Table of Content

Volume 10 Issue 10
26 October 2005

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Current progress on functions and heterogeneity of endothelial cells

GUO Jian-you, HUO Hai-iu, JIANG Ting-liang

2005, 10(10):  1081-1085. 

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Endothelial cells (ECs) play various roles in a number of physiological and pathological processes. Based mainly on data available within the last decade, this review described the functions of ECs, including an­giogenesis, coagulation, inflammation and immune re-sponse, synthesis of stromal components, vascular tone regulation, and lipid metabolism. The heterogeneity of the functions is also described.

Relationship between Glutathione and related enzymes and multidrug resistance

JIANG Yi, LI Yun-man

2005, 10(10):  1086-1091. 

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Multidrug resistance to chemotherapeutic drugs is an important reason for clinieal chemotherapy failure. The mechanisms of the classical drug resistancesuch as P-gp, MRP have been clarified. Hence, it isvery important to further study the non-classical mechanism of multidrug resistance. We introduced the effects on MDR, the possible mechanisms of glutathione and relatedenzymes, as well as the relationship between structure of GSH analogues and the transport activity in this paper

Effects on mRNA expression of muscarinic acetylcholine receptors in aorta endothelium by carbachol and pilocarpine

CHEN Kai, WANG Hai

2005, 10(10):  1092-1095. 

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AIM: To study the modulation on mRNA expression of muscarinic acetylcholine receptors in bovine aorta endothelial cells by carbachol and pilocarpine.METHODS: Total RNA was extracted from the bovine aorta endothelial cells having been incubated with carba-chol and pilocarpine at the dose of 10^-4 mol·L^-1for 10hr. The expression of muscarinic acetylcholine receptor subtypes mRNA was measured by RT-PCR.RESULTS: The mRNA expression of five muscarinic acetylcholine receptors were allmeasuireed. These five genes were up-reg ulated after incubated with carbachol and pilocarpine atthe dose of 10^-4 mol·L^-1 for 10hr and therre was no diference in them.CONCLUSION: Carbachol and pilocarpine has the same effect on genes expression of muscarinic acetylcholine receptor subtypes in aorta endothelialcells. Their effects on muscarinic acetylcholine receptorsubtypes can not explain the influence to vascular tension

Group I and III metabotropic glutamate receptors agonists reverse 1-methyl-4-phenylpyridinium-induced glutamate uptake inhibition in C6 glioma cells

WANG Fang, YAO Hong-hong, HU Gang

2005, 10(10):  1096-1099. 

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AIM: To study the effect of group II and Ill metabotropic glutamate receptors (mGluRs) agonistson 1-methyl-4-phenylpyridinium (MPP⁺) induced gluta-mate uptake inhibition in C6 glioma cell.METHODS: The glutamate uptake into astrocytes was measured by using radio-ligand binding assay method.RESULTS: It was shown that Group II mGluRs agonist (2 ‘S, 2'R, 3'R)-2-(2 ‘ 3'-dicarboxycyclopropyl glycine (DCG-IV(100μmol·L^-1) and Group II mGluRs agonist L (+)-2amino-4-phosphonobutyric acid (L-AP4) (100μmol·L^-1) significantly reversed Mpp⁺-induced gluta-mate uptake inhibition. Furthermore, the enhancementeffects of DCG-IV and L-AP4 were blocked by their re-spective antagonists, (RS)^-1-Amino-5-phosphonoinan^-1carboxylic acid (APICA and (RS)-α-methylserine-Ophosphate (MSOP).CONCLUSION: Group II and Ill mGluRs agonists produce neuroprotective effects byenhancing the activity of glutamate transporters.

Effects of a new drug NMF for Alzheimer s disease on neurons in vitro

WU Yu-mei, XIONG Xiao-yun, JIN Rong, SUN Jing-min, YANG Lin, LUO Xiao-xing

2005, 10(10):  1100-1103. 

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AIM: To observe the effects of NMP, adrug synthesized for Alheimer's Disease in our laboratory, on viability of mouse cortical neurons and provide pro -tection against the excitotoxic effect of kainic acid ( KA )on primary cortical cultures.METHODS: Primary cultured neurons were dissociated from 15 d old mouse em -bryo and plated on 96-well culture-plates for 48 NMF was added in medium for 72 h, and MTT methodwas used to determine the effect of NMF on neuron viability. At the same time, neurons plated on 24-well culture-plates with NMF in the medium treated with or without KA on d 3. Dying cells were identified by trypan blueunder phase contrast microscope and survival rate carneup.RESULTS: NMF increased the viabilityneurons, especially on the dose of 0.1, 1μmol·L^-1, 10nmol·L^-1 and the rate enhanced was 34.7%, 37.4 and 36.7%, respectively; culturing cortical neurons with NMF at 1, and 10 nmol·L^-1 for 4d increase the survivalof neurons at 39.3%, 0.73.5% and decreased the deathrate of cells. Damaged neurons induced by cultured with KA for 30 min showed various changes and higher mortali While pretreated with NMF 0.1, 10nmol·L^-1, 10 nmol·L^-1 for 4d. the cortical neurons were resistant tothe injury of KA and the protective rate were 77. 30%, 80. 10%, and 84. 15%, respectively.CONCLUSION: NMF can increase the viability and survival rate of mousecortical neurons, and decrease the mortality and protectneurons against KA induced neurotoxicity.

Effects of rutecarpine on movement of gastrointestinal tractin experimental animals

Wang Xiao-hu, Wu Wei-wei, Liu Bao-li

2005, 10(10):  1104-1107. 

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AIM: To evaluate effects of rutecarpine on the movements of gastrointestinal tract in experiment alanimals.METHODS: In mice, the accelerated movement model of intestinal transit was induced by neostig-mine, and metoclopramide or apoplon was applied to induce the accelerated gastric emptying movements. Acetylcholine or histamine was used to induce the contractions occurring in the isolated ileum from guinea pigs.RESULTS: Rutecarpine inhibited normal intestinal transit and demonstrated more effective suppression on the accelerated movement induced by neostigmine in mice; meto clopramide and apoplon induced-accelerated gastric emp-tying movements were also significantly inhibited by rutecarpine in a dose-dependent manner. Meanwhile rute-carpine significantly inhibited the isolated ileum contractions induced by acetylcholine or histamine.CONCLUSION: Rutecarpine is an effective inhibitor to intestinal motility and this activity is probably mediated by its an-tagonistic effects on the cholinergic nerve or its responsible modulations.

Sequence analysis of muscarinic receptors M₂, and M₄ expression by cultured rat astrocyte cells

ZHANG Xiao-juan, WANG Hai

2005, 10(10):  1108-1111. 

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AIM:To clone the muscarinic receptor M₂, M₄ sequence of astrocyte cell, and compare the geneand protein sequence with those of neuron.METHODS: The specific primers were designed to clone the M₂ and M₄, sequence of astrocyte cellng to the sequences that of neuron by RT-PCR, and then the sequences were sequenced. RESHLTS AND CONCLUSIONS: The M₂ and M₄ sequences expression were compared by astrocyte cells and neurons, and the difference was marked. The differences of the gene and protein sequences are evidentof M₂ and M₄ between astrocyte cell and neuron.

Protective effects of pioglitazone on heart in ischemia-reperfusion injuryrat

CAO Ze-ling, YE Ping, LONG Chao-ling, CHEN Kai, LI Xiao-wei, WANG Hai

2005, 10(10):  1112-1117. 

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AIM: To observe the effects of pioglitazone on the hearts of the rat's models of ischemia-reperfusion in vivo.METHODS: Sprague-dawley rats were randonnly divided into two groups. One was the group of 30 min reperfusion, which was subdivided into sham (n=5), model (veahic, n=6) and pioglitzone (3mg·kg^-1, n = 7) with 30 min ischemia followed by 30min reperfusion to detect some data related to cardiac function and the area of myocardium infarction (MI). Another was the group of 2 h reperfusion, which was fur-ther subdivided into the sham (n = 5), model (venicle,n = 6), pioglitazone 0.3 mg·kg^-1 (n = 6), 1 mg·kg^-1 (n = 7) and 3 mg·kg^-1. (n = 5). Then Immunohistochemistry and in situ hybridization were performed todetect the express of MMP-2 and PPARTY and RNA.RESULTS: Compared with the model group nec/aar after injecting pioglitazone decreased by 28% (P< 0.01). The ratio of nec/lv reduced to 32% (P <0.01). Heart rate, + dp/dt_max, as well as-dp/dt_max improved dramatiely at 1 min and 30 min after reperfusion, respectively (P 0.05). In dose-dependent manner,the expression of MMP-2 protein and MRNA were de-resseed, while the PPARY protein and MRNA were en-hanced by pioglitazone.CONCLUSION: Pioglitazonehas the protective ability against I/R injury evidenced byreducing area of MI and improving cardiac function. Thismay take place through the pathway in which PPARY inhibiting MMP-2.

Ettect of curcumin on pulmonary arterial pressure and c-Jun, c-FOS in chronic hypoxic hypercapnic rats

LIN Quan, WANG Liang-xing, ZHOU Xiang-feng, HUANG Xiao-ying, CHEN Shao-xian

2005, 10(10):  1118-1122. 

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AIM: To investigate the effect of curcumin on pulmonary arterial pressure and the expression of c-Jun and c-FOS in chronic hypoxia hypercapnia rats.METHODS: SD rats were randomly divided into normal control group (NC), hypoxic hypercapnic group (HH)hypoxic hypercapnia + curcumin group (HC). c-FOS, c-Jun and their MRNA were observed in pulmonary arte-roles of rats by the technique of immunohistochemistry and in situ hybridization.RESULTS: Hemodynamics showed that MPAP was markedly lower in group HC thanthat in group HH (P < 0.01). Differences of MCAP werenot significant in three groups. Iight microscopy showed meclia thickness of pulmonary arterioles was markedly higher in group HH than that in group NC and vessecavity turned more strait in group HH than that in group NC. However, the damage of pulmonary arterioles ingroup HC was significantly slighter than that of group HH. Electron microscopy showed that structure of the en-dothelial cells in pulmonary arterioles in group HC was near to normal, and the liferation of medial smooth muscle cells and collagen fibers in adventitia is markedly lighter than those of group HH. Expression of c-Jun andC-FOS in pulmonary arterioles were significantly higher ingroup HH than NC group (P < 0. 01), and they were lower in group HC than those of group HH (P <0.01). In situ hybridization showed that c-Jun MRNA inulmonary arterioles was significantly lower in rats of group HC than that in group HH.CONCLUSION: Curcumin can inhibit hypoxic hypercapnic pulmonary hypetension and pulmonary vessel remodeling, and it may be avital mechanism of curcumin to decrease the expression ofc-Jun, c-FOS and to inhibit the proliferation of medial Smooth muscle cells.

Protection effect of β₁ receptor mRNA antisense inhibition on heart of renal hypertensive rats

Wuyuan-xiong, WANG Jin-ming, ZHANG Mei-chun, LIANG Yuan-hong

2005, 10(10):  1123-1127. 

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AIM: To explore the effect and mechanism on blood pressure and heart protection of renal hypertension in rats treated with β₁ receptor antisense oli-godeoxynucleotides (β₁-AS-ODN) by delivery with cation-icliposomes DOTAP/DOPE.METHODS: 24 SD rats were divided randomly into 4 groups of 6 each group two groups of 2KIC rats were treated via tail vein injection with β₁-AS-ODN or inverted oli gonucleotides against rat β₁-AR MNA (β₁-IN-ODN) of 0.5 mg·kg^-1 once. 6 unltreated 2K1C rats and shamed rats served as positive andnormal controls. Blood pressure (BP), cardiac haemodynamics, and left ventricular index (LVW/BW) were measured. The histological changes of myocardium were observed by optical microscope and the expressions of Bcl-2 and Bax in myocardium were examined by immunohistochemical method.RESULTS: The single dose management of β₁-AS-ODN decreased blood pressure to 120 mm-Hg for 27 days and improved the LV function obviously P < 0.01). The value of LVW/BW in β₁-AS-ODN oup is much less than the value of that in 2K1C group(P 0.01). Compared with that of 2K1C group, thethological changes of myocardium inβ₁-AS-ODN groupmeliorated. The radio of bcl-2/Bax in 2KIC group wasless than sham group, and the radio of that in β₁-AS-ODN group was more than 2KIC group (P < 0. 05).CONCLUSION: β₁ receptor antisense oligodeoxynucleotidescan maintain anti-hypertension effect for atime and improve LV function, effectively reverses left ventricular hypertrophy in 2K1C renal hypertensive rats. The mecha-nism of which may be related to the suppressing of cell apoptosis of myocardium by increasing Bcl-2/Bax. It sug-gests that, receptor mRNA antisense had the heart protection effect in renal hypertensive raf.

A microplate-based screening method for alpha-glucosidase inhibitors

Li Ting, ZHANG Xiao-dong, SONG Yu-wen, LIU Jian-wen

2005, 10(10):  1128-1134. 

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AIM: To establish a new sensitive micro-late-based method to determine alpha-glucosidase inhibiting activity and provide a reliable high-through put way for screening alpha-glucosidase inhibitors in vitro.METHODS: The fitting combination of enzyme and sub-strate in a certain reaction was tested. Acarbose, the most popular alpha-glucosidase inhibitor in clinical use was used to validate the established method. Calibration curve, wavelength fidelity and kinetic analysis, together with the effect of altered incubation time, temperature and PH were then studied.RESULTS: The details of assayprocedure and evaluation of factors affecting thee measure-ment are described. As little as 160 μl assaythe combination of 2.5 mmol·L^-1 PNPGU and alpha-glucosidase was performed in a 96-well plate. The optimal action was finally achieved by incubat-ed at 37 C, PH 7.0 for 15 min and measured at 400nm.RESULTS: from the validation exercises by Acartosestrongly demonstrated the accuracy and reliability of the pmposed approach.CONCLUSION: This method re-ported in the current paper makes it possible to rapidlyexamine large numbers of samples for the presence of al-pha-glucosidase inhibitors in very small sample volume Such action may help to pace the development of potentialoral medications from natural products protecting patienagainst postprandial hyperglylyceruic toxicity andoretreating (iabetes mellitus and the related complications.

Effect of seal oil for protecting liver cells from acutely or chronically dam aged in mice and rats

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

2005, 10(10):  1135-1139. 

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AIM: To study the effect of seal oil for protecting liver cells from acutely damaged by chemicals or chronically damaged by feeding with high fat diet in mice or rats.METHODS: KM mice and Wistar rats were divided randomly by body weight to 6 groups (n = 10 in each including placebo control group received only oliveil, model group received olive oil too, low or medial orlarge dose of seal oil groups received seal oil, control drgroup received dimethyl-4, 4'-dimethoxy-5, 6, 5',6'-dimethylenedioxybiphenyl-2, 2' dicarboxy late or simvastatin for 9, 7 days or 10 weeks. Except for placebo control group the mice or rats were acutely damaged by Dir ethionine or carbon tetrachloride on 7 or 6th day. The content of triglyeeride (TG) in liver of both mice and rats or se-rum transaminase ALT, and AST of rats were tested in the end. The rats were chronically damaged byntaneous injecting a low dose of carbon tetrachloride on the first day and feeding with high fat diet for 10 weeks. The lipid levels in both serum and liver and the hepatic weight were pathology was evaluated.RESULTS: while the mice and rats were damaged by DL. ethionine, the content of TG was 23% and 16% lower than model group(P < 0. 01) in the mice Of 7.2 g·kg^-1 seal oil groupand in the rats of 4.8 g·kg^-1 seal oil group, respectively. In damaged rats by carbon tetrachloride, serum ALTand AST decreased 24% and 16% comparing with modelgroup (P < 0.01) in 4.8 gkg seal oil group. Inchronically damaged rats by feeding with high fat diet, thetotal cholesterol (TC) and free fatty acid (FFA) in serum, TG, TC, FFA, malonyldialdehyde (MDA) in liverand hepatic weight decreased significantly than modelgroup (P < 0.01) and superoxide dismutase (SOD) inliver increased significantly than model group (P < 0. 01)4.8 gkg seal oil group. Pathologic histomorphologyinvestigation showed hepatocytes with lipid droplet decreased than model group in seal oil groups.CONCLUSION: Seal oil can protect liver cells from acutely damaged by DI-ethionine or carbon tetrachloride and significant prevention effect on fatty liver.

Antitumor activities of extracts from Stellera chamaejasmel L by various polarity of solvent extraction in vitro

LUO Hui-ying, WANG Ai-qin

2005, 10(10):  1140-1142. 

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AIM: To find the optimal polarity zone by comparing the antitumor effects of various polarity solvent extracts.METHODS: The various polarity solvent was used to separate the plant dry powder (petroleum mether, acetate, acetone, and ethanol) The antitumor activities of the different extracts on human cancer cell lines in witro were analyzed using MTT assay.RESULTS: The petroleum ether extract and the ethyl acetate extract strongly inhibited the proliferation of leukemia K562 cells, oesopnagus cancer Eca109 cells and hepato careinoma HepG₂ cells, and showed significant dose-dependent response while thele acetone extract and the ethanolextract exhibited low antitumor activities in wtro. The petroleum ether extract was the most active part.CONCLUSION: The petroleum ether extract is the principalantitumor extract from Stellera chanraeiasmel L.

Effect of BCEF0083, bioactive compounds from Entomogenous fungi, on AVP content of hypothalamus, pituitary and expression of glucocorticoidreceptor MRNA of hippocampus in chronic unpredictable stress model ofdepression in rats

KAN Hong-wei, CHENG Yan, ZHOU Lan-lan, MING Liang

2005, 10(10):  1143-1146. 

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AIM: To study the effect of bioactive compounds from Entomogenous ungl(BCEF0083), on AVP content of hypothalamus, piry and expression glucocorticoid receptor (GR) MRNA of hippocampus in chronic unpredictable stress model of depression in rats.METHODS: The depression animal model was induceby chronic unpredictable stress. The effect of BCEF0083 on AVP content in hypothalamus and pituitary was tested by radioimmunoassay. RT-PCR was used to test the expression of GR MRNA in hippocampus.RESULTS: BCEF0083 decreased the AVP content of hypothalamus and pituitary in chronic unpredictable stressed rats, an dincreased the expression of GR MRNA of hippocampus inchronic stressed rats.CONCLUSION: BCEF0083 ex-hibits antidepressant effect by attenuating the stimulatedfunction of hypothalamus-pituitary-adrenal axis in chronicunpredictable stress model of depression in rats.

Determination method of CYP3A activity and individualization dosage regimen of etoposide

ZHANG Shun-guo, ZHANG Jian, CHEN Min-ling

2005, 10(10):  1147-1151. 

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AIM: To explore the correlation between Drug concentration of etoposide (VP16) and CYP3A activity (CA) in leukemia.METHODS: The urinary 6β-hydroxycortisol/hydrocortisone ratio is a useful marker for CA. Concentration of Vpl6 in plasma and CA was determined by HPLC in 20 leucemia patients, and the correla-tion analysis was performed using the SPSS software.RESULTS: Correlation analysis between drug concentration of VP16 and CA in leukemia was poor correlated (r=0.725), but concentration of VP16 and IGCA showed good correlated (r = 0. 969).CONCLUSION: It is feasible to adjust the therapeutic regimen of VP16 by determing CA.

Effect of luteolin on ulcerative colitis in mice

ZHOU Zhu-cheng, LIU Bao-lin, WU Wei-wei

2005, 10(10):  1152-1155. 

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AIM: To evaluate the effect of luteolin onulcerative colitis in experimental animals.METHODS: The mouse model of acute colitis was induced by instillation of dinitrochlorobenzene (DNCB)/alcohol. Luteolin(1, 10 and 50 mg·kg^-1 were orally administrated tomice for 3 days. Dartheas, colon weight index, macro-scopic damage in the colon were observed and the activityof MPO and the content of PGE, in colon were also examined.RESULTS: The diarrhea and the colon weight in dex were reduced and the macroscopic damage in the inflammatory colon was effectively attenuated by luteolinThe elevated level of MPO and PGE₂ were also significantly decreased.CONCLUSION: Luteolin can effectively inhibit the inflammatory infiltration, bleeding andproliteration in experimental ulcerative colitis.

Protective effects of G004 on vascular endothelial cells

WU Guan-zhong, ZHANG Wen-ping, LV Zheng-bing, LIU Guo-qing

2005, 10(10):  1156-1161. 

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AIM: To study the protective effects of a novel sulfonylureous compound 1-[4-[2-(4-bromobenze-nesulfonaminoethyl) phenylsufonyl]-3-(trans-4-methylcyclohexyl) urea, G004, on vascular endothelial cells.METHODS: They were determined for the effects of compound G (04 on cell viability, concentration of malon-dialdehyde (MDA, a main decomposed product in lipicperoxidation) and activity of superoxide dismutase (SODin supernatant of oxidative injury endothelial cell(ECV304) of human umbilical vein caused by hydrogen peroxide. The activity of reactive oxygen species (ROS)in rat blood plasma was examined. The mode of vascularendothelial cell injury in rats was established by a higdose of adrenaline in combination with cold-water irritation. Then, the influence of compound GOO4 on plateletaggregation, the content of 6-K-PGENA, TXB2 T-PA, PATin blood plasma was investigated. The permeability of Evans blue in aortic wall and the blood plasma content ofGMP140 were studied in rats with injured vascular endothelial cell resulted from histamine.RESULTS: The compound C004 significantly improved the structuralchange of ECV304 cells damaged by hydrogen peroxidele prodt of MDA, increased activity ofSOD and the rate of animate cells. The compounreduced the production of ROS in the blood plasma ofrats. Compound G% 04 not only enhanced PGL] T-PA re-lease but reduced TXA2 PAI and potently inhibitedplatelet aggregation. The compound G004 decreasedGMP140 secretion from endothelial cells and permeability of Evans blue through aortic wall in rats injured by hista-mine with dose-dependence.CONCLUSION: The com-pound G004 can maintain the integrity of vascular endo-thelia cells, remove the ROS, modulate the secretion of TXA2, PGI2,, t-PA, PAL derived from endothelial cells and inhibit the increase of GMP140. The compound G004 shows the protective effect on vascular endothelial cell.

Effects of BCPT on blood level of CORT and ACTH and expression of CRH MRNA of hypothalamuc in chronic stress rats

ZHENG Li-fang, KAN Hong-wei, YIN Yan-yan, ZHANG Shen-quan, CHEN-BING, MING Liang

2005, 10(10):  1162-1165. 

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AIM: To study the effect of bioactive compounds from paecilomyces tenuipes (BCPT) on the blood level of CORT, ACTH and expression of CRH MR-NA of hypothalamus in chronic unpredictable mild stress model (CUMS) of depression in rats.METHODS: The epression animal model was induced by CUMS. The reward reaction was tested by the sweet water consumptionThe effect of BCPT on the blood level of CORT and ACTHwas tested by radioimmunoassay RT-PCR was used totest the expression of CRH MRNA of hypothalamus.RESULTS: BCPT (40,80 mg·kg^-1) improved the reward re-action by increasing sweet water consumption, decreasing the expression of CRH MRNA of hypothalamus and the blood level of CORT and ACTH in chronic stressed ratsobviously.CONCLUSION: BCPT exhibited antidepres-sant-like effeet may in part be associated with regulating the hyperactingunction of hypothalamic-pitultaryadrenal axis (HPAA).

Effect of midazolam, fentanyl and propofol coinduction on hypnotic andsedation in gengerl anesthesia

XU Hui, JIN Xiao-ju, GUO Xien

2005, 10(10):  1166-1170. 

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AIM: To investigate hypnotic and seda-lion interaction between midazolam, fentanyl and propofolin coinduction in general anesthesia.METHODS: Sixty patients', ASA class I orll, scheduled for elective celo Nc ope (peration were evenly distributed to 6 different com-pound dose groups according to weighted modificationmethodl Anesthesia was induced with midazolam which was administered over 15 s, and fentanyl which was administered over 15 s, and propofol which was administerel over 30 s. then monium 0.6 mg·kg^-1 was adwinisteredl to facilitate tracheal intubation. BIS, MAPHR were recorded at following times: before induction, Iand 2 tnin after induction, just at intubation, I and 3 and 5 and 7 min after intubation.RESULTS: The importantdegree of every drug was as follow: propofol > nltanylmidazolam. The optimal combinations was midazolam 0.02 mg·kg^-1, fentanyl 0.0025 mg·kg^-1 and propofol 0.8 mg·kg^-1. The optimal ratio was 1.0. 0.125: 40. Thenature of interaction was additive.CONCLUSION: Themidazolam, fentanyl and propofol combination possess ad-dtitive interaction in sedation and hypnosis. The optimcombinations was midazolam 0.02 mg·kg^-1, fentanyl 0.0025 mg·kg^-1 and propofol 0.8 mg·kg^-1.

Effect of Xingnaojing injection on metabolism of arachidonic acid in rabbits following cerebral ischemia-reperfusion injury

HUANG Wei-jia, CHEN Shou-quan, WANG Wan-tie, LI Hui-ping, CHENG Jun-yan, ZHAO Chuhuan, LI Zhang-ping, WANG Ming-shan, WANG Wei

2005, 10(10):  1171-1174. 

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AIM:METHODS: The acute complete cerebrali schemia model and the ischemia-reperfusion model were made by eluding four-vessel, both bilateral carotid an dvertebral arteries, and removing the occlusion of bilateral caroli at the end of 30 minutes ischemia. Control group(A) was intravenously infused. 9% saline (1 ml· kg^-1 before ischemia and before reperfusion, but XNJI group(B) were inlused XNJI (1 ml· kg^-1) The contents and of 6-KETO-PGF_1a in both plasma and braintissue were separalely measured with radioimmunoassayIe ore isehemia. 30 min after ischemia and 30 min, 1 h and 2 h after reperfusion. Cerebral ultrastruc true changes were observed at the end of experiment.RESULTS: Forthe XNJI group, compared with control group, TXB₂ > content and the radio of TXB2/6-KETO-PGFLA in both plasma and brain tissue decreased (P < 0.05). The observation of the pathologic changes of ultrastruc true in rain tissue showed that the injury was relieved in XN JI group.CONCLUSION: XNJI can effectively decrease the radio of TXB2/6-KETO-PGF_1a, by decreasing the synthesis of TXBand accelerating the growing of 6-KETO-PGF_1a, and it maybe another mechanism in protecting the brain from ischemia and reperfusion injury.

Effect of chimonin on expression of inducible-nitric-oxide-synthase andCO₂nstitutive-nitric-oxide-synthase in chronic hypoxic hypercapnic rat pulmonary arterioles

HUANG Xiao-ying, WANG Liang-xing, LI Ming, CHEN Shao-xian

2005, 10(10):  1175-1180. 

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AIM: To study the effect of chmonin onexpression of inducible-nitric-oxide-synthase and CO₂ stitutive-nitric-oxide-synthase in chronic hypoxic hypercapnicrats, and to explore the mechanism of. inhibition on pulmonary hypertension induced by hypoxic hypercapnia.METHODS: Thirty-six Sprague-dawley rats were ran-domly divided into three groups: normal CO₂ group(A), hypoxic hypercapnic group (B), hypoxic hypercapnia chimonin group (C). NO, INOS, CNOS in blood lung homogenate were measured. INOS MRNA and CNOS MRNA was observed in arterioles from rats bthe technique of in situ hybridization. The average valueof integral light density (ID) of INOS MRNA and CNOSMRNA in pulmonary arterioles was detected by an imageanalysor and the relative CO₂ of MRNA and CNOS MRNA was calculated.RESULTS: MPAP was higher in ratsof B group than that of A group and it was much lower inrats of C group than that of B group. Differences of mCAP were not significant in three groups; NO CO₂ncentration inblood serum and lung homogenate in rats of B group were significantly lower than those of A group, and those of Cgroup were significantly higher than those of B group (P< 0.01). The activity of CNOS in blood serum and lunghomogenate in rats of B group were lower than those of Aand C group (P < 0.01). Activity of INOS in blood seand lung homogenate of B group were higher thanof A group (P < 0.01), and there were not signif-cant difference between blood serum INOS in B and Cgroup. C group INOS in lung homogenate were higherthan those of B group (P < 0. 05). Iight microsCO₂py and electron microsCO₂py showed that chimonin reversed the remodeling of pulmonary arterioles induced by hypoxic hypereapnia.CONCLUSION: Chimohin can increase the expression of inducible-nitric-oxide-synthase gene andCO₂nstitutive-nitric-oxide-synthase gene on chronic hypoxichypercapnic rats pulmonary arterioles, and up regulateCNOS/NO system in hypoxic hypercapnic rats may be oneimportant mechanism of the eftect that chimonin inhibithypoxic hypercapnia pulmonary hypertension.

Experimental study on the effects of dehydroepiandrosterone on osteoarthritis in rats

HUANG Yi-xing, CHEN Liao-bin, WANG Hui, YI Xian-hong, WANG Peng

2005, 10(10):  1181-1185. 

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AIM: To investigate the effects of delydmepiandrosterone (DHEA on experimental osteoarthritis in rats.METHODS: Forty rats were randomly divided into four groups. Group A is normal control group Osteoarthritic models of rats were established by intraarticular injections of papain into the right knee joints of groups B, C and D. Then the right knee joints of rats in groups C and D, respectively, received 150μl intraarticular injections of DHEA at a concentration of 50μmol·L^-1 and 100μmol·L^-1 and the right knee joints of rats in groups A and B both received 150 ul physiological saline, twice weekly for five weeks. Six weeks laterall rats were sacrificed, and the articular cartilage was assessed by gross morphologic, histologic, biochemical and immunohistochemical methods.RESULTS: The cartilagedamage in groups C and D was much less than that ingroup B through observation under a surgical microscope.The Mankin s score, nitric oxide (NO) in the douche of articular cavity, malondialdehyde (MDA) in synoviumthe expression of matrix metalloproteinase^-1 and 9 in articular cartilage in groups C and D decreased in comparison with group B, and the for egoingndexes Ingroup Ddecreased signiticantly compared with group C. However the activities of superoxide dismutase (SOD) in thedouche of articular cavity and blood serumand D increased in comparison with group B, and the foregoing indexes in group D increased significantly compared with group C.CONCLUSIONS: DHEA shows acartilage-protecting effect which is in a dosage-dependentmanner. The mechanism probably is to inhibit the expression of matrix metalloproteinases and to decrease the release of (NO and enhance the antioxidation.

Effects of isoproterenol on myocardial fibrosis and related cytokines in rats

ZHANG Ling, WANG Hong-xin

2005, 10(10):  1186-1189. 

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AIM: To study the effects of isoproterenol(Iso on cardiac fibrosis and related cytokines in rats.METHODS: 20 SD rats were divided into control and Isgroup in random, with 10 rats each group. After injectedIso, cardiac histology was observed and cardiac function collagen volume fraction (CVF), content of collagen protein and the concentrations of Angiotensin II (Angll) andnitrogen monoxide (NO were measured in the two groups.RESULTS: Compared with control group, mi) scopic examination Showed that fibrosis Increased In Iso group. Iso did decrease cardiac function and NO levelsand increase CVF, content of collagen protein and Anglllevels. Left ventricular pressure maximal rate of rise (+dp/dt_max) and left ventricular systolic pressure (LVSP) were not significantly different from that of control group.CONCLUSIONS: Iso can induce myocardial fibrosis andchange levels of related cytokines in rats.

Effects of aspirin on promoter activities of human MMP-9 gene

QI Yong, GAO Jiang-ping, LI Qi, WU Zhi-qiang, HONG Bao-fa, ZHAO Ya-li

2005, 10(10):  1190-1193. 

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AIM: To understand the role of aspirin inthe prevention and cure of prostatie carcinoma, and the effects of Aspirin on the promoter actr of humanMMP-9 gene were studied.METHODS: DU145 cells were cultured and subcultured. Different concentrations of Aspirin (10, 5, 2.5, 1, 0.5, 0.1 and 0.2 mmol·L^-1)were added into the plates to co-incubated with the cell MTT method was used to detect cytotoxicity of Aspirin af-ter 24, 48 and 72 hours. Cells were transient transfected with PCAT 1.28, PCAT 0.65, PCAT 0.54 and PCAT0.52 containing^-1 28 kb, 0.65 kb, 0.54 kb, 0.52kb of 5 flanked sequence of human MMP-9 gene, fused to CAT reporter gene by CAT-ELISA.RESULTS: Aspirin (< 1 mmol·L^-1) had no cytotoxicity of DU145 cells (P> 0.05). CAT expression of PCAT 1.28 and PCAT 0.65are 2 and 1.6 times as high as the control groups. CAT expression of PCAT 1.28, PCAT 0.65 and PCAT 0.54were 2.5, 2.2 and 1.3 times as high as the contre groups. Aspirin inhibited the promoter activities of PCAT 1.28, PCAT 0.65. And the inhibition of Aspirin was reversed by PMA.CONCLUSION: Aspirin can inhibit the expression of human MMP-9 gene in the tramscriptional level and can inhibit the formation and development of prostatic carcinoma.

Clinical study of therapeutic effects of aripiprazole in treatment of patients with schizophrenia

ZHU Pei-jun, CHENG Zhi-en, ZHANG Jing, ZHU Pei-ling, ZHAN Xue-mei

2005, 10(10):  1194-1197. 

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AIM To evaluate the therapeutic effects and the safety of aripiprazole in the treatment of patients with schizophrenia.METHODS: 80 schizophrenic patients were randomly divided into two groups. Aripiprazole group was treated with 10-20 mg d " aripiprazole, poqd. Clozapine group was treated with clozapine 300~500 mg·d^-1, po, bid. Clinical effects were assessed with th Positive and Negative Syndrome Scale for8 weeks. Clinical effects were assessed with the Positive and Negative Syndrome Scale (PANSS), and side effects were assessed with the Treatment Emergent Symptom Scale (TESS) in following 8 weeks.RESULTS: Reduction rate in PANSS total scores in ariprazole group was 50.4%, and the efficacy was 87.5%. Reduction rate in PANSS total scoresin clozapine group was 49.4%, and the efficacy was 85%. The therapeutic effects were similar in the two groups (P > 0.05). There were some side effects such as EPS (17. 5%), headache (12. 5%), nausea and vomit-ing (10%) in aripiprazole group, but they were milderand the blood and glycometabolism was normal. Therewas no significant difference in two groups. Comparedwith the too much sedation (37.5%), secretion of paroid gland (45%), constipation (25%), gain weight(25%) in clozapine group, there was a significant differ-ence in two groups (P < 0.05 or P < 0.01).CONCLUSION: Aripiprazole is a safety and efficacy drug intreatment of patients with schizophrenia.

Optimizing method of Michaelis-menten pharmacokinetic parameters of bolus intravenous administration

SU Yin-fa

2005, 10(10):  1198-1200. 

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As the fitting value of Michaelis-Menten pharmacokinetic parameters K_m and V_m of accurate linearre gress (AIR) or improved Hanes-woolf method has some deviation, a optimizing method of K_m and V_m was used in this paper. The result of ALR or improved Hanes-Woolf method was taken as the primary value of parameters (V_m and K_m). The method combined Runge-kutta alorithm with program solution in Excel software (RK-PS was used to minimum weighting residual square sum [$\sum$(c-c *) 2/c] of concentration. The primary value of parameters was optimized. The RK-PS method was better than ALR method and improved Hanes-woolf method intwo examples.