Table of Content

Volume 11 Issue 6
26 June 2006

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Overview and research progress of dipetidyl peptidase I

YANG Ya-bin, YUAN Sheng-tao, ZHANG Lu-yong

2006, 11(6):  601-605. 

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Dipeptidyl peptidase I (DPPI), a lysosomal cysteine proteinase also known as cathepsin C, functions as a key enzyme in the activation of many granule serine proteases in the granules of activated cytotoxic T lymphocytes and natural killer cells (granzymes A and B), mast cells (chymase and tryptase), and neutrophils (cathepsin G, proteinase 3 and elastase).It is well established that DPPI-deficient mice have severe defects in serine protease activities in these hemopoietic lineages.In light of the present investigators'work regarding the important role of DPPI-dependent effector on mechanisms in several human pathophysiological processes, the development of selective DPPI inhibitors would provide an important therapeutic tool in the treatment of immune inflammation lymphoma-related diseases.

Advances in cannabinoid receptor 1 antagonistic effect in obesity

PANG Xiao-yi, DONG Zhi, FU Jie-min

2006, 11(6):  606-609. 

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Obesity which is harmful to human health has become epidemic all over the world.Nowadays, it is reported that cannabinoid receptor 1(CB1-R) is significantly associated with obesity.CB1-R belongs to g-protein coupled receptors(GPCRs).Its distribution and genetic structure have been identefied.Recently it is reported that CB1-R antagonist can regulate energy metabolism and reduce body weight through central and peripherial gateways.Meanwhile, it is helpful in treating alcohol, tobacco and drug addiction.At present, rimonabant (SR141716) has already been applied to phase III clinical trial and it can effectively reduce body weight without causing serious adverse effects.Therefore, CB1-R antagonist can be a better choice for treating obesity in the near future.

Effect of sodium-calcium exchanger and its inhibitors on arrhythmia

SHEN Lei, WU Yu-lin

2006, 11(6):  610-613. 

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In cardiomyocytes, sodium-calcium exchanger (NCX) is regarded to play an important role in the regulation of intracellular Ca²⁺concentration.During the cardiac ischemia reperfusion or cardenolide intoxication, the inflow Ca²⁺through NCX reverse mode induce calcium overload and arrhythmia.Recently, the benzyloxyphenyl derivatives have been developed as selective NCX inhibitors, which may have therapeutic potential as a new remedy for arrhythmias.

Recent advancement in pharmacological effects of artemisinin and its derivatives

GUO Yan, WANG Jun, CHEN Zheng-tang

2006, 11(6):  615-620. 

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Artemisinin, an active compound extracted from Artemisia annua, L.together with its derivatives are widely used as anti-malarial drugs.In recent years, artemisinin and many of its analogs were reported to possess some other effects such as anti-inflammatory, immuno-modulation and antitumor activities besides antiparasitic actions against Plasmodium falciparum and Schistosoma.Based on an introduction of the conventional actions and mechanisms of these drugs, we reviewed the recent progress of their new biological actions in this article.

Determination of antipyrine in plasma by reversed phase high-performance liquid chromatography

YANG Hai-feng, HU Yi-yi, JIANG Shan-xiang

2006, 11(6):  621-624. 

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AIM: To establish a reversed phase highperformance liquid chromatography method for the determination of antipyrine in plasma.Methods: Plasma samples were prepared with acetonitrile.The chromatographic separation was performed on a Kromasil C18 column at column temperature of 30 ℃.The mobile phase, a mixture of 0.025 mol·L^-1 aqueous solution of sodium acetate and acetonitrile (74:26, v v), was delivered at a flow rate of 0.8 ml·min^-1.The detection wavelength was 254 nm and the sample size was 20 μl.Results: Excellent line relationship was obtained in the range of 0.1 to 30 μg·ml^-1 (r=0.9995).The average recovery rate was 93.44%-97.21%.The intra-day and interday coefficients of differentiation were both less than 4.26%.CONCLUTION: The method is simple, accurate and can be used for studies on the model of antipyrine pharmacokinetics.

Expression of PER2 protein in hypertrophic myocardium and aorta of hypertensive rats

DING Yan-kui, HUANG Jian-zhai, ZHANG Li, ZHONG Xiao-hua, LI Qing-ping

2006, 11(6):  625-628. 

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AIM: To explore the expression of PER 2 (Period 2) protein, one clock protein, in aorta and myocardiums from Sprague-Dawley(SD) rats and spontaneous hypertensive rats(SHR).Methods: Spontaneous hypertensive rats and SD rats were housed in a dark room for 36 h, followed by a strict 12 h light 12 h dark cycle regimen for 2 weeks (lights on at 09:00, zeitgeber time [ZT] 0).On the day of experiment, rats were sacriticed every 4 h.The expression of PER 2 protein was detected by Western blot analysis.Results: PER 2 protein expression exhibited a rhythm of approximately 24 h in normal myocardium and aorta, and its expression in hypertrophic myocardium and aorta also exhibited this rhythm. However, PER 2 protein expression of SHR was significantly higher than that of normal rats.Conclusion: There might be a positive relationship between hypertension-induced myocardial hypertrophy and aortal disorder and the enhancement of expression of clock protein.

Clinical evaluation of prescription salvia miltiorrhiza and ginkgo biloba in treating hyperlipemia

HE Guo-rong, QI Bei, YU Li-ping, HU Wen-li, DU Guan-hua

2006, 11(6):  629-633. 

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AIM: To compare the curative effect of simvastatin, xuezhikang and prescription of salvia miltiorrhiza and ginkgo biloba (SMGB) in hyperlipemia.Methods: Three hundred and ten patients with hyperlipemia were randomly divided intofour groups.Patients in the placebo group (n=30)were administered 2 capsules thrice daily.Patients in simvastatin group (n=50) were given 20 mg of the drug at bed time.Patients in xuezhikang group (n=50)were administered 2 capsules of the drug twice daily.Patients in the prescription of SMGB group (n=180)received 2 tablets of the drug twice daily.The course of treatment in each of the 4 groups lasted 12 weeks.Seventy patients in the prescription of SMGB group were treated for 24 weeks.Results: Of one hundred and eighty patients in the prescription of SMGB group, total cholesterol (TC)and triglyceride (TG)were decreased significantly.Low-density lipoprotein (LDL-C) was decreased similarly compared to the other two groups. High-density lipoprotein (HDL-C)was elevated as treatment time was prolonged.Conclusion: The prescription of SMGB has curative effect and safety comparable to xuezhikang and simvastatin.The side effects were minimal even after treatment with prescription of SMGB for half a year.

Effect of levcromakalim on ET-1 induced proliferation and expression of protein kinase C in vascular smooth muscle cells

HUANG Wen-xin, MO Bi-wen, YANG Yao-zhong, FANG Chun-sheng, XIA Zhong-hua, PAN Di-hua, XU Tong-tong, MO Xin-ling

2006, 11(6):  634-639. 

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AIM: To observe the effect of levcromakalim (Lev) on endthelin-1(ET-1) induced proliferation and the expression of protein kinase C (PKC) in cultured rat vascular smooth muscle cells (VSMCs).Methods: VSMCs were isolated from rat aorta and were cultured with different concentrations of Lev in vitro after stimulated to proliferation by ET-1(10^-8mol·L^-1). Vitality of VSMCs was detected by MTT;DNA replication was evaluated by 3H-TdR method.Flow cytometry was used to analyze cell cycle and apoptosis.The expression of PKCαprotein and mRNA were determined by Western blot and reverse transcription-polymerase chain reaction (RT-PCR).Results: Vitality of VSMCs and 3H-TdR intermingle rate were decreased (P<0.05) in a dose dependent manner which indicated Lev inhibited VSMCs proliferation by inducing ET-1.Levcromakalin increased the ratio of VSMCs apoptosis (P<0.01).The cell cycle was blocked at G0 G1 phase by Lev in a dose dependent manner (P<0.05).Levcromakalim decreased the expression of PKCαprotein and mRNA in VSMCs (P<0.05).Conclusion: Levcromakalim inhibits VSMCs proliferation by inducing ET-1 through reducing the expression PKCα.

Inhibitory effects of carboxymethyl-chitosan on proliferation and in vitro metastatic ability in human highly metastatic lung carcinoma 95-D Cells

YANG Jing-ya, LIU Jian-wen, LIU Cheng-chu, CHEN Bi-wen

2006, 11(6):  640-643. 

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AIM: To study the inhibitory effects of carboxymethyl-chitosan on proliferation and metastatic ability in human highly metastatic lung carcinoma 95-D Cells.Methods: The inhibitory effect of carboxymethyl-chitosan on the migration of 95-D cells was tested by cell migration assay.Cell invasion was analyzed by the matrigel invasion assay.Soft agar colony formation assay and adhesion assay were also used to evaluate the suppression of carboxymethyl-chitosan on 95-D cells.Results: Carboxymethyl-chitosan dose-dependently inhibited the soft agar colony formation, migration, invasion, adhesion and proliferation of 95-D cells.Conclusion: Carboxymethyl-chitosan can significantly repress the proliferation and in vitro metastasis of 95-D cells.

Apoptosis induce effect of epristeride on benign prostatic hyperplasia model cells in vitro

JIANG Zhen-zhou, SHU Wen-hui, ZHANG Lu-yong, YAN Ming, SUN Li, WANG Guang-Ji

2006, 11(6):  644-649. 

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AIM: To establish a benign prostatic hyperplasia (BPH) cells model in vitro and investigate the mechanism of epristeride to BPH cells based on this model.Methods: Establishing the primary cultural process of rat prostatic cells.In order to stimulate proliferation of the prostatic cells we simulated the pathophysiological environment and added testrone and polypeptide growth factors (PGFs) into the culture medium.MTT reduction assays were used to observe the inhibition effect of epristeride on BPH model cells in vitro.and the apoptosis induce effect of epristeride was observed by flow cytometry (FMC).Results: In comparison with normal group, the density of BPH model cells was significantly increased by the stimulation effect of testrone (9.08×10^-8mol·L^-1) and PGFs after 9 days;the content of prostate specific antigen in culture medium was increased compared with normal group.The IC₅₀ values of Epriteride to BPH model cells in vitro is 5.0×10^-6mol·L^-1;The cell apoptosis peak was demonstrated by FMC assay.Conclusion: BPH model cells can be establish in vitro by the stimulation of testrone and PGFs;epristeride can induce apoptosis of BPH model cells in vitro and this mechanism is probably the therapeutical effect in clinical use of epristeride.

Quick method for simultaneously establishing hepatic fibrosis and hyperlipemia double diseases model in rats

LIU Gui-liang, GAO Li-zhong, LANLAN Xiu-zi, CHEN Ding-ding

2006, 11(6):  650-654. 

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AIM: To establish a relatively simple but reliable rat model of liver fibrosis.Methods: A mixture composed of ethanol (60%)、lard (5 g·kg^-1) and cholesterol(1 g·kg^-1) was supplied in a concentration of 15 ml·kg^-1·d^-1 for one month.Animals are concurrently supplied a normal diet.Results: Biochemical analysis and polarization microscopy combined with image analysis liver sections stained with F3B Sirius red revealed that the whole collagen quantity and type Ⅰ collagen in mixturetreated rat livers were increased very significantly than those of control group.Tissue pathological assay revealed middle to heavy degree cellular swelling and obvious sinus hepaticus hyperaemia in liver.Real time PCR assay showed that type Ⅳ collagen gene expression in model rat liver was very significantly elevated than that of normal rat.The triglyceride contents of liver and blood in model rats were significantly elevated than those of normal control rats.Conclusion: The model provides a convenient method for the production of liver fibrosis and hyperlipemia, and it may be useful for the study of the medicines treating hepatic fibrosis adiposis-hepatca and hyperlipemia.

Construction of eukaryotic expression vector expressing double shRNA sections targeting Survivin gene in Bx-PC3 cells

HUANG He, WU Pei, HONG Shu-jian, MAO Jia-ding, RUI Jing

2006, 11(6):  655-658. 

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AIM: To construct eukaryotic expression vector expressing double shRNA sections targeting Survivin gene.Methods: Eukaryotic expression vector expressing double shRNA sections targeting Survivin gene were designed and chemically synthesized.They were directionally inserted into plasmid pGenesil-1 with respectively U6 promoter and termination code, the common green fluorescence protein (EGFP) gene and Neo gene. In this way, the vector of pGenesil-1 shRNA containing 2 sections of Survivin shRNA were constructed and they were transfected into the pancreatic cancer cell Bx-PC3. Transfection was detected by fluorescence microscope. The inhibition expression of Survivin mRNA was measured by RT-PCR.Results: HE1 and HE2 plasmids were identified by the biocatalyst cut which confirmed the exactitude and were analyzed by the sequence analysis which verified the perfect clone plasmid inserted by them.Conclusion: A eukaryotic expression vector of double short hairpin RNA for Survivin gene is successfully constructed.The pancreatic cancer cells Bx-PC3 succeed to be transfected and expression of Survivin mRNA is inhibited obviously.

Protective effects and mechanism of low dose aspirin on focal cerebral ischemia-reperfusion rats

QIU Li-ying, YU Juan, ZHOU Yu, CHEN Chong-hong

2006, 11(6):  659-664. 

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AIM: To investigate the protective effects and the mechanism of low dose aspirin on focal cerebral ischemia-reperfusion rats.Methods: Right middle cerebral artery was occluded by inserting a thread through internal carotid artery for 2 h, and then reperfused for 24 h.6 mg·kg^-1 dose of aspirin was intragastric administered at reperfusion 0 and 6 h.The brain injuried area, the neuronal density, the numbers of apoptotic cells and the ratio of Bcl-2 protein and Bax protein from occluded brain were estimated.The ratio of prostacyclin (PGI₂) and thromboxane (TXA₂) in plasma, the contents of malondialdehyde (MDA), adenosion 5'-triphosphate (ATP) and myeloperoxidase(MPO) in brain tissue from the occluded side were assayed.Apoptosis was measured in paraffin sections with TUNEL method.Bcl-2 and Bax were detected by immunohistochemical staining method.Adjacent sections were stained with hematoxylin and eosin, and neuronal density subfield was counted.The contents of PGI₂ and TXA₂ in plasma were measured by ¹²⁵I radioimmunoassay method.The content of MDA and MPO in brain tissue was determined by biochemical method.The content of ATP in brain tissue was separated by capillary electrophoresis.Results: The injuried area of brain occluded side was dramatically reduced after 6 mg·kg^-1 dose of aspirin was intragastric administrated.Most of neurons in the injuried regions survived ischemia-reperfusion result when 6 mg·kg^-1 dose of aspirin was given, where as most of vehicle group neurons were lost without aspirin treatment.The numbers of apoptotic cells were dramatically reduced by 6 mg·kg^-1 dose of aspirin.The ratio of Bcl-2 and Bax was increased by aspirin.The ratio of PGI₂/TXA₂ in plasma was increased by aspirin.In brain tissue of occluded side, no significant change between 6 mg·kg^-1 and vehicle groups in MDA content, ATP level, and MPO content were discovered.Conclusion: The neuroprotective effects of low dose of aspirin on focal cerebral ischemia-reperfusion rats might be attributed to its effects by increasing the ratio of PGI₂/TXA₂, inhibiting apoptosis and improving the ratio of Bcl-2 Bax.

Protective effects of ligustrazine and sodium hyaluronate and contrast study on rabbit's postoperative pericardial adhesion

HAN Lian-he, CHEN Teng, FENG Guo-qing

2006, 11(6):  665-668. 

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AIM: To evaluate the protective effect on rabbit's postoperative pericardial adhesion of ligustrazine and sodium hyaluronate on adhesions, pathological histology, fibrinogen and white blood cells.Methods: Rabbits were randomly divided intofive groups, 24 rabbits were used to make model with pericardial adhesions tofour groups.Sodium hyaluronate group was injected with 5 mg sodium hyaluronate to pericardial cave of each rabbit after the operation;ligustrazine group was injected 6.7 mg·kg^-1 ligustrazine to vein after the operation, qd, 7 d enough;equal quantity of normal saline was injected in model group and sham operation group.The rabbits were sacrificed 20 days later.Adhesions tissues and pathological morphous were observed and analysis were done, FIB and WBC were tested at 7 d time point.Results: Pericardial adhesions and fiber hyperplasia were significant in model group.Compared with sham group, the concentration of FIB and the amount of WBC were obviously increasing (P<0.01).Compared with model group, sodium hyaluronate group and ligustrazine group could significantly reduced the concentration of FIB(P<0.01).There was no statistical meaning between sodium hyaluronate group and ligustrazine group (P>0.05).Conclusion: These results demonstrate that sodium hyaluronate and ligustrazine can effectively prevent postoperative pericardial adhesion.The protective effect is, to some degree, related to the inhibition of FIB and WBC.

Experimental study on effect of Tetrastigma hemsleyanum Diels et Gilg flavone on inducing apoptosis of SGC-7901 cell line iv vitro

FENG Zheng-quan, NI Ke-feng, HE Yu, DING Zhi-shan, ZHU Feng, WU Liang-cun, SHEN Min-he

2006, 11(6):  669-672. 

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AIM: To study the effect of Tetrastigma hemsleyanum Diels et Gilg flavone (TDGF)on inducing SGC-7901 tumor cell apoptosis and to approach its mechanism.Methods: MTT assay was carried out to evaluate TDGF's activity;cell morphology change was monitored through optical microscope and electron microscope; cell apoptosis was detected by flow cytometry with Annexin Ⅴ PI staining assay;the concentration of MMP-2 protein in the supernatant of tumor cell culture was also measured by zymography essay.Results: Tetrastigma hemsleyanum Diels et Gilg flavone inhibited SGC-7901 cell proliferation in a concentration-related manner, and SGC-7901 cells had the characteristic changes of apoptosis in morphology.Tetrastigma hemsleyanum Diels et Gilg flavone could also down-regulate the concentration of MMP-2.Conclusion: Tetrastigma hemsleyanum Diels et Gilg flavone promotes tumor cell apoptosis significantly, which may be related to down-regulating the expression of MMP-2.So TDGF is a new promising anti-tumor TCM drug.

Effect of chlorotoluron system on the testis of mice

MU Hong, ZHANG Ping, YANG Sheng-ying, XU Jian

2006, 11(6):  673-676. 

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AIM: To study the effect of chlorotoluron system on the tesis of mice.Methods: Male mice were contaminated with chlorotoluron by oral for 25 days.Results: It indicated that all doses of herbicide had different changes.It was detected that under the light microscope seminaferous epithelium arrayed loosely and disorderedly, spermatogenic cell shed, layers lessened, while under the electron microscope mitochondria in the seminaferous epithelium appeared vacuolated, karyotheca swelled and bent, the amount of sustentacular cell declined, and part of tight junction destroyed.Conclusion: The trend of degeneration and more seriously pathological changes appeared with increasing doses.

Effects of chloride channel blocker on hypoxia induced rat pulmonary hypertension

MO Bi-wen, ZENG Jin-rong, LI Guo-jian, HUANG Wen-xin, YU Fang, WANG Ji-ying, WANG Chang-ming

2006, 11(6):  677-680. 

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AIM: To investigate the therapeutic effect of chloride channel blocker tamoxifen on hypoxia pulmonary hypertension in rats.Methods: Sixty male Wistar rats were randomly divided intotherapeutic group (H/Q group), hypoxia group(H group), normal control group(C group).Mean pulmonary artery pressure(mPAP), the ratio of the weight of right ventricle to that of left ventricle plus septum[RV(LV+S)], and the ratio of the pulmonary arteriole wall area to that of vascular total area(WA/TA), were measured at 4, 7, 14, 21 days.Results: The mPAP began to increase from 7 days, and reached peak at 21 days in hypoxia group, however it is obviously lower in therapeutic group at same time.The ratio of RV/(LV+S) began to increase from 14 days, and reached peak at 21 days in hypoxia group, however it is obviously lower in therapeutic group at same time.The ratio of WA/TA at 21 days in hypoxia group was significantly higher than therapeutic group, respectively(P<0.05).The ratio of VA/TA at 21 days in hypoxia group was significantly lower than therapeutic group, respectively (P<0.05).Conclusion: The data suggested Tamoxifen could reduce hypoxia-induced increased pulmonary artery pressure, inhibit hypoxia-induced hypertrophic right ventricle and pulmonary small artery thickness.Tamoxifen may be used in the treatment of hypoxia induced pulmonary hypertension.

Significance of coronary collaterals in patients with acute coronary syndrome

LIU Yan, CHEN Shao-liang, LIU Zhi-zhong

2006, 11(6):  681-683. 

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AIM: To study the relation between development of coronary collaterals and clinical outcome in patients with acute coronary syndrome (ACS).Methods: 251 patients with clinical diagnosed ACS were consecutively enrolled into the present study and divided into two groups according to the presence of coronary collaterals by quantitative coronary angiography (QCA).Serial venous blood samples were collected at admission for determining of high-sensitive C-reactive protein(hs-CRP), brain natriuretic peptide (BNP), and cardiac troponin I (cTnI).Baseline left ventricular ejection fraction(LVEF) was determined by cardiac echo.Results: Coronary collaterals were detected in 38 patients(as CC group), another 213 patients without coronary collaterals were served as control group.Serum levels of cTnI in patients in CC group was significantly higher than in control group(0.91±1.13 vs 0.29±0.23 ng·ml^-1, P<0.01).There was no differences in plasma level of hs-CRP and BNP between two groups (hs-CRP, 5.00±3.67 vs 5.66±3.83 mg·dL^-1;BNP, 828.8±757.6 vs 829.6±784.6 fmol·ml^-1, P>0.05).Serum levels of cTnI in patiemets of CC group was significantly lower than those of control group (0.29±0.23 vs 0.91±1.13 ng·ml^-1, P<0.01).Compared with patients in control group, left ventricular function in CC group was better reserved and improved(0.43±0.11 vs 0.48±0.11, P<0.01).Conclusion: The development of coronary collaterals in patients with ACS contributes to protection of left ventricular function, which is favorable to clinical outcome.

Immunoloregulation effect of SK Royaljelly R-1 in mice

TAN Hu, QIAN Zhi-yu

2006, 11(6):  684-686. 

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AIM: To investigate the effect of SK Royaljelly R-1(SKR)on the innate immunity, humoral immunity, cell immunity in mice.Methods: Observe the effect of SKR on immunity function in mice, the phagocytotic rate and phagocytotic index, haemolysin in serum, plaque forming cell, and the proliferation of splenocyte following administration SKR for 15 days.Result: SK Royaljelly R-1 improved the formulation of serum haemolysin significantly (P<0.01), increased PFC and Il-2 production significantly (P<0.01), and stimulated the splenocyte proliferation stimulated by ConA of normal mice (P<0.01).Conclusion: The results suggeste SKR could potentiate the immunological function of normal mice.

Dosage of insulin treatment on newly diagnosed type 2 diabetics

TANG Ping, YANG Chuan, LI Li, ZENG Ying-juan, DU Jing

2006, 11(6):  687-690. 

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AIM: To study the insulin dosage on newly diagnosed type 2 diabetics.Methods: Thirty-twonewly diagnosed type 2 diabetics were treated by biphasic insulin aspart 30(BIAsp30) (group Asp30, n=20) and Novolin 30R (group Novolin 30, n=12) respectively. The levels of plasma glucose and insulin dosage were evaluated.Results: There were no significant change in fasting plasma glucose and postprandial glucose before treatment in the two groups.After one week's treatment there was no significant change in fasting plasma glucose in both groups, while the postprandial plasma glucose in Asp30 was significantly lower than that in Novolin 30(P<0.05).When the controlling of plasma glucose meets the standard, the time costed in group Asp30 was significant lower compared with group Novolin 30.The maintenance dosages before breakfast and before dinner were also significantly lower in group Asp30 than that in group Novolin 30 (P<0.05) in further observation.Conclusion: It is better to use BIAsp30 than to use Novolin 30R on newly diagnosed type 2 diabetics.

Pharmacokinetic study on compound aluminum sulfate injection after i.v.and in situ administration in rabbits

XU Feng-hua, CHEN Yi-hong, FANG Yi, GAO Xiu-yun

2006, 11(6):  691-695. 

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AIM: To study the pharmacokinetics of compound aluminum sulfate injection after i.v.administration and aluminum absorption after i.m.and s.c. administration in New Zealand rabbits.Methods: Compound aluminum sulfate injection was administrated i.v.to the left-earat the dose of 1 mg·kg^-1, i.m.in quadriceps at the dose of 80 mg·kg^-1 or s.c.under back skin at the dose of 160 mg·kg^-1 (anhydrous aluminum sulfate body weight).Blood samples were collected at different time after injection from the right-ear vein. ICP-MS assay was used to determine the aluminum (Al) concentration.Pharmacokinetic parameters were calculated with DAS program.Results: The blood Al concentration-time profiles after i.v.injection fitted to a twocompartment model, with t_1/2β 1.08±0.46 h and AUC_0-12h1.52±0.92 mg·h·L^-1 (n=5).There was no obvious increase in Al concentration after i.m.injection of 80 mg·kg^-1 or s.c.injection of 160 mg·kg^-1 aluminum sulfate.The average AUC_0-24h of i.m.injection was 2.93±1.82 mg·h·L^-1 (n=5), and that of s.c.injection was 0.88±1.14 mg·h·L^-1 (n=5), corresponding to the bioavailability of i.m.and s.c.injection being about 2.41% and 0.36%, respectively.Conclusion: Blood Al eliminates very quickly.The absorbed Al after i.m.or s.c.injection is very low, suggesting compound aluminum sulfate injection a safe preparation.

In vitro studies of mutant prevention concentration and mutant selective window for staphylococcus aureus and its isogenic mutants strain

LI Zhao-xia, LIU You-ning, WANG Rui, CUI Jun-chang, CHENG Shi-hu, TONG Wei-hang

2006, 11(6):  696-701. 

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AIM: To measure minimal inhibitory concentration (MIC), mutant prevention concentration (MPC) and mutant selection window (MSW) of fluoroquinolones for staphylococcus aureus strain ATCC29213, and isogenic mutants of strain ATCC29213 in vitro,MSW and the capacity of fluoroquinolones for restricting the selection of next-step staphylococcus aureus resistant mutants were evaluated.In the meantime, the emergence and development of fluoroquinolones resistant were observed.Methods: The celles of 1010 colony form units per milliliter staphylococcus aureus were enriched in broth, and theMIC, provisional MPC (MPCpr) and MPC of fluoroquinolones against different strains were determined by agar plates dilution method.Results: The MPCs of moxifloxacin, gatifloxacin, Sparfloxacin, levofloxacin and Ciprofloxacin for staphylococcus aureus strain ATCC29213 were 0.2, 0.3, 0.3, 1.4, 3.2 μg·ml^-1, and the MPC MICs were 6.5, 4.8, 9.7, 11.2 and 12.8 respectively. The MICs of 5 fluoroquinolones for the first-step isogenic mutants were 2-8 folds greater than those of ATCC29213.The MICs of levofloxacin for the secondstep mutants were 8-16 folds greater than those of the first-step isogenic mutants.The MSWs of 5 fluoroquinolones for the mutants were wider than those for its isogenic strain.Conclusion: For staphylococcus aureus strain ATCC29213 and its isogenic mutants, the capacity of moxifloxacin and gatifloxacin for restricting the selection of next-step resistant mutants is stronger than that of sparfloxacin, levofloxacin and ciprofloxacin.The staphylococcus aureus resistance of fluoroquinolones is developed step by step.The emergence of the first-step mutants is more easily to select new mutants.

Clinical evaluation of efficacy of fluticasone propionate/salmeterol in treatment of mild to moderate asthma

XIA Qing, DAI Xing-ling, WANG Ru-tao

2006, 11(6):  702-705. 

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AIM: To evaluate clinical efficacy and safety of seretide in the treatment of patients with mild to moderate asthma.Methods: This was an opened, self-comparison study.43 patients with mild to moderate asthma were given seretide 50 250 μg inhalation twice daily via accuhaler for 20 weeks.The levels of symptoms and signs before and after therapeutics were recorded as the quality of life.The peak expiratory flow (PEF), forced expiratory volume in one second(FEV₁), peak expiratory flow rate(PEFR), forced vital capacity(FVC) and symptomless time were detected.Results: The treatment with seretide resulted in remarkably improvement in efficacy variables of morning and evening PEF, asthma symptom scores.FEV₁ and FVC were notably increased after 1 week of treatment and during the treatment period (P<0.01).At the end of 20 weeks treatment, asthma quality of life scores were improved significantly (P<0.01).The amount of asymptomatic day of patients with mild to moderate asthma were increased.There were 39 patients achieving the criteria for well-controlled.Only 1 patient had hoarseness.Conclusion: Seretide possesses the advantage of effectiveness, safety and well tolerance in patients with mild to moderate asthma.

Clinical observation and research of angiotensin converting enzyme inhibitor and angiotensin Ⅱ antagonist on diabetic renopathy

LUAN Xu

2006, 11(6):  706-708. 

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AIM: Tofind out a more effective therapy to cure diabetic renopathy through observing whether combination of angiotensin converting enzyme inhibitor (ACEI) and angiotensin Ⅱ antagonist (ARB) treatment is more effective than that of using single medicine.Methods: Seventy-two selected patients were divided into three groups in which are ACEI group (representative medicine is monopril, ARB group (representative medicine is valsartan) and ACEI+ARB group (representative medicines are monopril and valsartan.The period of treatment is 8 weeks.The 24-hour uric albumen examination was detected before and after the treatment.Results: No significant difference showed before the treatment (P>0.05).There was significant difference in the decrease of the amount of 24-hour urine protein examination before and after the treatment among three groups.Compared with the single drug group, the effects of the combination group was better.Conclusion: Using monopril or valsartan solely or the combination of monopril and valsartan can decrease the 24-hour urine protein effectively. The effect of monopril and valsartan are same.However, the effect of the combination group was better than the two single drug groups.

Effects of D-galactose on ultrastructure of rats'hypothalamic arcuate nucleus

LUO Hong-mei, CUI Liao, WU Tie

2006, 11(6):  709-711. 

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AIM: To investigate the effects of D-galactose on ultrastructure of rats'hypothalamic arcuate nucleus.Methods: 12 rats at age of 6 months were divided into two groups at random, the control and D-galactose group.Rats of control group were treated with saline solution by sc, and rats of D-galactose group were treated with D-galactose by sc at dose of 100 mg·kg^-1. Three months later the rats were killed by exsanguinating from heart.After being infused into the left ventricle with 2%-2.5% polyformaldehyde at the dose of 50 mg·kg^-1, the brains were taken and immerged in 2.5% polyformaldehyde, then the arcuate nucleus was taken according to the atlas of brain, the tissues taken were made into ultrathin sections to be observed under electron microscope.Results: comparing torats in control group, neurons of the arcuate nucleus of rats in D-galactose group appeared aging, the number of organelle in plasma decreased, but the number of lipochromesome in plasma increased significantly, and the size of neurons decreased also.Furthermore the apoptosis neuron was observed, the chromosome of which congregated around the nucleus'membrane, the typical aging neuron was also observed, the neuraxon of which was atrophying.But there were no obvious changes observed in neurons of the arcuate nucleus of rats in control group, plenty of organelles were observed under electron microscope clearly.Conclusion: Dgalactose can cause neurons of rats'arcuate nucleus aging, the neurons appeared atrophying and apoptosis.

Systemic analysis of the efficacy and safety of Cerebrolysin in the treatment of Alzheimer's disease

WEI Zhao-hui, HE Qing-bo, WANG Hao, SU Bing-hua, CHEN Hong-zhuan

2006, 11(6):  712-716. 

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AIM: To evaluate the efficacy and safety of Cerebrolysin in the treatment of mild to moderate Alzheimer's disease (AD).MOTHODS: Data source: searching the Cochrane Library, Medline, and Chinese Biomedical Literature Analysis and Retrieval System for Compact Disc (CBMDISC) and communicating with EBEWE Pharmaceutical Ltd for the randomized trials comparing Cerebrolysin with placebo in AD.Data extraction: available data on clinical global impression (CGI), cognitive performance and Activities of Daily Living (ADL) were extracted from 5 trails and combined with standard meta-analysis methods.Results: There was some heterogeneity, which was mainly caused by the trial Ruether E (1994), among the 5 clinical trials in this meta-analysis (Q=8.295, P=0.081) Comparing Cerebrolysin with placebo, the estimator of treatment effect (log (OR)) based on the random-effect model was 1.080 (95% IC [0.645, 1.481]).Sensitivity analysis showed that the treatment effect was robust to different models or different estimate methods.In clinical practice, the safety of Cerebrolysin was documented with the incident rate of adverse event as 2%-7%.And the most common adverse events were headaches, dizziness and anxiety.Conclusion: Cerebrolysin is a safe drug that could significantly improve the clinical global impression in patients with mild to moderate AD.

Selection of cooperative unit in large sample and multicenter clinical trial

DAI Guo-hua, ZHANG Bo-li, GUO Zhi-xin, SHANG Hong-cai, ZHANG Jun-hua, ZHAO Min, ZHANG Jun-ping

2006, 11(6):  717-720. 

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Selection of cooperative unit directly influences the progress and quality of clinical trial, so the lead group or responsible unit must strictly monitor.Selecting cooperative unit must consider such aspects as the origin, regionalism and race of subjects, related results of clinical epidemiologic survey, the quantity of cooperative unit required, the condition of cooperative unit to be selected, the attitude to this study of cooperative unit, and so on. The organization and management to cooperative unit must be reinforced and the problems appeared during practice must be dealt with in time, for example, adjusting some cooperative unit, thinking highly of the role of sub-centers, monitoring cooperative hospitals and so on.