AIM To study the pharmacokinetic characters following oral administration of colon specific tinidazole tablets in healthy dogs METHOD The plasma and intestine content concentration of tinidazole was determined by RP HPLC method following a single oral dose of 500 mg of two formulations given to each dogs in an open randomized two way crossover design RESULT The main pharmacokinetic parameters of test and reference tablets were as follow: T max : (6 3?1 2) h and (2 4?1 1) h; C max : (46 23?8 93) mg?L -1 and (58 08?14 65) mg?L -1 ; AUC 0-t : (423 21?93 08) mg?h?L -1 and (458 22?112 07) mg?h?L -1 The relative bioavailability of tinidazole colon specific enteric tablets was 92 9%?6 6%. 6 5 h after intake of colon specific tablets, there were a great deal of tinidazole in dogs colon but almost no tinidazole in small intestine CONCLUSION The result demonstrated that the colon tropic effect of the tablets is significant in dogs

AIM　To study the phase I metabolites of phenoprolamine hydrochloride (DDPH) in rat bile. METHODS　DDPH was administered ip to bile duct-cannulated rats. Bile samples were collected before administration and up to 12 h after administration. After being treated with β-glucuronidase, the bile samples were purified and enriched with C-18 SPE columns, and then were analyzed by LC/DAD/MSD. The samples containing synthesized reference standards of DDPH metabolite 1-(2,6-dimethylphenoxy)-2-(3-methoxy-4-hydroxyphenylethylamino)-propane (M1), 1-(2,6-dimethyl-3-hydroxyphenoxy)-2-(3,4-methoxy-phenylethylamino)-propane (M2), 1-(2,6-dimethyl-4-hydroxyphenoxy)-2-(3,4-methoxyphenylethylamino)-propane (M3), 1-(2,6-dimethyl-4-hydroxyphenoxy)-2-(3-hydroxy-4-methoxyphenylethylamino)-propane (M4), 1-(2,6-dimethyl-3-hydroxyphenoxy)-2-(3-hydroxy-4-methoxyphenylethylamino)-propane (M5) and 1-(2,6-dimethyl-4-hydroxyphenoxy)-2-(3-methoxy-4-hydroxyphenylethylamino)-propane (M6) were analyzed by LC/DAD/MSD under identical conditions. RESULTS　The retention times, UV spectra, molecular weights and production spectra (obtained by collision-induced dissociation)of the apparent ions of peak A, B, C, D, E and F in the total ion chromatogram of DDPH treated rat bile sample were consistent with those of M1, M2, M3, M5, M4 and M6, respectively. CONCLUSION　M1, M2, M3, M4, M5 and M6 were identified as the phase I metabolites of DDPH in the rat.

Exocyst complex is known to function in the exocytosis network, however, the molecular mechanism is unclear yet. Using UV/trimethylpsoralen mutagenesis, the sec-10 (one component of the exocyst complex) knockout mutant of C. elegans was obtained for the first time. The drug sensitive assays revealed clearly that the sec-10 gene affected the neural signal transmission, however, the electrophysiological assay showed the function of the ionotropic receptors in the neuromuscular junctions (NMJs) were unaltered compared with the wild type (WT). Thus it was assumed that the sec-10 gene might not influence the known ionotropic receptors in the NMJs, but some other pathways instead.

Overexpression of multidrug resistance gene, (MDR1) is responsible for the resistance of anticancer agents in cancer cells. In this study, we designed three pairs of DNA primers to clone MDR, cDNA from human normal liver by polymerase chain reaction. The sites of these primers in MDR cDNA are (I)-64-46 (5') and 1680-1698 (3'); (II) 1471-1489 (5') and 2905-2923 (3'); (III)2729-2747 (5') and 3845-3863 (3). The three reactions were underwent after the human normal liver mRNA was reverse transcripted into single strand DNA. The lengths of PCR products are 1762bp, 1452 bp and 1134bp, respectively. The former two products were subcloned in pBluscript SK, respectively and the latter product was subcloned in pGEM7Z (named as pMDR1.7, pMDR1.4 and pMDRl.l, respectively). Cloned genes were certificated as MDR1 cDNA by sequence analysis. Full-length MDR, cDNA was obtained after further subcloning. Full-length MDR1 cDNA we obtained will be a very important tool in molecular diagnosis and gene therapy of anticancer drug resistance.

AIM: To investigate the role of p38 mitogen-activated protein kinase (p38MAPK) signaling pathway in the Kupffer cells (KCs) production of pro-inflammatory cytokines, tumor necrosis factor-?(TNF-?) and interleukin-1?(IL-1?), in severe acute pancreatitis (SAP) rats. METHODS: Sprague-Dwaley rats were randomized into three groups: ①sham operation rats, ②SAP rats, ③SAP rats given the p38 MAPK inhibitor CNI-1493(10 mg/kg, iv). The SAP model was induced by the bili-pancreatic duct infusion with 5% sterile soduim taurocholate solution. Rats from each group were killed at 12 h after sham operation or SAP and Kupffer cells (KCs) were isolated. The mRNA expressions of TNF-? and IL-1? (by quantitative real-time RT-PCR) and p38 MAPK activity (by Western blot analysis) in KCs were examined. The levels of TNF-? and IL-1? in plasma were determined by ELISA. RESULTS: There was a significant acvitation of p38 MAPK in KCs harvested from SAP rats than those from sham operation rats. SAP also promoted the mRNA expressions of TNF-? and IL-1? in KCs and the plasma levels of TNF-? and IL-1?. These events were significantly inhibited by treatment with CNI-1493.CONCLUSIONS: p38 MAPK activation is one important aspect of the signaling events that may mediate the KCs production of pro-inflammatory cytokines, TNF-? and IL-1?, in SAP rats. The inhibition of the p38 MAPK may be a potential target in the prevention and treatment of SAP.

Obiective To explore the risk factors of endometriosis-associated ovarian cancer (EAOC) in women with ovarian endometriosis aged 45 years and older in China. Methods The medical records of total 1038 women aged 45 years and older with a surgicopathological diagnosis of ovarian endometriosis treated at Peking Union Medical College Hospital from December 1994 to December 2014 were reviewed. Histology evaluation determined ovarian endometriosis with (n=30) or without (n=1008) ovarian cancer. Results (1) There were 30 (2.9%, 30/1018) cases confirmed as having EAOC. Clear cell carcinoma (63.3%, 17/30) and endometrioid adenocarcinoma (23.3%, 7/30) were commonly observed subtypes and 70.0%of EAOC patients were at stageⅠ. (2) Compared women with ovarian endometriosis in the same age group,patients with EAOC were older (50.8 vs 48.5 years, P=0.002). There were more in postmenopausal status at diagnosis of EAOC (P＜0.01). There were more found with a mass ≥8 cm (P＜0.01). Women with EAOC had higher prevalence of coexisting endometrial disorders (P=0.003). No differences were found in preoperative CA125 value and infertile or nulliparous women (P＞0.05). Conclusions For women with ovarian endometriosis aged 45 years and older, the subgroup of patients characterized by postmenopausal status and ovarian endometrioma (≥8 cm) have a higher risk of EAOC. Active intervention or intensive follow-up should be considered for this population group, especially for those concurrent with endometrial disorders.

We have cloned full-length MDR1 cDNA from human normal liver tissue in previous study. Using this MDR1 cDNA as probe, we observed the MDR1 gene expression in human hepatocellular carcinoma treated with and without chemotherapy by Northern blot. The results showed that expression of MDR1 gene in hepatocellular carcinoma tissues was higher than that in their adjacent normal liver tissues; and enhanced MDR1 gene expression was also observed in hepatocellular carcinoma treated with chemotherapic agents. We also explored a method for quantitative analysis of MDR1 gene expression in hepatocellular carcinoma by polymerase chain reaction. This study suggests that overexpression of MDR1 gene may be responsible for the intrinsic and acquired drug resistance of human hepatocellular carcinoma, and PCR is a preferable method for quantitative analysis of MDR1 gene expression in hepatocellular carcinoma.

In this paper we synthesised two kinds of hydrophilic liquid crystal, i.e. cholesteryl triethenyl glycol carbonate (TCC), cholesteryl tetraethenyl glycol carbonate (TeCC), which were blended with PLA with certain contents to form composite membranes. Contact angle test showed that the contact angle decreases with the increase of liquid crystal. The blood-compatibility of the composite membranes was assessed by blood clotting time and hemolysis ratio which showed that these PLA/liquid crystal composite membranes with the content of 30%-40% liquid crystal appeared to be beneficial in improving the blood compatibility and anticoagulation.
Biocompatible Materials ; chemistry ; Blood Coagulation ; Lactic Acid ; Materials Testing ; Membranes, Artificial ; Polyesters ; Polymers

Objective To investigate the clinical efficacy of percutaneous minimally invasive anchorage in the treatment of acute closed rupture of Achilles tendon. Methods A retrospective casecontrol study was conducted on the clinical data of 32 patients (16 cases on the left side and 16 cases on the right side) with acute closed Achilles tendon rupture treated from January 2015 to January 2017. There were 27 males and five females, aged 24-67 years (mean, 40.8 years). The patients were divided into treatment group which adopted percutaneous minimally invasive combined with anchor suture and control group which used simple minimally invasive suture, with 16 cases in each group. The operation time, hospitalization time, sural nerve injury, single foot heel raise at 3 months and 6 months, difference of calf circumference on the rupture surface between the affected side and healthy side at 6 months, ankle back foot score scale (AOFAS), and infection at 6 months were recorded. Results All patients were followed up for average 8.9 months (range, 6-12 months). In treatment group, the operation time was (35.75 ±3.10) minutes and hospitalization time was (8.38±1.62) days. The AOFAS score was(92.12 ±5.86)points. The result of single foot heel raise was positive in one case at 3 months and in 0 case at 6 months. The difference of calf circumference on the rupture surface between the affected side and healthy side at 6 months was (2.23 ±0.97)cm. In the control group, the operation time was (33.43± 3.89)minutes and hospitalization time was (8.50±1.75)days. The AOFAS score was (91.00 ±7.15) points at 6 months. The result of single foot heel raise was positive in eight cases at 3 months and in 0 case at 6 months. The difference of calf circumference on the rupture surface between the affected side and healthy side at 6 months was (1.64 ±2.34) cm. There were no significant differences between the two groups in operation time, hospitalization time, the AOFAS score at 6 months, and the results of single foot heel raise at 6 months(P ＞0.05). Treatment group had better results than control group in terms of the difference of calf circumference on the rupture surface between the affected side and healthy side at 6 months as well as the result of single foot heel raise at 3 months (P ＜ 0.05). No infection and sural nerve injury were found in either group. Conclusion The repair of Achilles tendon rupture by percutaneous minimally invasive anchor technique can help patients achieve heel raise early, obtain better muscle capacity, and return to work earlier.