AIM: To study the bioequivalence of two tadalafil tablets in Chinese healthy male subjects. METHODS: A randomized, open-label, two-period, two-sequence, crossover study designing was adopted in the study. Thirty-six healthy male subjects were enrolled under fasting condition and fed condition, respectively. Each subject was given a single oral dose of tadalafil tablet (20 mg). The concentration of tadalafil in plasma was determined by LC-MS/MS. The pharmacokinetic parameters were calculated by WinNonlin 8.0 program, and statistical analysis was performed by using SAS 9.4 statistics software. RESULTS: Under fasting condition, the pharmacokinetic parameters of tadalafil of the test (T) and reference (R) preparation were as follows: C

AIM: To study the bioequivalence of two metformin hydrochloride sustained-release tablets in Chinese healthy subjects. METHODS: A randomized, open-label, two-period, crossover study design was adopted in the study. In fasting test 36 and in fed test 23 healthy subjects were given a single oral dose of metformin hydrochloride sustained-release tablet (0.5 g). The concentration of metformin in plasma was measured by HPLC-MS/MS. The pharmacokinetic parameters were calculated by WinNonlin 7.0 program, and statistical analysis were performed by using SAS9.4 statistics software. RESULTS: In the fasting test, the pharmacokinetic parameters of metformin of the test (T) and reference(R) preparation were as follow: C

Objective: To explore the diagnostic value of serum NSE, S100B protein and myocardial zymogram in premature infants with intrauterine infection. Methods: From January 2016 to December 2017, 60 preterm infants with intrauterine infection in the Integrated Chinese and Western Medicine Hospital of Wenzhou were selected in the study.According to whether brain injury occurred, they were divided into brain injury group (28 cases) and non-brain injury group (32 cases). Serum NSE content was detected by chemiluminescence method, serum S100B protein level was detected by enzyme linked immunosorbent assay (ELISA), and serum CK and HBDH levels were detected by automatic biochemical analyzer.The serum levels of NSE, S100B, CK and HBDH were compared between the two groups, the combined diagnostic efficacy of NSE+ S100B protein+ CK+ HBDH was analyzed, the correlation of serum NSE, S100B protein, CK, HBDH with brain injury wasanalyzed. Results: The levels of serum NSE [(2.43±0.54)μg/L] and S 100B [(14.36±3.21)ng/L] in the brain injury group were higher than those in the non-brain injury group [(0.97±0.27)μg/L and (8.10±1.87)ng/L] (t=13.498, 9.370, all P<0.05). The levels of serum CK [(437.64±54.12)U/L] and HBDH [(387.91±56.45)U/L] in the brain injury group were significantly higher than those in the non-brain injury group [(183.54±32.58)U/L and (174.3±26.63)U/L] (t=22.347, 19.126, all P<0.05). The sensitivity and specificity of the combined diagnosis of NSE+ S100B protein and myocardial zymogram were higher than those of each single index.Serum NSE, S100B protein, CK and HBDH were positively correlated with brain injury. Conclusion The elevation of serum NSE, S100B protein and myocardial zymogram in preterm infants with intrauterine infection after birth has certain clinical significance in judging whether brain injury occurs or not.

Objective To evaluate the efficacy of a sustained releasing mosquito larvicide package against larval breeding and its impact on water and plant,in order to provide a scientific evidence for its application in control and prevention of Dengue.Methods Guangzhou Center for Disease Control and Prevention was chosen as the test place.Twenty test sites were set up,2 bags of sustained releasing larvicides package,1 bag of sustained releasing larvicides package,3 g 1％ temephos granules and nothing were put into 4 glass bottles for each test site from July to December in 2014,respectively.The 4 glass bottles were called high dose (H) group,low dose (L)group,positive control (P) group and blank control (B) group,respectively.The 4 groups were observed at intervals of 10 days for 19 times.Environmental air temperature,turbidity of water,number of larvae and damage of plant were recorded.And 5 test sites were selected to collect water specimen.The chemical oxygen demand,ammonia nitrogen concentration and temephos concentration of water specimen were detected.Results The larval breeding rates were 0 (0/380),1.1％ (4/380),0.8％ (3/380) and 63.4％ (241/380),damage rates of plant were 5.0％ (19/380),5.5％ (21/380),4.7％ (18/380),4.7％ (18/380) and turbidty rates of water were 24.5％ (93/380),19.7％ (75/380),33.4％ (127/380) and 20.3％ (77/380) in H,L,P and B groups,respectively.Statistically significant differences were seen in larval breeding rate and turbidity rate of water between different groups (x2 =823.565,24.715,all P ＜ 0.05),but they were not seen in damage rate of plant (x2 =0.332,P ＞ 0.05).The temephos concentrations were 1.24,0.78 and 2.33 mg/L in H,L and P groups,respectively.Statistically significant differences were seen in temephos concentration between different groups (H =35.426,P ＜ 0.01),but they were not seen in chemical oxygen demand and ammonia nitrogen concentration (H =0.239,0.013,all P ＞ 0.05).Conclusions The sustained releasing package of mosquito larvicide makes less pollution to water and has no impact on water turbidity.Moreover,it doesn't damage the aquatic plant.The efficacy of the sustained releasing package of mosquito larvicide could effectively prevent mosquito larval breeding in Dengue epidemic period.

OBJECTIVE: Three fractions (SM, SM-A, SM-B) were prepared from different polarity parts of Ipomoea batatas Lam. (cv.simon) leaves and the anti-tumor potency as well as the dose-response relations were evaluated. METHODS: The anti-tumor activities of fraction SM, SM-A or SM-B were screened by MTS in human hepatic cancer Hep3B cells, lung cancer A549 cells or gastric carcinoma MGC803 cells, respectively. RESULTS: The three fractions all showed anti-tumor activities in three cancer cells with different sensitivity. Among them, SM-B was the most potent fraction with IC50 values at 15.17 mg/L, 72.64 mg/L or 165.47 mg/L in MGC803 cells, A549 cells or Hep3B cells, respectively (P<0.05). CONCLUSION Th e extraction of Brazil sweet potato leaves displayed anti-tumor activity and SM-B was the most potent fraction.
Antineoplastic Agents, Phytogenic ; chemistry ; isolation & purification ; Cell Line, Tumor ; Humans ; Ipomoea batatas ; chemistry ; Plant Extracts ; chemistry ; Plant Leaves ; chemistry

OBJECTIVETo evaluate the relationship between CT findings and immunohistochemical types of gastrointestinal stromal tumors (GIST).

METHODSCT imaging and clinicopathological data of 85 patients with GIST were analyzed retrospectively. The CT findings of GIST including lesion location, size, contour, boundary, tumor growth pattern, degree of enhancement, necrosis and calcification, were summarized and compared with the immunohistochemical types of the GIST.

RESULTSOf the 85 patients, smooth muscle differentiation was in 26 cases (30.6%), neural differentiation in 20 (23.5%) , both smooth muscle and neural differentiation in 10 (11.8%) and no obvious differentiation in 29 (34.1%) cases. GISTs occurred in the duodenum were more frequently seen in muscle type than in any other types, GIST with smooth muscle differentiation had higher prevalence of huge mass (larger than 10 cm), distinctive enhancement and extensive necrosis than other types (P < 0.05). There was no significant difference in the relationships of immunohistochemical types with tumor contour, boundary, growth pattern and calcification among the four groups of GIST (P > 0.05).

CONCLUSIONSCT scan is the most important and effective method for diagnosis of GIST. Analyzing CT signs has some potential value in judgmet of immunohistochemical types of GIST.

Lipid droplets, which are conserved across almost all species, are cytoplasmic organelles used to store neutral lipids. Identification of lipid droplet regulators will be conducive to resolving obesity and other fat-associated diseases. In this paper, we selected 11 candidates that might be associated with lipid metabolism in Caenorhabditis elegans. Using a BODIPY 493/503-based flow cytometry screen, 6 negative and 3 positive regulators of fat content were identified. We selected one negative regulator of lipid content, C13C4.5, for future study. C13C4.5 was mainly expressed in the worm intestine. We found that this gene was important for maintaining the metabolism of lipid droplets. Biochemical results revealed that 50% of triacylglycerol (TAG) was lost in C13C4.5 knockout worms. Stimulated Raman scattering (SRS) signals in C13C4.5 mutants showed only 49.6% of the fat content in the proximal intestinal region and 86.3% in the distal intestinal region compared with wild type animals. The mean values of lipid droplet size and intensity in C13C4.5 knockout animals were found to be significantly decreased compared with those in wild type worms. The LMP-1-labeled membrane structures in worm intestines were also enlarged in C13C4.5 mutant animals. Finally, fertility defects were found in C13C4.5(ok2087) mutants. Taken together, these results indicate that C13C4.5 may regulate the fertility of C. elegans by changing the size and fat content of lipid droplets by interfering with lysosomal morphology and function.
Animals ; Biological Evolution ; Caenorhabditis elegans ; genetics ; growth & development ; metabolism ; Caenorhabditis elegans Proteins ; genetics ; metabolism ; Fertility ; Flow Cytometry ; Gene Knockout Techniques ; Humans ; Lipid Metabolism ; genetics ; Lysosomes ; genetics ; metabolism ; Membrane Proteins ; genetics ; Metabolic Networks and Pathways ; genetics ; Triglycerides ; metabolism

Caenorhabditis elegans hid-1 gene was first identified in a screen for mutants with a high-temperature-induced dauer formation (Hid) phenotype. Despite the fact that the hid-1 gene encodes a novel protein (HID-1) which is highly conserved from Caenorhabditis elegans to mammals, the domain structure, subcellular localization, and exact function of HID-1 remain unknown. Previous studies and various bioinformatic softwares predicted that HID-1 contained many transmembrane domains but no known functional domain. In this study, we revealed that mammalian HID-1 localized to the medial- and trans- Golgi apparatus as well as the cytosol, and the localization was sensitive to brefeldin A treatment. Next, we demonstrated that HID-1 was a peripheral membrane protein and dynamically shuttled between the Golgi apparatus and the cytosol. Finally, we verified that a conserved N-terminal myristoylation site was required for HID-1 binding to the Golgi apparatus. We propose that HID-1 is probably involved in the intracellular trafficking within the Golgi region.
Animals ; Brefeldin A ; pharmacology ; Cell Line, Tumor ; Cytosol ; drug effects ; metabolism ; Humans ; Intracellular Space ; drug effects ; metabolism ; Membrane Proteins ; metabolism ; Protein Transport ; drug effects ; Rats ; Vesicular Transport Proteins ; metabolism ; trans-Golgi Network ; drug effects ; metabolism

Objective: To study the relationship between occurrence and development of chronic periodontitis and neuropeptide substance P (SP) in gingival crevicular fluid. Methods: There were 48 patients in experimental group and 42 patients in the control group. Gingival crevicular fluid samples were collected from the patients′ intraoral chronic periodontitis inflammatory positive sites and healthy sites. Neuropeptide substance P levels in gingival crevicular fluid from two groups were measured by radioimmunoassay. Gingival index, pocket depth, attachment loss, alveolar bone resorption were recorded and their correlations with SP were analyzed. Results: SP levels of the experimental group were significantly higher than those of the control group(P<0.01). There were significant differences(P<0.01)between SP level and periodontal clinical index in slight periodontitis and the control group. There were significant correlations(P<0.05)between GCF SP content and all PD, AL, ABL but GI in slight periodontitis, and there were significant correlations in between GCF SP content and GI for both moderate periodontitis and severe periodontitis. There were significant correlations(P<0.01) between GCF SP content and PD,AL,ABL for both moderate periodontitis and severe periodontitis. Conclusion:GCF SP level is closely related to occurrence and development of chronic periodontitis.GCF SP level can reflect the degree of the damage of periodontium.Determination of patients′ GCF SP level has important significance for the patients′ condition judgement and treatment guidance.

OBJECTIVE:To establish a method for determination of carbazochrome sodium sulfonate for injection.METH_ ODS:C 18 was used as chromatographic column;the mobile phase consisted of0.12%ammonium dihydrogen phosphate buffer solution-absolute alcohol(925∶75)with detection wavelength at363nm and flow rate at0.8ml/min.The sample size was10?l and the column temperature was25℃.RESULTS:Linear relation was achieved when the concentration of carbzochrome sodium sulfonate was within the range of0.08865mg/ml～0.4432mg/ml(r=0.9999,n=5).The mean recovery rate was99.89%(RSD=1.53%,n=9).CONCLUSION:This method is simple,rapid,accurate,precise,and which can be used as the quality control of carbzochrome sodium sulfonate for injection.