Table of Content

Volume 17 Issue 11
26 November 2012

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The influence of palmitic acid to TLRs and inflammatory factors of C2C12 cell line

ZHAO Bao-sheng, LIU Yang, GAO Xiao-yan, WU Rui-guang, GUI Hai-shui, ZHU Yin-di, XU Tun-hai

2012, 17(11):  1201-1205. 

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AIM: To discuss the influence of palmitic acid to TLRs and inflammatory factors of C2C12 cells, and analyze the relationship between insulin resistance (IR) and immuno-inflammation induced by TLRs. METHODS: Palmitic acid in different concentration was co-cultured with C2C12 cells for 16 hours, after that, the consumption of glucose was analyzed to estimate the cell model of IR, TLR1-5 mRNA was observed with real-time PCR and the contents of TNF-α and IFN-β were measured with ELISA method. RESULTS: Palmitic acid decreased the glucose consumption of cells, showed IR character. It also obviously induced the hyper-expression of TLR2,TLR4 mRNA and increased the amount of TNF-α and IFN-β, but had no influence to that of TLR1, TLR3 and TLR5 mRNA.CONCLUSION: Palmitic acid stimulation induced the formation of IR, this may due to the hyper-expression of TLR2, TLR4 and the inflammation which was induced by TLRs and their signaling transdution pathway..

LC-MS/MS determination of HHY-002 in rat plasma

WANG Meng, ZHOU Jian-cai, ZHANG Yong, SUN Jian-guo, WANG Guang-ji

2012, 17(11):  1206-1210. 

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AIM: A highly sensitive and reliable LC-MS/MS method was validated for the determination of HHY-002 in rat plasma, a novel antiarrhythmic. METHODS: After addition of diazepam as internal standard(IS); LC separation with a Phenomenex Luna C₁₈ analytical column (150 mm×2.00 mm, 5 μm, 5 micron) and quantification by MS/MS after positive ESI. The mobile phase consisted of acetonitrile∶water∶formic acid (65∶35∶0.1, V/V/V) in an isocratic elution mode pumped at 0.200 mL/min, and with the injection volume of 10 μL and column oven temperature of 35 ℃. RESULTS: The calibration curve ranging from 1.98 to 1013.50 ng/mL. Lower limit of quantification (LLOQ) was 1.98 ng/mL in 100 μL of plasma. Extraction recovery was above 80%, inter- and intra- day accuracy and precise was below 10%.The method recovery was over(81.4±4.5)%.This method was shown to meet all requirements in bioanalytical determination.CONCLUSION: The method was successfully applied to the determination of HHY-002 in rat plasma.

Pharmacokinetics of clematichinenoside AR and its absolute bioavailability in Beagle dogs

WANG Da-wei, LI Feng, XU Ping, ZHOU Lei, LIU Li, LIU Xiao-dong

2012, 17(11):  1211-1215. 

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AIM: To investigate the pharmacokinetics and absolute bioavailability of clematichinenoside AR (C-AR) in Beagle dogs. METHODS: By applying four cycle crossover design, a single dose of C-AR was administrated (i.v. 0.75 mg/kg or i.g. 7.5, 15 or 30 mg/kg) to 8 Beagle dogs.Blood samples were collected before and at different intervals after C-AR administration. The concentration of C-AR in dog plasma was determined by LC-MS/MS method.The pharmacokinetic parameters were estimated by DAS 2.0 pharmacokinetic program,and the absolute bioavailability was calculated.RESULTS: After single dose ig of 7.5, 15 and 30 mg/kg C-AR, the pharmacokinetics parameters were estimated as follows: t_1/2: (14.3±2.7), (13.3±1.3) and (13.7±2.4) h; AUC_0-36: (1.9±1.2), (4.5±1.9) and (8.0±3.3) μg·h·mL^-1; C_max: (0.14±0.08), (0.27±0.10) and (0.52±0.28) μg/mL. After single dose i.v. of 0.75 mg/kg C-AR, the pharmacokinetics parameters were estimated as follows: t_1/2: (13.3±3.0) h,AUC_0-36:(66.2±12.8) μg·h·mL^-1. The absolute bioavailability of C-AR following i.g. administration was 0.32%, 0.35% and 0.30%. CONCLUSION: The absolute bioavailability of C-AR in dogs is low, and the pharmacokinetic properties were linear in Beagle dogs.

Effect of the extract of cordyceps militaris on senescence in cultured human umbilical vein endothelial cells treated with high glucose

ZHU Peng-li, YE Zhang-zheng, YU Hui-zhen, HUANG Hua-wei, RUAN Jing-ming, LIN Fan

2012, 17(11):  1216-1222. 

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AIM: To determine the effect of the ethyl acetate extract of cordyceps militaris (CME) on senescence in cultured human umbilical vein endothelial cells (HUVECs) treated with high glucose. METHODS: The HUVECs senescence model was established by incubation with high glucose(40 mmol/L) , the extract of Cordyceps Sinensis(CSE) (50 μg/mL) was treated as a positive control, and then CME (12.5-100 μg/mL) was treated to observe its effect on cell senescence. Cell proliferation was determined by the methylthiazolyl tetrazolium (MTT) reduction assay , SA-β-galactosidase (SA-β-gal) positive cells were detected by X-gal, and phase distribution of cell cycles and cellular reactive oxygen species (ROS) were detected by flow cytometry. RESULTS: Compared with unintervented cells, cell OD value significantly decreased in cells treated with high glucose for 24, 48, and 72 h (P<0.01). The percentage of cells positive for SA-β-gal, the percentage in G₀/G₁ phase and ROS levels notably increased after cells incubated by high glucose for 96 or 48 h (P<0.01). Compared with high glucose intervention cells, cell OD value significantly increased in cells intervented by CME (25-50 μg/mL) for 48 h and 72 h ( P<0.05); CME(12.5-100 μg/mL)stimulating for 96 h significantly lowered the percentage of cells positive for SA-β-gal (P<0.01); CME(12.5-100 μg/mL)incubation for 48 h significantly lowered the percentage of G₀/G₁ phase of HUVECs (P<0.01) and ROS production (P<0.05); All these effects of CME 25, 50 μg/mL groups were better than those12.5, 100 μg/mL groups (P<0.05), and were similar to CSE 50 μg/mL group(P>0.05). CONCLUSION: Ethyl acetate extract of cordyceps militaris may promote the HUVECs growth and proliferation, protecting from high glucose-stimulated vascular endothelial senescence. The effects may be associated with ethyl acetate extract of cordyceps militaris inhibiting reactive oxygen species and alleviating oxidative stress injury.

Protection of modified wuweixiaoduyin extracts on the peridentalt of diabetic rats

XIANG Min, ZHANG Ya-qin, WU Ping-ping, GAO Zhen-yu, LIU Jing-tian, GU Yao-hua, WANG Jian-mei

2012, 17(11):  1223-1228. 

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AIM: To observe the protection effect of modified Wuweixiaoduyin extracts (MWE) on peridentalt of diabetic rats and investigate its possible mechanisms. METHODS: Diabetic periodontitis models were induced by combination periodontal ligation and injection of streptozotocin (STZ, 50 mg/kg). There were 5 experimental groups as followed: Normal, model groups, Aminoguanidine (AG) positive control groups (100 mg/kg), low dosage (20 g/kg, crude drug, the same below) and high dosage (40 g/kg) of MWE, with 10 rats in each group. Rats were killed after treatment for 6 weeks, the levels of fasting blood glucose and glycosylated hemoglobin (GHb) were determined, AGEs in serum was analyzed by ELISA. Depth of periodontal pocket was measured by periodontal probe. Left alveoli dentales maxillae were checked by dental X machine. In addition, expression of RAGE protein was detected by sABC methods.RESULTS: After treatment for 6 weeks, MWE didn't decrease blood glucose. However, compared with model group, MWE decreased depth of periodontal pocket, level of GHb and AGEs in serum (P<0.01). And derangement of Trabeculae bone and horizontal resorption in alveoli dentales maxillae were also ameliorated. In addition, expression of RAGE protein was reduced, too. CONCLUSION: MWE has protection effect on peridental of diabetic rats and the possible mechanism is related with interference AGEs-RAGE by MWE .

Effect of MG-132 in mice with acute viral myocarditis

ZHANG Xin-min, LI Yue-chun, CHEN Peng

2012, 17(11):  1229-1232. 

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AIM: To determine the effect of proteasome inhibitor MG-132 in mice with acute viral myocarditis induced by coxsackievirus B3 virus (CVB3) infection. METHODS: BALB/C mice were intraperitoneally inoculated with CVB3 to induce myocarditis. From 24 h after infection, MG-132 was administered at a dose of 0.75 mg/kg for 7 d continuously by intraperitoneal injection. Normal controls were treated with same volume of PBS. Then, the myocardial histopathological changes, HW/BW ratio, expression of myocardial CVB3 mRNA and serum cTnⅠ and BNP were determined. RESULTS: MG-132 significantly attenuated myocardial lesions and decreased HW/BW ratio. It also remarkably decreased serum cTnⅠ and BNP, down-regulated CVB3 mRNA expression compared with myocarditis controls. CONCLUSION: MG-132 protects against CVB3 induced viralmyocarditis in mice. MG-132 exerts its beneficial effect by downregulating CVB3 mRNA expression probably.

Determination of diclofenac sodium in dialysate of joint cavity in rats based on microdialysis and HPLC-ESI-MS and its application

ZHANG Jing, CHEN Yang, LI Pei, GUO Hai-fang, LIU Xiao-dong

2012, 17(11):  1233-1239. 

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AIM: To develop and validate a high liquid chromatography-electrospray ionization-mass spectrometry (HPLC-ESI-MS) method for the quantification of diclofenac sodium in dialysate of joint cavity in rats in order to meet the requirement of collection and determination of non-steroidal anti-inflammatory drugs (NSAIDs) in target site based on microdialysis and use diclofenac sodium as paradigm drug. METHODS: A sensitive and specific liquid chromatography-electrospray ionization-mass spectrometry (LC-ESI-MS) method using a unipolar quadrupole technology by optimizing chromatography and mass spectrometry conditions has been applied to determine the concentration of diclofenac sodium in dialysate of joint cavity in rats.Dialysate samples were separated by HPLC on a reversed phase C₁₈ column [Waters Symmetry-C₁₈ (dp 5 μm, 150 mm×2.1 mm ID)]with a mobile phase of methanol-0.1% formic acid (80∶20, V/V).RESULTS: The method was validated over the concentration range of 1.95-125 ng/mL with the low limit of quantitation of diclofenac sodium in dialysate was 1.95 ng/mL.Within-batch and between-batch precision (RSD.%) were all within 10% while matrix effect were between 99.9%-113.4%. CONCLUSION: The microdialysis technology was successfully applied in the collection of dialysate samples in joint cavity of rats, the determination method described in this paper is rapid also has a high sensitivity.The combination of two technologies were suitable for the collection of synovial samples, also will be helpful to study the pharmacokinetic profile of non-steroidal anti-inflammatory drugs (NSAIDs) in target site.

Synergy inhibition effect of 17-AAG in combination with cisplatin on lung adenocarcinoma A549 cells

WANG Gui-ping, LIAO Hong-ying, WEI Min, WANG Yan, ZHOU Qiong, LIN Zhu-zhen, ZHANG Yan-tao

2012, 17(11):  1240-1244. 

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AIM: The aim of our present study is to assess of synergy inhibition effect of 17-AAG combinated with cisplatin on lung adenocarcinoma A549 cells. METHODS: MTT assay was used to detect the inhibiton of the various concentrations of 17-AAG, cisplatin, or the two combination on A549 cells. The median-effect method of Chou and Talalay was used to evaluate the combination effect. RESULTS: 17-AAG or cisplatin alone inhibited the growth of A549 cells in a concentration-dependent manner. The IC₅₀ for 48 h was 69.627 μmol/L for cisplatin, and 0.455 μmol/L for 17-AAG. The effect was greater when the two agents were combined, even at the lowest dosage combination.CONCLUSION: Our results demonstrated that the combination of 17-AAG and cisplatin showed synergy inhibition effect on lung adenocarcinoma A549 cells.

Effects of etomidate and propofol on insulin resistance in rabbits with type 2 diabetes mellitus

WANG Shou-yi, LIU Zhao-fang

2012, 17(11):  1244-1248. 

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AIM: To investigate the effects of etomidate and propofol on insulin resistance in rabbits with type 2 diabetes mellitus(T2DM). METHODS: 18 successed model of the T2DM rabbits were randomly divided into three groups (n=6): control group (group C), etomidate group (group E), 1% propofol group (group P). 0.9% sodium chloride infusion for group C, 1% propofol infusion for group P, etomidate infusion for group E respectively, before the start of administrating (T₁), administrating for 2 h (T₂), 4 h (T₃), 6 h (T₄) and after the administration for 24 h (T₅) , pumping blood through ear vein to determine BG,IN,TNF-α,Cor and calculate IRI = (BG × IN)/22.5 by HOMA-IR formula. RESULTS: Compared with group C, group E and group P could significantly reduce the concentration of serum BG (P<0.05), the effect of Group E was more stronger and more durable. Compared with group C, group E and P could reduce serum TNF-α concentration in vary degree, there were no significant different (P>0.05). Compared with group C, group E and P had lower concentration of serum IN in the different time points (P<0.05). Compared with group C, both of Group E and P could significantly reduce the concentration of serum Cor (P<0.05). The effect of Group E was more stronger and more durable. CONCLUSION: Both etomidate and propofol can decrease the IR and improve the insulin sensitivity in rabbits with T2DM. Etomidate has a more lasting effect compared with propofol. The potential mechanism of the impact of etomidate,propofol on IR is that the two can inhibit the body's stress response through internal and external.

Pharmacokinetics/pharmacodynamics evaluation of two injection formulations of propofol in Chinese healthy volunteers

CHEN Lin-yao, ZHOU Xing-chen, GUO Xin, SU Tao, CHENG Ze-neng

2012, 17(11):  1249-1257. 

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AIM: Propofol is a widely used intravenous anesthetic agent. Few pharmacokinetic (PK) and pharmacodynamic (PD) information of propofol is available in a Chinese population. The aim of the study is to evaluate PK and PD characteristics, assessing the therapeutic equivalence between two injection formulations of propofol in Chinese healthy volunteers. METHODS: Twenty-four healthy male volunteers were enrolled in a randomized, double-blinded, crossover study, receiving a 2 mg/kg bolus injection of test or reference formulation in two study arms. Plasma propofol concentration was determined by a validated HPLC-Flu method. PD parameters, Bispectral Index (BIS) and A-line ARX Index (AAI), were recorded by EEG monitor till 15 min postdose. In addition, times to onset of and emergence from hypnosis were observed. RESULTS: Twenty-three subjects accomplished the trial. The mean values of C_max, t_max, AUC_0-t, AUC_0-∞ of test and reference formulations were 2.284 and 2.452 mg/L; 4 and 4 min; 0.706 and 0.423 mg·h·L^-1; 0.471 and 0.506 mg·h·L^-1, respectively. The mean values of PD parameters of test and reference formulations were as follows: BIS_min, 51 and 53, respectively; AAI_min, 18 and 20; BISAUC_{0-15 min}, 373.4 and 342.7; AAIAUC_{0-15 min}, 892.5 and 850.5. The 90% CIs for the logarithmic transformations of C_max, AUC_0-t, AUC_0-∞, BISAUC_{0-15 min}, BIS_min, AAIAUC_{0-15 min}, AAI_min (0.795-0.999, 0.838-0.985, 0.861-0.989, 1.023-1.151, 0.865-1.025, 0.999-1.099, 0.826-1.008, respectively) were within the bioequivalence acceptance limits. No serious adverse events occurred in the trial.CONCLUSION: Results indicated that no significant difference was found between test and reference formulations of propofol in the aspects of pharmacokinetic and pharmacodynamic. Both formulations were well tolerated. Therefore, we believe that the two injection formulations of propofol are therapeutic equivalence in Chinese healthy volunteers.

Meta-Analysis of ACEI combined with ARB on the effect of renal function with Diabetic Nephropathy

HAN Su-fang

2012, 17(11):  1257-1262. 

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AIM: To evaluate the clinical treatment effects on renal function of angiotensin-converting enzyme inhibitors (ACEI) combined with angiotensin II receptor blocker (ARB) in patients with diabetic nephropathy (DN). METHODS: Retrieve the domestic literatures for the randomized controlled clinical trials about ACEI/ARB combined or mono-therapy on renal function in DN patients during the period January 1990 to March 2012.The difference of indicators for the renal function before and after treatment for the included literaturs was carried out RevMan 5.0 software. RESULTS: Total of 12 studies, including 900 cases of patients with DN, were included in this study. Meta-analysis showed that compared with ACEI or ARB mono-therapy, the combined treatment affection on the standardized mean difference for 24-hour urinary albumin excretion rate, 24-hour urine albumin and 24 urinary protein were significantly improved (P<0.05). However, there was no significant difference of serum creatinine, blood urea nitrogen and electrolytes between two groups.CONCLUSION: Compared with mono-therapy, ACEI and ARB combined treatment could exert anti-proteinuria effects in patients with DN, but no improvement on the serum creatinine, blood urea nitrogen and electrolytes. However, further large-scale trials are required to define the role of ACEI and ARB combined treatment in patients with DN.

Neuromuscular pharmacodynamics of rocumnium bromide in thymectomy of myasthenia gravis patients

QIN Xue-mei, LU Wei-hua, JIN Xiao-ju, YAO Wei-dong, TANG Ning

2012, 17(11):  1263-1267. 

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AIM: To investigate the neuromuscular pharmacodynamics of rocuronium on thymectomy in myasthenia gravis (MG) patients. METHODS: Twenty-three Ⅰ-Ⅱa MG patients undergoing elective thymectomy (Group M) since January 2006 were studied. Another twenty non-MG patients undergoing other elective surgery were included as control group (Group C). All patients were performed under total intravenous anesthesia by tracheal intubation, given a loading dose of rocuronium 0.6 mg/kg as anesthesia induction. Neuromuscular transmission was monitored by measuring the twitch tension of the adductor pollicis muscle. And the heart rate variability (HRV) was analyzed during the surgery. RESULTS: Anesthesia and surgery were carried out successfully without any adverse reaction. The analysis revealed that the MAP, HR, HRV, LF/HF had no significant difference between the two groups at all time points. The onset time was significantly shorter in group M than that in the group C (P<0.05). There were no significant group differences in the recovery time of T₁ to 25%, the recovery time of T₁ to 50%, and the recovery indices (interval, 25%-75%). CONCLUSION: The results show that rocuronium, as anesthesia induction at a dose of 0.6 mg/kg, has a shorter muscle relaxants onset time and a small influence on the maintaining time. It also can result in fewer perioperative complications and provide optimal operating conditions.It is a safe anaesthesia method in thymectomy of Ossermen Ⅰ-Ⅱa MG patients with anesthesia induction by injecting rocuronium.

Clinical study of combination treatment with clofazimine and others for patients with multi-drug-resistant tuberculosis

WANG Huai-chong, XU Ying-ying, ZHANG Xiang-cai, ZHANG Li-bin, CAO Jia-wei, WANG Cui-lian

2012, 17(11):  1268-1271. 

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AIM: To investigate the efficacy of combination treatment with clofazimine and other antituberculosis drugs for patients with multi-drug-resistant tuberculosis. METHODS: 72 cases with multi-drug-resistant tuberculosis were randomly divided into experimental group (n=32) and control group (n=40). The treatment effect was observed at the 6th month and 18th month after treatment. RESULTS: 6 months later, the sputum negtive conversion rate in smear and in culture were 81.3% and 84.4% respectively and the rate in X-rays focus absorption was 37.5% in experimental group, which were significantly higher than those in control group. CONCLUSION: Combination treatment with clofazimine and others for patients with multi-drug-resistant tuberculosis can improve the curative effect and shorten course of treatment especially in the stage strengthened.

Clinic effects of irbesartan combined with glutathione sodium on kidney in patients with diabetic nephropathy

FEI Mei-jiao

2012, 17(11):  1272-1275. 

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AIM: To investigate the effects of irbesartan combined with glutathione sodium on oxidative stress in patients with diabetic nephropathy(DN) and to explore its function in the protection of kidney. METHODS: A total of 120 cases of DN were retrospectively analyzed in this study. The patients were divided into three groups: normal treatment group(A, n=34), irbesartan treatment group(B, n=42) , irbesartan combined with glutathione sodium treatment group(C, n=44). The 24 h urine protein quantitation, FGB, TG, BUN, SCr, K⁺ were determined before and after treatment. The activity of SOD was detected by spectrophotometer. The expression of MDA was detected by chromatometry. RESULTS: The 24 h urine protein quantitation, FGB, BUN, and SCr became better after different treatment(P<0.05). However, the TG and K⁺ were not changed after different treatment(P>0.05). The changes of 24 h urine protein quantitation, FGB, BUN, and SCr were better in group B than those in group A(P<0.05). The changes of 24 h urine protein quantitation, FGB, BUN, and SCr were better in group C than those in group B(P<0.05). After treatment, the SOD activity was elevated and the expression of MDA was decreased in group C. However ,no change was found in group A and B(P>0.05). The total effective rate in group A, B, and C was 44.1%, 61.9%, and 81.8%, respectively. The total effective rate in group C was higher than that in group A and B(P<0.05).CONCLUSION: Irbesartan combined with glutathione sodium treatment significantly increases the activity of SOD and decreases the levels of MDA in patient with DN, which downregulates oxidative stress, decreases urine protein quantitation, and shows protective function of of kendey.

A comparison among butorphanol,pethidine and tramadol in treating perioperative chilling

CAO Ya, LU Wei-hua, LIU Zhao-fang, LU Mei-jing

2012, 17(11):  1276-1278. 

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AIM: To study the effects of butorphanol , pethidine and tramadol in treatment of patients with perioperative shivering. METHODS: Sixty ASAⅠ-Ⅱ patients with shivering response during anesthesia were randomly divided into three groups(n=20): butorphanol group (group B), intravenous injection of butorphanol 0.02 mg/kg; pethidine group (group P), intravenous injection of pethidine 0.5 mg/kg; and tramadol group (group T), intravenous tramadol 1 mg/kg. Observed the degree and time of occurrence of shivering, shivering response after treatment and adverse effect in sedation score. RESULTS: Butorphanol group and tramadol group were effective than pethidine group in treatment of shivering(P<0.01). Butorphanol group was significantly higher than tramadol group and pethidine group in sedation(P<0.05).Tramadol group was significantly higher than pethidine group and butorphanol group in incidence of nausea and vomiting(P<0.05).CONCLUSION: Butorphanol and tramadol can effectively treat perioperative shivering,but clinical patients should be reasonable select different drugs according to particular case.

Comparison of cough induced by equivalent doses of alfentanil and fentanyl

SHUAI Xun-jun, AI Deng-bin, CAO Xi

2012, 17(11):  1279-1282. 

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AIM: To evaluate the effects of cough induced by equivalent doses of alfentanil and fentanyl. METHODS: Fifty patients undergoing general anesthesia were randomly assigned to alfentanil group ,and fentanyl group.Two groups were received equivalent doses of alfentanil 8 μg/kg, and fentanil 2 μg/kg, via IV push within 5 seconds respectively. To observe the starting time ,incidence and severity of cough, heart rate (HR) and mean arterial pressure (MAP) were recorded immediately before injection (T₁) and 2 min (T₂) after injection. RESULTS: Alfentanil group had an earlier starting time than fentanyl group. alfentanil group had a significantly lower incidence of cough than fentanyl group(P<0.05). Compared with T₁, the HR and MAP of alfentanil group and fentanyl group at T₂ were significant lower(P<0.05).Compared with fentanyl group, the extent of decrease in the HR and MAP of alfentanil group were significant higher(P<0.05).CONCLUSION: Alfentanil induces a lower incidence of cough and more steadier circulation than equivalent doses of fentanyl.

Influence of related genetic polymorphisms to pharmacokinetics and pharmacodynamics of Fluvastatin

LIU Jing, XIONG Yu-qing

2012, 17(11):  1282-1288. 

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Fluvastatin is the first all chemical synthesis of cholesterol drugs. In the clinical treatment of the application of existing large differences.Muscle toxicity, liver toxicity,rhabdomyolysis is fluvastatin potential adverse reactions. In order to reduce the incidence of adverse reactions, so the lead to fluvastatin individual differences of the big reason has the great significance. This paper reviewes the CYP450 enzyme, drug transport body (OATP1B1, OATP1B3, OATP2B1, ABCG2) to fluvastatin pharmacokinetics characteristics of the influence and pharmacophore (CETP, ApoE) to fluoride polymorphisms of simvastatin pharmacodynamics characteristics influence. So as to ensure that the safety and efficacy of clinical medicine, and achieved the clinical personalized medicine.

Progress in uric acid transporters

ZHU Li-ran, CHEN Guang-liang

2012, 17(11):  1289-1294. 

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Transport of uric acid by the kidneys rely on the transport protein in the renal tubular epithelial cells. Four kinds of urate transporters are involved in proximal tubular urate transport: human urate-anion exchanger 1(hURAT1) , which is responsible for the reabsorption of urate, human urate transporter (UAT) and organic anion transporter (OAT1 and OAT3),there are responsible for uric acid secretion. Recently, also found that the one responsible for uric acid secretion into the extracellular, involved in the renal proximal tubule reabsorption of urate transporter protein - glucose transporter protein (GLUT9). This article summarized the features, functions and regulatory mechanisms of uric acid transport protein.

Effects and mechanisms of metformin on lifespan extension

QI He, LIU Ting-ting, LI Guo-rong

2012, 17(11):  1295-1301. 

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A research of pharmacological intervention that decreases the rate of organism aging to extend their life span is a perspective direction. Several studies have shown that metformin which is a biguanide class drug used in the treatment of type 2 diabetes mellitus can slow down aging and prolong life span.The possible mechanisms may be related to AMPK activation, mTOR inhibition and its downstream molecules.This review describes the effects of metformin on lifespan extension in nematode, transgenic mice , rats and potential mechanisms.

Research progress on chemical constituents and pharmacological effects of poplar bud extracts

CHEN Shu-qing, ZHONG Zheng-ling, LI Hai-tao, LI Juan, CHU Ji-ru

2012, 17(11):  1302-1306. 

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Poplar bud extracts contain flavonoids,terpene,phenolic acids and esters.The modern pharmacological studies show poplar bud extracts have wide pharmacological actions such as antioxidation,anti-tumor,antibiosis,anti-ulcer,etc.This review summarizes recent advances in the research of chemical compositions and the pharmacological effects of poplar bud extracts.

Advances in pharmacogenetics of systemic therapies for psoriasis

MENG Xiang-guang, NI Wen-qiong, WANG Chao, MA Deng-xuan, LI Zhi, ZHOU Hong-hao

2012, 17(11):  1307-1313. 

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Psoriasis is an inflammatory hyperproliferative skin disease with a strong genetic susceptibility and influenced by genetic, immunological and environmental factors. Because most patients with moderate to severe psoriasis cannot benefit from the topical treatment, they have to treat with systemic agents. While the systemic treatment is characterized of high medical cost and large inter-individual variations in efficacy and adverse reaction, the studies on pharmacogenetics of systemic therapies for Psoriasis play an important role in clinic.This review summarizes the correlations between genetic factors and systemic agents to provide the theoretical guidance for the personalized medication in psoriasis.

Effects of metformin on bone metabolism

ZHEN Dong-Hu, LIU Li-Juan, TANG Xu-Lei, CHEN Jian-Guo

2012, 17(11):  1314-1320. 

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Metformin [1-(diaminomethylidene)-3,3-dimethylguani-dine] is an antihyperglycemia drug commonly used for the management of type 2 diabetes, which has been widely used for more than fifty years and had safety, valid and full-scale effects on controlling plasma glucose in patients with diabetes mellitus. Recent years, more and more studies found that metformin induced osteoblastic growth and differentiation, increased the mineralization of the extracellular matrix, reversed the deleterious effects of high glucose on osteoblast function and also inhibited osteoclastogenesis; Furthermore, in vivo, treatment of mice with metformin has been found to increase bone mineral content, trabecular bone volume and induce bone formation. In addition, using a model of minimal bone defect metformin treatment stimulated bone reossification in both control and diabetic rats. Furthermore, in clinical research, metformin influenced bone mineral density in patients with diabetes mellitus. However, the effects of metformin on bone metabolism and the molecular mechanisms for the action of metformin are still unclear. This article reviews the effects of metformin on bone metabolism and discusses its possible mechanisms.