Table of Content

Volume 10 Issue 4
26 April 2005

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Research advances of pharmacokinetic-pharmacodynamic model

ZHAO Gang, TIAN Chang-qing, LI Jing

2005, 10(4):  361-366. 

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In this article we reviews, the recent ad-vances of pharmacokinetic-pharmacodynamic model reviews in building model and the application in pharmacol-ogy, toxicology, clinical trials, and predicts the development of the PK-PD model in the future.

Advancement of drug therapy of Parkinson' s disease

YAO Yao, DU Jun-rong

2005, 10(4):  367-370. 

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Parkinson' s disease (PD) is a degenera-tive disease of the basal ganglia which caused tremor at rest, muscle rigidity and hypokinesia. The exact cause of PD is not clear so far, but what can be certain is that it has something to do with many factors.Administration of drugs is the major therapy for patients all over theworld at present. This article introduces the characteristics of most of the drugs used in PD, as well as the trend of PD' s drug therapy.

Relationship between transforming growth factor-β₁ signal transduction and renal fibrosis of diabetes

WANG Jian-yun, YIN Xiao-xing

2005, 10(4):  371-376. 

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Diabetic nephropathy is one of the leading causes of the end-stage renal failure, and its major patho-logic feature is the renal fibrosis.Transforming growth factor-β₁ is a key factor in the progression of the disease. Two signal pathways, Smads and MAPK following the fac-tor, are closely connected with extracellular matrix accu-mulationwhich leads to renal fibrosis.Smads and MAPK also have a cross talk in extracellular matrix accumula-tion.The relationship between the two signal pathway and ECM accumulation offers us a new therapeutic strategy for renal fibrosis of diabetes.

Effects of iptakalim hydrochloride on H₂O₂ induced cytotoxicity in pheochromocytoma(PC12) cells

CHAI Yi, DING Jian-hua, LI Hao, HU Gang

2005, 10(4):  377-381. 

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AIM: To investigate the protective effects and mechanisms of iptakalim hydrochloride(Ipt) on H₂O₂ induced neurotoxity. METHODS: Neurotoxity injury was induced by H₂O₂ in PC12 cells.The cell viability was tested by MTT assay. The glutamate released from PC12 cells was measured by HPLC combined with fluorescent detector analysis.Changes in the intracellular free Ca²⁺ concentration ([Ca²⁺]_i) were determined in fluo-3 AM loaded PC12 cells.RESULTS: Ipt (1, 10 and 100μmol°L^-1) markedly mitigated H₂O₂ -induced neurotoxi-ty, 10μmol°L^-1 Ipt inhibited the release of glutamate and the increase of ([Ca²⁺]_i) induced by H₂O₂. The pro-tective effectswas incompletely blocked by 5-HDwhich is a mitochondrial K ATP channels antagnist. CONCLUSION: Ipt provides neuroprotective effects on H₂O₂ in-duced cytoxixity in cultured PC12 cells and the protective effects may be partially related with mitochondrial KATP channels.

Effects of roxithromycin on contact sensitivity and functions of T Lympho-cytes

LIU Kang, XU Qiang

2005, 10(4):  382-386. 

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AIM: To observe effects of roxithromycin on contact sensitivity induced by picryl chloride (PCl) and on the functions of T cells.METHODS: Contact sensitivity was induced with picryl chloride, two-way mixed lymphacyte reaction and Concanavalin A were used to induce T cell proliferation. The viability and cell pro-liferation were examined by MTT method, mRNA expres-sion was analyzed by RT-PCR and densitometry. RESULTS: Roxithromycin 20 mg°kg^-1 significantly sup-pressed contact sensitivity induced by picryl chloride in mice. In vitro assay, roxithromycin dose-dependently in-hibited splenic T lymphocyte proliferation induced by con-canavalin A, 5 and 25μg°ml^-1 of roxithromycin sup-pressed mRNA expressions of T-bet, IL-2 and IFN-γ.25 μg°ml^-1 of roxithromycin also decreased two-way mixed lymphocyte reaction.CONCLUSION: Roxithromycin suppresses picryl chloride-induced contact sensitivity. The inhibitory effect may be related to the suppression on the viability, activation and proliferation of T lympho-cytes.

Establishment of mouse model of Cytosine arabinoside-induced thrombocy-topenia

XU Guo-liang, XIAO Bing-hua, CHEN Qi, XU You-mei

2005, 10(4):  387-390. 

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AIM: To establish a mouse model of cy-tosine arabinoside (Ara-c) induced thrombocytopenia which leads inducement time more quickly and stably. METHODS: The mice were injected different dosages cytosine arabinoside (Ara-c)in two groups, respectively. The change of thrombocytopenia was observed in peripher-al hemogram and smear of marrow, andweightsof spleen, adrenal gland and thymus gland also were observed. RESULTS: The high dosage (200 mg°kg^-1)to the model formation was better than low dosage (100 mg°kg^-1)at inducement time and stability. The index showed no sig-nificant different between two groups except the volume of thrombocyte. CONCLUSION: Cytosine arabinoside-in-duced thrombocytopenia at high dosage (200 mg°kg^-1) can induce thrombocytopenia more effectively.

Construction of recombinant adenovirus vector encoding the antisense RNA of rat NF-κB and its expression in vascular smooth muscle cells

HU Rong, WU Ke-gui, XU Chang-sheng

2005, 10(4):  391-396. 

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AIM: To construct the recombinant aden-ovirus contained antisence RNA of rat nuclear factor κB (NF-κB, p65) gene and investigate the change of the gene expression in the infected vascular smooth muscle cells (VSMCs). METHODS: Total RNA was extracted from VSMCs of spontaneously hypertensive rats (SHR) and it wasused for amplifing the 1653 bp fragment of NF-κB (p65) gene by RT-PCR.The amplified product was inserted into the pMD18-T vector and identified subse-quently by enzyme digestion analysis and sequencing. The downstream 269 bp of NF-κB (p65) gene was amplified from the recombinant pMD18-T/1653 plasmid and cloned in reverse orientation into the eukaryotic expression vec-tor, pcDNA3.1(+), under the CMV promoter.The in-tact antisense RNA expression frame from pcDNA3. 1 (+) /269 was inserted into entry vector pENTR4 to form medium recombinant pENTR4/CMV/269 plasmid, fol-lowed by homologous recombination technique, the ex-pression frame was integrated into adenovirus.The lin-earized recombinant adenovirus plasmid, pAd/CMV/269, infected the monolayer 293 cells, the adenovirus packag-ing cell line. Western blot was employed to determine the changes of NF-κB (p65) gene expression level in the virus-infected VSMCs.RESULTS: A 1653 bp fragment of NF-κB (p65) gene was amplified from VSMCs, and its sequence analysiswas documented as expected.The tran-sition-vectors contained 269 bp of reverse sequence were identified by restrictive endonuclease and PCR analysis. Recombinant adenovirus that expressed NF-κB (p65) an-tisense RNA was constructed correctly and the titer of virus was generally up to 9.23 ×10⁹ plaque form units per milliliter (pfu°ml^-1). In vitro, western blot results showed that the NF-κB (p65) expression level in the in-fected VSMCs was markedly reduced compare with that in the normal cells.CONCLUSION: Recombinant aden-ovirus that expressed NF-κB (p65) antisense RNA is con-structed successfully and the virus possesses the biological feature of down-regulated expression of NF-κB (p65) in the infected VSMCs.The production of the recombinant adenovirus encoding NF-κB (p65) antisense RNA pro-vides a foundation for investigation of its activity and fur-ther gene therapy.

Effects of dexameathone on pulmonary fibrosis induced by bleomycin and oxygen-derived free radicals in rats

YE Jin-yan, XIE Yu-peng, MAO Sun-zhong, FANG Zhou-xi, CHEN Shao-xian

2005, 10(4):  397-400. 

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AIM: To study the ultrastructure of dex-amethaone on the bleomycin induced pulmonary fibrosis.METHODS: Thirty Sprague-Dawley (SD) rats were ran-domly divided into three groups (n =10 in each):control group, bleomycin (BLM) group and dexamethasone (DXM) group.After 28 days, the MDA and SODof lung were measured and the histology was detected.RESULTS: In DXM group, the concentration of SOD was lower than that in the BLM group (P<0.01), and the degree of fibrosis was more mitigative than that in the BLM group by microscope and ultrastructure. CONCLUSION: Dexamethasone can reduce the damage of oxygen-derived free radicals of bleomycin.Treatment of dexam-ethasone may be useful in inhibiting pulmonary fibrosis.

Effects of puerarin on proliferation of vascular smooth muscle cells and c-fos protein expression and TR mRNA expression

XU Yi-zhou, LI Pei-zhang, WANG Ning-fu, XU Hai-ying, PENG Wen-hui

2005, 10(4):  401-406. 

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AIM: To observe the effects of puerarin on the proliferation of vascular smooth muscle cells (VSMC) induced by thrombin and the effects of puerarin on the c-fos protein expression and thrombin receptor (TR) mRNA expression.METHODS: DNA contents were detected by cell number and cell cycle analysis and effects of puerarin on proliferation of VSMC were detected by flow cytometry. The changes of c-fos protein was indi-cated by Western blot, and TR mRNA expression was e-valuated by Reverse Transcription Polymerase Chain Re-action (RT-PCR) which was treated with T and puerarin after 24 hours. RESULTS: T increased the cell numbers of VSMC, the peak of proliferation curve was at 24 h, and the effects of T was in a dose-dependent manner (0.1 -1.0 U°L^-1). 1.5 ×10^-5 -1. 5 ×10^-3mol°L^-1 puerarin significantly suppressed this stimulation of VSMC proliferation and DNA synthesis induced by T. Western blot demonstrated that T increased c-fos protein which treated with T and puerarin after 24 hour. 1.5 ×10^-5 -1.5 ×10^-3mol·L^-1 puerarin suppressed thisincrease. RT-PCR demonstrated that T can significantly increase TR mRNA expression and 1.5×10^-3mol°L^-1 puerarin sup-pressed this increase. CONCLUSION: Puerarin can suppress the proliferation and DNA synthesis of VSMC promoted by T. The inhibitory effects of puerarin are closely related with the suppression of c-fos protein, and partly related with the suppression on TRmRNA.

Chinese herb compounds meliorate bone loss and abnormity of blood cir-culation in rats under simulated weightlessness

DONG Qi, SHEN Xian-yun, XIE Li-qin, MENG Jing-rui, JIANG Shi-zhong, YANG Guang-hua

2005, 10(4):  407-412. 

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AIM: To investigate the role of Chinese herb medicine in improving the changes of bone mass, bone biomechanical properties and hemorheological pa-rameters under simulated weightlessness.METHODS: 120 ratswere divided into 6 groups:control group, head down tilts -30°group (HDT), Danhuangci group (HDT +Dansheng, Huangqi, Ciwujia), Shenchuanshu group (HDT + ginseng, Chuanxiong, Shudi), Shenshandu group (HDT + American ginseng, Haw, Duzhong), and Shenyingsheng group (HDT +ginseng, the leaves of gingkgo, Shengdi). The bone mineral content, bone biomechanical properties and hemorheological parameters were observed following HDT for 30 days.RESULTS: After 30 day HDT, the body weight of rats, content of bone mineral salt, biomechanical indices, and the area of cortex decreased. The blood viscosity in low and middle shear, plasma fibrinogen and the rate of erythrocytes with abnormal shape increased significantly, and erythrocyte deformability (DImax, IDI) and hematocrit (HCT) de-creased.Chinese herb medicines were available to im-prove the hemorheological parameters and some bone biomechanical indices.CONCLUSION: Chinese herb medicines are effective to prevent the changes of blood circulation and bone properties under simulated weight-lessness.

Effects of anti-apoptosis drugs on signal transduction of lens epithelial cell damaged by oxidative stress

YAN-Jing, QIMing-xing, HUANG Xiu-rong, WU Zheng-zheng, HU Yan-hong

2005, 10(4):  413-416. 

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AIM: To investigate the prevention ef-fects of sodium ferulate (SF) on lens epithelial cells (LEC) damaged by oxidative stress, and to study the changes of intracellular-free calcium, cyclic adenosine monophosphate (cAMP) and cyclic guanine monophos-phate (cGMP). METHODS: Bovine LEC were primarily cultured and sub-cultured, and used for experiment in generation 3.LEC were incubatedwith hydrogen peroxide (H₂O₂). SF 25, 50, and 100 mg°L^-1 were added into the LEC damaged by oxidative stress and incubated for 12, 24 and 36 hours, respectively. The LEC activities were observed by 3-(4, 5-dimethy-thiazol-2-yl)-2, 5-diphenyltetrazolium bromide(MTT) assay. Intracellular-free calcium content of LEC was detected by spectrofluo-rophotometer using Fura-2/AM as an indicator.Intracel-lular cAMP and cGMP concentrations of LEC were deter-mined by radioimmunoassay (RIA). RESULTS: The ab-sorbance values (A values) in LEC of H₂O₂ groupsobvi-ously reduced compare with that in the control group(P< 0.01). The activities of LEC treated with SF obvious dose-dependent and time-dependent increased.The intra-cellular-free calcium contents of LEC in H₂O₂ group by spectrofluorophotometer increased compared with that in the control group (P<0.01). However, it obvious time-dependent decreased in SF groups (P<0.01). The cAMP concentration of LEC increased and the cGMP con-centration of LEC decreased in H₂O₂ group by radioim-munoassay compared with that in the control group (P< 0.01). The cAMP concentration of LEC decreased and the cGMP concentration of LEC obvious time-dependent increased in SF groups (P<0.01). CONCLUSION: SF can protect LEC from oxidative damages and inhibit apoptosis of LEC.The mechanisms of preventing and de-laying cataract formation by four anti-apoptosis drugs may be related to the cross-talk among calcium signal trans-duction system, cAMP signal transduction system and cGMP signal transduction system.

Pharmacokinetics and relative bioavailability of telmisartan in male healthy Chinese volunteers

YU Jun-xian, ZHANG Yin-di, ZHUO Hai-tong, SHEN Jian-ping, YIN Xiao-xing

2005, 10(4):  417-420. 

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AIM: To compare pharmacokinetics and relative bioavailability of telmisartan capsule (T)and telmisartan tablet (R).METHODS: 20 male healthy Chinese volunteerswere enrolled in a randomized two-way crossover designs with a single-oral dose study (80 mg once per day for each preparation).The plasma telmisa-tan concentration was determined by HPLC-fluorescence detector.Plasma levels of telmisatan were followed up to 96 h. Area under the telmisartan concentration time curve was calculated by variance analysis and the bioequivalent was determined by two one-side t-test. RESULTS: A two-compartment model was adopted in telmisartan plasma concentration-time data analysis.The pharmacokinetic parameters of T and Rin single-dose study including C max (μg°L^-1), T_max (h), T_1/2β (h), MRT(h), AUC_0-92 (μg°h°L^-1)were as following:456 ±253 and 760 ± 314, 1.61±0.71 and 1.08 ±0.36, 22. 39 ±6.29 and 21.08±5.24, 27. 02 ±6. 23 and 24.27 ±5.79, 3454 ±1050 and 3635±1300, respectively. Statistically sig-nificant differences were observed between the parameter values of the two products in C max and T max;whereas there was no statistically significant difference between AUC_{0 -∞} μg°h°L^-1 (3601 ±1095 and 3767 ±1399). The relative bioavailability for T was 97.28% ± 12.74%.CONCLUSION: The test telmisartan capsule is bioequivalent to the reference tablet.

Experimental study of effects of tetramethylpyrazine on Lewis lung carci-noma in mice

WANG Wen-wu, DAI Xi-hu, OUYANG Xue-nong

2005, 10(4):  421-423. 

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AIM: To study the therapeutic effects of tetramethylpyrazine (TMP) in mice and possible mecha-nism. METHODS: The mice with Lewis lung carcinoma was used as a model for observing the therapeutic effect, the immunomodulatory functions, changes of quality of life, and adverse reactionsof TMP. RESULTS: TMP in-hibited the growth of tumor, and increased life quality and the immunity of mice with Lewis lung carcinoma. CONCLUSION: TMP have therapeutic effects in mice with Lewis lung carcinoma. Its mechanism might be associated with improving the immunity of mice with Lewis lung car-cinoma.

Influence of estrogen on metabolism and antioxidative functions in old cas-trated female rats

ZHANG Shao-ying, PING Jie, WANG Hui

2005, 10(4):  424-427. 

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AIM: To investigate the influence of di-ethylstilbestrol on metabolism and antioxidative functions in old castrated female rats in order to elucidate the physi-ological and pharmacological effects of estrogen therapy in climacteric. METHODS: The old female rats had been castrated, liver drug-metabolizing enzyme activities and antioxidative indexes were measured in rats treated with andwithout diethylstilbestrol (100 μg°4kg^-1, qd×40 d, ig). RESULTS: The activities of microsomal NADPH-Cyt C reductase, benzphetamine N-demethylase, aminopyrine N-demethylase, glutathione S-transferase, and the contents of microsomal cytochrome P450, cy-tochrome b₅ and homogenate glutathione remarkable de-creased in the liver of castrated female rats. Meanwhile, an increase of liver malondialdehyde content was also ob-served. Treatment with diethylstilbestrol could reverse the changes of above indices except for cytochrome b₅. CONCLUSION: The decreased metabolism and antioxidative functions are related to the lower level of estrogen in old castrated female rats.Estrogen plays a significant role in keeping normal metabolism and antioxidative capacities of the liver.

Effects of combination of ketamine and N-acetylcysteine on brain damage following cerebral ischemia /reperfusion in mice

YU Xi-chong, CHEN Xian-yan, ZHOU Hong-yu, LIN Dan, ZHU Tong-jun

2005, 10(4):  428-431. 

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AIM: To evaluate the effects of the com-bination of ketamine (KT) and N-acetylcysteine (NAC) on damage following cerebral ischemia/reperfusion in ICR mice. METHODS: Male ICRmice were randomly divid-ed into seven groups:Sham group, NS (saline 0.1 ml°kg^-1) group, KT (15 mg°kg^-1) group, NAC (75 mg°kg^-1) group, NAC+KT (75+15 mg°kg^-1) group. (1) ICR mice underwent two hours cerebral ischemia by transient right middle cerebral artery occlusion (tMCAO) and followed 6 h and 24 h reperfusion. Then brainswere prepared for the determination of the infarction volume. Before the death, neurological deficits were scored. (2) ICRmice subjected to five minutes ischemia by two com-mon carotid arteries occlusion (2-VO) and followed 0.5, 2 and 6 h reperfusion.Brains were prepared for the deter-mination of the activities of superoxide dismutase (SOD), glutathione peroxidase (GSH-Px) and the content of MDA.RESULTS: (1) tMCAO produced severe neuro-logical deficits, decreased the average score and brought about large infarction volume. KT, NAC showed the im-provement of the average score and reduced infarction vol-ume to some extent, and KT +NAC improved significant-ly. (2) The content of the MDA, the activities of GSH-Px and SOD in 2-VO mice deteriorated sharply, KT, NAC reduced the content of the MDA, enhanced the ac-tivities of GSH-Px and SOD, NAC +KT significantly ameliorated the levels of MDA, increased the activity of SOD and GSH-Px. CONCLUSION: The damage of cerebral ischemia/reperfusion leads to the decrease of neurological score, the increase of infarction volume, the reduction of activities of SOD and GSH-Px and the eleva-tion of MDA.KT and NAC partly relieve the damage, and NAC and KT in combination attenuates the damage more effectively.

Cardioprotective effects of magnesium gluconate on myocardial ischemia reperfusion injury in rats

ZHANG Ying, Qi Zhi-min, GUO Lei, GAO Dong-ming, WANG Hua-zhou

2005, 10(4):  432-435. 

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AIM: To observe the effects of magne-sium gluconate on myocardial ischemia reperfusion injury in anesthetized rats and to investigate the cardioprotective effects of magnesium gluconate. METHODS: The im-proved model of myocardial ischemia reperfusion injury in anesthetized ratswas adopted. Na⁺-K⁺ -ATPase activity, malondialdehyde (MDA) and Ca²⁺ contents in myocardi-um were assayed.The platelet aggregation AGG(M) and Mg²⁺ in blood serum were assayed at the same time. RESULTS: Na⁺ -K⁺ -ATPase activity decreased and MDA and Ca²⁺ contents increased in the ischemia reperfusion group compared with sham.The AGG(M) and Na⁺ -K⁺ ATPase activity increased, and MDA and Ca²⁺ contents and AGG (M) decreased in the three different dosages group of magnesium gluconate comparedwith the ischemia reperfusion group.The cardioprotective effects increased with the dose increasing of magnesium gluconate. CONCLUSION: Magnesium gluconate has protective effects on myocardial ischemia reperfusion injury in rats.It may be related to increasing the activity of Na⁺ -K⁺ -ATPase, and to relieving calcium overload and inhibiting lipid per-oxidation and platelet aggregation.

Effects of C-reactive protein on artery relaxation in LDLr(-/-), db/db (+/ ?) and eNOS mice

CHEN Xiao-liang

2005, 10(4):  436-442. 

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AIM: To determine whether CRP is rele-vant to pathological arterial smooth muscle and to investi-gate both aorta and carotid arteries response to CRP in LDLr(-/-), eNOS(-/-) and db/db(+/ ?) mice arteries.METHODS: CRP was added in these kinds of arterial rings in order to check arterial tension response. Tension was recorded in isolated rings of aorta and carotid arteries taken from low-density lipoprotein receptor gene knockout mice, endothelial nitric oxide synthase knockout mice (eNOS(-/-) mice), diabetes mellitus mice (db/db+/ ? mice) and the corresponding wild -type strain.RE-SULTS:CRP relaxed aorta and carotid artery by phenyle-phine or prostaglandin F2α(PGF 2α) in normal mice, LDLr(-/-), eNOS(-/-) and db/db(+/ ?) mice.CRP relaxed aorta to (90±2) %and carotid to (54±3) %in LDLr(-/-), aorta to (74 ±2) % and carotid to (38 ± 4) %in eNOS, aorta to (47±6) %and carotid to (52± 8) % in db/db(+/ ?), and aorta to (66 ±8) % and carotid (32 ±4) %in normal mice. CRP-induced vessel dilation was abolished in carotid impaired endothelium, but not in aorta. CRP relaxed aorta, and carotid in LDLr (-/-) mice better than others.CRP only relaxed (9 ± 4) %in carotid endothelium damaged and relaxed (58± 4) % in aorta endothelium damaged. CONCLUSION: CRP is a very strong vascular muscle relaxation similar to NO.Its effect time is similar to that in NO. It is similar to normal mice arteries in CRP relaxing aorta and carotid, and independent of and depend on endothelium to dilate artery smooth muscle.

Effects of active ingredient of soybean isoflavoneson on PC12 cell injuries induced by H₂O₂

CHEN Wei-qiang, ZHAO Yu-hong, LUO Shao-hong, YANG Hong, JING Gui-fang, PAN Wei

2005, 10(4):  443-446. 

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AIM: To explore the effects of active in-gredient of soybean isoflavones on PC12 cells injuries in-duced by H₂O₂. METHODS: Active ingredients of soy-bean were extracted and purified.PC12 cells cultured in vitro was pretreated by different dosage of the ingredients about 12 hours and then injured by H₂O₂ (10 mmol°L^-1). Cell viability rate in all groups was tested by MTT assay. Activity of LDH of all groupswas tested. RESULTS: The viability rates in all groups pretreated was significantly increased compared with only H₂O₂ treat-ment group (P<0.05). The activity of LDH in all pre-treatment group was significantly decreased (P<0.05) compared with H₂O₂ treatment group.CONCLUSION: Active ingredient of soybean isoflavoneson can restrain cy-totoxicity induced by H₂O₂ and protect cells from peroxy-dation.

Determination of biological activity of atranticance by orthogonal test

LE Jia-jing, LI Zhan-jun, XU Kang-sen

2005, 10(4):  447-450. 

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AIM: To develop a method for determi-nation of the biological activity of atranticance. METHODS: The conditions of the experiment were determined by orthogonal test, then IC 50 which was the concentration of the sample when the 50% death of cells was tested. RESULTS: The mortality rate had a good correlativity with Log consistency of the sample, (r =0.9515, P<0.01). And the coefficients of variation of reproducibility of intra-, inter and different test assays were 12.3%, 16.6% and 17. 8%, respectively. CONCLUSION: Thismethod is superfine, simple and highly reproducible. It can be used for determining the biological activity of a-tranticance.

Efficacy and safety of fuyantai pellets in treatment of patients with chronic pelvic inflammation

ZHANG Qiong, XUN Cai-qin, JIANG Kun

2005, 10(4):  451-455. 

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AIM: To evaluate the clinical efficacy and safety of the fuyantai pellets in treatment of patients with chronic pelvic inflammation.METHODS: 222 sub-jects were involved in a multi-center, randomized, dou-ble-blinded, double-simulation, and positive drug paral-lel-controlled clinical trail. 113 patients were enrolled in the fuyantai-pellets group, while 109 cases were enrolled in the control group.RESULTS: The total effective rate in fuyantai pellet group was better than that in the control group (P<0.05). CONCLUSION: Fuyantai pellets is an effective and safe drug in treatment of patients with chronic pelvic inflammation.

Effects and mechanisms of epidermal growth factor receptor of tyrosine kinase on cancer

WU Nan, WANG Ai-ping, WANG Yin-xiang

2005, 10(4):  456-461. 

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AIM: To investigate the effects and mechanisms of BPI-2009, an orally active inhibitor of EGFR (Epidermal Growth Factor Receptor) tyrosine ki-nase on cancer therapy, and evaluate BPI-2009 as an an-ti-cancer drug targeting EGFR.METHODS: The tyro-sine kinase inhibition and the EGFR autophosphorylation inhibition of BPI-2009 were detected by Western Blot analysis.Cell growth inhibition was determined by MTT assays.In vitro tumor xenografts studies were tested in nude mice carried with A431 epidermoid tumor xenografts.RESULTS: BPI-2009, a leading com-pounds, was a potent inhibitor of EGFR kinase with an IC 50 of 5 nmol°L^-1 (completed inhibitory concentration at 62.5 nmol°L^-1), and it had no inhibitory activities a-gainst Abl, Abl-related gene (Arg) and c-Src tyrosine ki-nases at 100 nmol°L^-1. BPI-2009 blocked EGFR-medi-ated intracellular tyrosine phosphorylation (IC₅₀ 45nmol°L^-1) in the human epidermoidA431 carcinoma cell line.In cell proliferation assays, tumor cell growth was inhibited by BPI-2009 in the presence of FCS.In studies of nude mice which carried human-derived tumor, BPI-2009 produced significant and dose-dependent anti-tumor effects (human epidermoid A431 carcinoma). When oral-ly administered 100 mg°kg^-1 BPI-2009 once a day, total 24 days in mice, there was no mortality or obviously body weight loss during the treatment. CONCLUSION: BPI-2009 isan selective anti-cancer drug targeting EGFR tyro-sine kinase.

Pharmacokinetics and relative bioavailability of ribavirin in Chinese healthy volunteers

GAO Na, GUO Yu-zhong, QIAO Hai-ling, JIA Lin-jing, ZHANG Li-rong, ZHANG Qi-tang, TIAN Xin

2005, 10(4):  462-465. 

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AIM: To study the pharmacokinetics and bioavailability of ribavirin in 18 young healthy volunteers.METHODS: The ribavirin concentrations in plasma were determined by HPLC after a single oral dose of the stan-dard formulation and the tested formulation which were re-spectively given to 18 volunteers in randomized cross-over test. RESULTS: The concentration-time curves of three formulations fitted to one-compartment open model. The C max were 0.76 ±0.37, 0.72 ±0.22 and 0.76 ±0.40 mg°L^-1;T_max were 2.07±0.89, 1.67±0.49 and 1.86 ±0.41 h;T_1/2ke was 22 ±3, 24 ±4 and 22 ±4 h; $AUC^{t}_{0}$ were 12±4, 14 ±4 and 12 ±4 mg°h°L^-1;and $AUC^{∞}_{0}$ were 16±5, 18±5 and 15±5 mg°h°L^-1 in a standard formulation and two tested formulations, respec-tively. The pharmacokinetic parameters showed no signifi-cant difference among three formulations (P>0.05). The relative bioavailability of two tested formulations was (112 ±21) % and (100 ±18) %.CONCLUSION: The two tested formulations are bioequivalent with refer-enced formulation.

Analysis of utilization of antihypertensive drugs

ZHOU Si-xi

2005, 10(4):  466-470. 

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AIM: To investigate the clinical utiliza-tion of antihypertension agents in a hospital. METHODS: By the method of retrospective study, 301 medical records (286 was selected) of discharged patients with hypertension who were admitted from June 2003 to June 2004 were investigated.RESULTS: The angiotensin converting enzyme inhibitors (ACEI) and calcium antago-nists were used with the highest frequency, and the use frequency from high to low listed as enalapril, metoprolol, felodipine, benazapril and losartan.All drugs were ad-ministrated in combined therapy. CONCLUSION: The usage of antihypertensive drugs is rational in this hospital, and the tendency of drug utilization is similar to interna-tional standard.

Cost-effective analysis about treatment of azithromycin and levo-ofloxacin in suspected SARS patients

YUAN Jian-zhang, DENG Zhe-tong, YANG Xiu-wen, WANG De-xi, WANG Xiong-wen

2005, 10(4):  471-474. 

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AIM: To explore the cost-effective quali-ty about the treatment of azithromycin and levo-ofloxacin in suspected contagious atypical pneumonia (SARS) pa-tients.METHODS: Azithromycin and levo-ofloxacin were administered intravenously and orally, respectively. All suspected SARS patients (n =75) were divided into three groups according to their responses to the therapy: clinically diagnosed patients (group A, n =18), clini-cally excluded patients (group B, n =51), and patients with suspected bacterial pneumonia (group C, n =6). Duration of fever, temperature at admission, time of fever reduction, duration of hospitalization and total expenditure were recorded for each patient. RESULTS: There were no differences (P>0.05) in age and temperature at ad-mission between SARS group (group A) and non-SARS group (group B and C). 51 patients were excluded from SARS after 3-day treatment. The duration of hospitaliza-tion in non-SARS group was significantly shorter than that of group A (8.0 ±4.0 days vs 13.4 ±4.8 days, P<0.01), and the total medical expenditure of the former was markedly lower than that of the latter (4973 ±3410 yuan vs 7363±2835yuan, P <0.01). All patientswere restored well. A follow-up study showed that no patients of non-SARS group were misdiagnosed. The therapeutic expenditure for all 3groupswas far lower than the average cost for SARS and suspected SARS patients of Guangzhou City. CONCLUSION: Treatment with intravenous ad-ministration of azithromycin and oral administration of lev-o-ofloxacin provides an effective method to early exclude the SARS-free patients, and it is cheap according with the basic sanitary hygiene rules.This protocol deserves long-term clinical utilization, investigation and further im-provement.

Explorative clinical trial on effect of relieving pain in treatment of patients with primary acute gouty arthritis by cortex fraxini total coumarin

LUO Mei, LIU Fang, ZOU Jian-dong, YU Jiang-yi, HUANG Li-ji, YE Li-fang, XIONG Ning-ning

2005, 10(4):  475-478. 

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AIM: To evaluate the effect of cortex fraxini total coumarin on relieving pain in treatment of pa-tients with primary acute gouty arthritis which belongs to the sign of dampness obstructing connecting vessel of TCM. METHODS: Cortex fraxini total coumarin was in-volved in a randomized, double-blind, placebo parallel control, dosage-reaction design and superiority test. The total case number of observed primary acute gouty arthritis with the sign of dampness obstructing connecting vessel was 109, which included 36 cases of low-dosage group, 36 cases of high-dosage group, and 37 cases of control group.RESULTS: After 5 day-treatment of cortex fraxini total coumarin, both the evaluation of patients on the im-provement of joint pain grades and the appraisement of physicians on relieving joint tenderness were superior to those in the placebo group, and they were in a dosage-re-latedmanner.But the disappearance rate of joint pain and joint tenderness had no difference between two groups. CONCLUSION: Cortex fraxini total coumarin has some-what pain relieving effect on acute gouty arthritis.

Design of dose titration in clinical trial of new drug

ZHENG Qing-Shan, SUN Rui-Yuan

2005, 10(4):  479-480. 

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Titration to optimal effect is the central principle in the treatment of diseases with medications, and an important approach for the study of dose-response relationship.This paper lists different types, characteris-tics and important pointsin the design.An example of ro-suvastain calcium is given by the design in clinical trail.