Table of Content

Volume 18 Issue 11
26 November 2013

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Effect of candesartan on HOMA-IR and serum adiponectin of spontaneously hypertensive rats

LI Xiao-yan, ZHANG Ping, TAO Ling, LIU Yu-xing

2013, 18(11):  1201-1204. 

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AIM: To investigate the effect of candesartan, an angiotensin II receptor antagonist, on HOMA-IR and serum adiponectin of spontaneously hypertensive rats(SHRs).METHODS: SHRs were divided into two groups: Hypertension group (SHR, n=30), Candesartan group (Candesartan, 1 mg·kg^-1·d^-1, n=30, gavaging for 12 weeks).WKY rats were the control group(WKY, n=30). The other two groups were given a placebo. Fasting blood glucose and serum insulin were measured by biochemistry methods, insulin resistance index (HOMA-IR) was calculated,OGTT was tested by biochemistry methods. Changes of serum adiponectin were measured by ELISA.RESULTS: No difference in the fasting blood glucose of the three groups (P>0.05) was observed. Serum insulin level and HOMA-IR of SHRs were higher than those of WKY and drug groups (P<0.05). Candesartan could not reduce those of SHRs. Serum adiponectin level of SHRs was lower than that of WKY, and candesartan could obviously increase that of SHRs (P<0.05). The result of OGTT showed that blood glucose level at 30 min or 120 min in hypertension group compared with control group and candesartan group were higher.CONCLUSION: Candesartan could ameliorate the upregulaiton of serum adiponectin in SHR, improve insulin resistance and reduce blood glucose level of SHR at 30 min and 120 min.

Pharmacokinetics of Combretastatin A4 and Combretastatin A4 Phosphate in SD rats

ZHANG Xiao-lan¹, WANG Zhi-qiang², SUN Jian-guo¹, PENG Ying¹, ZHONG Yun-xi¹, HAO Kun¹, ZHANG Cang², WANG Guang-ji¹

2013, 18(11):  1205-1210. 

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AIM: An LC-MS/MS method was set up for the comparative evaluation of pharmacokinetics of CA4P and CA4 in SD rats. METHODS: 12 fasted SD rats were single intravenous administration of 50 mg/kg CA4P or 36 mg/kg CA4 (same molar amount). Plasma samples were collected at different time points and concentrations of CA4P and CA4 were analyzed by LC-MS/MS.The pharmacokinetic parameters were calculated and CA4P-CA4 transformation were simulated by pharmacokinetic model.RESULTS: After i.v. administration of 50 mg/kg CA4P or 36 mg/kg CA4, the AUC_0-∞ of CA4P or CA4 were (27126±4142), (7751±801) and (5037±1433) ng·h·mL^-1, respectively, the t_1/2 were (0.85±0.35), (1.27±0.33) and (0.95±0.65) h, respectively. No gender differences were found in rats.CONCLUSION: The exposure of CA4 was increased significantly by soluble CA4 phosphate in SD rats. CA4P was rapidly transformed into CA4 after a single i.v. administration of CA4P in rats, according to the pharmacokinetic model of CA4P-CA4 transformation set up by us.

Inhibition study of cytochrome P450 isozymes by (5R)-5-hydroxytriptolide using in vitro “cocktail” method

LIU Hai-yan, ZHANG Le-duo, XIANG Zhi-xiong, MIAO Hong

2013, 18(11):  1211-1218. 

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AIM: To evaluate whether 5-hydroxytriptolide (T8) is a direct inhibitior or time-dependent inhibitor of CYP3A/5, CYP2D6, CYP2C9, CYP1A2, CYP2C19, CYP2B6 and CYP2C8, and to evaluate the potential of drug-drug interaction with the substrates of above seven CYPs in clinical study, which provide a reference for clinical drug-drug interaction study.METHODS: IC₅₀ and IC₅₀ shift method were used in this study.RESULTS: The IC₅₀ of T8 on above seven CYPs was more than 100 μmol/L in direct inhibition experiment, and no IC₅₀ shift occurred in time-dependent inhibition experiment.CONCLUSION: T8 is neither a direct inhibitor nor time-dependent inhibitor of above seven CYPs, and the potential of drug-drug interaction caused by T8 inhibition on CYP450 isozymes is slim.

The protective effects of Jidesheng Sheyao pian on lung ischemia-reperfusion injury in rats

TAO Dong-ying, NI Jing-jing, REN Dian-huan, YU Ji-mian, ZHANG Xiu-juan, WANG Yong

2013, 18(11):  1219-1223. 

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AIM: To investigate the protective effects and the mechanisms of Jidesheng Sheyao pian on lung ischemia-reperfusion injury of rats.METHODS: Thirty SD male rats were divided into Jidesheng Sheyao group (n=10), control group (n=10) and ischemia-reperfusion injury group (I/R, n=10). The models of lung ischemia-reperfusion injury of SD rats were established. Then, the wet/dry ratio was measured, the histopathology of the lung injury was observed by light microscope and electron microscope, the activity of matrix metalloproteinase-2 (MMP-2), matrix metalloproteinase-9 (MMP-9) in the lung homogenates were detected by zymography, RT-PCR the expression of MMP-2, MMP-9 mRNA were detected in rat lung tissues.RESULTS: Compared with the I/R group, the wet/dry ratio were significantly decreased (P<0.01), the degree of lung injury showed lighter, the activity of MMP-9 in lung homogenate presented inhibition (P<0.01) in the drug group and the expression of MMP-9, MMP-2 mRNA was also depressed than that of the I/R group.CONCLUSION: Jidesheng Sheyao pian can inhibit the expression and activity of MMP-9 and MMP-2, attenuate basement membrane degradation, sequentially, has protective effects on lung ischemia-reperfusion injury in rats.

Cardioprotective effect and its mechanism of total saponin from Panacis majoris rhizoma on myocardium ischemia/reperfusion injury in rats

LIU Ai-hua¹, SHI Meng-qiong¹, YAN Wen-yan¹, YANG Wei-hong¹, GONG Xue-qian¹, XIONG Yan-qiang¹, ZHOU Ji-gang², LUO Tao², ZHANG Ji-hong²

2013, 18(11):  1224-1232. 

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AIM: To investigate the cardioprotective effects of total saponin from Panacis majoris rhizoma on myocardium ischemia/reperfusion injury (MI/RI) and its mechanism.METHODS: All rats were randomly divided into four groups: sham-operated, model group and total saponin of Panacis majoris rhizoma (100, 200 mg/kg); The pretreated group was given total saponin of Panacis majoris rhizoma. After pretreating for 7 days, the myocardium ischemia model was induced by ligating the left anterior descending coronary artery in rats. After ligating 30 min, and then reperfusing 24 h. The incidence of arrhythmia at the begining 30 min, and hemodynamic parameters after 24 h were measured; The serum levels of LDH, CK, SOD, GSH-Px, CAT and MDA were also measured; Real-time PCR was applied to detect the mRNA expressions of SOD1-SOD3, GPX1 and CAT antioxidative genes, the expressions of Nrf2 in the cell hyalomitome and nucleus were detected by Western blotting.RESULTS: Total saponin from Panacis majoris rhizome (100, 200 mg/kg) might significantly decrease incidence of arrhythmia, improve heart function and heart histomorphpolgy, decrease the levels of serum LDH, CK, MDA and infarct size, improve the activities of SOD, GSH-Px, CAT (P<0.05, P<0.01, respectively); Moreover, the mRNA expressions of SOD1-SOD3, CAT and GPX1 in the myocardial tissues decreased remarkably in the model group, while were up-regulated in total saponin from Panacis majoris rhizome-pretreatment groups (P<0.05, P<0.01, respectively), the protein expressions of Nrf2 in the nucleus were significantly increased compared with model group (P<0.01, respectively), but it did not influence in the cell nucleus among the group.CONCLUSION: Total saponin from Panacis majoris rhizome exerts beneficially cardioprotective effects on MI/RI rats, mainly activating anti-oxidative pathway of Nrf2 and opposing lipid peroxidation.

Effects of atorvastatin on ApoA-I and SR-B1 in ApoE-deficient mice

DING Jie-wei¹, WANG Jian-ping²

2013, 18(11):  1233-1237. 

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AIM: To study the effects of atorvastatin on the atherosclemtic (AS) lesion formation and expression of the hepatic ApoA-I and scavenger receptor-1 (SR-B1) in apolipoprotein E-deficient (ApoE^-/-) mice.METHODS: Thirty male ApoE^-/- mice were randomized into three groups: control group (group B, saline vehicle), atorvastatin low dose group (group C, 10 mg·kg^-1·d^-1) and high dose group (group D, 20 mg·kg^-1·d^-1).Ten male C57BL/6J mice as normal group (group A, saline vehicle) were treated with saline vehicle. At the end of twelve weeks of drug administration,all mice were sacrificed.The serum levels of total cholesterol (TC),triglyceride (TG) and high density lipoprotein cholesterol (HDL-C) and low density lipoprotein cholesterol (LDL-C) were measured.Atherosclerotic plaque in the thoracic aorta was examined using Hematoxy-Eosin staining and oil red O staining. ApoA-I and SR-B1 were detected by Western blot. Real-time quantitative PCR was used to determine the ApoA-I and SR-B1 mRNA expressions in the liver.RESULTS: Significant hyperlipidemia and atherosclerotic plaque formation were detected in ApoE^-/- mice, compared with group A [TG: (2.93±0.18) mmol/L vs (0.59±0.09)mmol/L;TC:(21.78±2.03) mmol/L vs (2.13±0.24) mmol/L;HDL-C:(2.86±0.26) mmol/L vs (0.57±0.10) mmol/L;LDL-C:(18.92±1.87) mmol/L vs (1.54±0.21) mmol/L;P<0.01]. Treatment with atorvastatin decreased serum concentration of TC and LDL-C [TC group B:(21.78±2.03) mmol/L, group C:(11.79±0.98) mmol/L,group D(10.07±1.03) mmol/L;LDL-C group B:(18.92±1.87) mmol/L,group C:(8.76±1.15)mmol/L,group D:(7.91±0.77) mmol/L;P<0.01], and reduced area of the atherosclerotic plaque compared with ApoE^-/- control mice [group B:(23.12±3.46)×10⁴ μm²,group C:(11.42±1.25)×10⁴ μm²,group D:(7.34±1.03)×10⁴ μm²,P<0.01]. Atorvastatin up-regulated the expression of ApoA-I and SR-B1 compared with ApoE^-/- control mice (ApoA-I group B:1.08±0.10,group C:1.36±0.11,group D:1.78±0.14;SR-B1 group B:0.72±0.07,group C:1.46±0.14,group D:1.50±0.21, P<0.01).CONCLUSION: Atorvastatin impeded the progression of atherosclerosis in ApoE^-/- mice possibly through improvement of lipid metabolism and up-regulation of ApoA-I and SR-B1.

Differences in anxiety-related behavior induced by mCPP and responses to diazepam in two strains of mice

YAN Li-ping, ZHANG Li-quan, YI Hui-min, ZHOU Xue-jun, WANG Jue, ZHANG Qi, YE Yi-lu

2013, 18(11):  1238-1243. 

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AIM: To compare the differences in anxiety-related behavior induced by chlorophenylpiperazinehydrochloride (mCPP) and response to diazepam in BALB/c mice and ICR mice.METHODS: Each were divided into four groups: saline group, mCPP group, diazepam group and (diazepam+mCPP) group. Diazepam was administrated intraperitoneally and mCPP was administrated subcutaeously 30 min before behavioral test. Open-field test, light-dark transition test and elevated plus maze test were used.RESULTS: In open-field test, the central distance ratio and the central time ratio were increased in the (diazepam+mCPP) group of BALB/c mice. But there were no effects on ICR mice.Only was there significant difference on total distance between two mice strains.In light-dark transition test, latency into dark box and number of transitions were increased, and time ratio in dark box was decreased in (diazepam+mCPP) group of two strains mice. The response to diazepam was were more sensitive in BALB/c mice than ICR mice. Number of open-arm entries, time and exploring time ratio in open-arm in the elevated plus maze all increased in (diazepam+mCPP) group of two strains mice. There were differences of time and exploring time in open-arm between them.CONCLUSION: The response to diazepam is more sensitive in anxiety mice than normal mice.BALB/c mice have low level of anxiety, high baseline exploration and risk assessment of a new environment, which is a suitable mice strain to develop anxiolytic drugs.

Application of SAS procedures in evaluation of trough／peak ratio in ambulatory blood pressure monitoring

HUANG Yao-hua, TANG Xin-ran, WANG Yang, ZHAO Yan-yan, LI Wei

2013, 18(11):  1246-1250. 

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AIM: To explore the SAS macros implementation of trough/peak in ambulatory blood pressure with different kinds of records.METHODS: Implying procedure retain, SQL and cycling do, create macro procedure outputting statistical analysis report forms.RESULTS: After checked data entered into the SAS procedure, average difference of blood pressure values per hour in 24 hours after drug administration was created when running the macros. The whole trough/peak ratios of treatment and control groups were finally calculated.CONCLUSION: Trough/peak ratio required by clinician could be obtained by using macros dealing with ambulatory blood pressure with records exceeding 24 hours after taking medicine.

Bleeding risk is higher when warfarin used alone compared to the associated use of aspirin with clopidogrel

YUN Wen-bo¹, JIANG Peng-li¹, WU Jing¹, SUN He^1,2

2013, 18(11):  1251-1259. 

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AIM: To compare the risk of bleeding complication due to the associated use of aspirin with clopidogrel compared to those warfarin used alone based on FDA Spontaneous Reporting System and Adverse Events Reporting System (SRS/AERS) database.METHODS: After excluding duplicated records, reports were divided into three index groups i.e. associated use of aspirin with clopidogrel group, warfarin group and reference group,and define haemorrhages-related adverse events (HRAEs) according to Medical Dictionary for Regulatory Activities. Descriptive statistics, logistic regression and odds ratios were used to estimate the risk and difference of bleeding complications for these three scenarios.RESULTS: frequency of HRAE connected with the associated aspirin/clopidogrel use was 20.80%, and gastrointestinal system HRAEs were the most frequently reported bleeding event (8.23%). The frequency of HRAE connected with the warfarin used alone was 22.30%, and gastrointestinal system HRAEs were the most frequently reported bleeding event (7.81%). The frequency of nervous system HRAEs for different groups has no significant difference (P>0.05). The frequency of HRAEs increased as age increases for both groups.CONCLUSION: The risk of HRAEs with warfarin used alone (20.80%) is higher than the associated aspirin/clopidogrel use (22.30%) in the clinical use based on FDA SRS/AERS (P<0.05). The types of bleeding complications are not similar for both situation.

Single-dose and multi-dose pharmacokinetics and bioavailability of ofloxacin sustained-release tablets in healthy volunteers

ZHONG Guo-ping¹, CHEN Xiao², REN Bin², ZHONG Shi-long³, KUANG Cui-yi², HUANG Li-hui¹, ZENG Gui-xiong¹, WANG Xue-ding¹, LIAO Xiao-xing², HUANG Min¹, ZHAO Xiang-lan¹

2013, 18(11):  1260-1265. 

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AIM: To study the single-dose and multi-dose pharmacokinetics and bioavailability of ofloxacin sustained-release tablets in healthy volunteers.METHODS: The plasma concentrations of ofloxacin were determined by a RP-HPLC method. The reference or test preparation was given to healthy male volunteers according to an open randomized crossover study.The pharmacokinetic parameters and bioavailability of test preparation were compared with reference preparation.RESULTS: The main pharmacokinetic parameters of the test preparation and the reference preparation, the single-dose were as follows: C_max were (5382± 1558)and (3419±1034) μg/L, T_max were (1.7±0.6)and(4.2±1.8) h, t_1/2 were(8.2±1.0) and(7.6±1.8) h, MRT were(8.6±0.9) and(10.3±1.4) h;AUC_0-t were (33764±5297) and(31280±4412) μg·L^-1·h,AUC_0→∞ were (34643±5356)and (32642±4257) μg·L^-1·h. The relative bioavailability of reference to test preparation was (97.9±12.4)%.There were statistically significant difference about C_max,T_max,MRT between the reference preparation and test preparation, but there were no statistically significant difference about t_1/2,AUC_0-t,AUC_0→∞. The 90% confidence limit of AUC_0-t and AUC_0→∞ between the reference preparation and test preparation were 89.0%-97.0% and 91.4%-97.8% respectively. The multi-dose were as follows: C_max were (3732±1502)and (3564±982) μg/L, C_min were (750±193),(438±89) μg/L,T_max were (1.5±0.5) and(3.7±1.7) h, AUC_SS were (32689±4786) and(33591±7929) μg·L^-1·h, C_av were(1362±199)and (1405±337)μg/L,DF were (216±76)and(222±34)%.The relative bioavailability of reference to test preparation was (102.9±22.5)%. There were no statistically significant difference about C_max,C_av,AUC_SS, DF between the reference preparation and test preparation. The 90% confidence limit of C_max, AUC_SS,C_av and DF were 80.8% -114.6%,89.3%-111.9%,89.5% -112.4% and 93.7%-122.4%.CONCLUSION: The results of statistics analysis showed that the test preparation exhibited sustained-release characteristics, and it was bioequivalent between the test preparation and the reference preparation.

Determination of glimepiride and its active metabolite in human plasma by HPLC-MS/MS

LI Ting^1,2, NAN Feng¹, CHEN Zhi-hui¹, YU Qin¹, XIANG Jin¹, QING Yong-ping¹, XIE Kun¹, LIANG Mao-zhi¹, CHAO Ruo-bing²

2013, 18(11):  1266-1269. 

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AIM: To develop a sensitive liquid chromatography tandem mass spectrometry(HPLC-MS/MS)method for analyzing glimepiride(G)and its active metabolite hydroxyl-glimepiride(M₁)in human plasma.METHODS: G and M₁ were extracted from plasma samples by ethyl acetate after acidification,with gliclazide (IS) serving as an internal standard. The analytes went through the column of Phenomenex Gemini C₁₈ (50 mm× 3.0 mm,5 μm) with mobile phase methanol-water-formic acid (80∶20∶0.1) and were analyzed under the multiple reaction monitoring mode using the eletrospray ionization (ESI) technique. The ion pairs being detected were( m/z) 491.4→352.4,507.4→352.4,324.4→127.2,respectively.RESULTS: The standard curves of G and M₁ were linear in the range 1.25-400 ng/mL and 0.313-100 ng/mL,with a low limit of quantification of 1.25 and 0.313 ng/mL.The intra and inter day RSD were below 10%,with recovery rates ranging from 96.4% to 102.5%.CONCLUSION: The method is simple, rapid, sensitive, and suitable for the determination of glimepiride and its metabolite in human plasma.

Efficacy comparison of two methotrexate regimen in the non-surgical treatment for ectopic pregnancy with different pre-treatment β-HCG rising ratio

CHEN Jun-xia, WANG Yun-gen, SHAN Jiang-jing, RUAN Ya-wen

2013, 18(11):  1270-1274. 

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AIM: To compare the curative effect of different methotrexate medication in ectopic pregnancy with different β-human chorionic gonadotropin (β-HCG) rising ratio.METHODS: A retrospective study was conducted on 90 patients treated with methotrexate intramuscular injection due to unruptured ectopic pregnancy. According to different pre-treatment β-HCG rising ratio(pre-treatment β-HCG rised more or less than 20% in 48 hours) and different methotrexate regimen(methotrexate 75 mg one dose intramuscular injection or 100 mg divided into five doses intramuscular injection),all the 90 patients were divided into four groups,and we compared the efficacy and side effects between groups.RESULTS: For patients whose pre-treatment β-HCG rised more than 20% in 48 hours,given 100 mg methotrexate divided into five doses intramuscular injection resulted in less repeat therapy(P<0.05) and shorter time for β-HCG levels to fall to normal(P<0.05).For patients whose pre-treatment β-HCG rised less than 20% in 48 hours,both two treatments had similar effection(P>0.05).However, receiving 100 mgmethotrexate divided into five doses intramuscular injection would result more side effects(P<0.05).CONCLUSION: For unruptured ectopic pregnancy,if the pre-treatment β-HCG rised rapidly, 100 mg methotrexate divided into five doses intramuscular injection would be more effective,but may cause more side-effects. If the pre-treatment β-HCG rised slowly, methotrexate 75 mg one dose intramuscular injection would be the preferred alternative.

Letrozole combined with gestrinone compared with gestrinone alone in the treatment of endometriosis

SHI Shao-quan, HONG Ting, JIANG Fang-fang, WANG Gui-rong, WANG Feng

2013, 18(11):  1275-1279. 

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AIM: To compare the efficacy of the aromatase inhibitor letrozole combined with gestrinone versus gestrinone alone in treating endometriosis.METHODS: 78 endometriosis patients were randomly divided into two groups:38 patients in letrozole + gestrinone group(LE+GE)and 40 patients in gestrinone alone group(GE). Letrozole (2.5 mg/day) and gestrinone(2.5 mg,2 times per week) were administered in LE+GE group and gestrinone(2.5 mg,2 times per week) were administered in GE group. The treatment was started on the first day of menstruation and continued for 6 months. Each patient completed visual analogue scale (VAS) of dysmenorrhea and pelvic tenderness before the onset of therapy, at the firs menorrhea and at 6 -month follow-up after the completion of treatment, assayed for serum CA-125 concentration and measured ovrian cyst size by ultrasonography at same time.RESULTS: The intensity of dysmenorrhea were significantly decreased at the first menorrhea and at 6 -month follow-up after the completion of treatment both in LE+GE group and GE group, but the drop VAS scale in LE+GE group was more obvious than that in GE group(t=2.54, P<0.05;t=3.23,P<0.05). At the first menorrhea after the completion of treatment, pelvic tenderness had released in two groups, but VAS score in LE+GE group had more sharply dropped than those in GE group (t=2.73, P<0.05). VAS score of pelvic tenderness pick-up in two groups at 6 -month follow-up after the completion of treatment (t=1.76,P>0.05). The serum CA-125 levels had dropped in two groups at the first menorrhea after the completion of treatment, but diffrentiaton was not signifcant (t=1.29, P>0.05). The serum CA-125 levels pick-up in two groups at 6 -month follow-up after the completion of treatment (t=1.82, P<0.05). Maximum diameter of ovarian cysts did not change significantly in each group after 6 -month treatment (t=0.86, P>0.05;t=1.51, P>0.05). No patients with from the study because of adverse effects.CONCLUSION: Letrozole combined with gestrinone was more effective in reducing dysmenorrhea caused by endometriosis than gestrinone alone, but to inhibit endometriosis lesions was no better than gestrinone alone.

Clinical observation of the formation of fatty liver after anti-tuberculosis treatment

LIU Yan^1,2, LIU Dan^1,3, ZHU Cui-ming¹,HUANG Ze-zhi², ZHU Jin², MENG Song-nian², LI Ping³

2013, 18(11):  1280-1283. 

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AIM: To understand the Occurrence mechanism of the anti-tuberculosis drug-induced fatty liver and drug-induced liver injury (DILI). METHODS: 200 tuberculosis(TB)patients were received,liver function and serum lipid were monitored before and after anti-TB treatment,underwent X-ray computer tomography scan fatty liver before and complete treatment. The experimental data were treated statistically.RESULTS: :The incidence of fatty liver was 28.00% (56/200) and the incidence of DILI was 32.00% (64/200) after treatment. The serum ALT, AST levels after treatment were higher than those before treatment ( P<0.05). The ALT levels after treatment in first, second, third months,AST levels after treatment in first, second, third ,fourth months was the most statistically significant difference than before treatment (P<0.01). TG, HDL-C, LDL-C, apoB levels were significantly higher than that before treatment (P<0.05). The TG levels after treatment in second,third,fourth months, LDL-C levels after treatment in third, fouth months, apoB in first, second, third,fourth,fifth months was the most significant than before treatment (P<0.01). The increase　of ALT, AST levels in the serum were significantly postive correlation with the levels of TG, apoB, HDL-C, LDL-C (P<0.05,P<0.01).CONCLUSION: The formation of fatty liver suggests DILI has undergone in anti-tuberculosis treatment. To strengthen the monitoring of blood lipid indexes can, reduce the occurrence of DILI, prevent the formation of fatty liver, ensure the implementation scheme in treatment of tuberculosis.

Effects of rosiglitazone on lipid and visfatin in patients with type 2 diabetes mellitus

SHOU Rong-wei

2013, 18(11):  1284-1287. 

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AIM: To investigate the effects of rosiglitazone on lipid and visfatin in patients with type 2 diabetes mellitus (T2DM) and analysis its clinical efficacy.METHODS: A total of 84 patients with T2DM were enrolled in this study. All cases were divided into control group (n=42) and rosiglitazone treatment group (n=42). Before and after the treatment, FPG, Hbalc, TC, TG, LDL, HDL, visfatin and other biochemical indicators were compared.RESULTS: Before treatment, FPG, Hbalc, TC, TG, LDL , HDL and visfatin had no significant difference between the two groups (P>0.05). After treatment, FPG and Hbalc expression level were significantly reduce (P<0.05, P<0.01), the rosiglitazone group FPG and Hbalc reduce amplitude were significantly higher than that control group (P<0.05). Before and after treatment, treatment group TC, TG, LDL, HDL and visfatin expression difference was not statistically significant (P>0.05), the treatment group TC, TG, LDL and visfatin express were significantly lower than before treatment (P<0.05, P<0.01), HDL were significantly higher than before treatment (P<0.05). Rosiglitazone group clinical efficient (95.2%) were higher than that control group (P<0.05). The adverse reaction rates of rosiglitazone group (23.8%) and control group (21.4%) showed no significant difference (P>0.05).CONCLUSION: Rosiglitazone treatment showed more effective to reduce the serum level of glucose, lipid and visfatin, with the low rate of adverse reactions.

The immunomodulatory role of azithromycin in acute exacerbations of chronic obstructive pulmonary disease

QIAN Xiao-ying, WU Li-feng, XU Bin

2013, 18(11):  1288-1290. 

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AIM: To investigate the clinical efficacy of azithromycin in acute exacerbations of chronic obstructive pulmonary disease (AECOPD) and explore its immunomodulatory role.METHODS: 76 cases of AECOPD patients were enrolled in this study. All the 76 cases were divided into two groups: control treatment group (A, n=38) and azithromycin treatment group(B, n=38). Another 30 healthy person were used as normal control group (C, n=30). The clinic efficacy and effects of drugs was compared between the two groups. The serum levels of IL-17 and TGF-β₁ was measured with ELISA analysis.RESULTS: The clinic efficacy in group A and B was 63.2% and 84.2%, respectively, which was higher in group B than in group A (P<0.05). The serum levels of IL-17 and TGF-β₁ in group A and B were significantly different as compared with group C at pretreatment (P<0.05). Compared with pretreatment, in group A and B the IL-17 level was significantly decreased (P<0.05), and TGF-β₁ level was significantly increased (P<0.05) at post-treatment. At post-treatment, the IL-17 level was significantly lower in group B than that in group A (P<0.01), and the TGF-β₁ level was significantly higher in group B than that in group A (P<0.05). The incidence of side effects in group A and B were 7.9% and 10.5%, respectively. There was no significant difference between the two groups (P<0.05).CONCLUSION: Azithromycin showed more effectively clinical efficacy on AECOPD patients. The regulation of IL-17/TGF-β₁ balance disorder may play a key role on the mechanism of its significant effect.

Progress in studies of reproductive toxicity of solanine

ZHOU Guo-liang, SONG Yi-sheng, XIN Yan-fei, XUAN Yao-xian

2013, 18(11):  1291-1296. 

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Solanine is widely distributed in potatoes, tomatoes and eggplant and other solanaceous plants. It causes widespread concern for anti-tumor and potential toxic effects. This paper reviewed the research progress in the reproductive toxicity studies of solanine.

Overview and progress on the study of the pharmacokinetics of naringin

ZHU Hong-ping, XIONG Yu-qing

2013, 18(11):  1297-1303. 

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Naringin is a dihydroflavone compound with the function of promoting gastrointestinal motility, which was found in some Chinese medicine such as Fructus Aurantii, Fructus Aurantii Immaturus, Rhizoma Drynariae, Pummelo Peel and so on. Naringin's oral absorb was bad, extensive distributed in the body, and produced metabolin like p-hydroxybenzoic acid and p-hydroxycinnamic acid by the way of opening loop, dehydrogenation, splitting, then eliminated from the body. Naringin also could interact with other drugs with the inhibiton of some transporters and metabolic enzymes, then influenced the pharmacokinetics of other drugs. This text reviews the pharmacokinetics of naringin and it's influence on other drugs, then points out that the mechanism of interaction through the metabolic process and the influence of genetic polymorphism on its pharmacokinetics still need to be studied.

Research progress on the relationship between calcium-independent phospholipase A₂ and myocardial ischemia/reperfusion

WAN Xing, SHI Gang-gang

2013, 18(11):  1303-1309. 

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Calcium-independent phospholipase A₂ (iPLA₂) is a subfamily of phospholipase A₂ (PLA₂), which plays an important role in signal transduction and phospholipid remodeling. Although PLA₂ enzymes were first purified from cobra venom and have been known for over 100 years, only within the last 20 years has their importance in physiologic and pathologic processes been widely recognized. Meanwhile, over the past 15 years, more and more studies have showed that iPLA₂ was activated and played a significant role in myocardial ischemia and reperfusion (I/R). In this review, the functional role of iPLA₂ in I/R is the focus.

Research progress on the relationship between calcium-independent phospholipase A₂ and myocardial ischemia/reperfusion

WAN Xing, SHI Gang-gang

2013, 18(11):  1304-1309. 

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Calcium-independent phospholipase A₂ (iPLA₂) is a subfamily of phospholipase A₂ (PLA₂), which plays an important role in signal transduction and phospholipid remodeling. Although PLA₂ enzymes were first purified from cobra venom and have been known for over 100 years, only within the last 20 years has their importance in physiologic and pathologic processes been widely recognized. Meanwhile, over the past 15 years, more and more studies have showed that iPLA₂ was activated and played a significant role in myocardial ischemia and reperfusion (I/R). In this review, the functional role of iPLA₂ in I/R is the focus.

Advance in mechanism of the surgical treatment for type 2 diabetes mellitus

WEI Qiang, HUANG He

2013, 18(11):  1310-1314. 

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Type 2 diabetes mellitus shows an upward trend year by year.At present,more mature treatment is still oral hypoglycemic drugs.However,hypoglycemic drugs are not able to prevent complications. More research proves that the Surgery treatment on type 2 diabetic rats have an significant effection for type 2 diabetes(T2DM) treatment.Surgical treatment provides a new way on 2 diabetes treatment,but we still do not know the mechanism of the surgical treatment. This paper mainly reviewed therapy mechanism of the treatment of type 2 diabetes mellitus.

Cross-talk between NF-κB and mTOR signaling pathways and its effects on tumor biological characteristics

CHEN Hua-jiao, SHI Dao-hua

2013, 18(11):  1315-1320. 

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Tumor development involves multiple cell signaling pathways. The most important of them are nuclear factor-kappaB (NF-κB) pathway and mammalian target of rapamycin pathway (mTOR), which is the new target for cancer treatment of drug therapy. Further exploration on the cross-talk between these two signaling pathways and its effects on tumor biological characteristics might be useful to control the malignant behavior of tumor cells.