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• 01 May 2013 Volume 32 Issue 5

    

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  药物研究
  药物制剂与药品质量控制
  

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药物研究
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  药物研究

  In vitro Antioxidant Activity of Ethanol Extracts from Macrothelypteris oligophlebia

  WU Guanghua;SUN Minghui;WEI Han;RUAN Jinlan

  2013, 32(5): 558-561.

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  ObjectiveTo investigate the total flavonoid content and in vitro antioxidant ability of the ethanol extract from Macrothelypteris oligophlebia.MethodsThe content of total flavonoids was tested by using rutin as atandard product；antioxidant activity was measured by various established in vitro systems， including 2， 2’azinobis3ethylbenzothiazoline6sulphonic acid (ABTS)， superoxide anion， hydrogen peroxide and hydroxyl radicals.ResultsThe extract exhibited potent free radical scavenging activity in a dosedependent manner.The total flavonoid content was (28.23±0.18) mg.ConclusionThe ethanol extract posses apparent antioxidant property.
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  药物研究

  The Mechanism of Curcumin Inhibitting Breast Cell Proliferation and Migration

  CAI Shaoxin;CHEN Cheng;YANG Xi;LI Xiaolan;LI Zhaoming;HU Junbo

  2013, 32(5): 561-564.

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  To investigate the influence of curcumin on hypoxiainducible factor R1， α subunit (HIF1α) and cell proliferation and migration of the MDAMB453 cell line.MethodsThe effects of curcumin on MDAMB453 cell growth was studied by means of MTT and cell count assay， cell migration analysis was determined by a transwell assay.After cells were treated with curcumin under normoxia and hypoxia， the mRNA and protein levels of HIF1α were measured by Realtime PCR and Western blot， while the mRNA and protein levels of vascular endothelial growth factor (VEGF) were measured by Realtime PCR and ELISA， respectively.ResultsCurcumin inhibited cell growth and migration of the MDAMB453 cell line.Being treated with curcumin， either normoxia or hypoxia， the mRNA level of HIF1α was unchange， while the protein level of HIF1α was significantly decreased.Both the mRNA and protein levels of VEGF were obviously downregulated.ConclusionCurcumin regulates the proliferation and migration of MDAMB453 cells through HIF1α.
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  药物研究

  The Effect of Alcohol Extracts from Caulis Sinomenii on Articular Bone Destruction of Rats with Arthritis

  ZHANG Mengying;GE Weihong;YAO Yao

  2013, 32(5): 565-568.

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  ObjectiveTo investigate the effect of alcohol extracts from Caulis sinomenii on articular bone destruction of rats with collageninduced arthritis（CIA）， and preliminarily explore its mechanism of action.MethodsThe total of 32 female SD rats were randomly divided into the control and model groups， and the latter and the latter was randomly devided into model control and Caulis sinomenii groups.The Caulis sinomenii group was treated with alcohol extracts from Caulis sinomenii，while the model and control groups were treated with equal volume of saline solution.The feat of the articular score was observed every three days；the serum levels of IL17， RANKL and OPG were test by ELISA.The dead rats’ feet were taken for histopathologic slice and HE staining to detect the bone destruction.ResultsThe articular score of model group was significantly higher than that of the Caulis sinomenii group (P＜0.01)；IL17 level of three groups showed a statisticant difference （P＜0.05）， IL17 of the Caulis sinomenii group was remarkablly lower than that of the model group (P＜0.05)， but higher than that of the control group（P＜0.01）.The levels of RANKL，OPG and RANKL/OPG ratio of the three groups also showed obviously difference（P＜0.01）.The level of RANKL of Caulis sinomenii group was lower than that of the model group（P＜0.05）and the OPG significantly higher than that of the model group (P＜0.05).The RANKL/OPG ratio of the Caulis sinomenii group was fewer than that of the model group ，but more than that of the model group；the HE staining results showed that the extent of article bone destruction of Caulis sinomenii group was less severe than that of the model group.ConclusionCaulis sinomenii can inhibit articular bone destruction CIA rats’ by reducing the peripheral by reducing the peripheral serum of RANKL and IL17， elevating OPG level， downregulating RANKL/OPG ratio and thus inhibiting intraarticular osteoclastogenesis.
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  药物研究

  Antiinflammatory Effect of the Miao Traditional Medicine jinwu jiangu Decoction on Collageninduced Arthritis

  MA Wukai;YAO Xueming;HUANG Ying;LU Daomin;LONG Xiaoqin;TANG Fang;AN Yang;LIU Zhengqi;WANG Ying;ZHOU Jing

  2013, 32(5): 569-572.

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  ObjectiveTo study the influence of the jinwu jiangu decoction on the levels of TNF alpha， IL1 and IL1β in rats with collageninduced arthritis.MethodsA total of 60 female Wistar rats were randomly divided into normal control， model control， tripterygium glucosides positive control and jinwu jiangu decoction at high， medium and low dose groups.Collagen induced arthritis(CIA) was established in all groups but the normal control.The toes volume and the arthritis index were recorded；the level of serum tumor necrosis factor alpha (TNFα)、interleukin1 (IL1) and interleukin1β (IL1 β) was tested by ELISA .ResultsThe joint swelling and arthritis index in the high and medium dose groups of jinwu jiangu Decoction were lower than those in the tripterygium glucosides control group (P＜0.01 or P＜0.05）.The serum TNFα， IL1， IL1 β expression in the CIA model were higher than those of the model group but similar to the positive control group.Compared with the model group， serum TNFα， IL1and IL1β expression of high and medium dose groups decreased significantly， showing no significant difference from the tripterygium glucosides control group， except for IL1β (P＜0.01).ConclusionJinwu jiangu decoction could relieve ankle swelling， decrease arthritis index and downregulate serum TNFα， IL1 and IL1β expression of CIA rats.
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  The Effects of Scopolamine at Different Doses on Learning and Memory Function in Mice

  GAO Li;PENG Xiaoming;ZHANG Fuchun;HUO Shixia;LIN Juan;YAN Ming

  2013, 32(5): 573-576.

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  ObjectiveTo compare the effects of different doses of scopolamine on behavior，learning and memory function in mice and determine the appropriate dose of scopolamine for inducing memory impairment of mice model.MethodsThe total of 48 kunming mice were randomly divided into 4 groups (control group and three model groups， each containing 12 mice) were given with scopolamine by intraperitoneal injection at the doses of 2，3 and 5 mg•kg－1，and the same volume of saline， respectively.Learning and memory ability were investigated by avoidance reaction and the content and vitality of Ach， AChE and ChAT were determined by a spectrophotometric method.Results① The latency period of scopolamine at 3 mg•kg－1 dose and 5 mg•kg－1 dose was significantly reduced (P＜0.05)；②The vitality and content of AChE， ChAT and Ach in the brain of these mice were remarkably affected.Conclusion①The degree of damage of scopolamine to the behavior and memory of mice is increased with the dose；learning and memory behaviors in mice were significantly injury by 3 mg•kg－1 dose and 5 mg•kg－1 of mice ；② Scopolamine can significantly impact acetylcholine synthesis and metabolism in the cerebral cortex and hippocampus of mice at the doses of 3 mg•kg－1 and 5 mg•kg－1；③The appropriate dose of scopolamine on the behavior and memory function injury of mice is 3 mg•kg－1.
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  Comparation of Antioxidant Activity Between Total Flavonoids Isolated from Two Different Plants in vitro

  HUANG Qiujie;YE Yong;OU Xianhong;LIU Huagang;SONG Yunfei

  2013, 32(5): 576-578.

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  ObjectiveAntioxidation of total flavonoids from Ampelopsis grossedntata and Berchemia lineata(L.) DC was studied in vitro.MethodsScavenging effects of total flavonoids from Ampelopsis grossedntata and Berchemia lineata(L.) DC on DPPH free radical， hydroxyl free radical， and superoxide free radical were determined by ELISA.ResultsThe activity of total flavonoids from Ampelopsis grossedntata was the strongest，with the IC50 of three systems being （3.32±0.18）， （227.41±184.45），（5.22±3.75） mg•L－1 ，respectively， while the activity of total flavonoids from Berchemia lineata(L.) DC was the lowest， with the IC50 of DPPH•system being （36.41±9.68） mg•L－1.ConclusionThe total flavonoids from Ampelopsis grossedntata have strong antioxidant activity ，but the total flavonoids from Berchemia lineata(L.) DC could not be employed as antioxidant alone.
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  The Effect and Mechanism of Xuefu Zhuyu Decoction on the Rats with Atherosclerosis

  DONG Chao;HUANG Wei;YANG Yang;JI Pengxian;LIU Haoran;YAO Qi

  2013, 32(5): 579-582.

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  ObjectiveTo investigate the effect and mechanism of xuefu zhuyu decoction on rats with atherosclerosis.MethodsForty SD rats were randomly divided into the control， model， xuefu zhuyu and xuezhikang groups， with 10 rats in each.The group was fed with normal diet，the model was fed with high fat diet，while the treatment groups were fed with high fat diet and drugs.After 12 weeks， the rats were sacrificed.The expression of MMP2 protein in the endarterium of AS rats was detected by immunohistochemical technique.the level of hsCRP was detected by full automatic biochemical analyzer. the MCP1 was detected by ELISA method.ResultsThe level of MMP2， hsCRP and MCP1 increased significantly in the model group(P＜0.05) ， but decreased in the treatment group(P＜0.05) .ConclusionXuefu zhuyu decoction can improve elasticity of blood vessels and inhibit expression of inflammatory factor so as to prevent and treat atherosclerosis， the mechanism of which may be associtated with decreasing the expression of MMP2， hsCRP and MCP1.
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  药物研究

  Influence of Emodin on VEGFC and MMP9 of Mice with Colon Cancer

  ZHANG Yanxin;SONG Wengang;GAO Fenglan

  2013, 32(5): 583-585.

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  ObjectiveTo explore antitumor effect of emodin on nude mice with human colon cancer xenografts， and VEGFC and MMP9 expression.MethodsThe human colon cancer xenografts model in nude mice were established and the mice were randomly divided into 5 groups with 10 mice in each.The emodin group were injected daily with emodin at doses of 50，100 and 150 mg•kg－1， and the positive control group was injected daily with 5Fu at the dose of 20 mg•mg－1 while the positive control group was injected daily with normal saline.The tumor inhibition rate was observed and apoptosis index was detected by TUNEL， the expression of matrix metalloproteinase (MMP)9 and vascular endothelial growth factor (VEGF)C were investigated by immunohistochemical analysis.ResultsCompared with the model group，the tumor volume， tumor mass， tumor inhibition rate and apoptosis index of each dose group were significantly decreased(P＜0.05， P＜0.01)， and the expression of VEGFC and MMP9 was lowered at various degree.VEGFC expression in the medium and high dose of emodin group was significantly weaker（0.68±0.36），（0.22±0.41） than that in the model group（2.11±0.45）(P＜0.05， P＜0.01) and MMP9 expression（1.11±0.41），（0.38±0.44）was significantly lower than that in the model group（2.31±0.39） (P＜0.05， P＜0.01).ConclusionEmodin effectively inhibits tumor growth， the mechanism of which may be related to the induction of apoptosis and inhibition of VEGFC and MMP9 expression.
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  Antitumor and Immunoregulatory Activities of Indocalamus tessellatus Polysaccharides on the Tumorbearing Mice

  WANG Enjun;JI Wenqi;FAN Linlin;HU Yanan;JIN Yi;GUO Xiaojun;LI Shuna

  2013, 32(5): 586-589.

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  To explore the inhibitory action and its immunoregulatory mechanism of Indocalamus tessellatus polysaccharides on the transplantable mammary cancer mice.MethodsThree different doses (60，30 and 15 mg•kg－1)of Indocalamus tessellatus polysaccharides and the medium dose combining with cyclophosphamide were given to TA2 tumorbearing model mice in treatment groups， respectively.The index of spleen， lymphocyte transformation and the level of serum IL2 were determined.ResultsThe index of spleen， lymphocyte stimulation，and IL2 in serumwere significantly increased.ConclusionIndocalamus tessellatus polysaccharides display inhibitory action on the mice with transplantable mammary cancer and enhance their immune functions.Indocalamus tessellatus polysaccharides combined with CTX show more efficacy and less toxicity.
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  Heatclearing And Detoxifying Effects of Eupatorium chinense L.

  JIANG Yiping;XU Jiangping;HUANG Fang

  2013, 32(5): 589-592.

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  ObjectiveTo preliminary study the antipyretic and detoxifying effect of Eupatorium chinense L.MethodsThe antipyretic and detoxifying effects of Eupatorium chinense L.were demonstrated through experiments on auricle swelling induced by xylene in mice， immune insufficientcy induced by glucocorticoid in mice and fever induced by dry yeast in rats .ResultsEupatorium chinense L.inhibited ear swelling and the effect enhanced with the dose；Eupatorium Chinese L.improved the immune function in immunosuppressed mice and reduced the fever in rats， especially for which at the dose of 1 g•kg－1；Eupatorium Chinese L.1.5 g•kg－1 relieved fever induced by dried yeast.ConclusionEupatorium chinense L.presents antipyretic and detoxifying function.
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  Protective Effects of Extracts from Rhizoma Polygonatum on Acute Hepatic Injury in Mice

  ZHANG Guanghai;WANG Meng;LIU Yanan

  2013, 32(5): 593-595.

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  ObjectiveTo investigate the protective effects of extracts from Rhizoma polygonatum on acute hepatic injury in mice.MethodsThe model of CCl4induced acute hepatic injury was set up in mice，and the mice were treated with extracts from rhizoma polygonatum to determine the content of ALT and AST in serum and the levels of SOD and MDA in hepatic tissue and observe the pathological changes in the liver of mice.ResultsThe high，middle and low dose of extracts from Rhizoma polygonatum remarkably reduced the activities of ALT and AST in serum， compared with the control group (P＜0.05).Meanwhile，the high and middle dose group of extracts increased the level of SOD and reduced the content of MDA， compared to the control group (P＜0.05).ConclusionThe extracts from Rhizoma polygonatum reduce the content of ALT，AST and MDA，increase the activity of SOD，and show protective effects on acute hepatic injury in mice.
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  Protective Effect of Chaenomeles on Experimental Hepatic Injury in Mice

  CHEN Zhuang;XIAO Gang;QIN Honghan

  2013, 32(5): 596-599.

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  ObjectiveTo study the protective effect and mechanism of alcohol extracts of Chaenomeles on experimental hepatic injury in mice.MethodsAcute hepatic injury model was induced by injecting CCl4 in mice， and the immunological hepatic injury model was induced in mice by injecting bacilluscalmette guer in (BCG) and lipopolysaccharide ( LPS) .The activities of ALT and AST in serum， SOD and content of MDA in liver were investigated；and the histological changes of liver were observed.ResultsChaenomeles decreased the activities of ALT and AST in mice with acute hepatic injury and immunological hepatic injury， increased the activity of SOD but lowered MDA in liver of mice with immunological hepatic injury， and relieved the histological injury of liver(P＜0.01，P＜0.05).ConclusionChaenomeles has protective effect on acute and immunological hepatic injury in mice， the mechanisms of which may be related to its antioxidant activity.
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  药物研究

  The Effect of Betaglucan from Cell Wall of Candida albicans on Immunological Function in Mice

  NING Li;ZHANG Jingwei;WEI Dianjun

  2013, 32(5): 600-602.

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  ObjectiveTo study the effect of βglucan extracts from the cell wall of Candida albicans on immunosuppressive mice induced by cyclophosphamide (CTX).MethodsThe immunosuppressive model was established by intraperitoneal injection of CTX.Three kinds of βglucan were extracted from the cell wall of Candida albicans.The effects of βglucan on leukocytes were studied by cell counting and histopathological observation.ResultsCompared with the control group， three kinds of Candida albicans βglucan raised the number of leukocytes， neutrophilic granulocytes and monocytes in the peripheral blood.The spleen index in all groups was increased， and so was megakaryocyte in spleen and marrow.ConclusionCandida albicans βglucan， specially insoluble βglucans is a kind of promising immunomodulator that can increase the leukocyte counts in the peripheral blood.
药物制剂与药品质量控制
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  Determination of Dehydrodiisoeugenol from Uygur Medicine Arillus Myristicae by HPLC

  WANG Hangyu;WANG Shuyun;LI Guoyu;HUANG Jian;ZHANG Ke;ZHANG Xiuting;WANG Jinhui;

  2013, 32(5): 647-649.

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  ObjectiveTo establish a HPLC method for determining dehydrodiisoeugenol in Uygur Medicine Arillus Myristicae.MethodsThe analysis was performed on a SunFireTM C18 column (4.6 mm×150 mm， 5 μm) at 30 ℃ using methanol /water (65：35) system at a flow rate of 1.0 mL•min－1 and UV detection wavelength at 274 nm.ResultsThe linear range of dehydrodiisoeugenol was 0.060 16～12.032 μg(r=0.999 9).The average recovery rate was 98.39% with RSD1.68%.ConclusionThis method is accurate， convenient and reproducible for the determination of dehydrodiisoeugenol in Uygur Medicine Arillus Myristicae.
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  药物制剂与药品质量控制

  Determination of Five Main Free Amino Acids in Kangfuxin Liquid by HPLC

  ZHANG Li;LI Zhiyuan;LI Hui

  2013, 32(5): 650-652.

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  ObjectiveTo establish a quantitative method with dinitrofluorobenzene DNFB procolumn derivtization for determining the five main free amino acids in kangfuxin liquid by HPLC.MethodsContents of glycine， proline， alanine， valine， and leucine were determined in kangfuxin liquid by HPLC using DNFB as the derivatization reagent.The analysis was performed on EliteAAK C18 chromatographic column（4.6 mm×250 mm，5 μm）at 27 ℃，using 0.05 mol•L－1 sodium acetate solution（containing 1% DMF， pH6.8） and 50% acetonitrile with gradient elution as the mobile phase at a flow rate of 1.2 mL•min－1.The detection wavelength was 360 nm， and the injection volume was 20 μL.ResultsThe linear range of glycine was 2.25－18.06 μg ， and the proline1.81－14.53 μg，the alanine 3.73－29.8 μg ，the valine1.76－14.12 μg ，and the leucine 2.06－16.48 μg ，with the correlations coefficient of 0.999 9.The average recoveries of the glycine， proline， alanine， valine， and leucine were 98.53%，99.60%，100.26%，96.90%，99.91% with the average RSD being 1.99%，1.68%，1.85%，1.69%，1.80%（n=9）， respectively.There was great difference in the content of five main free amino acids from four different manufacturers.ConclusionThis method is convenient， accurate and steady.
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  Determination of Related Substances in Atorvastatin Calcium Tablets by HPLC Gradient Elution

  XIONG Miaomiao;WANG Qiulan;XIE Bin;WANG Wenqing;FANG Jianguo

  2013, 32(5): 656-660.

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  ObjectiveTo establish a method for determination of related substances in atorvastatin calcium tablets by high performance liquid chromatography (HPLC).MethodsThe gradient elution was used with the column Apollo C18 (4.6 mm×250 mm， 5 μm).Ammonium acetate buffer solution (1.54 g ammonium acetate dissolved in 1 000 mL water and adjusted to pH 4.50±0.05 with acetic acid)acetonitrile (70：30) and acetonitrile was served as the mobile phase A and B， respectively.The flow rate was 1.1 mL•min－1， detective wavelength was 244 nm， column temperature was at 40 ℃， and sample was load as 20 μL.Determination with reference substance and main component selfcomparison without calibration factor were performed.ResultsAtorvastatin was isolated from the impurities successfully.Impurity A， B， C， D， H and I had a good linearity in the range of 0.190 4－9.519 8， 0.203 2－10.160 0，0.191 2－9.560 0，0.208 0－10.400 0，0.198 8－9.940 0 μg•mL－1，and 0.205 2－10.260 0 μg•mL－1， respectively.And the average recoveries were 100.24%， 99.73%， 94.47%， 92.17%， 103.76% and 101.23%.ConclusionThis method is proved to be rapid， accurate and reliable.It is suitable for determination of related substances in atorvastatin calcium tablets.
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  Technological Optimization on Preparation of Oxaliplatin Longcirculating Liposome

  QI Meifang;LI Junli;LIU Xiaoping;LIU Yang;YANG Liu

  2013, 32(5): 660-663.

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  ObjectiveTo optimize technology on preparation of oxaliplatin longcirculating liposome.MethodsThe liposome was prepared by ethanol injection method.Orthogonal design was used to optimize the prescription and preparation.Encapsulate rate of the liposome was determined by high performance liquid chromatography.ResultsThe optimum prescription was as follows: the quality ratio of lecithin to cholesterol was 5：1， the amount of oxaliplatin was 10 mg， and the concentration of polyethylene glycol 2000 was 0.05%, the average coating rate is （51.87±0.90）%.ConclusionThe optimized formulation of PEG2000conjugated oxaliplatin longcirculating liposome is reasonable， practicable and stable.
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  Technological Optimization on Complex Enzyme Assisted Ultrasonic Wave Extraction of Flavonoid Glycoside from Cudrania tricuspidata

  HUANG Xiuxiang;LAI Hongfang;LI Zhiwei

  2013, 32(5): 664-666.

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  ObjectiveTo optimize technology of extracting flavonoid glycoside from Cudrania tricuspidata by complex enzyme assisted ultrasonic wave process.MethodsThe optimum process was determined with the orthogonal test by evaluating effects of solid to liquid ratio， enzyme dosage， ultrasonic temperature, duration and amount of flavonoid glycoside extracted.ResultsThe best extraction condition was that taking solid to liquid at a ratio of 1：25(g：mL）， using enzyme at 30 mg， setting ultrasonic temperature at 40 ℃ and ultrasoning for 15 min.The highest concentration of flavonoid glycoside was 3.96 mg•g－1， with RSD of 0.04%.ConclusionEnzymeassisted ultrasonic extraction presents the feature of high extraction rate，time saving，less damage components and stable results.