types of macroporous resin for TSG of water extract from Polygonum multiflorum Thunb. were different. The D101 macroporous adsorption resin had the best separation performance and was the most suitable resin for purification of water extract of Polygonum multiflorum Thunb. The adsorption equilibrium time of TSG on D101 was 7 h. ConclusionThe D101 macroporous adsorption resin fits for isolation and purification of water extract from Polygonum multiflorum Thunb.
    • 药物与临床
  • 药物与临床
    Propofolsufentanil versus Propofolremifentanil as Total Intravenous Anesthesia for Neurosurgery
    BI Jiangjiang;LUO Ailin;FAN Longchang;JIANG Hui
    2011, 30(02): 210-213.
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    ObjectiveTo compare the efficacy and postoperative analgesia of either sufentanil or remifentanil combined with propofol as total intravenous anesthesia in patients undergoing nonemergency neurosurgery. Methods80 patients of ASA Class Ⅰ～Ⅱ who were scheduled for a neurosurgery were randomized into two groups: sufentanil(S) group and remifentanil(R) group. Anesthesia was induced with propofol and either sufentanil 0.25 μg•kg1 or remifentanil 1 μg•kg1. Infusion rate of propofol were 610 mg•kg1•h1 in both groups. Maintenance infusion rates for sufentanil and remifentanil were 0.002 5 μg•kg1•min1 and 0.1－0.2 μg•kg1•min1, respectively. Patients’ hemodynamic condition was monitored throughout the anesthesia procedure. And the awakening time, extubation time, postoperative complications,visual analogue scale（VAS）and tramadol consumption were recorded. ResultsThe awakening and extubation time in R group were significantly shorter than those in S group (6.4±2.5),(11.6±5.3)min vs(12.6±6.4),(16.2±7.4)min(P＜0.05). Side effects in both groups showed no significant difference within 6 h after extubation.Tramadol consumption for postoperative pain relief in R group was greater than in S group ［(557.6±54.3) mg］ vs ［(312.4±47.7) mg］（P＜0.05). VAS of 60,90,120 min postoperation in S group were lower than those in R group(P＜0.05). ConclusionTotal intravenous anesthesia by using either sufentanil or remifentanil in combination with propofol can be effectively applied in neurosurgery, with a faster awakening time by remifentanil and a satisfactory postoperative analgesia effect by sufentanil.
  • 药物与临床
    赵静，樊理华
    2011, 30(02): 213-215.
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