hydroxysteroid dehydrogenase (11? HSD) catalyzes the interconversion of cortisol with its inactive metabolite cortisone. The congenital deficiency of 11? HSD2 induce hypertension and hypokalemia. This disorder is called "Apparent Mineralocorticoid Excess(AME)". Glycyrrhizic acid and other endo and xenobiotics have been found to inhibit the activity of 11? HSD and cause excess mineralocorticoid effects that is similar to AME. The decrease in 11? HSD activity is related with the acquired and congenital hypertention.

Objective:To study the impact of smoking on C-reactive protein(CRP)concentration in gingival crevicular fluid(GCF) before and after initial treatment.Methods:18 smokers and 18 non-smokers with moderate or severe periodontal disease were recrui-ted into this study.The clinical indexes of periodontal examination of the patients were recorded,GCF samples of the patients were collected,CRP level in the samples was measured by radioimmunoassay balance method before and 4 weeks after initial treatment. Results:4 weeks after initial treatment,the clinical indexes and CRP concentration in GCF of the smoking group and non-smoking group were significantly lower than those before treatment(P <0.05),the changes of the smoking group were less than those of the non-smoking group(P <0.05).Conclusion:Smoking is an unfavorable factor of the initial periodontal therapy.

AIM: To compare pharmacokinetics and relative bioavailability of telmisartan capsule (T) and telmisartan tablet(R). METHODS: 20 male healthy Chinese volunteers were enrolled in a randomized two-way crossover designs with a single-oral dose study(80 mg once per day for each preparation). The plasma telmisatan concentration was determined by HPLC- fluorescence detector. Plasma levels of telmisatan were followed up to 96 h. Area under the telmisartan concentration time curve was calculated by variance analysis and the bioequivalent was determined by two one-side t-test. RESULTS: A two-compartment model was adopted in telmisartan plasma concentration-time data analysis. The pharmacokinetic parameters of T and R in single-dose study including Cmax (μg·L-1), Tmax (h), T1/2β (h), MRT(h), AUC0-92(μg·h·L-1) were as following: 456±253 and 760±314, 1.61±0.71 and 1.08±0.36, 22.39±6.29 and 21.08±5.24, 27.02±6.23 and 24.27±5.79, 3454±1050 and 3635±1300, respectively. Statistically significant differences were observed between the parameter values of the two products in Cmax and Tmax; whereas there was no statistically significant difference between AUC0-∞μg·h·L-1 (3601±1095 and 3767±1399). The relative bioavailability for T was 97.28%±12.74%. CONCLUSION: The test telmisartan capsule is bioequivalent to the reference tablet.

Aim To investigate the effects of co-administration of Astragalus Saponin Ⅰ(ASI)and bendazac lysine(BDL)on hypertrophy of cultured rat mesangial cells and its mechanism.Methods The levels of collagen Ⅳ and laminin,the percentages of cells in S phase,the relative quantity of transforming growth factor ?1(TGF-?1) mRNA and indexes of oxidative status were assayed after the cells were incubated in different agents for 36 h.Results The percentage of S phase cells in high glucose group(HG) was greatly decreased while those of vitamin E group(VE) and co-administration groups were increased.The relative quantity of TGF-?1 mRNA and the collagen Ⅳ level in co-administration groups were significantly decreased,and the levels of total anti-oxidative capability(T-AOC),activity of catalase(CAT),GSH-PX,and SOD were greatly increased.Furthermore,the significant differences were found between low ASI(AL)group,low BDL(BL) group and co-administration of low ASI and low BDL(AL+BL) group for TGF-?1 mRNA,T-AOC and GSH-PX;the high ASI group(AH),high BDL group(BH) and co-administration of high ASI and high BDL group(AH+BH) for TGF-?1 mRNA and collagen Ⅳ,respectively. Conclusion Co-administration of ASI and BDL has synergetic effects on regulating TGF-?1,collagen Ⅳ,and radical oxidative stress,therefore,is beneficial to protecting rat mesangial cells against hypertrophy.

To investigate the protective effects of bendazac lysine (BDL) on diabetic nephropathy (DN) in vitro and in vivo experiments. METHODS: After rat mesangial cells were cultured in 3 concentrations of BDL for 36 h, the percentages of S phase of cells were determined by flowcytometry; the transforming growth factor β1 (TGF-β1) mRNA level was assayed by reverse transcription PCR; and two main components of extracellular matrix (ECM), collagen Ⅳ and laminin, were determined by radioimmunoassay. Streptozotocin (STZ) induced diabetic rats were administered BDL at doses of 100, 200, 400 mg/kg for 8 weeks. The physical behavior and HbAlC levels of rats were observed. RESULTS: In the presence of high glucose and H2O2, the percentages of S phase of cells were lowered, and TGF-β1 mRNA level, collagen Ⅳ and laminin level were significantly increased. When compared with those in the high glucose group, the percentages of S phase of cells were significantly raised, and the levels of TGF-β1 mRNA, collagen Ⅳ and laminin were statistically decreased. The physical behavior of high BDL treated rats restored to be vibrant, vigorous and weight gaining, and the HbAlC level was significantly reduced. CONCLUSION: BDL has the protective effects against damage caused by DN, and is a potential drug candidate worth further study in preventing and treating DN.

Objective To study the protective mechanism of astragaloside on skin photoaging. Methods BALB/c mice were randomly divided into four groups: model group irradiated with ultraviolet rays (UV), model plus matrix group pretreated with the matrix before UV irradiation, model plus astragaloside group pretreated with astragaloside 0.08% cream before UV irradiation, normal control group received no irradiation or pretreatment. After 4-week irradiation, the mice were sacrificed, and skin tissues were resected from the back of these mice. Then, reverse transeription PCR (RT-PCR) and immunohistochemistry were performed to detect the mRNA and protein expression of TGF-βR Ⅱ and Smad 7, respectively. Gray scale ratio was used to represent the mRNA levels of TGF-βR Ⅱ and Smad 7. Results There was a significant difference in the mRNA level (F = 80.98, 736.80, respectively, both P < 0.01) and protein positivity rate (F = 45.36,132.25, respectively,both P < 0.01) of TGF-βR Ⅱ and Smad 7 among the 4 groups. The mRNA level and protein positivity rate of TGF-βR Ⅱwere 0.2588±0.0283 and (28.20 ± 5.24)% respectively in the model group, significantly lower than those in the normal control group[0.5688 ± 0.0439, (53.00 ± 4.72)%, both P < 0.01] and model plus astragaloside group [0.3767 ± 0.0374, (41.64 ± 2.59)%, both P< 0.01]; on the contrary, the mRNA level and protein positivity rate of Smad 7 in the model group [0.8637 ± 0.0514, (82.06 ± 2.18)%] were significantly higher than those in the normal control group [0.5900 ± 0.0585, (47.50±3.81)%, both P < 0.01] and model plus astragaloside group [0.7131 ± 0.0410, (64.36 ± 2.62)%, both P< 0.01]. In the model plus astragaloside group, the mRNA level and protein positivity rate of TGF-βR Ⅱ were significantly higher than in the model plus matrix group [0.2653 ± 0.0456, (28.74 ± 2.28)%, both P < 0.01], while those of Smad 7 were statistically lower than in the model plus matrix group [0.8553 ± 0.0575, (82.62 ± 4.02)%, both P < 0.01]. However,no significant difference was observed in the mRNA level or protein positivity rate of TGF-βR Ⅱ or Smad 7 between the model group and model plus matrix group (all P > 0.01). Conclusion Astragaloside can prevent skin photoaging by the alteration of TGF-β pathway via up-regulating TGF-βR Ⅱ expression and down-regulating Smad 7 expression.

AIM: To establish a sensitive method for quantitative determination of astragaloside Ⅳ (AGS-Ⅳ) in plasma and a preliminary evaluation of its pharmacokinetics parameters in intact rats. METHODS: A liquid chromatography-electrospray ionization-mass spectrometry (LC-ESI-MS) was applied for determining AGS-Ⅳ in plasma by using digoxin as the internal standard (I.S.). Six rats were given AGS-Ⅳ 2.0 mg/kg by intravenous infusion for 5 min. Blood samples were drawn intermittently with each intact rat from left femoral artery at 0.025, 0.05, 0.1, 0.25, 0.5, 1, 2, 4, 6, 10, 14 and 24 h after medication. The samples were prepared by solid phase extraction and analyzed through a triple quadrupole mass spectrometer equipped with an electrospary probe. The samples were monitored in selected ion recording (SIR) mode of positive ions by using target ions at m/z 807.5 for AS- Ⅳand at m/z 803.5 for I.S. RESULTS: Calibration curves were linear over the ranges 1-1 000 ng/mL for AGS-Ⅳ (r=0.9992). The intra-and inter-day assay variability values were less than 6% and 8%, respectively. Extraction recoveries from plasma were 92.8%-98.4% for AGS-Ⅳ and 80.0%-90.9% for digoxin, respectively. The lower limit of quantitation (LLOQ) for AGS-Ⅳ was 0.5 ng/mL. The concentration-time curves of AGS-Ⅳ for each rat were fitted to an open two-compartment model by CAPP program. The pharmacokinetics parameters of AGS-Ⅳ were as following: the elimination half-life (t1/2β), clearance rate (CL), distribution volume at steady state (Vss), and AUC0-∞ were (3.46±0.52) h, (0.47±0.02) L/h, (0.76±0.16) L/kg and (4.27±0.19) μg·mL-1·h, respectively. CONCLUSION: These results show that this method is satisfied for the measurements of pharmacokinetics study for AGS-Ⅳ.

Objective　To evaluate whether the stimulation on eyes of bendazac lysine eyedrops could be reduced by cold storage.Methods　 Mate design scheme and double-blind clinical trial were performed. 160 healthy eyes was divided into two groups: the test group was given bendazac lysine eyedrops which was stored in refrigerator at 4℃ over night, and the control group was given it which was stored at room temperature.Results　ln the control group and the test group, the occuring rate of stimulation was 19.30% and 6.25%. The cases of B、C stimulation degrees were 31 and 10; the average stimulation degrees of each group were 1.21 and 1.07, the scoring change for eye stimulation were 1.57±1.50,0.79±1.40,all respectively. The statistical difference was significant (P＜0.05 or P＜0.01).Conclusion　The eye stimulation of bendazac lysine eyedrops can be reduced by cold storage.

Objective To observe the treatment response and potential issues related to antiretroviral therapy (ART) in pediatric patients with acquired immunodeficiency syndrome (AIDS) and to provide a basis for revising the treatment guideline and improving the clinical practice. Methods Children eligible for ART according to the current treatment guideline were recruited from Dehong area. Enrolled patients were provided with ART and followed up for regular clinical check and laboratory tests. Results By the end of March 2009, a total of 70 children had received ART. Among them, 60 patients were treated with regimen including zidovudine (AZT)+ lamivudine (3TC)+nevirapine (NVP). Twelve, eighteen, twenty-three and nineteen patients have tested for HIV viral load after 3 month, 6 month, 12 month and 18 month treatment, respectively. Among them, 7, 12,14 and 14 patients respectively achieved HIV viral load lower than 1000 copy/mL. Average CD4+ Tlymphocyte count increased from (317.8±288.8) × 106/L at baseline to (1037.2±1086. 1) × 106/Lafter 18 month treatment. Side effects mainly occurred within the first 3 months of treatment. Nearly 50% of children had gastrointestinal symptoms. Resistance to 3TC, NVP and efavirenz (EFV) were found in five patients who have completed 12 months of treatment. Conclusions Pediatric AIDS patients show good compliance and treatment response to ART. Most side effects happen in the first 3months of treatment and the most common side effects are gastrointestinal symptoms.

Objective To study the relationship between polymorphism of NAT2 gene and the susceptibility of osteosarcoma. Methods Using serum samples of patients with osteosarcoma , NAT2 gene polymorphism was determined by PCR-RFLP to observe M1, M2 and M3 mutant genes, NAT2 genotype and allele distribution. Slow acetylation and rapid acetylation genotype between groups in the distribution were also detected. Moreover , the relationship between the clinical characteristics of osteosarcoma and NAT2 genetic polymorphism were analyzed. Results From January 2010 to September 2015, 126 patients with osteosarcoma were enrolled as a case group, and 119 healthy persons in the same period were as the control group. In the control group, the frequency of NAT2 genotype (homozygous wild type (wt/wt and miscellaneous synthetic mutant WT/ MX, homozygous mutant MX/MX) were 30.95%, 50.79% and 18.25% respectively; In the experimental group were 47.06%, 46.22% and 6.72% respectively. The frequency of the two groups was statistically significant (P <0.05). Rapid NAT2 acetylator genotype of suffering from the risk of osteosarcoma 1.782 times slow acetylation genotype (P < 0.05). Compared to rapid acetylation genotype patients with osteosarcoma, slow acetylation genotype patients has smaller tumor volume (P = 0.008),lower differentiation degree of tumor (P = 0.011) and less occurrence of distant metastasis (P = 0.001). Conclusion The rapid acetylation genotype of NAT2 gene may be a risk factor for osteosarcoma.