Table of Content

Volume 14 Issue 5
26 May 2009

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Effects of leonurine on uterus induced by drug-abortion in rats

LI Xia, CHEN Fei-hu, YUAN Feng-lai, LU Wei-guo, WU Fan-rong, ZHANG Yan-na, LI Xiao-xiang

2009, 14(5):  481-486. 

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AIM:To study the effects of leonurine on uterus induced by drug abortion in rats. METHODS: Early pregnancy rats were intragastrically (i. g.) administrated with mifepristone(8. 3 mg/kg) and misoprostol(100 μg/kg) to induce incomplete abortion model. The changes of uterine bleeding amount and time, its morphous were observed in incomplete abortion model rats. The residues of decidual membranes and chorionic villus were observed with light microscope. The levels of estradiol(E₂) and progesterone in blood serum were detected by radioimmunoassay (RIA), the contraction activity of rat uterine smooth muscle by BL- 420E biological function of the experimental system and JH-2 muscular tension sensor. RESULTS:Compared with model group, leonurine markedly reduced the uterine bleeding amount and time, the intrauterine residues were reduced significantly and the contraction activity of rat uterine smooth muscles was strengthened obviously, the level of E₂ in serum was higher (P <0. 01). CONCLUSION:Leonurine has an obvious depressant effect on uterus haemorrhage induced by drug-abortion, which could result from the enhancement of the level of E₂ and the contraction activity of rat uterus.

Study on the apoptosis of human vascular smooth muscle cells induced by proteasome inhibitor MG132 and its mechanisms

GUO Fang, QU Shun-lin, SUN Wen-qing, HE Hui, YANG Xiang-dong

2009, 14(5):  487-492. 

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AIM:To study the effect of proteasome inhibitor MG132 on the expression of caspase 3 and the apoptosis in cultured human umbilical vascular smooth muscle cells. METHODS:Human umbilical vascular smooth muscle cells were treated with MG132 (2. 5, 5, 10 μmol/L) for 24 hours and for 48 hours. The apoptotic cells were determined by flow cytometric analysis. The levels of Ub, E1, E₂, E₃, 26S and caspase 3 mRNA expression were detected by reverse transcription- polymerase chain reaction (RT-PCR). The expression of caspase 3 protein was detected by immunocytochemistry. RESULTS: The results showed that the expressions of Ub, E1, E₂, E₃, 26S genes were decreased in treatment group and the apoptosis rates were increased obviously. MG132 could up-regulate the gene/protein expression of caspase 3. CONCLUSION: The results implicate that proteasome inhibitor MG132 could dose-dependently induce human umbilical vascular smooth muscle cells apoptosis, the apoptosis of human umbilical vascular smooth muscle cells induced by MG132 probably is relates to the decreases of Ub, E1, E₂, E₃ and 26S expressions and the increase of caspase 3 expression.

Experimental study on restoration action of Fum extract on skin destruction

MAO Xiao-jian, ZHAO Jie, WANG Min-jiang, LI Qing-sheng

2009, 14(5):  493-497. 

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AIM:To observe the restoration action of topical Fum extract (FumE) on skin destruction. METHODS:The skin destruction on rats was caused by ultraviolet radiation. The changes of body weight and skin appearance of rats were compared, and the content of MDA and the activity of SOD were measured. The burn on rats was caused by sodium hydroxide, the growth rate of weight and the healing time were recorded. RESULTS:FumE could relieve the skin destruction caused by ultraviolet radiation, reduce the content of MDA and increase the activity of SOD. FumE could shorten the healing time of rats burned by sodium hydroxide. CONCLUSION:FumE has protective effects on skin destruction caused by ultraviolet radiation, and can repair raw surface caused by sodium hydroxide.

Pharmacological characteristic of new benzothiadiazine derivatives, targeting the cardiac mitochondrial ATP-sensitive potassium channel

ZENG Yuan, QIU Cai-rong, YANG Yong-lin, PAN Zhi-yuan, JIN Jun-hua, WANG Hai

2009, 14(5):  498-503. 

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AIM:Series of new benzothiadiazine derivatives were designed and synthesized, which were considered to be the openers of mitoK_ATP channel. The pharmacological activity of these compounds were researched and compared with the effects of Diazoxide. METHODS:The effects of new benzothiadiazine derivatives on rat myocardial mitochondrial respiratory functions such as R3, R4, RCR were evaluated by oxygen electrode method. After Wistar rats were anesthetized with pentobarbital-Na and catheterized into carotid artery, the effects of these new compounds and Diazoxide on blood pressure were recorded by eight channel electrophysiolograph. RESULTS:The mitochondrial respiratory parameters R3 and R4 were both decreased while oxidizing FAD-dependent substrates (succinate)by the compound 16/17 at the concentration of 100 μmol/L, but RCR were not affected; those effects were similar to Diazoxide. However, the compound 15 could not only decrease R3 and R4, but also increase RCR. The blood pressure was quickly decreased through intravenous injection diazoxide (10 mg/kg)in anesthetized rats.Compared with control group, the blood pressure was decreased by 28% at the time of 3 min after administration. The other 20 new benzothiadiazine derivatives had no effects on blood pressure. CONCLUSION: The compound 15, as a selective opener of mitoK_ATP channel, can improve the mitochondrial respiratory function and has no effect on the blood pressure, and its cardiovascular selectivity is prior to Diazoxide.

Influence of complex prescription traditional Chinese medicine on polycystic ovarian syndrome model rats in glycometabolism

DEN A-li, XIANG Nan, ZHOU Zhong-ming, JIANG Hui-zhong, ZHANG Ya-bing

2009, 14(5):  504-508. 

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AIM:To observe the changes of weight, fasting plasma glucose (FPG), insulin (INS) and insulin-like growth factor-1 (IGF-1) of polycystic ovary syndrome (PCOS) model rats, and to explore the influence of complex prescription traditional Chinese medicine on glycometabolism. METHODS:PCOS rat models induced by Poresky method were intervened, and the changes of weight, plasma glucose, and the influence of INS and IGF-1 in serum were observed after treatment. RESULTS:The complex prescription traditional Chinese medicine could decrease the weight, the levels of INS and IGF-1 in serum of PCOS model rats, but the glucose-lowering effect was not significant. CONCLUSION:The complex prescription traditional Chinese medicine can improve the glycometabolism abnormal occurrence of PCOS model rats.

Effects of fenofibrate and rosiglitazone on the signal passway of p38MAPK in glomerular mesangial cells cultivated in high concentration of glucose

NI Lian-song, JIN Jie-na, ZHENG Jing-chen, SHEN Fei-xia

2009, 14(5):  509-514. 

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AIM:To investigate the effects of fenofibrate (FB)and rosiglitazone(RG)on the signal passway of p38 mitogen-activated protein kinases (p38 MAPK)in glomerular mesangial cells cultivated in high concentration of glucose. METHODS:Rat mesangial cells(MC)were incubated in 5. 5 mmol/L normal control glucose, 25 mmol/L high glucose (HG), HG + 100 μmol/L fenofibrate (FB +HG), HG +20 μmol/L rosiglitazone maleate (RG +HG), respectively. The fibronectin (FN)and type Ⅳ collagen (Col-Ⅳ)in supernatant were determined by ELISA. The expressions of p38MAPK and phospho-p38MAPK proteins in cytoplasm and nuclei were detected by Phospho-ELISA. The mRNA expression of p38MAPK was detected by semi-quantitative reverse transcription polymerase chain reaction (RT-PCR).RESULTS:Compared with normal control, the Col-Ⅳand FN in supernatant in HG group were much higher, the expression of p-p38MAPK was increased in cytoplasms and nuclei. Col-Ⅳ and FN were obviously decreased with the treatment of FB or RG, and the expression of p-p38MAPK in nuclei was down-regulated, but the expression of p-p38MAPK in intracytoplasm had no changes. There were no significant differences of the expressions of total protein and mRNA of p38MAPK among four groups. CONCLUSION: FB, RG could inhibit the activation of p38MAPK in nuceli of MC cultivated in high concentration of glucose, and then reduce the synthesis of extracellular matrix.

Observing the change of cerebral blood flow perfusion in acute vertebral artery stenosis in dogs by ⁹⁹T^cm-ECD imaging

CHENG Guang-hua, WU Ke-fang, DAI Yun-hai, LUO Fu-rong

2009, 14(5):  515-518. 

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AIM:To observe the early changes of local cerebral blood supply in dogs during the acute vertebral artery stenosis by ⁹⁹T^cm-ECD cerebral blood flow perfusion imaging (CBFPI). METHODS:Twenty- four dogs were randomized into groups of normal controls (A), moderate stenosis (B), severe stenosis (C) and arterial occlusion (D), with 6 in each group. Group A were free from any intervention, but Group B, C and D were undergone ligation of the right vertebral arteries by the extent of 50% ～ 69% (Group B), 70% ～ 99% (Group C) or 100% (Group D). The imaging agents were injected intravenously 0. 5-1 h after ligation and the single photon emission computed tomography (SPECT) was performed after 1 h. RESULTS: CBFPI examination of the early changes of cerebral blood supply during the acute vertebral artery stenosis by visualization showed that the sensitivity was 33. 3%, 83. 3% and 100% in Group B, C and D, respectively, with an average sensitivity of 72. 2%, while semi-quantitative assessment suggested that the sensitivity was 50%, 100% and 100% in the three groups, respectively, with an average sensitivity of 83. 3% .When examining the activity ratio for regions of interest(ROI) by semi-quantitative ⁹⁹T^cm-ECD CBFPI, the findings suggested that Group D and C decreased significantly (exception in cerebellum in Group C), but Group B had no evident changes, as compared with Group A. By comparison of the groups of B-C, BD and C-D, differences were observed in the right temporal lobes, whereas the changes in left temporal lobes were seen in Group B-C or B-D. The changes were seen in occipital lobes when groups of B and D were compared, but with no differences in cerebellum. CONCLUSION:The degree of stenosis in vertebral arteries may involve varied regions, the temporal lobe is susceptive, followed by occipital lobe, while cerebellum is somewhat resistant from the involvement.

Studies on the antiobesity action and mechanisms of daidzein derivative:LRXH609

WU Guan-zhong, GUO Yong-qi, SU Xin, YANG Hong-xia, ZHANG Jian

2009, 14(5):  519-523. 

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AIM:To approach the antiobesity action and mechanisms of the daidzein derivative: LRXH609 (LRX). METHODS:The body weight, Lee′s index, total weight of celiac fat tissue, food intake, serum glucose and lipids in obese rats induced by a high-fat diet were measured and the antiobesity action was tested after LRX was administered for 30 days. 3T3-L1 pre-adipocytes were induced by in vitro culture, the effects of LRX on cell proliferation, lipogenesis, lipolysis were observed. RESULTS:The body weight, Lee′s index, fat tissue weight in obese rats were significantly decreased by LRX, and the concentrations of TC, FFA in serum were decreased, the proliferation of 3T3-L1 pre-adipocytes was inhibited, the activities of hormone sensitive lipase in 3T3-L1 pre-adipocytes were significantly elevated, the glycerine release from adipocytes was promoted and the concentrations of TG in adipocytes were decreased. CONCLUSION: LRX plays a role in antiobesity action and regulating blood lipid and the mechanism might be related to inhibiting proliferation and differentiation of pre-adipocytes, stimulating TG decomposition by activating hormone-sensitive lipase and decreasing the TG storage in adipocyte.

Study on the pharmacodynamics of different administration methods of insulin on type II diabetes model

DENG Shan-shan, ZHANG Chao, TANG Li-na, XIANG Li, SUN Hong-fan

2009, 14(5):  524-527. 

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AIM:To observe the effects of subcutaneous and intraperitoneal injection for insulin on the rats with Type II diabetes. METHODS: Kk mice with fasting blood sugar level higher than 20 mmol/L was set as Type II diabetes model and divided into subcutaneous injection group (s. c. group, n =6) and intraperitoneal injection group (i. p. group, n =6) with different dosis of insulin, and the tail blood sugar levels were monitored for two continuous hours after administration. RESULTS:Under non-fasting condition, the blood sugar levels of s. c. group and i. p. group were (32. 0 ±1. 5), (31. 0 ±1. 5) mmol/L, respectively before insulin injection, and were decreased gradually after injecting. When insulin dose was not sufficient, the blood sugar level was at the bottom at the 30th minutes, and then went upwards gradually. When the dose was appropriate, the blood sugar level was at normal level at the 30th minutes, and then went upwards gradually after maintaining a certain time. When insulin was overdose, the blood sugar level was below normal level and decreased gradually and slowly. The dose-response curve was drawn according to the blood sugar level at the point of 30 minutes. When the insulin dose was in the range of 1. 1-1. 7 U/kg, the blood sugar level could be stably controlled within normal scope(5. 1 ± 0. 2) mmol/L in i. p. group, and the dose-response curve showed an obvious plateau phase. The dose-response curve showed a linear relation with the blood sugar level in the range of 2. 1-9. 2 mmol/L in s. c. group. The effective dose scope of insulin intraperitoneal injection was ±21% of the subcutaneous injection dose. CONCLUSION:Compared with subcutaneous injection, ntraperitoneal injection can control blood sugar level more stably, cause less fluctuation and a lower chance of hypoglycemia.

Analgesic effect of Yatongling Spray on experimental pain in mice

GAO Wei-song, ZHU Jian-ping

2009, 14(5):  528-530. 

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AIM:To investigate the analgesic effect of Yatongling Spray and to provide an experimental basis for its clinical use. METHODS:Experimental pain models of mice were established to investigate the analgesic effect of Yatongling Spray. (1)Writhing test: Fifty Kunming mice were divided into 5 groups(n =10 in each group, 5 male and 5 female). The mice were gavaged with physiological saline 10 mL/kg in control group, with Yatongling Spray 0. 36, 1. 08, 3. 24 g/kg in Yatongling Spray groups, and with aspirin 0. 4 g/kg in aspirin group(positive control group). Drugs were given once a day for 10 d. After the last administration, the writhing response times of mice were recorded during 5-20 min after intraperitoneal injection of acetic acid. (2) Hot plate test: A hot plate with a temperature of (55 ±1) ℃was used to test the pain threshold of mice. The time from putting on the hot plate to licking postpedes was defined as pain threshold time of mice. Fifty female mice with pain threshold times from 5 to 30 s were divided into 5 groups as described above. The pain threshold time was recorded after drug administration for 10 d. RESULTS:(1) Compared with control group, the writhing response times of mice were significantly decreased with inhibition rates of 25. 6%, 30. 6% and 43. 5% after gavaged with Yatongling Spray 0. 36, 1. 08 and 3. 24 g/kg for 10 d(P < 0. 05, P <0. 01), respectively. (2) The pain thresholds were not significantly different among the groups before drug administration(P >0. 05). After gavaged with Yatongling Spray 0. 36, 1. 08 and 3. 24 g/kg for 10 d, the pain thresholds were significantly prolonged compared with that of control group(P <0. 05, P < 0. 01). CONCLUSION:Yatongling Spray has an analgesic effect on experimental pain of mice.

Effects of rosiglitazone coadministration with compound sulfamethoxazole on the pharmacokinetics

HE Jun , DUAN Li-fang , ZHANG Wei , LI Zhi , FAN Lan , SHEN Jie , ZHOU Hong-hao

2009, 14(5):  531-535. 

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AIM:To investigate the effect of compound sulfamethoxazole on the rosiglitazone pharmacokinetics in normal Chinese subjects and assess the safety when they are coadministrated in clinic. METHODS: Ten male healthy volunteers completed a randomized, two-period, double-blind crossover study. Volunteers received single dose rosiglitazone (4 mg)in the presence and absence of compound sulfamethoxazole 1g given twice daily for 4. 5 days. The plasma drug concentrations were determined at each time point after oral rosiglitazone. The related pharmacokinetical parameters in vivo were computed. The concentrations of rosiglitazone and N-demethylrosiglitazone were assessed by HPLC-MS/MS. RESULTS:The C_max and t_maxof rosiglitazone and N-demethylrosiglitazone were not changed by compound sulfamethoxazole treatment, respectively(P >0. 05).But the AUC_0-48 of rosiglitazone was increased by 40% (P =0. 000)from (6768 ±900)ng·mL^-1·h to (9485 ±1638)ng·mL^-1·h, and the t_maxwas increased by 44% (P =0. 007)from (4. 4 ±0. 8)to (6. 1 ±1. 2)h. The AUC_0-48 of biotransformation rate of N-demethylrosiglitazone/rosiglitazone was decreased to 59. 8% (P =0. 001).CONCLUSION: Compound sulfamethoxazole decreases the rosiglitazone biotransformation rate and increases the plasma rosiglitazone concentrations in healthy volunteers when they are co-administrated.

Pharmacokinetics of chlorogenic acid in Mailuoning injection for healthy volunteers

ZHANG Jun, JU Wen-zheng, CHEN Min, LIU Fang, TAN Heng-shan, SONG Ru-jun

2009, 14(5):  536-540. 

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AIM:To study the pharmacokinetics of chlorogenic acid with a single and multiple doses of Mailuoning injection in healthy volunteers. METHODS: The concentration of chlorogenic acid in plasma was determined by LC/MS/MS after a single and multiple doses of Mailuoning injection via intravenous guttae (ivgtt) to 10 healthy volunteers. The concentrationtime curves were simulated by Drug And Statistic software (1. 0) and the pharmacokinetic parameters were calculated. RESULTS: After a single and multiple injections, the concentration-time curves of chlorogenic acid were consistent with the two-compartment model. The pharmacokinetic parameters after a single injection were as follows: C_max (252 ±66) μg/L, t_1/2β (1. 35 ± 0. 53) h, V(0. 70 ±0. 24) L/kg, CL(0. 37 ±0.10) L·kg^-1·h^-1, AUC_0-tn (404 ±110) μg·L^-1·h. The pharmacokinetic parameters after multiple injections were as follows: C_max (262 ±87) μg/L, t_1/2β (1. 37 ± 0. 27) h, V(0. 68 ±0. 24) L/kg, CL(0. 34 ±0.11) L·kg^-1·h^-1, AUC_0-tn (455 ±151) μg·L^-1·h. CONCLUSION: There were no significant differences on the pharmacokinetic parameters of chlorogenic acid after a single and multiple injections in healthy volunteers, there were no accumulations with multiple injections and no differences of physiological disposition between the male and female for chlorogenic acid.

Study on cisplatin pharmacokinetics:preoperative intraperitoneal administration versus intravenous chemotherapy with cisplatin for advanced gastric carcinoma

LI Hao-xia, CHEN Xiao-liang, MA Zhi-min

2009, 14(5):  541-545. 

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AIM:To compare the characteristics of cisplatin pharmacokinetics: preoperative intraperitoneal administration versus intravenous chemotherapy with cisplatin for advanced gastric carcinoma. METHODS: 50 patients with resectable advanced gastric cancer were randomly divided into 2 groups: 26 cases with preoperative intraperitoneal administration of cisplatin (i. p. group)and 24 cases with preoperative intravenous administration of cisplatin (i. v. group).Each patient was given 60 mg/m² cisplatin intraperitoneally or intravenously. The peritoneal fluid, blood from gastric sinistral vein and peripheral blood were taken on the 180th minutes after the drug was administrated. Cancer tissues and normal tissues beside the cancer tissue were collected at the 270th minutes during operation. Another 8 cases were used to study the pharmacokinetics of intraperitoneal administration and intravenous chemotherapy with cisplatin. The concentrations of cisplatin in different samples were measured by the flameless type of atomic absorption spectrometry. RESULTS: The high cisplatin concentration in abdominal cavity could maintain for fairly longer time by intraperitoneal administration more than by intravenous administration. And the plasma concentrations of cisplatin in peritoneal cavity were similar by the two injection styles. The AUC with intraperitoneal administration was about five times than that with intravenous administration. The cisplatin concentrations of peritoneal fluid and vena gastrica sinistra blood in the i. p. group were 23. 4 and 2. 53 times higher than those in the i. v. group respectively (P <0. 01).The cisplatin of the cancer tissue in the i. p. group was higher than that in the i. v. group(P <0. 05).CONCLUSION:The intraperitioneal cisplatin chemotherapy has better pharmacokinetics parameters and could be a useful accessory treatment for the advanced gastric carcinoma cancer.

Tolerability research of single dose of iptakalim hydrochloride in healthy Chinese volunteers

FANG Yi, WANG Rui, CHAI Dong, CUI Wen-yu, WANG Hai, GUAN Hua-shi

2009, 14(5):  546-550. 

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AIM:To evaluate the safety and tolerability of single dose of iptakalim hydrochloride in healthy Chinese volunteers. METHODS:52 healthy volunteers in 18-50 years old were chosen and randomized into 6 dose groups, including 2. 5, 5, 10, 15, 20, 25 mg. Group B, C, D, E contained 10 volunteers respectively, and Group A and F contained 6 volunteers. Each group contained 2 volunteers (1 male and 1 female)who were administrated with placebo. Clinical symptoms, vital signs, the changes of laboratory examination indexes, and all adverse drug events were observed. RESULTS:After single dose of 2. 5-25mg, the clinical symptoms, vital signs and index of laboratory examination were in normal range. There were no severe adverse events, and no adverse events were related to the drug. CONCLUSION:The single-dose of iptakalim hydrochloride range from 2. 5 mg to 25 mg in healthy Chinese volunteers were safe and tolerable in 52 healthy Chinese volunteers.

Study on toxicokinetics in wild aconite poisoned rabbits after hemoperfusion

QIU Qiao-meng, LIANG Huan, HONG Guang-liang, LU Zhong-qiu, LIU Gang, WANG Zhi-yi

2009, 14(5):  551-556. 

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AIM:To establish an HPLC/MS method for simultaneous determination of mesaconitine, aconitine and hypaconitine in rabbit plasma, and study their toxicokinetics in wild aconite poisoned rabbits after hemoperfusion. METHODS:Eight health grownup male Japan big ear white rabbits [the body weight (2. 5 ±0. 2)kg] were intragastrically poisoned by wild aconite liquor 1. 0 mL/kg and the hemoperfusion was given for 2 h at 0. 25 h after poisoning. The blood was taken after poisoned 0. 5, 1, 1. 5, 2, 3, 6, 12, 24 h respectively. The concentrations of mesaconitine, aconitine and hypaconitine in plasma were detected by HPLC/MS. The toxicokinetics parameters were calculated by DAS 2. 0 program. RESULTS:The parameters of toxicokinetics for mesaconitine in wild aconite poisoned rabbits after hemoperfusion were as following: t_max(3. 1 ±0. 8)h, C_max(11. 5 ±2. 1)μg/L, K_a(1. 6 ±0. 9)h, K_e(0.13 ±0. 05)h, t_1/2(5. 9 ±1. 7)h, V/F (85. 4 ±20. 9)L/kg, CL/F (10. 28 ±1. 46) L·h^-1 ·kg^-1. The parameters of toxicokinetics for aconitine were as following: t_max(3. 2 ±0. 5)h, C_max (18. 7 ±5. 5)μg/L, K_a (1. 2 ±0. 4)h, Ke (0.10 ± 0. 03)h, t_1/2(7. 5 ±2. 4)h, V F(2. 7 ±1. 0)L/kg, CL/F(0. 25 ±0. 08)L·h^-1 ·kg^-1. The parameters of toxicokinetics for hypaconitine were as following: t_max(3. 0 ±0. 8)h, C_max(14. 6 ±11. 0)μg/L, K_a(1. 4 ± 1. 2)h, K_e(0. 09 ±0. 03)h, t_1/2(8. 3 ±2. 1)h, V/F (10. 7 ± 6. 9) L/kg, CL/F (0. 85 ± 0. 38) L·h^-1 ·kg^-1. CONCLUSION:The toxicokinetics of mesaconitine, aconitine and hypaconitine in wild aconite poisoned rabbits after hemoperfusion are fitted to the one-compartment model with first-order absorption.

Study on the dose-effect relationship of Danggui-Shaoyao-San′s ingredients proportion in dysmenorrhea mice

HUA Yong-qing, XIE Hai-tang, DUAN Jin-ao, SU Shu-lan, QING Ping

2009, 14(5):  557-563. 

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AIM:To analyze the influence of different combinations and proportions of Danggui- Shaoyao-San′s ingredients in treating primary dysmenorrhea. METHODS:The dysmenorrhea mouse model was established by oxytocin. The ingredient compatibility was analyzed by orthogonal t design and the appropriate proportion relationship was researched by uniform design. The latent period and number of twisting body were recorded to evaluate the intensity of dysmenorrhea. The algomenorrhea effect was observed with the treatment of Danggui-Shaoyao-San or the combination of different ingredients in a prescription. RESULTS: The orthogonal t design experimental results showed the latent period was significantly prolonged by Paeonia lactiflora Pall. (B), Angelica sinensis Diels. (A)and Ligusticum chuanxiong Hort. (C), the number of twisting body was decreased by B. Poria cocos Wolf. (D), Alisma orientalis Juzep (E)and Atractylodes macrocephala Koidz. (F)had no significant influence on the latent period and the number of twisting body. The uniform design results showed the indexes were fitted with regression equation, the data of each variable had mild surface effect, the proper proportion between A∶B∶C was 8. 28∶13. 3∶4. 6 through surface analysis, and the above conclusion was proved. CONCLUSION: The influnce on twisting body in algomenorrhea mouse of B was obvious, while A, C take the second place, D E, F played auxiliary function. The study gave strong support to the original formula to put B in a very important position, and it was speculated that slightly modulating the proportion of ingredients might bring better effects. The orthogonal t design and uniform design are valuable methods in studying multi-ingredient formulae of traditional Chinese medicine.

Expressions of epithelial cell-derived neutrophil-activating protein-78 in moderate and severe acute asthma children and the influence of methylprednisolone

JIN Xiao-hong, CHEN Cun-guo, LI Feng-xian, LI Shao-bo, CHEN Li-li, CHEN Bao-guo, TONG Xia-shen

2009, 14(5):  564-566. 

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AIM:To observe the expressions of epithelial cell-derived neutrophil-activating protein-78 in acute asthma of severe cases and the influence of methylprednisolone. METHODS:Children with moderate and severe acute asthmawere divided into urbason pre-interfere group, post-interfere group, and the pediatric surgery indirect hernia children as control group (without asthma case history), the numbers of heterophil granulocyte(PMN) in peripheral blood preparation were detected, and the expressions of EAN-78 protein were measured by flow cytometry. RESULTS:Compared with the control group, the levels of ENA-78 protein in asthma group were higher(P <0. 01). Compared with post-interfere group, the levels of ENA-78 protein in pre-interfere group were significantly higher (P <0. 01). Compare with the control group, the numbers of peripheral blood PMN in pre-interfere and post-interfere group were increased, there were significant differences(P <0. 01), and there were no significant differences about the numbers of PMN between pre-interfere and post-interfere group (P >0. 05). There was a positive correlation between the levels of ENA-78 protein and the numbers of PMN by methylprednisolone (n =32, r =0. 865, P <0. 01). CONCLUSION: The levels of ENA-78 protein and the numbers of PMN in blood are increased in moderate and severe acute asthma children. They may be involved in the inflammation process of asthma pathogenesis. Methylprednisolone can relieve the airway inflammation by inhibiting the expressions of ENA-78 protein.

Effects of valsartan-hydrochlorothiazide combination on early renal damage of the patients with essential hypertension

CAO Dong-ping, PENG Ying-xin, YAO Wen-jing, RONG Chun-li, YU Wei, QIAO Shu-zhang

2009, 14(5):  567-571. 

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AIM:To evaluate the efficacy and safety of valsartan-hydrochlorothiazide combination on renal early damage of the patients with essential hypertension. METHODS:Sixty-four patients with essential hypertension whose serum and urine levels of β₂- microglobulin were high were randomly single-blindly divided into two groups. 32 patients in valsartan-hydrochlorothiazide combination group took the compound preparation containing valsartan 80 mg and hydrochlorothiazide 12. 5 mg once a day. 32 patients in valsartan group took valsartan 80 mg once a day. The treatment were lasted for two months. The static and dynamic blood pressure, blood urea nitrogen, serum creatinine, urine α1-microglobulin, serum and urine β₂-microglobulin and urinary microalbumin were determined before and after the treatment. RESULTS:After the treatment, the levels of systolic and diastolic blood pressure were decreased significantly in two groups. The decrease amplitude in valsartan-hydrochlorothiazide combination group was superior to that in valsartan group (P <0. 01).Urine α1-microglobulin, β₂-microglobulin in serum and urine were all decreased in two groups, and those in the valsartan-hydrochlorothiazide combination group were significantly lower than those in valsartan group(P <0. 01).The blood urea nitrogen, serum creatinine and urine α1-microglobulin were all decreased in two groups(P <0. 05).CONCLUSION: Both of the two regimens have protective effects in early renal damage of the patients with essential hypertension and the combined treatment has better effect on reducing hypertension along with the concentration of urinary microalbumin and β₂-microglobulin in serum and urine.

Clinical study on total intravenous anesthesia with sufentanil-profofol given by target-controlled infusion in neurosurgical operations

JIN Li-da, JIANG Liu-ming, ZHAO Xi-yue, LIN Li-na

2009, 14(5):  572-576. 

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AIM:To evaluate the anesthetic effect and the safety of total intravenous anesthesia (TIVA) with sufentanil-profofol given by target-controlled infusion in neurosurgical operations and to compare with intravenous inhalational anesthesia. METHODS:30 patients scheduled for craniocerebral operations were randomly divided into 2 equal groups: the TCI group (target- controlled infusion anesthesia) and combined IV and inhalation anesthesia (control group). Patients in the TCI group were anesthetized by TIVA with target controlled infusion of sufentanil (0. 2-0. 6 ng/mL) and propofol(3 μg/mL). Patients in the control group were given disconnected IV injections of vecuronium bromide combined with inhalation of 1% -2% isoflurance. The spectral index (BIS), mean arterial blood pressure (MAP) and heart rate (HR) of the patients were recorded at eight time points:before induction (T₀), after induction (T₁), after tracheal intubation (T₂), scalp incision(T₃), skull opening (T₄), tumor resection(T₅), scalp closure (T₆), extubation (T₇). Recording the awakening time, extubation time, anesthesia adverse reaction, degree of vigilance (OAAS scores) and pain degree(VRS scores) immediately and 30 min after extubation. RESULTS:The values of BIS in patients of both groups were significantly decreased after the induction of anesthesia and were maintained among 40 to 60, there were no significant differences between two groups(P >0. 05). At the T1, T3, T4, T7 time point, changes of the MAP and HR were more stable in TCI group than those in control group. The awakening time and extubation time in TCI group was obviously shorter in than that in control group. The OAAS scores after extubation were higher and the VRS scores 30 min after extubation were lower in TCI group than those in control group (P <0. 05). The occurrences of postoperative nausea, vomiting and restlessness were more frequently observed in patients in the control group than those in the TCI group. CONCLUSION:Target controlled infusion with sufentanil and propofol for TIVA has advantages of stability in hemodynamics, rapid recovery, less complications, no air pollution and is suitable for neurosurgical operation.

Effects of ketamine on preventing the increase of postoperative morphine requirement induced by fentanyl

YU Xue-rong, HUANG Yu-guang, WANG Hai-lan, JU Xia

2009, 14(5):  577-581. 

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AIM:To observe the effects of ketamine on preventing the increase of postoperative morphine requirement induced by fentanyl.METHODS: Sixty women undergoing total abdominal hysterectomy by spinal anaesthesia were assigned to 4 groups consisting of placebo (normal saline, C), fentanyl (3 bolus of 1 μg/kg, at 15 min intervals, F), ketamine (infusion of 15 μg·kg^-1 ·min^-1 ketamine from the skin incision until 20 min before the end of the surgery, K), ketamine and fentanyl (infusion of 15 μg·kg^-1·min^-1 ketamine from the skin incision until 20 min before the end of the surgery plus 3 bolus of 1 μg/kg fentanyl, at 15-min intervals, FK). The cumulative morphine consumption, pain score, and adverse effects (nausea, vomiting, hallucination, dizziness and itching) were recorded at 1, 3, 6, 12, 24, 48 h postoperatively. RESULTS:There were no significant differences in age, weight, duration of surgery and the post-operative sensory block time. The cumulative morphine consumption in group F was significantly higher than those in group C at 3, 6, 12 h postoperatively (P <0. 05). The postoperative cumulative morphine consumption was similar in group C, K and FK. No differences in posterative pain score were observed among the group. More patients in K and FK group had hallucination during and or after the surgery than those in group C (P <0. 05). CONCLUSION: These results suggested that intraoperative administration of fentanyl increased postoperative morphine consumption, which could be prevented by coadministration of ketamine.

Effects of Quyuningxin pill to unstable angina pectoris efficacy and serum C-reactive protein

SHI Hai-xia, HUANG Ji-han, LI Qing-hai, BIAN Ka

2009, 14(5):  582-585. 

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AIM:To observe the clinical effect of Quyuningxin pill on the serum concentration of C-reactive protein (CRP) from coronary heart disease (CHD) patients with unstable angina pectoris, and explore the related mechanisms. METHODS:Sixty patients of CHD with unstable angina pectoris were divided randomly into treatment group (30 cases) and control group (30 cases). The treatment group was given conventional western medical combined with Quyuningxin pill. The control group was given conventional western medical only. The course of treatment lasted for four weeks.The serum CRP concentration was measured before and after treatment. The changes of angina pectoris and other clinical syndrome as well as electrocardiogram were also observed. RESULTS:The serum concentration of CRP of Quyuningxin pill treated group was decreased markedly comparing with that of control group (3. 8 ±0. 9 vs 5. 8 ±1. 8, P <0. 05). After the treatment, the total effective rate of angina pectoris remission, clinical syndrome, electrocardiogram in treatment group were significantly higher than those in the control group (89. 29%, 89. 29%, 75. 0% vs 66. 67%, 66. 67%, 55. 56% P <0. 05). CONCLUSION: Quyuningxin pill can significantly improve myocardial ischemia related symptoms together with the serum CRP concentration in the patients with unstable angina pectoris.

Effects of γ-globulin on MMP-2, MMP-9 and TNF-αsecretion in human umbilical veins endothelial cells stimulated by serum from children with Kawasaki disease

ZHANG Yuan-hai, HE Yue-e, XIANG Ru-lian, WU Rong-zhou, XU Qiang, RONG Xing, CHEN Qi

2009, 14(5):  586-590. 

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AIM:To investigate the inducible matrix metalloproteases-2 (MMP-2), matrix metalloproteases- 9(MMP-9)and TNF-αsecretion in human umbilical veins endothelial cells (HUVECs)stimulated by the serum from children with acute phase of Kawasaki disease (KD)and the regulation effect of γ-globulin on MMP-2, MMP-9 and TNF-αsecretion. METHODS: HUVECs were cultured in six different conditional mediums with normal serum group (Group C), febrile serum group(Group F), KD without coronary artery lesion serum group(Group NAC), KD without coronary artery lesion serum added γ- globulin group (Group NACI), KD with coronary artery lesion serum group (Group AC), and KD with coronary artery lesion serum added γ-globulin group(Group ACI).The activities of MMP-2, MMP-9 and TNF-αin supernatant were detected using enzyme-linked immunosorbent assay (ELISA)after 12 h cultivation. RESULTS:The concentrations of MMP-2, MMP-9 and TNF-αin supernatant inHUVECs cultured with 10% serum from KD patients were significantly higher in Group AC or Group NAC than those in Group C and Group F (P <0. 01), there was statistical significance between in Group AC and Group NAC (P <0. 01).The concentrations of MMP-2, MMP-9 and TNF-αin supernatant in Group F were significantly lower than those in Group AC or Group NAC (P <0. 01), but were significantly higher than those in Group C (P <0. 01).The levels of MMP-2, MMP-9 and TNF-αin supernatant in HUVEC cultured with γ-globulin significantly were decreased in Group AC and Group NAC, there were statistical difference (P <0. 01).The levels of MMP-2 andMMP-9 in supernatant and the content of TNF-αhad significant positive correlation(r =0. 839, 0. 765, P <0. 01). CONCLUSION:The levels of MMP-2, MMP-9 and TNF-αin HUVEC induced by the serum f rom KD patients are increased and might take part in the formation and development of coronary artery lesions. The inhibition effects of γ-globulin on MMP-2, MMP-9 and TNF- αsecretion in endothelial cells could be related to the mechanism which γ-globulin prevents the happening of coronary artery of KD.

Clinical evidence-based study on new-generation drug-eluting stent: everolimus-eluting stents (Xience V)

GAO Wen-jun, LIU Wen-jie, KE Yong-sheng

2009, 14(5):  591-595. 

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Percutaneous coronary intervention (PCI) has been a mainstay in the management of coronary artery disease since its introduction in the late 1970s. Bare-metal stents and, more recently, first-generation drug-eluting stents (DES), such as sirolimuseluting (Cypher) and paclitaxel-eluting stents (Taxus), have further improved results of percutaneous coronary intervention by improving early results and reducing the risk of restenosis. There are currently debates on the safety of these first-generation DES, given the potential for late stent thrombosis which is a first-generation drug-eluting stent of the largest security issue, especially after discontinuation of dual antiplatelet therapy. Next-generation DES such as everolimus-eluting stents (Xience V) holds the promise of superior antirestenosis efficacy as well as long-term safety. This review makes a presentation of the evidence-based clinical research according to everolimus-eluting stents (Xience V).