Table of Content

Volume 9 Issue 10
26 October 2004

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Resent studies on cytochrome P450 and drug metabolism

ZHU Li-Qin, LOU Jian-Shi

2004, 9(10):  1081-1086. 

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Cytochrome P450 is one of the important drug metabolization enzymes in humans. This paper reviews drug-relevant CYP, the relationship of CYP and drug interaction, and effects of Chinese medicine on CYP. The aim is to answer and predict the clinical drug interaction and the adverse drug reactions. Moreover, suitable drug can be selected to evaluate the action of CYP, and it can offer the scientific assurance for clinical individual therapy.

Progress in the research of P-gp inhibitors

ZHANG Yu

2004, 9(10):  1087-1090. 

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Multidrug resistance (MDR) is one of the major obstacles to cancer chemotherapy. It is now well established that MDR phenotype is strongly correlated with the over-expression of P-glycoprotein (P-gp), a membrane glycoprotein encoded by MDR1 gene. There is very great progress in the research of the P-gp inhibitors in recent years. This article describes the current research state of the P-gp inhibitors.

Inhibition of prodigiosin on migration and invasion of cancer cells and expression of MMPs

ZHANG Jing, SHEN Ya-Ling, LIU Jian-Wen

2004, 9(10):  1091-1095. 

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AIM: To observe the inhibition and mechanisms of prodigiosin on migration and invasion of cancer cells in vitro.METHODS: The migration and invasion of cells was measured by wound healing assay and the transwell assay. The expression of MMP-2,-9 was analyzed by gel zymography assay. The expression of NF-κB protein in cytoplasm was measured by western-blot. The concentration of prodigiosin in 95-D cells was analyzed by HPLC.RESULTS: The inhibitive effects on migration of the cells reached 42 %when cells were treated with 2. 5 μmol·L^-1 prodigiosin for 12 h and under the concentration of no cytotoxicity actions. The invasion of 95-D cells was dose-dependently inhibited by prodigiosin with EC50 of 5 μmol·L^-1.In addition, prodigiosin effectively inhibited the activity of MMP-2,-9. Prodigiosin also elevated the protein level of NF-κB in cytoplasm and then inhibited the activity of NF-κB. The results of HPLC showed that prodigiosin effectively entered cells, and the pharmacological effect of prodigiosin was dependent on the drug concentration in cells.CONCLUSION: Prodigiosin can effectively enter cells and inhibit the expression of MMP-2,-9 through the inhibition of the activity of the NF-κB, thereby it can inhibit the invasion and metastasis of tumor cells.

Effects of kwoninone on experimental liver fibrosis and expression of matrix metalloproteinase-2 in rats

ZHOU Ai-Ling, LUO Lin, MAO Jia-Hui, ZHU Yan

2004, 9(10):  1096-1100. 

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AIM: To investigate the prophylactic and therapeutic effects and mechanisms of kwoninone in rats with experimental liver fibrosis.METHODS: The animal models with liver fibrosis were prepared in rats by administration of carbon tetrachloride (CCl₄ ). 28 SD rats were randomly divided into 4 groups: normal control group, model control group, kwoninone prophylactic group and kwoninone therapeutic group. After 10 weeks of administration, the levels of ALT, AST, TBA and GGT were measured in rat serum. The histopathological changes were observed by light microscopy and electromicroscopy. The expressions of matrix metalloproteinase-2 (MMP-2) mRNA in liver were detected by reverse transcription polymerase chain reaction. The expressions of proteins of MMP-2 in liver were determined by gelatin zymography.RESULTS: The serum levels of ALT, AST, TBA and GGT in liver fibrosis rats were decreased in the kwoninone prophylactic groups and therapeutic groups(P<0. 05, or P<0. 01). The levels of fibrogenesis in liver tissues were more significantly decreased in the kwoninone prophylactic groups and therapeutic groups than that in the model control groups. The formations of liver pseudoluboli were alleviated in the kwoninone prophylactic groups and therapeutic groups. Structures of liver cells were recovered and few collagenous fibers were found in Disse space in the kwoninone prophylactic groups and therapeutic groups. The levels of the liver fibrosis in kwoninone prophylactic group were lighter than that in the therapeutic groups.The levels of MMP-2 mRNA and proteins of MMP-2 in the liver significantly decreased in the kwoninone prophylactic groups and therapeutic groups.CONCLUSION: Kwoninone can protect and therapy liver fibrosis induced by CCl₄ in rats, down-regulate the expression of MMP-2mRNA and proteins of MMP-2 levels, accelerate the degradation of ECM, and inhibit the deposition of the ECM in liver.

Effects of simvastatin on myocardial fibrosis and connective tissue growth factor in renovascular hypertensive rats

WANG Yan-Wu, XIONG Yong-Yan, CHEN Zhi-Long, LI Li

2004, 9(10):  1101-1104. 

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AIM: To investigate the effects of simvastatin on myocardial fibrosis and connective tissue growth factor (CTGF ) in renovascular hypertensive rats.METHODS: The experimental rats were randomly divided into three groups, such as sham operation group rats, hyperpiesia rats and hyperpiesia rats treated with simvastatin (5 mg㎏kg^-1·d^-1). Systolic blood pressure (SBP) was measured and collagen concentration (Coll) was also detected in terms of hydroxyproline concentration. VanGieson and immunohistochemistry staining combined with computed morphometry were used to evaluate the total collagen volume fraction (CVF) and CTGF expression in left ventricular tissue.RESULTS: Compared with sham operation group rats, the SBP, CVF, Coll and CTGF expression increased markedly in hyperpiesia rats (P<0. 01). Compared with the hyperpiesia rats, simvastatin inhibited myocardial fibrosis significantly and decreased CTGF expression (P<0. 05).CONCLUSION: Simvastatin can inhibit the development of myocardial fibrosis in renovascular hypertensive rats, which may be related to the decreased expression of cardiac CTGF.

Inhibition of active fraction separated from Naja Atra venom on three-dimensional angiogenesis

YU Qing-Sheng, LIU Xiao-Ying, QIU Yuan, HANG Shao

2004, 9(10):  1105-1109. 

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AIM: To study the anti-angiogenesis effects of the active fraction separated from Naja Atra venom.METHODS: The inhibiting effect of active fraction in angiogenesis was detected by the three-dimensional angiogenesis model. RESULES: The active fraction in different concentrations inhibit the action that vascular endothelial cells (ECs) developed into three-dimensional capillary-like networks in vivo. ECs in matrigel only developed into incomplete capillary-like networks in 0. 6 μg·ml^-1 dose group, the sprouts differentiated from ECs did not spread and contract each other and form the nets in 1. 2mg·L^-1 dose group, ECs did not adherent together and alternate in 2. 4 mg·L^-1 dose group.CONCLUSION: The active fraction separated from Naja Atra venom has the anti-angiogenesis effect in in vitro.

Effects of Angiotensin Ⅱ and valsartan on expression of AT₁/AT₂ and eNOS in human umbilical vein endothelial cells

WANG Yan, WANG Pei-Hua, WANG Dao-Wen

2004, 9(10):  1110-1114. 

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AIM: To investigate the effects of angiotensin Ⅱ (Ang Ⅱ) and valsartan on the expression of Ang Ⅱ type 1 receptor (AT₁), Ang Ⅱ type 2 receptor (AT₂) and endothelial nitric oxide synthase (eNOS) and the synthesis of nitric oxide (NO) in human umbilical vein endothelial cells (HUVECs, ECV304 cells).METHODS: Human umbilical vein endothelial cells (HUVECs) were incubated by Ang Ⅱ or valsartan for various periods. The expression of AT₁/AT₂, eNOS and the production of NO were detected. Potential mechanism of the above effects was explored by using the relevant inhibitors of the signal molecules and antioxidants.RESULTS: Both Ang Ⅱ and valsartan significantly inhibited the mRNA and the protein expression of AT₁in HUVECs. The combination of the two drugs caused more significantly inhibitory effects. Ang Ⅱ showed a slightly promotive effect at first and a significantly inhibitory effect afterward on the expression of eNOS and synthesis of NO in HUVECs. MAPK inhibitor reversed the promotive effect whereas valsartan and antioxidant vitamine C significantly reversed the inhibitory effect.CONCLUSION: Valsartan can downregulate the expression of AT₁in HUVECs. Long time action of Ang Ⅱ can significantly inhibit the expression of eNOS and synthesis of NO in endothelial cells, while valsartan can significantly reverse this inhibitory effect.

Protective effects of Rheum tanguticum polysaccharides on stress induced by gastric ulcer in rats

CAO Xiao-Lin, LIU Li, WANG Zhi-Peng, LIU Zhen-Guo, MEI Qi-Bing

2004, 9(10):  1115-1118. 

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AIM: To evaluate the protective effects of Rheum tanguticum polysaccharides (RTP) on stress induced by gastric ulcer in rats.METHODS: Water immersion and restraint stress (WRS) induced gastric injury was used as the experimental model of acute gastric ulcer. Rats were orally administrated with RTP before stressed. 6 hours after WRS, all the animals were sacrificed and the stomachs of rats were taken out to examine the ulcer index and observe histologically. The activity of total superoxide dismutase (SOD) and malondialdehyde (MDA) were measured in serum and gastric mucosa.RESULTS: Six hours of water immersion and restraint stress (WRS) resulted in appearance of acute gastric mucosal lesions. RTP significantly decreased the ulcer index and the level of MDA in mucosa of stressed rats, and increased the activity of SOD both in serum and gastric mucosa.CONCLUSION: RTP has remarkable protective effects on WRS induced gastric ulcer in rats, which suggests that the effective component of rhubarb on stress induced by gastric injury is perhaps RTP.

Protective effects of mycophenolate mofetil on kidneys of type 2 diabetic rats

YU Tang-Hong, JIA Ru-Han, DING Guo-Hua, XIONG Yan, CHEN Jian

2004, 9(10):  1119-1122. 

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AIM: To evaluate the protective effects of mycophenolate mofetil on the kidneys of type 2 diabetic rats and discover their mechanisms.METHODS: Wistar rats were divided into three groups, such as normal control rats, diabetic rats, and diabetic rats in the treatment with mycophenolate mofetil (MMF, 15 mg·kg^-1·d^-1). Thirteen weeks later, urinary albumin excretory rate (UAE), creatine clearance (Ccr), blood glucose, blood insulin and blood lipid were measured, and kidney pathology was observed. Inmmunohistochemistry was used to analyze the expression of CTGF, ColI and Col Ⅲ.RESULTS: Mycophenolate mofetil decreased UAE, Ccr and reduced glomerular volume. The expression of CTGF and deposition of ECM decreased after diabetic rats received mycophenolate mofetil.CONCLUSION: Mycophenolate mofetil can protect the kidney of diabetic rats. Its mechanism may be related to the decrease of CTGF expression and extracellular matrix deposition in renal tissue.

Observation of morphology in Escherichia coli with atom microscope during the cefmetazole-induced post-antibiotic effect period

ZHANG Yong-Qing, WANG Rui, ZHU Man, ZHANG Jian-Peng, ZHANG Yong-Mei, TONG Jun

2004, 9(10):  1123-1127. 

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AIM: To study the mechanism of postantibiotic effect (PEA) by observing the changes of morphology.METHODS: The morphological effects of Escherichia coli were studied with atomic force microscopy (AFM) during the cefmetazole-induced post-antibiotic effect.RESULTS: The cefmetazole-induced (4 ×MIC, 128 ×MIC) PAE as defined by viability counting were-0. 03 h and 3. 65 h in Escherichia coli There was noted formation of filamentous structures at low concentrations (4 ×MIC) and the formations of spheroplasts at higher concentrations (128 ×MIC) by atomic force microscopy (AFM), and this morphological form persisted past the classically defined PAE.CONCLUSION: The mechanism of PAE is different at different concentrations through the inhibition of different protective bacterial enzymes.

Influence of different dosages and injecting times of streptozotocin on islets of diabetic rats

WEN Zhi-Ming

2004, 9(10):  1128-1133. 

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AIM: To investigate the damage of alpha and beta cells on islets of diabetic rats in different dosages and injecting times of streptozotocin (STZ).METHODS: Wistar rats were divided into six groups: control group, group A (single injection with 50mg·kg^-1STZ), group B (injection with 50 mg·kg^-1·d^-1STZ for two days), group C (injection with 50mg·kg^-1·d^-1STZ for three days), group D (injection with 30 mg·kg^-1·d^-1 STZ for five days) and group E (single injection with 80 mg·kg^-1STZ). The body weights and concentrations of peripheral glucose of rats were measured regularly. Then the pancreases of rats were selected to make tissue slices. The tissue slices embedded in paraffin were histological observes under the light microscope after staining with Hematoxlin and Eosin (HE), Azan and immunohistochemical techniques.RESULTS: Insulitis was observed in each group throughout the term of experiment. It was more serious in all rats that were injected with STZ than those in the control group. The inflammation, vacuolization and fibrosis of islets in the group D were more serious than those in the other groups. The amount of islets, the average area of islets, the area of beta cells, the ratio of the area of beta cells and the average area of islets in each group were significantly decreased, especially in the group C, D and E. Conversely, the area of alpha cells, the ratio of the area of alpha cells and the average area of islets in each group significantly increased as alpha cells appeared.CONCLUSION: STZ can induce chemical insulitis and autoimmune insulitis, destroy both alpha and deltas cells, and make vacuolization and fibrosis in islets. Single, high dose of STZ can cause the greatest damage.

Molecular mechanisms of antianxiety drugs on rats with restraint stress

HUANG Huan-Jie, SHAO Bei, ZHENG Rong-Yuan, LI Jian-Min, WANG Zong-Min, YAN Zhi-Qin, XIE Li-Wei

2004, 9(10):  1134-1136. 

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AIM: To investigate the molecular mechanisms of antianxiety drugs on the rats with restraint stress.METHODS: The rat stress model was made by restraint stress. The behaviors of rats were tested in openfield conditions, and the expression of c-fos positive cells was detected by S-P immunohistochemical assay in hypothalamus.RESULTS: The crossing scores, the rearing scores and the expression of c-fos positive cells increased more significantly in the other groups than that in the control group, but decreased in the paroxetine group. The paroxetine inhibited the behaviors and the expression of cfos positive cells in the hypothalamic paraventricular nucleus (PVN)of rats after immobilization stress.CONCLUSION: The effects of paroxetine on the anxiety disorders in rats may be related to the downregulation of the expression of the c-fos in the hypothalamic paraventricular nucleus (PVN).

Effects of valsartan and spironolactone on insulin-like growth factor-1 in cardiacmyocytes of spontaneously hypertensive rats

DUAN Xiao-Chun, WANG Jin-Ming, WANG Fang, LI Heng, QIN Jin-Mei

2004, 9(10):  1137-1141. 

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AIM: To study the inhibitive effects of valsartan and spironolactone on expression of insulin-like growth factor-1 in cardiacmyocytes of spontaneously hypertensive rats.METHODS: 18 SHRs were randomly divided into 3 groups (n =6 in each): valsartan group treated with 30 mg·kg^-1·d^-1 valsartan, spironolactone group treated with 20 mg·kg^-1·d^-1 spironolactone, and control group treated with placebo. All were administrated by gastric perfusion. 6WKY rats were served as control. After 13 weeks administration, the expressions of IGF-1 in cardiacmycytes were measured by immunohistochemistry and the IGF-1 concentrations in myocardium were measured by radiommunoassay.RESULTS: The expression of IGF-1 was higher in SHR group than that in the WKY group (P<0. 01). Valsartan and spironolactone inhibited the expression of IGF-1. The inhibitive effects of IGF-1 in valsartan group were more significantly higher than those in spironolactone group. Valsartan and spironolactone decreased blood pressure and left ventricular mass to body weight ratio (LVM/BW).CONCLUSION: IGF-1 may play an important role in the development of cardiac hypertrophy in SHR.Valsartan and spironolactone treatment can inhibit the expression of IGF-1 and prophylaxi myocardial hypertrophy.

Inhibitory effect of pioglitazone on hypertrophy of cultured neonatal rat ventricular myocytes induced by high glucose and norepinephrine

ZHOU Qing-Feng, WANG Hong-Xin, FU Li-Juan, YANG Yu-Hong

2004, 9(10):  1142-1146. 

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AIM: To study the inhibitory effect of pioglitazone on cultured hypertrophic ventricular myocyte induced by high glucose and norepinephrine (NE ).METHODS: Using cultured ventricular myocytes as a model, the protein contentss was assayed with Lowry' s method, the protein synthesis was assayed with [³H] leucine intake method, the cardiomyocytes' volumes were measured by computer photograph analysis system, and the cellular hypertrophy was observed. The contracting frequency was counted by the inverted microscope.RESULTS: Compared with 1 μmol·L^-1 verapamil, pioglitazone at the concentration of 1-10 μmol·L^-1 inhibited the protein contents, cellular protein synthesis and volumes of the ventricular myocytes in a dose dependent manner. Meanwhile, 10 μmol·L^-1 pioglitazone and 1 μmol·L^-1 verapamil inhibited cellular contracting f requency too.CONCLUSION: Pioglitazone at the concentration of 1-10 μmol·L^-1 can effectively inhibit hypertrophy of cultured ventricular myocytes induced by high glucose and NE.

Changes of reactive oxygen species in apoptosis induced by resveratrol in K562 cells

HAO Chun-Yan, SU Hai-Xiang, WEI Hu-Lai, ZHANG Zhe-Wen

2004, 9(10):  1147-1149. 

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AIM: To investigate the apoptosis of K562 cells induced by resveratrol and the influence of intracellular reactive oxygen species (ROS) level.METHODS: MTT assay, light microscopy, DNA agarose gel electrophoresis and cell cycle analysis were used for examine apoptosis in K562 cells. Intracellular ROS level was measured with flow cytometry (FCM).RESULTS: Resveratrol inhibited growth of K562 cells. Agarose gel electrophoresis showed evident DNA fragmentation. Cell cycle analysis indicated increased S phase proportion, as well as apparent S/G2 phase arrest. After application of resveratrol, the level of the markedly increased of ROS.CONCLUSION: Resveratrol induces apoptosis in K562 cells may be through stimulating ROS production.

Efficacy of intracranial injection of the nerve growth factor (NGF) in treatment of patients with hypertensive cerebral hemorrhage after intracranial hemorrhage mini-invasive drainage

LI Jun-Rong, CAO Hui, LI Xue-Ping, YANG Weng-Juan, QIAN Ji-Yue

2004, 9(10):  1150-1153. 

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AIM: To evaluate the efficacy of intracranial injection of the nerve growth factor (NGF) in treatment of patients with hypertensive cerebral hemorrhage after intracranial hemorrhage mini-invasive drainage.METHODS: 90 hypertentive cerebral hemorrhage patients after intracranial hemorrhage mini-invasive drainage were divided into three groups:Group A (n =30), patients were intracranial injected with 2 ml normal saline per day for 4 days, and then intracranial injected with 2 ml water per day for 10 days; Group B (n =30), patients were intracranial injected with 2 ml normal saline per day for 4 days, and then intracranial injected with 2 ml NGF per day for 10 days; Group C (n =30), patients were intracranial injected with 2 ml NGF per day for 4 days, and then intracranial injected with 2 ml NGF per day for 10 days. The curative effect was evaluated by neurological function scoring, ADL scoring and mortality after 1 month therapy.RESULTS: There was no significant difference on mortality in group A (13. 3 %), group B (10. 0 %) and group C (10. 0 %). The effective rates in group B (40 %) and group C (70 %) were higher than that in group A (20 %) (P<0. 05), and the total effective rate in group B (66. 67 %) and group C (80 %) were higher than that in group A (36. 67 %) (P<0. 05). Meanwhile, the values of ADL scoring were more significantly increased in group B and group C than that in group A.CONCLUSION: NGF can increase the clinical curative effect and decrease the disability rate in patients with hypertensive cerebral hemorrhage, and it can obviously improved the patient' s life quality. Furthermore, the effect of intracranial injection of NGF is marked.

Extraction of garlic flavone and its antiendotoxin activity

JIANG Dong-Neng, ZHENG Jiang

2004, 9(10):  1154-1156. 

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AIM: To extract garlic flavone and evaluate its antiendotoxin activity.METHODS: The two fractions (garlic flavone 1, garlic flavone 2)were screened and extracted by ion exchange-HPLC, and the neutralization ability of the garlic flavone to lipopolysaccharide (LPS)was determined by kinetic turbidimetric assay. The protective effect of the garlic flavone 2 was observed in mice attacked by 20 mg·kg^-1 of LPS.RESULTS: The garlic flavone 2 could neutralise LPS and protect mice from the attack of LPS.CONCLUSION: The garlic f lavone 2 has a significant antiendotoxin activity on LPS-attacked mice.

Protective effects of total of flavone c on cerebral ischemia injury in mice

LUO Sheng-Yong, DONG Liu-Yi, FAN Li, FANG Ming, CHEN Zhi-Wu

2004, 9(10):  1157-1159. 

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AIM: To investigate the protective effects of total of flavone C (TFC) on acute cerebral ischemia in mice and focal cerebral ischemia in rats.METHODS: The occlusion of bilateral common carotid arteries with vagus nerves in mice was used for make the acute cerebral ischemia models. The survival time and the death rate were observed. The permanent occlusion of the proximal of the right middle cerebral artery (MCA) was used for make the focal cerebral ischemia models. The extent of neurological deficits was observed, and the infarct area was measured by NBT staining technique. The activity of LDH and the content of MDA and NO in the ischemic cerebral cortex were determined.RESULTS: TFC of 80 and 40 mg·kg^-1 prolonged the survival time and decreased the death rate of mice with acute cerebral ischemia injury. TFC of 60, 30, and 15 mg·kg^-1 ameliorated neurologic deficits score and the infarct size of rats with MCAO.CONCLUSION: TFC provides significant protective effects against cerebral ischemia injury.

Efficacy and safety of yanshenjianwei capsules in treatment of patients with chronic atrophic gastritis

DU Bao-Jun, LI Zhen-Hua, LI Bao-Shuang

2004, 9(10):  1160-1164. 

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AIM: To evaluate the efficacy and safety of yanshenjianwei capsules in the treatment of patients with chronic atrophic gastritis.METHODS: Yanshenjianwei capsule was observed in a randomized, doubleblind, double-modeling, and apositive drug-controlled clinical trail. 202 patients were divided into two groups: yanshenjianwei capsule group (n =103) and control group (n =99).The symptoms of the traditional Chinese medicine were observed. Atrophy of glandular organ in gastric mucosa, intestinal metaplasia and atypical hyperplasia were observed by gastroscope and biopsy of gastric mucosa.RESULTS: The cure rate of the yanshenjianwei capsule group and the control group were 21. 36 % and 14. 14 % on the symptoms of pathology, and the effective rate were 28. 16 % and 16. 16 %, respectively. The yanshenjianwei capsule group was superior to the control group (P<0. 05).The cure rate of the yanshenjianwei capsule group and the control group were 25. 24 % and 12. 12 %on the symptoms of the traditional Chinese medicine, and the effective rate were 16. 16 % and 36. 36 %, respectively. There was a significantly statistical difference between the two groups (P<0. 05).No serious side effects were found on blood-routine, urine-routine, stool-routine, electrocardiogram, liver function and kidney function in the two groups.CONCLUSION: Yanshenjianwei capsule is an effective and safe drug for patients with chronic atrophic gastritis and cold-heat complicated syndromes in TCM.

Effects of combination of amoxicillin, metronidazole and colloidal bismuth subcitrate on gastric ulcer in rats

ZHANG Jie-Bing, GU Zhuo-Liang, ZHOU Guo-Hua

2004, 9(10):  1165-1167. 

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AIM: To study the effects of combination usage of amoxicillin (A), metronidazole (M) and colloidal bismuth subcitrate (B) on gastric ulcer in rats and to provide the clinical reasonable medication reference on peptic ulcer.METHODS: 40 rats were divided into 5 groups (n =8 in each): the test groups with the administration of mixture of A, M and B 225, 112 and 56 mg·kg^-1, respectively; the positive control group with the administration of cimetidine 112 mg·kg^-1and the negative control group with the administration of 2 % CMCNa. Two-thirds of rats in each group were given drugs before being made the gastric ulcer animal models induced by stress and pyloric ligation, and the other one-third of rats in each group were given drugs after being made the gastric ulcer models induced by acetic acid injury.RESULTS: The mixture prevented the formation of gastric ulcer induced by stress and pyloric ligation, and healed the gastric ulcer induced by acetic acid injury at the dosage of 112, 56 and 56 mg·kg^-1, respectively.CONCLUSION: The mixture can dose-dependently protect the gastric ulcer induced by stress, reduce the degree of gastric ulcer induced by pylorus ligation, and advance the healing rate of gastric ulcer induced by acetic acid injury, but its effect is lower than that of cimetidine.

Efficacy and safety of xuesetong pills in the treatment of patients with angina pectoris

HU You-Zhi, SHI Jie, XIANG Nan, ZHANG Feng, WANG Yan-Li, Feng DE-Xun, DENG A-Li

2004, 9(10):  1168-1171. 

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AIM: To evaluate the efficacy and safety of xuesetong pills in the treatment of patients with angina pectoris.METHODS: Regard xuesetong tablet as contrast, xuesetong pill was observed in a random, doubleblind, double-modeling, positive drug parallel contrast and multi-center clinical trial.RESULTS: The total effective rate of xuesetong pill was 82. 1 %on angina pectoris and 67. 2 % on the amelioration of ECG, and there was no significant difference on the symptoms and ECG between the two groups (P >0. 05). Xuesetong pill can significantly relieve the symptoms of angina pectoris, and the total effective rate of xuesetong pill was 86. 6 %on the symptoms of the traditional Chinese medicine. Comparing with the xuesetong tablet, xuesetong pill can markedly relieve the symptoms of the traditional Chinese medicine after the treatment of xuesetong pills for 1 week, and there was a significant difference on the symptoms of the traditional Chinese medicine and the amount of the symptoms of the traditional Chinese medicine between the two groups (P<0. 01). But there was no marked difference after the treatment of xuesetong pills for 4 weeks (P >0. 05). The blow result time of xuesetong pill is superior to that of the xuesetong tablet (P<0. 01). No serious side effects on general health exam, blood-routine, urine-routine, stool-routine, liver function and kidney function were observed in the two groups.CONCLUSION: Xuesetong pill has a characteristic of safe, effective, fast result blowing in the treatment of angina pectoris.

Transdermic absorption of terbinafine liquor

CHEN Tie-Feng, YU Xi-Yong, LIN Shu-Guang, YANG Min, JIANG Gui-Fen, QIAN Yi-Zhi

2004, 9(10):  1172-1174. 

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AIM: To investigate the transdermic absorption and accumulation in vivo after dermic administration of 1 % liquor of terbinafini hydrochloridum.METHODS: 6 New Zealand white rabbits were used in this experiment. 8 ml of the liquor was coated on the back skin of each rabbit. Blood were collected at 0. 5, 1, 1. 5, 2, 3, 4, 6, 8, 12 and 24 h before and after single administration. Blood were collected at peak and trough points everyday in the continuous multiple administrations which was once per day for 7 days. The serum concentrations of terbinafine were determined by high-performance liquid chromatography.RESULTS: The peak concentration of terbinafine arrived at 2-3 h and C_max was 8. 6 ± 1. 8 μg·L^-1.The peak concentration of terbinafine increased gradually after continuous multiple administrations, but there only increased 1. 33 times in fourth day, and more than that in first day. In following three days, the peak concentrations tend to steady-state. Therewas no significantly increase or decrease in trough concentration.CONCLUSION: There is no accumulation in vivo after dermic administration of 1 % liquor of terbinafini hydrochloridum.

Effects of ovariectomized on different parts of bones in rats

XU Bi-Lian, WU Tie, CUI Liao, LIU Yu-Yu, ZOU Li-Yi

2004, 9(10):  1175-1178. 

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AIM: To observe the changes of different parts of bones in rats 90 days after ovariectomized (OVX).METHODS: Twenty 4. 5-month-old virgin female Sprague-Dawley rats were randomly divided into 2 groups: sham group and OVX group. Rats in sham group were sham-operated, while rats in OVX group were bilaterally OVX. Rats in two groups were treated with 5 ml·kg^-1·d^-1 ethanol for 90 days. Parameters of the proximal tibial metaphysis (PTM), tibial shaft (Tx) and the fifth lumbar vertebral body (LVB) were analyzed by bone histomorphometry method.RESULTS: %Tb. Ar and Tb. N were decreased by 80. 5 % and 76. 1 %, Tb. Sp and Oc. N were increased by 468. 0 % and 356. 6 %, and MAR and BFR BV were increased by 43. 9 % and 95. 9 %, respectively, in PTM. The changes in LVB were not remarkable as those in PTM. %Tb. Ar and Tb. Th were decreased by 35. 0 % and 31. 0 %, while Oc. N and BFR BV were increased by 106. 9 % and 126. 8 %, respectively. The cortical bone and marrow areas of tibial shaft did not change in Tx, but bone formation parameters (%P-LPm, %E-LPm ) were increased.CONCLUSION: After OVX for 90 days, high bone turnover osteopenia model is duplicated successfully in rats. Different parts of the bones have different reaction to ovariectomization in rats.

Quantitative determination of two active constituents of 10-hydroxycamptothecin(HCPT)in whole blood of dog by HPLC

ZHANG Xu-Ning, DING Jian-Hua, LIU Su-Yi, LIU Qiang, FAN Yi, HU Gang

2004, 9(10):  1179-1182. 

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AIM: To quantify the lactone form and carboxylate form of 10-hydroxycamptothecin (HCPT)in whole blood of dog by develop a simple, rapid, and sensitive high-performance liquid chromatography (HPLC) method.METHODS: The concentration of hydroxycamptothecinum was assayed on a DiscoveryC18 column with a mobile phase consisting of methanol-acetonitriletriethylamine-0. 05 mol·L^-1 dipotassium hydrogen phosphate buffer solution(34 ∶5 ∶1 ∶60, pH =6. 8)at a flow rate of 1. 0 ml·min^-1, and HCPT was monitored with fluorescence detector, excitation and emission wavelengths being 363 nm and 550 nm, respectively.RESULTS: There was a good linear response range of 2. 5-1500 μg·L^-1 while the limit of quantification was 2. 5 μg·L^-1.The relative recovery rate C-HCPT of was 100. 7 %-103. 9 %, L-HCPT of was 96. 8 %-102. 0 %;the absolute recovery rate of C-HCPT was 85. 5 %-98. 6 %, and L-HCPT was 78. 4 %-89. 1 %. The intra-day and inter-day variations were all less than 15 %.The HCPT in supernatant in refrigerator was stable at-75 ℃ for 7 days. CONCLUSSION: The method is simple, sensitive, reliable, and suitable for the quantitative determination of hydroxycamptothecin following i. v. administration, and it is also helpful to improve the study on pharmacokinetics of two active constituents C-HCPT and L-HCPT of HCPT.

Bioequivalence of riluzole in healthy male volunteers

JIANG Gui-Ping, ZHANG Hong-Wen, WANG Wei-Qing, LIU Rei-Min, LIU Guang-yu, HU Gang

2004, 9(10):  1183-1186. 

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AIM: To develop a HPLC-UV method to determine the concentration of riluzole in human plasma and study its bioequivalence.METHODS: Single oral dose (150 mg)of riluzole (national procted and import) was given to 20 healthy male volunteers in a randomized cross-over study. Riluzole was extracted from plasma by solid-phase extraction and assaved by a validated highperformance liquid chromatography (HPLC)method with UV detection. Plasma samples (1. 0 ml) applied to a 1 ml C18 solid phase columns. The columns were washed sequentially with distilled water (1ml), and 30 %(volume/volume)methanol. The samples were eluted with 1 ml methanol and dried under a stream of nitrogen. The samples were applied to the HPLC in little methanol. Riluzole was isolated then and detected by UV absorption of 265 nm.Variance analysis and two-one sided test statistical analysis were performed for pharmacokinetic parameters.RESULTS: The main pharmacokinetic parameters of riluzole (the national procted and import)were as follows: C_max: 930 ±321 μg·L^-1 and 798 ±306 μg·L^-1; t_max: 0. 8 ±0. 5 and 1. 2 ±0. 7 h; AUC_{0 ～ t} 3361 ±890 μg·h^-1 ·L^-1 and 3301 ±886 μg·h^-1 ·L^-1; AUC_{0 ～ ∞}: 661 ±886 μg·h^-1·L^-1 and 3615 ±885 μg·h^-1·L^-1; t_1/2:8. 2 ±2. 8 and 8. 1 ±2. 6 h. The relative bioavailability of AUC_{0～ 36} was (102. 8 ± 15. 5)%.CONCLESION: The two formulations were bioequivalent.

Experimental study of anti-cold effects of gantong granules

ZHANG Xiao-Hui, XIE Xiang-Lin, ZHOU Ming, LI Lu

2004, 9(10):  1187-1189. 

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AIM: To observe anti-cold effects of the gantong granules in animals, such as inflammatory, febrifuge and relieving pain.METHODS: Some animal models were used to investigate the anti-inflammation, immunity functions of the gantong granules, including the auricular inflammation models, the feet swelling test, the cotton ball granulating proliferation test, the carbon particle clearance index test, hemolytic and febrifuge test, and lymphocyte counts.RESULTS: The gantong granules inhibited the auricular inflammation induced by dimethylbenzene in mice and the feet swelling induced be carrageenin in rats, and decreased the weights of cotton ball granulation tissues in rats. It also showed an increase in carbon particle clearance index K value and phagocytic index value in mice. Moreover it relieved pain with febrifuge, and potentiated the cellular immunity.CONCLUSION: The gantong granules show remarkable antiinflammatory effects and resistance to the cold.

Effects of administration of famciclovir and ganyanling injection alone or in combination on serum marker in patients with chronic hepatitis B

CHEN Xiao-Ping, CHEN Xue-Fu, CHONG Yu-Tian

2004, 9(10):  1190-1192. 

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AIM: To evaluate HBV-marks after administration of famciclovir and ganyanling injection alone or in combination in the patients with chronic hepatitis B.METHODS: 112 patients with CHB were randomly assigned to three groups: 39 patients were alone administration of famciclovir 0. 5 mg, tid, po (famciclovir group), 33 patients were alone administration of ganyanling injection 4 ml, im, qod (ganyanling group), 40 patients were combination administration of famciclovir 0. 5 mg, tid, po and ganyanling injection 4 ml, im, qod (combination group). All the three groups were investigated for 24 weeks and 24 weeks after therapy. The levels of serum ALT, HBV-marks and HBV-DNA were detected before and after the treatment of 1, 3, 6, and 12 month. In addition, the conversion of HBeAg into HBeAb and the curative effect were observed.RESULTS: The normalization rates of serum ALT and HBV-DNA in combination group were higher than those in famciclovir group and ganyanling group (P<0. 05). There was no significant difference of the normalization rate of HBeAg among three groups. Few side effects were found in the course of treatment. CONCULSION: Famciclovir can inhibit the replication of HBVDNA more effectively than ganyanling injection. The combination administration of famciclovir and ganyanling injection is safe and effective in comparison with administration alone in patients with chronic HBV infection.

Quantitative analysis of laboratory data in multi center clinical trials

DING Hong, ZHAO Yang, YU Hao, SU Bin-Hua, CHEN Feng

2004, 9(10):  1193-1196. 

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In order to study the quantitative methods for analyzing laboratory variables from multi-center clinical trial, the standardized methods were used to adjust the difference between centers. These standardized methods can eliminate the difference among centers, as well as the difference among age, groups or gender.

Problems and countermeasures of GCP practice in the new drug clinical trials

Deng A-Li, Xiang Nan, Zhao Ying-Qian

2004, 9(10):  1197-1200. 

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There are many problems in the process of GCP practice at present. This paper reviews the new edition of GCP, analyzes the problems in the clinical practice, and explores relevant countermeasures in order to meet the demand of GCP.