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    药物研究
  • 药物研究
    LI Shu-hui;ZHOU Jian-zhi;TANG Yuan;ZHANG Hai-gang;LI Xiao-hui
    2009, 28(10): 1247-1250. https://doi.org/10.3870/yydb.2009.10.001
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    Objective To study the antioxidative effects of melatonin and its effects on pethidineinduced physical dependence. Methods A traumapain model was established in Wistar rats by combining right limb amputation with 50 ℃ tailflick test. The contents of MDA and activity of total superoxide dismutase(SOD) in the brain tissue of traumapain rats and influence of melatonin were detected by thiobarbituric acid method and the xanthine oxidase one. A physical dependence model in mice was produced by subcutaneous injection of consistently increased dose of pethidine and effects of melatonin on pethidinedependent withdrawal syndromes were investigated. Results The contents of MDA enhanced, but the activity of SOD decreased greatly in brain tissues 3 days after injury in rats. Melatonin(30,60,120 mg•g-1) reduced the contents of MDA and enhanced activity of SOD dosedependently. The rates of hopping response in mice reached 90% by consecutively ip injection of pethidine for 7 times and stimulation with naloxone. Mice treated with melatonin for 7 times within 2 d alone showed no hopping response until the dosage accumulated to 840 mg•kg-1. Moreover, the combination of melatonin (5,15,20 mg•kg-1)with pethidine obviously inhibited the withdrawal hopping responses of mice dosedependently(P<0.01), which were decreased for 61.4%,72.8%,84.8%, respectively. Conclusion The present results indicate that melatonin has a good antioxidative effects on the trauma rats without generating obvious physical dependence. And melatonin might inhibit withdrawal syndromes in pethidinedependent mice in certain dosage range.
  • 药物研究
    SONG Min;LI Qi-xiong
    2009, 28(10): 1251-1253. https://doi.org/10.3870/yydb.2009.10.002
    Objective To observe the protective effect of Angelica extract on the acute myocardial infarction in rats.Methods Animal model of acute myocardial infarction were established by ligating the left anterior descending coronary artery of rats. 60 rats were randomly divided into 6 groups: sham operation, model control, positive control, low dose of extracts, middle dose of extracts and high dose of extracts groups. Rats in the extracts treated groups were i.p. injected with Angelica extract 0.07,0.14,0.28 g•kg-1,qd,for consecutive 7days; in positive control were i.p. injected with 1.4 g•kg-1 1,6fructose diphosphate at 10 mL•kg-1,qd,for 7days; rats in others were treated with normal saline at the same volume in the same way and duration. Results Angelica extract reduced the infarct area of acute myocardial infarction,decreased the release of creative kinase(CK) and lactate dehydrogenase(LDH).It also upregulated the expression of Bcl-2 and downregulated the expression of Bax.Conclusion The result indicates that Angelica extract could protect the acute myocardial infarction in rats significantly.
  • 药物研究
    MA Zu-fu;LIU Xiao-cheng
    2009, 28(10): 1254-1257. https://doi.org/10.3870/yydb.2009.10.003
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    Objective To investigate the αadrenoceptors and their interaction in the control of renal afferent arteriole tone, and explore the influence and mechanisms of α2adrenoceptors agonist clonidine underneath. Methods Isolated and micro perfused afferent arterioles from wildtype mice were used to determine isotonic contractions. The changes of arteriole diameters by administering with different subtypes of αadrenoceptors agonist were measured. Results Norepinephrine (NE)(10-12-10-4 mol•L-1) induced constrictions dosedependently and contracted afferent arterioles about 85.7% at 10-4 mol•L-1; the α1adrenoceptors agonist phenylephrine also induced constrictions dosedependently; although no differences in dose response curves were observed between phenylephrine and NE,the α2adrenoceptors agonist clonidine induced weaker afferent arteriole contractions with afferent arteriole constrictions about 18% at 10-4 mol•L-1. The strong contractile response in afferent arterioles by phenylephrine was inhibited while cotreated with clonidine (85.3% vs 31.6%, P<0.05). Conclusion Isolated and perfused afferent arteriole of mice was the good model for pharmacological researches. Clonidine can partly inhibit contractions in afferent arterioles induced by α1adrenoceptor, independent on the suppression of sympathetic nerves system, which may contribute to the mechanism of antihypertensive action of clonidine.
  • 药物研究
    LIU Meng;SONG En-feng;LUO Xiao-juan
    2009, 28(10): 1258-1261. https://doi.org/10.3870/yydb.2009.10.004
    Objective To investigate the effects of irbesartan on renal interstitial fibrosis and its mechanism. Methods Renal interstitial fibrosis in rats was generated by unilateral ureteral obstruction(UUO). Adult female SD rats(n=24) were randomly divided into three groups: sham operation group (Sham) ;UUO group and irbesartan (10 mg•kg-1•d-1) group with UUO. The renal interstitial fibrosis index was observed under light microscopy by Masson and HE staining. The expression of CTGF and MMP-2 were tested by immunohistochemistry 2 weeks after surgery. Results The levels of BUN and Scr in UUO group were significantly higher than those in sham operated group, but lower in irbesartan group.It was shown that there were denatured tubular epithelial cells, expanding or partly atrophy, interstitial macrophage and monocyte infiltration, interstitial widening, without obvious glomeruli change in the UUO group. However, these pathological changes in irbesartan group were ameliorated. The Masson stainning on renal tissue showed that there was interstitial expanding, fibrous tissues proliferation and no glomeruli change in UUO group. Compared with UUO group, the level of pathological change in irbesartan group was significantly lower (-0.05). The expression and distribution of CTGF was weak in sham operation group, while more obvious in other groups. Compared with UUO group, the level of CTGF in irbesartan group was significantly lower (-0.05). The expression and distribution of MMP2 was strong in sham group, while lower in other groups. Compared with UUO group, the level of MMP2 in irbesartan group was significantly higher (-0.05). Conclusion Irbesartan inhibits the over expression of CTGF and upregulates MMP-2 expression, abating the development of renal interstitial fibrosis.
  • 药物研究
    YE Yin-tao;YANG Fu-jun;XU Wen-qing
    2009, 28(10): 1261-1264. https://doi.org/10.3870/yydb.2009.10.005
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    Objective To investigate the effects of tanshinones on growth of HeLa cell line and their structureactivity relationship.Methods MTT was used to measure the proliferation of HeLa cells cultured with tailshinones at different concentrations at 24 h,48 h and 72 h.Results The different concentrations (0.516.0 μg•mL-1) of Tan Ⅱ A, Tan I, dihydrotanshinone, cryptotanshinone had cytotoxicities on HeLa cells in a dosedependent and timedependent manners., with IC50 of which were 24.1,20.1,8.4,17.8 μg•mL-1 at 24 h; 8.0,11.1,2.2,8.2 μg•mL-1 at 48 h; 4.6,3.5,1.5,8.1 μg•mL-1 at 72 h, respectively. Conclusion Tanshinones have proliferating inhibition effect on HeLa cell line, the dihydrotanshinone among which is the most active one. The structure disparity between aromatic ring A and furan ring D may produce the difference on growth inhibition in HeLa cells.
  • 药物研究
    XIONG Juan;PAN Yong-jun;GUO Gui-xiang;YANG Guang-tian;RUAN Yan-mei
    2009, 28(10): 1265-1268. https://doi.org/10.3870/yydb.2009.10.006
    Objective To study the interference effect and mechanism of tetramethylpyrazine(TMP) on myocardiac hypertrophy induced by angiotensin Ⅱ (AngⅡ). Methods The cardiomyocyte hypertrophy cell model was induced by stimulating with angiotensinII(AngⅡ) in vitro; The cell size was determined by phase contrast microscope and 3Hleucine incorporation were investigated; the concentration of Ca2+ was determined by fura3/AM fluorescent technique; the protein expression of CaN was measured by Western blot. Results After treatment with AngⅡ, the cell size ,3Hleucine incorporation rate,[Ca2+]i and the protein expression of CaN were increased significantly(P<0.01, P<0.05).Being treated with TMP, all indexes were obviously reduced by comparing with AngⅡ group(P<0.01, P<0.05),which were similar to losartan group. Conclusion TMP can prevent the cardiac hypertrophy and the mechanism could be related to interference on Ca2+/CaN signal pathway.
  • 药物研究
    SONG Zu-jun;MA Jun-qing;YU Hou-you;HUANG Yang;ZHANG Yong-he;CHEN Jun
    2009, 28(10): 1268-1270. https://doi.org/10.3870/yydb.2009.10.007
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    Objective To investigate the protective effect and mechanism of edaravone pretreatment on myocardial ischemia reperfusion injury(MIRI) in rats. Methods 60 SD rats were randomly divided into 3 groups: sham operation group (pretreated with normal saline), ischemia reperfusion injury group(pretreated with normal saline), and edaravone group (pretreated with edaravone) following the model of MIRI produced by the coronary artery ligation. Serum activity of superoxide dismutase (SOD), contents of malondialdehyde (MDA), creatine kinasemyocardial band(CK-MB), tumor necrosis factor-α (TNF-α) and myocardial infarct sizes were detected, respectively. Results The total activity of SOD in ischemia reperfusion injury rats was significantly decreased compared with that in sham operation group, while contents of MDA, CK-MB and TNFα significantly increased(P<0.01). Edaravone elevated the activity of SOD, lowed the levels of MDA, CK-MB and TNF-α accordingly(P<0.01), compared with MIRI group, and remarkably decreased AAR、IS/AAR (P<0.05). Conclusion Edaravone pretreatment can protect myocardial ischemia reperfusion injury in rats, the mechanism of which may be associated with enhancing the activity of SOD, attenuating damage of oxygen free radicals on myocardial cellular membrane.
  • 药物研究
    CAO Lian;WANG Lin-feng;LI Qing-yang;JIA Jun-feng;WANG Peng
    2009, 28(10): 1271-1273. https://doi.org/10.3870/yydb.2009.10.008
    Objective To explore the antiapoptosis effect and mechanisms of Ursolic acid on human glioma U251 cell line. Methods The effect of ursolic acid on U251 cells apoptosis was observed by Hoechst 33258 staining and sepharose electrophoresis. The expressions of survivin and caspase-3 were analyzed by Western blot and double immunofluorescence staining. Results It was showed that ursolic acid remarkably induced apoptosis of U251 cell line, nucleus DNA of which was stairlike degradation. Moreover, ursolic acid suppressed survivin and upregulated caspase-3 expression. Conclusion The anti-apoptosis mechanisms of ursolic acid on human glioma U251 cell line involve in decreasing survivin expression and enhancing expression and activity of caspase-3.
  • 药物与临床
  • 药物与临床
    XIE Yi-shan;ZHANG Yi-qiao;WANG Rui
    2009, 28(10): 1290-1292. https://doi.org/10.3870/yydb.2009.10.018
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    Objective To evaluate the therapeutic efficacy of shenqifuzheng injection combined with 3dimenation conformal radiotherapy(3D-CRT) for patients with advanced nonsmall cell lung cancer. Methods 97 eligible patients without operation were randomized into two groups, 46 in the treatment group and 51 in the control group. All patients received 3D-CRT for 60-70 Gy/ 6 to 7 weeks. During radiation, patients in thetreatment group were intravenously dripped with 250 mL,qd shenqifuzheng injection additionally. The shorttime curative effect and the acute radiation pneumonitis, esophagitis and myelosuppression in both groups were compared. Results The complete recovery (CR) and partly recovery (PR) rates were 11.3%(11/97) and 46.4%(45/97) in all patients. The overall response rate (CR+PR ) was 57.7%, and no differences were found between two groups(P>0.05). The incidences of 2 and 3 grade’s acute radiation pneumonitis, esophgitis and hemotologic toxicity occurred in the treatment group and the control group were 6.5%,21.7%,13.0% and 21.6%,25.5%,31.4%,respectively. The incidence of acute radiation pneumonitis and hemotologic toxicity in control group was significantly high than those in treatmentgroup (P<0.05). Conclusion Shenqifuzheng injection combined with 3DCRT decreases the acute radiationinduced injury without changing the shorttime curative effect in treating advanced nonsmall cell lung cancer.

  • 药物制剂
  • 药物制剂
    LIU Miao-na;HE Zhan-mei;ZHANG Li-dong;LIN Zhi-cheng;YAN Shu-chao;OU Sh-yun;YIN Chun-ping
    2009, 28(10): 1329-1331. https://doi.org/10.3870/yydb.2009.10.036
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    Objective To screen the optimal extraction technique for the urinary calculi prevention components from rhizome alismatis. Methods The content of Alisol B 23-acetate in the extraction of rhizome alismatis was determined by using HPLCELSD and used as a marker to investigate effects of 4 factors: methanol concentration, extraction time, extraction frequency, and methanol dosage on components extraction with an orthogonal test. Results The optimal extraction technique for effective components from rhizome alismatis was to extract the medicinal material with 8 times amount of 50% methanol for 3 times, 1.5 hours for each. Conclusion The extraction technique is reasonable and practicable.
  • 药物制剂
    LIU Hui;QI Zheng-lin;LIU Hong;TANG Ren
    2009, 28(10): 1331-1334. https://doi.org/10.3870/yydb.2009.10.037
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    Objective To prepare the venlafaxine hydrochloride (Ven) micro-porous osmotic pump tablet exhibiting zeroorder release. Methods Single factor tests for cumulative percentage of drug release were used to investigate effects of the core and coating material on it. Results It was proved that optimized Ven microporous osmotic pump fitted with the zero-order model in which osmotic pressure was the main driving force for controling drug delivery. The in vitro dissolution equation was as follows: Q=7.454 3t+2.877 1,r=0.998 3. Conclusion The osmotic pressure control based VEN microporous osmotic pump tablet is theoretically possible and controllable. It will profit the industrialized manufacture of osmotic pump controlled preparation.
  • 药物制剂
    LIU Shi-ping;QU Ting;HA Na;GUO Mei-hua
    2009, 28(10): 1334-1337. https://doi.org/10.3870/yydb.2009.10.038
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    Objective To prepare compound guchi ointment and establish the quality control method. Methods To establish the quality control standard. Radix salviae miltiorrhizae, Radix notoginseng and Flos lonicerae were identified by TLC. Tanshinone-ⅡA were determined by HPLC. Results TLC spots developed were fairly clear and the blank test showed no interference. HPLC method was accurate and reliable, The linear rangers was 0.016-0.128 μg(r=0.999 9)and the recovery was 94.21%. Conclusion The design of the preparation and manufacturing technique are rationa1. This method is accurate, reliable,and can be used for the quality control.
  • 药品质量控制
  • 药品质量控制
    ZHAI Xue-jia;XU Jin-feng
    2009, 28(10): 1345-1348. https://doi.org/10.3870/yydb.2009.10.045
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    Objective To establish a method for determination of the hydrophilic of danshensu, protocatechuic aldehyde, salvianolic acid B and lipophilic compounds of dihydrotanshinone I, cryptotanshinone, tanshinone I and tanshinone IIA in Radix Salviae Miltiorrhizae. Methods Chromatography was performed on a LichrospherC18 column (250 mm ×4.6 mm i. d.; 5 μm particle size). The separation was achieved by a linear gradient elution. Mobile phase was the mixture of solvent A (1% aqueous formic acid) and solvent B (acetonitrile). The gradient elution was conducted as follows: 10%-20% B in 0-10 min, 20%-33% B in 10-27 min, 33%-70% B in 27-30 min, and 70%-85% B in 30-50 min. The injection volume of 10 μL and the UV wavelength of 280 nm were used in the analysis. The flow rate was 1.0 mL•min-1 and the column operated at 20 ℃. Results A good linearity was obtained with the correlation coefficients of tanshinol, protocatechualdehyde, salvianolic acid B, dihydrotanshinone I, cryptotanshinone, tanshinone I and tanshinone IIA ranged from 0.037 2-118.000 0 mg•L-1, 0.017 4-8.900 0 mg•L-1, 0.141-450.000 mg•L-1, 0.018 8-56.800 0 mg•L-1, 0.049 7-158.000 0 mg•L-1, 0.021 5-78.500 0 mg•L-1, 0.096 2308.000 0 mg•L-1(R2≥0.999 2), respectively. The average recovery rates of the four investigated compounds were in the range of 98.5%-101.5% for all with RSD below 1.98% (n=6). The intraday and interday precision of the assay were no more than 2.16% (n=6). Conclusion The method is accurate and reliable with good reproducibility, and can be used as a determination standard for Radix Salviae Miltiorrhizae.

  • 药品质量控制
    ZHANG Hui-zong;LIU Jing;DI Zi-zhen;GUO Zhen-wu
    2009, 28(10): 1349-1351. https://doi.org/10.3870/yydb.2009.10.046
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    Objective To establish a content analysis method for determing α-asarone in different Radix et Rhizoma Asari and providing a scientific basis for quality analysis of it. Methods The content of αasarone was determined in 36 samples of Radix et Rhizoma Asari from 9 provinces by HPLC with KrouasilC18 column (4.6 mm×250 mm,5 μm). And the mobile phase was the mixture of methanol- potassium dihydrogen phosphate (55:45). The flow rate was 0.8 mL•min-1 and the UV wavelength was 313 nm. Results There is a great content variety in α-asarone, the highest content was 129.2 μg•g-1 , the content of 8 samples was undetectable. Conclusion This method is simple, rapid and repeatable for α-asarone determination in Radix et Rhizoma Asari, which could help for the quality analysis of Radix et Rhizoma Asari.
  • 药品质量控制
    ZHENG Guo-gang;LI Hui-lin
    2009, 28(10): 1351-1353. https://doi.org/10.3870/yydb.2009.10.047
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    Objective To establish a method for determining the dissolution of Huperzine A capsules by HPLC. Methods 100 mL Hydrochloric acid (9→1 000) was taken as solvent with the rotating speed at 35 r•min-1, and the sampling time 30 min. The dissolution of Huperzine A capsules was determined by dissolution test 3. Results The standard curve of Huperzine A showed as a good linear relationship in the range of 0.13-1.02 μg•mL-1(r=1.000 0,n=6);The average recovery rate was 98.0%(RSD=0.7%,n=9). The mean cumulative dissolutions of four batches of samples were all above 80%. Conclusion The method is simple, accurate and reproducible,which can be used for the quality control of. Huperzine A capsules.
  • 药品质量控制
    YANG Xin;SI Lu-qin;TU Zhi-ping;LI Gao
    2009, 28(10): 1354-1356. https://doi.org/10.3870/yydb.2009.10.048
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    Objective To detect quality the nucleosides contained in cultured Cordyceps militaris mycelia from different habitats and natural Cordyceps sinensis for qulity evaluation. Methods The contents of nucleosides in 11 batches of cultured Cordyceps militaris from 9 different places and 4 types of natural Cordyceps sinensis were determined by using a HPLC method with the evaluating markers of uridnine, adenosine and cordycepin. Results The contents of nucleosides in cultured Cordyceps militaris mycelia were varied from 0.27% to 0.87% and those in Cordyceps sinensis were 0.17% to 0.25%. Cordycepin levels differed more obviously, less or no cordycepin was detected in natural Cordyceps sinensis. Conclusion Different contents of nucleosides are presented in cultured Cordyceps militaris mycelia from different habitats, while much higher than those in natural Cordyceps sinensis. Among which, the contents of adenosine and uridnine are constant, and could be used as valuable bases for development and quality evaluation of artificial Cordyceps militaris mycelia.