Table of Content

Volume 10 Issue 3
26 March 2005

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Progress in research and evaluation on drug-plasma protein binding in pharmacology

GUO Bin, LI Chuan

2005, 10(3):  241-253. 

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Drug-protein binding changes involved in numerous factors in vivo may cause changes of pharmacokinetic parameters.The tendency gained from large numbers of articles overemphasized the clinical importance of these changes.However, theoretic analysis and review of available literature data indicated that changes in plasma protein binding are usually of no principle pharmacodynamic implication.And they have little effect on the clinical exposure of a patient to a drug in a practical sense. The progress is reviewed in research and current opinions on drug-plasma protein binding in pharmacological basis for pharmacokinetic consequence and clinical relevance in this article.

Research progress of non-neuronal acetylcholine systems in endothelium

CHEN Kai, WANG Hai

2005, 10(3):  254-258. 

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ACh widely distributes in non-nervous tissues and cells.The organic cation transporters (OCTs) are involved in the transportation and release of ACh. Wide expressions of AChE in endothelium limit the effects of non-neuronal acetylcholine on the area of its synthesis and release and it makes the non-neuronal acetylcholine be a cytokine.Muscarinic and nicotinic receptors are widely expressed on endothelial cells in comparison with the distribution of non-neuronal acetylcholine.Nicotinic receptors are involved in the synthesis and release of several bioactivity molecules.The α₇ subtype of nicotinic receptors participates in the angiogenesis.Non-neuronal acetylcholine induces the vascular relaxation with intact endothelium.The endothelial target for acetylcholine different from neuronal acetylcholine receptors plays an important role in vascular relaxation, and participates in the progress of atherosclerosis and thrombosis.

Analysis of withdrawal of rofecoxib-cyclooxygenase-2 specific inhibitor

LI Qin, WANG Rui, CHEN Kun

2005, 10(3):  259-264. 

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Rofecoxib, a COX-2 specific inhibitor, is approved for treatment of osteoarthritis, acute pain and primary dysmenorrhea.On September 30, 2004, Merck announced the voluntary worldwidewithdrawal of rofecoxib (Vioxx).This paper reviewed the pharmacological actions of the COX-2 specific inhibitors and the characterization, premarket study, clinical application and side-effects of rofecoxib and analyzed the withdrawal of rofecoxib.

Dynamic changes of ATPases and NOS activities and NO production at different anesthesia phases of thiopental and propofol anesthesia

LIU Hong-liang, DAI Ti-jun, YAO Shang-long

2005, 10(3):  265-269. 

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AIM: To investigate the dynamic changes of ATPases and NOS activities and NO production at different anesthesia phases using thiopental and propofol anesthesia.METHODS: Thiopental of 30 mg°kg^-1 or propofol of 100 mg°kg^-1 was administered respectively at different anesthetic phases (induction, anesthesia, restoration, and awake), the activities of NOS and ATPase and NO production in cortex and brain stem were measured.Saline 10 ml°kg^-1 was injected as the control group.RESULTS: Ca²⁺-ATPase and Na⁺, K⁺-ATPase activities in the cortex and brain stem were significantly decreased after administration of thiopental and propofol, especially at induction, anesthesia, or even restoration phase of thiopental group (P<0.05, P<0.01) and at anesthesia phase of propofol group (P<0.05).NOS activities and NO production decreased from induction to restoration phase with thiopental and propofol anesthesia (P<0.01).The parameters were returned near to the normal at awaken phase.CONCLUSION: Activities of ATPases and NOS and the production of NO may mediate the anesthesia effects of thiopental and propofol in the rat cortex and brain stem.

Assessment of coronary flow velocity pattern during no-reflow phenomenon by transthoracic Doppler echocardiography combined with administration of Albunex

CHEN Li-xin, WANG Xin-fang, XIE Ming-xing, ZHU Xiang-ming, WU Ying

2005, 10(3):  270-275. 

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AIM: To validate the alternations of flow velocity patterns in the infarct-related artery (IRA) during no-reflow phenomenon in a canine model of acute myocardial ischemia and reperfusion by transthoracic Doppler echocardiography (TTDE) combined with myocardial contrast echocardiography (MCE) by means of administration of Albunex.METHODS: Nineteen dogs first underwent 60 min myocardial ischemia and then followed by 60 min, 120 min and 180 min reperfusion (n=6, 6 and 7, respectively).The perfusion defect area determined by MCE at 60 min myocardial ischemia was regarded as risk area (RA_MCE).The perfusion defect area defined by MCE after reperfusion was considered as no-reflow area (NRA_MCE).The ratio between NRA_MCE and RA_MCE ≥25% was regarded as the development of no-reflow phenomenon and the ratio of NRA_MCE to RA_MCE <25% was considered as the myocardial reflow.The coronary flow velocity parameters in IRA were determined through TTDE.RESULTS: Two dogs died during experiment and the remaining seventeen dogs completed throughout the procedure. There were seven dogs in reflow group and ten dogs in noreflow group.No significant difference was present in reflow group between at baseline and at 60 min reperfusion in systolic peak velocity (PVs), systolic velocity time integral (VTIs), corrected systolic flow duration (cFDs), diastolic peak velocity (PVd), diastolic velocity time integral (VTId), corrected diastolic flow duration (cFDd), diastolic deceleration rate (DDR), corrected diastolic deceleration duration (cDDD) (P>0.05), however, a significant difference was found in no-reflow group between at baseline and at 60 min reperfusion in PVs, VTIs, cFDs, PVd, VTId and cFDd (P<0.05).The most marked alterations during diastolic phase were the increase of DDR and reduction of cDDD.CONCLUSION: The impaired microvasculature may profoundly affect the coronary flow velocity pattern in the IRA.The increase in microvascular resistance and decrease in coronary perfused pressure can contribute to the changes. Transthoracic Doppler echocardiography combined with MCE has the capability of noninvasive assessment of coronary flow velocity pattern in the IRA during no-reflow phenomenon.

Antinociceptive effect of choline on inflammatory pain in mice

SU Dong-mei, LIOU Yue, WANG Yue, WANG Ru-huan, WANG Hai

2005, 10(3):  276-280. 

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AIM: To investigate the antinociceptive effect of choline on inflammatory pain.METHODS: Formalin and hot-plate tests were used to study the antinociceptive effect of choline, and observe the synergetic antinociceptive effects of choline and its combination with aspirin or morpine.RESULTS: Early phase (0-5 min) response was induced by an immediate and intense increase in the spontaneous activity of afferent C fibers. Late phase (15-30 min) response was thought to be inflammatory response induced by the release of inflammatory factors after formalin administration.Choline (4, 8, 16, 32, and 64mg°kg^-1, iv) obviously shortened the paw licking time in phase Ⅱ in the formalin test.The conjoint administration of choline 2 mg°kg^-1 and aspirin 9.4 mg°kg^-1 produced a synergistic antinociception effect compared with that administration of choline 2 mg°kg^-1 or aspirin 9.4 mg°kg^-1, respectively.And the phenomenon was also observed on the conjoint administration of choline 2 mg°kg^-1 and morpine 0.165 mg°kg^-1 compared with that administration of morpine 0.165 mg°kg^-1 singly, but synergistic effect on the conjoint administration of choline 4 mg°kg^-1 and aspirin 23.5 mg°kg^-1 did not show obvious significance compared with that administration of choline 4 mg°kg^-1 or aspirin 23.5 mg°kg^-1, respectively.CONCLUTION: Choline can inhibit inflammatory pain induced by formalin.Co-administrations of choline and aspirin, or morpine have prominent synergetic antinociceptive effects.

Pharmacokinetics comparison between 10-hydroxycamptothecin nanoparticle injection and common injection in rabbits

YAN Zhao, JIAO Jian-jie, ZHAO Wen-hua, ZHAO Guo-chen, MIAO Wei, ZHANG Jin, LOU Jian-shi

2005, 10(3):  281-285. 

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AIM: To investigate the pharmacokinetics (PK) of 10-hydroxycamptothec (HCPT) nanoparticle injection iv by comparing with the HCPT common injection in rabbits.METHODS: HCPT in plasma were quantitated by reversed-phase HPLC and UV detector.3p97 software was used in calculation of compartment model and PK parameters.RESULTS: The concentration-time profile of HCPT nanoparticle injection was best described by three-compartment model, and the common injection was described by two-compartment model.Plasma peak concentration (C_max) of HCPT common injection was three times as many as that of nanoparticle injection in equal dosage.Area under curve (AUC) of HCPT common injection was twofold higher than that of nanoparticle injection.Apparent volume of distribution of central compartment (Vc) of HCPT nanoparticle injection was greater than that of nanoparticle injection in equal dosage.HCPT nanoparticle injection had a longer elimination half life (T_1/2β) than that of common injection.CONCLUSIOM: The blood drug concentration and PK characteristic of HCPT nanoparticle injection were very different from HCPT common injection in rabbits.

Effects of paroxetine on psychological stress induced by c-fos gene expression in rat hypothalamus paraventricular nucleus

HUANG Huan-jie, SHAO Bei, ZHENG Rong-yuan, LI Jian-min, YAN Zhi-qin, XIE Li-wei, WANG Zong-min

2005, 10(3):  286-289. 

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AIM: To study the effects of paroxetine on the psychological stress induced by c-fos gene expression in the rat hypothalamus paraventricular nucleus (PVN) and to explore the molecular mechanism of effects of paroxetine on the stress related anxiety disorders. METHODS: The rat psychological stress model was made by restraint stress.The cortisol was analyzed by radioimmnoassay, and expression of c-fos positive cells was detected by S-P immunohistochemical assay in the rat PVN.RESULTS: The level of cortisol 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 reduced the level of cortisol and inhibited the expression of c-fos positive cells in the PVN after psychological stress. CONCLUSION: The paroxetine can regulate the nerve centre by alleviating the expression of the c-fos in the hypothalamus paraventricular nucleus(PVN) and the activation of HPA pathway.

Protective effects of artemisinin challenged with CpG DNA in mice

WANG Jun, ZHOU Hong

2005, 10(3):  290-293. 

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AIM: To investigate the protective effects of artemisinin on mice and its inhibition effects on the release of pro-inflammatory cytokines challenged with CpG DNA.METHODS: A total of 60 mice of Kunming species were randomly divided into six groups.Animals received an intraperitoneal injection of D-galactosamine (D-Gal, 600 mg°kg^-1)1 hour prior to intravenous injection of CpG DNA.CpG DNA group received CpG DNA at 4 mg°kg^-1 via caudal vein, artemisinin group were orally administered artemisinin at 200 mg°kg^-1, CpG DNA plus artemisinin group first received artemisinin at 50, 100, and 200 mg°kg^-1, respectively, then received CpG DNA at 4 mg°kg^-1, and the control group received the saline only.The mortality was observed within seven days after injection.RAW 264.7 cell lines were cultivated in vitro and stimulated by CpG DNA to release TNF-α and IL-6, then various concentrations of artemisinin were administrated to observe its dose-dependent inhibitory effect, and artemisinin were also added at different time to observe the time-dependent effect.Contents of cytokines in culture supernatant were detected by ELISA.RESULTS: Different concentrations of artemisinin decreased the death of mice challenged with CpG DNA, and the mortality were dropped from 80% to 10% (P<0.01). 20 g°ml-1 artemisinin significantly inhibited the release of TNF-αand IL-6 from RAW 264.7 induced by CpG DNA.The cytokines was markedly inhibited when artemisinin was added first (P<0.01).And the release of TNF-αand IL-6 were obviously suppressed if the cells were stimulated by CpG DNA prior to artemisin (P<0.01).CONCLUSION: Atemisinin has a protective effect on mice challenged with CpG DNA, and it can obviously inhibit pro-inflammatory cytokines released from RAW 264.7 in a dose- and time-dependent manner.

Enzyme kinetics of genistein metabolism in rat liver microsomes

WANG Ru-tao, ZHOU Si-yuan, MEI Qi-bing, YANG Zhi-fu, LIU Zhen-guo, LIU Lin-na

2005, 10(3):  294-297. 

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AIM: To study the enzyme kinetics of genistein metabolism and the effects of selective CYP450 inhibitors on the metabolism of genistein in rat liver microsomes. METHODS: Rat liver microsome was used to perform enzyme kinetic studies.Various selective CYP inhibitors were used to investigate their inhibitory effects on the metabolism of genistein and the principal CYP isoform involved in genistein metabolicly ring.RESULTS: The metabolism of genistein was significantly inhibited by furafylline while quinidine, sulfaphenazole, tranylcypromine diethyldithiocarbamate and ketoconazole showed little inhibitory effect on the metabolism of genistein.CONCLUSION: CYP1A2 is involved in genistein metabolism.CYP1A2 inhibitors and genistein may interact metabolicly, thereby reduced the rate of genistein metabolism.

Determination of scutellarin in human plasma by LC-MS method and its clinical pharmacokinetics in Chinese healthy volunteers

JU Wen-zheng, ZHANG Jun, Tan Hen-shan, JIANG Meng, CHEN Ming, XIONG Ning-ning

2005, 10(3):  298-301. 

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AIM: To determination of scutellarin in human plasma by LC-MS method and investigate the pharmacokinetics of breviscapine tablets in Chinese healthy volunteers.METHODS: 20 male healthy volunteers were received a single oral dose of 120 mg breviscapine tablets.The plasma concentration of scutellarin aglycone was determined by HPLC-MS method.RESULTS: The linear range was 3.24-0.0126 mg°L^-1.Within-day RSD and between-day RSD were less than 12%.The main pharmacokinetic parameters were as follows:T_max was 7.0±2.3 h, C_max was 0.9±0.5mg°L^-1, AUC_0-24h was 5.6±1.6 mg°h°L^-1, AUC_0-∞ was 5.8±1.6 mg°h°L^-1, MRT_0-24h was 8.0±1.1 h, and MRT_0-∞ was 8.6±1.4 h.CONCLUSION: This method is sensitive, fast, and accurate, and it can be used for pharmacokinetic studies of scutellarin in humans.

Determination of sustained-release niacin formulation by RP-HPLC in dog plasma and its pharmacokinetic study

HUANG Min-wen, WANG Guang-ji, SUN Jian-guo, GU Yi

2005, 10(3):  302-305. 

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AIM: To establish a simple RP-HPLC method for the determination of niacin in dog plasma and calculate the relative bioavailability and the pharmacokinetic parameters of sustained-release niacin formulation. METHODS: Niacin was extracted from dog plasma with perchloric acid.The RP-HPLC was performed on a Lichrospher C18 column (5 μm, 250 mm×4.6 mm I.D.) with mobile phase of acetonitrile-10 mmol°L^-1 monopotassium phosphate (8∶92, v/v), and the pH of the water phase was adjusted to 4.0 with phosphoric acid at flow rate of 1.0 ml°min-1.Niacin was detected by UV absorbance at 263 nm.Single dose of sustained-release niacin formulation (500 mg)and rapid-release niacin formulation (500 mg)were given to six Beagle dogs.RESULTS: The t1 2, T_max, C_max and MRT of niacin in the sustained release formulation were 1.25±1.15 h, 2.3±0.8 h, 35.3±4.87 mg°L^-1 and 3.45±0.55 h, respectively.The T_max of sustained-release niacin formulation is significantly longer than that of the conventional niacin tablet (P<0.05), the C_max was significantly lower than that of the conventional niacin tablet (P<0.05). CONCLUSION: This method is simple, accurate, sensitive and applicable for pharmacokinetic study of niacin. The relative bioavailability is (40.7±8.6)% in the sustained- release formulation.

Effects of shenfu injection on nuclear factor-κB during myocardial ischemia/reperfusion injury in rats

ZHANG Ben-jing, WANG Yan-lin, WANG Cheng-yao

2005, 10(3):  306-309. 

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AIM: To study the protective effects of shenfu injection on myocardial ischemia/reperfusion (I/R) injury in rats and its potential mechanisms.METHODS: Myocardial ischemia/reperfusion was produced by tying and untying of left anterior descending coronary artery. Ischemia lasted for 30 min and reperfusion for 60 min. Twenty-four healthy male SD rats weighing 230-280 g were randomly divided into three groups (n=8 in each): sham-operation group, I/R group, and shenfu group which the shenfu injection (10 ml°kg^-1) were injected intraperitoneally 30 min before ischemia.The plasma concentration of tumor necrosis factor-α(TNF-α), interleukin- 6 (IL-6) were measured by ELISA.The heart was harvested and levels of the nuclear factor kappaB (NF- κB) activity were determined by Ecl-western blot analysis and ultrastructures were observed by electron microscopy. RESULTS: NF-κB binding activity in myocardial nuclear and the plasma concentration of IL-6, TNF-αwere significantly increased in I/R group than that in the sham-operation group (P<0.01), and they were markedly reduced in shenfu group compared with I/R group (P<0.01).In addition, electron microscopic examination showed more serious injury of the myocardium ultrastructure in I/R group, while in shenfu group the myocardial ultrastructure could improve close to normal.CONCLUSION: Shenfu injection can inhibit NF-κB activity in postischemic myocardium and lead to down-regulation of proinflammtory cytokine expression, which may be one of molecular mechanisms of shenfu injection in cardioprotection.

Pharmacokinetics of breviscapine in mice

LIU Yi-ming, LIN Ai-hua, CHEN Hui, ZENG Fan-dian

2005, 10(3):  310-313. 

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AIM: To study the pharmacokinetics and absolute bioavailability of breviscapine in mice.METHODS: After iv injection (50 mg°kg^-1)and ig administration (150 mg°kg^-1)of breviscapine in mice, the plasma scutellarin concentration were detected by SPE-HPLC method.The pharmacokinetic parameters were calculated by 3p97 program.RESULTS: The plasma scutellarin concentration-time curve after iv injection of breviscapine was fitted with a three compartment model.AUC, C₀ and T_1/2β were 12.97 mg°h°L^-1, 132.23 mg°L^-1 and 4.04 h, respectively.After ig administration of breviscapine, the drug absorption was rapid, but the plasma concentration was very low.The parameters of AUC and T_1/2Ke calculated with non-compartment model were 1.966 mg°h°L^-1 and 3.4 h, respectively.The absolute bioavailability was 5.05%.CONCLUSSION:The pharmacokinetics of breviscapine in mice after iv injection fitted with three-compartment model.After ig administration, the drug is absorbed rapidly but the absolute bioavailability is very low, and the changes of plasma concentration of scutellarin is not regulation.

Protective effects of CpG oligonucleotide on mice with bacterial sepsis and its mechanism

LIU Wei, ZHOU Hong, DING Guo-fu, LU Yong-ling, WANG Liang-xi, LUO Ping

2005, 10(3):  314-317. 

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AIM: To investigate the protective effects and mechanisms of CpG ODN on mice with bacterial sepsis.METHODS: The mice with bacterial sepsis were injected with CpG ODN before infected by inactivated Escherichia coli to observe the protective role of CpG ODN. The serum TNF-αwas tested.RESULTS: Adequate dosage (2.5 mg°kg^-1) of CpG ODN protected mice from lethal challenge by inactivated Escherichia coli in a dose and time dependent manner.CpG ODN inhibited the release of TNF-αinduced by inactivated Escherichia coli. CONCLUSION: The potent anti-inflammatory effect of CpG ODN on mice with bacterial sepsis.The mechanism may be related to CpG ODN inhibiting the release of TNF- αinduced by inactivated Escherichia coli.

Protective effects of CN802 on immunological liver injury in mice

CHENG Liang, XU Ping-xiang, TANG Yu

2005, 10(3):  318-320. 

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AIM: To study the protect effects of paecilomyceps sinensis sp nov (CN-802) on immunological liver injury in mice which induced by BCG+LPS. METHODS: LPS was injected into mice via the tail vein pretreated with BCG.The activity of serum ALT, the weighing indexes of liver and spleen, the levels of LPO in serum and hepatic tissues, and the numbers of subgroup of T lymphocyte were determined respectively.RESULTS: CN-802 at dose of 1.0 g°kg^-1 °d^-1 decreased the serum ALT level, the liver and spleen-enlarged index and the LPO levels in serum and hepatic tissues.Analysis of CD₄/CD₈ in the peripheral blood showed that CN-802 increased the number of CD₄ lymphocyte and the ratio of CD₄/CD₈.CONCLUTION: Pretreatment with CN-802 prevents the immunological liver injury induced by BCG+LPG, and the effect of CN802 may be related with the regulatory of immune cells.

Effects of seal oil ω-3 polyunsaturated fatty acids on blood glucose research in insulin resistance diabetes rats

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

2005, 10(3):  321-325. 

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AIM: To investigate the effects of seal oil ω-3 polyunsaturated fatty acids (ω-3 PUFA)on blood glucose research in insulin resistance diabetes rats. METHODS: Different dosage the seal oil ω-3 PUFA were administered to the insulin resistance diabetes rats model caused by the high fat feed chain streptozotocin. After administration for 6 weeks, the blood fats four items, blood sugar value, insulin value and liver glycogen were determined.RESULTS: The seal oil ω-3PUFA 4.8, 2.4, and 1.2 g°kg^-1 reduced the serum triglyceride levels by 44.1%, 43.5% and 6.5%, respectively, increased the serum HDL-cholesterol levels by 22.4%, 8.0% and 6.3%, respectively, and decreased the blood serum LDL-cholesterol levels by 27.9%, 23.6% and- 4.6%, respectively.The blood sugar value obviously decreased before the medicine by 31.6%, 13.3%,- 10.2%, respectively.But the insulin secretion was not decreased.The seal oil ω-3PUFA strengthened the sensitivity of organism to the insulin, and the sensitive index increased by 129.5%, 60.3%, 55.5%, respectively. CONCLUTION: The ω-3PUFA can effectively improve the insulin resistance syndrome caused by high glycerin trinitrate lipemia, and the mechanisms of it falls the sugar may be related to its enhancing the sensitivity of the organism to the insulin.

Experimental study on anti-endotoxin activity of Radix Paeoniae Rubra

WEI Li-zhao, ZHENG Jiang, JIANG Dong-neng

2005, 10(3):  326-328. 

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AIM: To isolate and extract anti-endotox effective components in Radix Paeoniae Rubra.METHODS: By the biosensor technology, the anti-endotoxin effective components were isolated and extracted with general separate technology of Chinese traditional medicine. Through quantificational mensuration for LPS and inhibition of TNF-αrelease from endotoxin-stimulated cells in vitro, anti-endotoxin activity of Radix Paeoniae Rubra were elucidated.RESULTS: The effective components had high binding capability with LPS.After incubation with endotoxin and cells, the capability showed anti-endotoxin and inhibition of TNF-αrelease from endotoxinstimulated cells in vitro.CONCLUSION: The anti-endotoxin effective components isolated and extracted using LPS as target by the biosensor technology are available in searching anti-endotoxin agents from Radix Paeoniae Rubra.It shows that Radix Paeoniae Rubra has high ability on neutralization with LPS.

Effects of different lipid on MIF mRNA and protein expression in cultural macrophage

LIN Qiu-xiong, SHAN Zhi-xin, YU Xi-yong, Yang Ming, LIN Shu-guang, Hui-yao LAN

2005, 10(3):  329-332. 

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AIM: To investigate the expression of MIF mRNA and protein in cultural human macrophages induced by different lipoproteins.METHODS: 28sc human macrophage cell lines were grown in RPMI-1640 medium containing 1×105 U°L^-1 penicillin, 100 mg°L^-1 streptomycin, 10% FBS at 37 ℃ and 5% CO₂.The concentrations of cells were adjusted as 10×10⁴ ml-1, and then macrophages were inoculated in 6 wells plate. Different lipoproteins with a final concentration as 150 mg°L^-1 were added respectively in each well.After culture 24 h together, the expression of MIF mRNA and protein were detected by RT-PCR and ELISA methods.RESULTS: The MIF mRNA and protein were expressed in macrophage.LDL, Ox-LDL, cholesterol and TG can significantly increased the expression of MIF mRNA and protein in macrophage compared with the control group(P<0.05).However, HDL and VLDL showed no effect on the expression of MIF mRNA and protein in macrophage (P>0.05).CONCLUSION: Different lipid including LDL, Ox-LDL, cholesterol and TG can up-regulate MIF mRNA and protein expression in macrophage.It suggests that MIF may involve in the progress of atherosclerosis.

Protective effects of 3,4,5,6-tetrahydroxanthone on damages of endothelium-dependent relaxation induced by high glucose

DAI Zhong, JIANG De-jian, DAI Bin, LU Cheng-yu, XU Wei-ming

2005, 10(3):  333-337. 

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AIM: To investigate the protective effects of 3, 4, 5, 6-tetrahydroxanthone on damages of endothelium- dependent relaxation induced by high glucose. METHODS: The aortic rings obtained from the rats were exposed to high glucose (25 mmol°L^-1) for 24 h or endothelial cells were incubated with high glucose (30 mmol°L^-1) for 48 h, respectively.Endothelium-dependent relaxation was measured.Activity of lactate dehydrogenase (LDH), contents of malondialdehyde (MDA) and nitric oxide (NO) in the medium were measured.RESULTS: Exposure of aorta rings to high glucose (25 mmol°L^-1) for 24 h caused a marked decrease in endotheliun- dependent relaxation.Pretreatment with 3, 4, 5, 6- tetrahydroxyxanthone (1, 3 or 10 μmol°L^-1) or probucol (10 μmol°L^-1) significantly improved endothelium-dependent relaxation in a dose-dependent manner.The release of LDH, the contents of MDA and NO in the medium marked increased after exposure of HUVEC to high glucose (30mmol°L^-1) for 48 h.Pretreatment with 3, 4, 5, 6-tetrahydroxyxanthone (1, 3 or 10 μmol°L^-1) or probucol (10 μmol°L^-1) significantly decreased the increased release of LDH, the increased content of NO and MDA in the medium.CONCLUSION: 3, 4, 5, 6-tetrahydroxanthone may preserve endothelial dysfunction induced by high glucose, and the protective effects of 3, 4, 5, 6-tetrahydroxanthone may be related to reduction of endothelial cells damages by inhibiting lipid peroxidation.

A method based on cumulative toxicity for evaluating pharmacokinetics of oral traditional Chinese medicine in animals

LU Cheng-yu, WANG Hai-yan, DAI Zhong, DAI Bin, WU Tie

2005, 10(3):  338-342. 

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AIM: To improve the acute cumulative death rates method (ACD method) in animal by oral administration.METHODS: A mathematic model was established to evaluate the dose-toxic effect relationship by twice oral administration and the experimental steps were improved too.The methodological quality was explored using the simulation data from computer program and the real experimental date from the reference paper.RESULTS: The results showed that the experimental data could be fitted to its theoretical data from LD₅/2 to LD₉₅/2.Concentration-time curve after po ordinary powder of Semen Strychni in mice were fitted to a one-compartment with T_1/2(ka)=1.136 h, T_1/2(ke)=7.100 h, and T_max= 3.576 h.CONCLUSION: The improved ACD method can be used in the pharmacokinetics of TCM by oral administration.

Antioxidative and lipid-lowering effects of phenolic alkaloids of Menispermum dauricum

LIU Chang-li, ZENG Fan-dian

2005, 10(3):  343-347. 

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AIM: To investigate the antioxidative effects of phenolic alkaloids of Menispermum dauricum (PAMD)and its lowering lipid effects.METHODS: The effects of PAMD on spontaneous and induced liver homogenate lipid peroxidation were studied by TBA method for testing the content of MDA.Reactions of Fenton and Marklund were used to test the scavenging capacity of PAMD on superoxide anion and hydroxyl radicals.The lipid-lowering capacity of PAMD was observed on hyperlipidemic animal model.RESULTS: PAMD inhibited the production of MDA in spontaneous and induced peroxidation of liver homogenate.It also scavenged superoxide anions and hydroxyl radicals.CONCLUSION: PAMD can inhibit the lipid peroxidate in vitro, scavenge free radicals, lower the contents of TC, TG, LDL, and MDA in serum and liver and heighten the activity of SOD and the content of HDL in serum.

Preparation of liposomes encapsulating dermatophagoides farinae antigen and it's influence on immunity of mites sensitized mice

YUE Wen-yan, ZHOU Shun-lin, LIU Wen-yan, WANG Shao-sheng, CHEN wen-kui

2005, 10(3):  348-351. 

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AIM: To investigate the changes on immunological function in antigen-sensitized mice injected by dermatophagoides farinaeliposomes (DF) subcutaneously.METHODS: BALB/c mice were sensitized with DF antigen injected subcutaneously.After injected by DF liposomes with 1, 3, and 9 μg°g^-1 dosage respectively, the total IgE, total IgG, DF specific IgE(sIgE), DF specific IgG (sIgG), IL-4, and IFN-γwere detected by ELISA.RESULTS: The total IgE, sIgE, total IgG, and sIgG in the serum of sensitized mice increased, the level of IFN-γreduced and IL-4 increased.After injected subcutaneously by DF liposomes, the total IgE, sIgE and IL- 4 in the serum of mice of all the treatment groups reduced, and IFN-γraised, and the total IgG, sIgG raised in the serum of mice administrated with small andmedium dosage, but the low dosage was more obvious.CONCLUSION: DF liposomes have some effects on the immunological function in mite-sensitized mice in the low dosage.

Quantitative analysis of focal ischemic cerebral infarction in mice

YU Yue-ping, XU Qiu-qin, ZHANG Qi, ZHENG Ming-zhi, HU Jue, WEI Er-qing

2005, 10(3):  352-356. 

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AIM: To confirm the action of the light transmission method in evaluating focal ischemic cerebral infarction on persistent focal cerebral ischemia in mice. METHODS: Persistent focal cerebral ischemia was induced by middle cerebral artery occlusion (MCAO).Bederson's neurological scores, climbing board and hanging test were performed 24 h after ischemia, and infarct volume, brain hemisphere area, neuron density of cortex and subcortex were measured with computer-assisted imaging. Pranlukast (0.1 mg°kg^-1) or nimodipine (0.4 mg°kg^-1) were injected ip once daily for 3 days and to 1 h before MCAO assess the neuroprotective effect.RESULTS: The infarct volumes measured by light transmission closely correlated with that measured by TTC staining and neuron densities.The infarct volumes measured by light transmission well correlated with the neurological scores measured by integrated graded approach, too.Both pranlukast and nimodipine significantly attenuated infarct volumes and the ratio of ischemic/non-ischemic hemispheres, and reduced neurological deficits and neuron death. CONCLUSION: Light transmission and integrated graded approach can be used not only for qualitative analysis of focal cerebral ischemia, but also for evaluating the neuroprotective effect of drugs.

Designing of SAS macro programs of fourfold table for report forms of statistical results

ZOU Jian-dong, XIONG Ning-ning, BO Qing-yan, JIANG Meng, LIU Fang

2005, 10(3):  357-360. 

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In the statistical analysis of fourfold table in clinical trial, we design some SAS macro programs to output the report forms of statistical results in this paper.