Clinical characteristics and risk factors for recurrence of anal fistula patients / 中华胃肠外科杂志

<p><b>OBJECTIVE</b>To investigate the epidemiology, internal opening location, and risk factors associated with recurrence of anal fistula.</p><p><b>METHODS</b>Clinical data of 1783 hospitalized patients admitted for anal fistula treatment to Shanghai Shuguang Hospital from January 2013 to September 2015 were retrospectively analyzed. Fistula passing through anorectal ring or locating above was defined as high anal fistula (n=125). Internal opening location was defined as follows: posterior (5 to 7 o'clock), front(11 to 1 o'clock), left (2 to 4 o'clock) and right (8 to 10 o'clock).</p><p><b>RESULTS</b>Among 1783 cases, 1526 were male with a median age of 36 years, 257 were female with a median age of 35 years, and the ratio of male to female was 5.9 vs 1.0. In high anal fistula cases, this ratio of male to female was 7.3 vs 1.0. Posterior internal opening accounted for 51.4%(884/1720), while this percentage was 66.4%(83/125) in high anal fistula cases, which was significantly higher than 50.2%(801/1595) in low anal fistula cases(P=0.002). Postoperative recurrence rate was 2.6%(45/1720) and the rates in high anal fistula and low anal fistula were 13.6%(17/125) and 1.8%(28/1595) respectively, with significant difference(P=0.000). Multivariate logistic regression analysis showed that fistula height(OR=5.475, 95%CI:2.230 to 13.445, P=0.000), treatment history(OR=2.671, 95% CI:1.315 to 5.424, P=0.007), seton placement history (OR=4.707, 95%CI:1.675 to 13.232, P=0.003) and concomitant colitis(OR=10.300, 95%CI:1.187 to 89.412, P=0.034) were independent risk factors for anal fistula recurrence. Seton placement history was an independent risk factor for high anal fistula recurrence (OR=6.476, 95%CI:1.116 to 37.589, P=0.037).</p><p><b>CONCLUSIONS</b>Anal fistula occurs in young and middle-aged male patient. Internal opening locates in posterior more commonly, especially in high anal fistula patients. Postoperative recurrence rate of high anal fistula is quite high. Patient with both high anal fistula and seton placement history has significantly high rate of postoperative recurrence.</p>

Design, synthesis and PPAR agonist activities of novel L-tyrosine derivatives containing phenoxyacetyl moiety / 药学学报

The design, synthesis and bioevaluation of a series of novel L-tyrosine derivatives as peroxisome proliferator-activated receptor (PPAR) agonists are reported. Four intermediates and twenty L-tyrosine derivatives containing phenoxyacetyl moiety TM1 were synthesized starting from L-tyrosine via four step reactions including the esterification of carboxyl group, phenoxyacetylation of a-amino group, bromoalkylation of phenolic hydroxyl group and then nucleophilic substitution reaction with various heterocyclic amines in 21%-75% overall yield. Subsequently TM1 were hydrolyzed to give sixteen corresponding target compounds TM2 in 77%-99% yield. The chemical structures of the thirty-nine new compounds were identified using 1H NMR, 13C NMR techniques and thirty-five were confirmed by HR-MS techniques. Screening results in vitro showed that the PPAR relative activation activities of the target molecules are weak overall, while compound TM2i reaches 50.01%, which hints that the molecular structures of these obtained compounds need to be modified further.

Synthesis and PPAR activities of novel phenylacetic acid derivatives containing sulfonamide moiety / 药学学报

The discovery of high performance leading antidiabetic compounds containing sulfonamide and 4-aminophenylacetic acid moieties is reported. This was achieved by the synthesis of 6 intermediates and subsequently 20 target molecules using 4-aminophenylacetic acid as the starting materials, and through a few synthetic routes aided by multi-step reactions including sulfonylation of amino group, deacylation of amides and esterification of carboxyl group, as well as acylation of amino group. The chemical structures of the twenty-four new compounds were determined using 1H NMR, 13C NMR and HR-MS techniques. Screening in vitro of their peroxisome proliferator-activated receptor (PPAR) activation activities showed weak relative PPAR activation activities to most of the target molecules. However, 4 target molecules exhibit PPAR over 58%, and as high as 81.79% for TM2-i, presenting itself as potent leading compound for antidiabetic drugs. This research also confirms that it is probable to achieve esterification of carboxyl group and deacylation of fatty acid N-phenyl amides concurrently in SOCl2/alcohol solvent system. This provides new synthetic method for the selective reaction within molecules containing both carboxyl and N-aryl amido groups of fatty acids.

Synthesis of novel beta-aminoalcohols containing nabumetone moiety with potential antidiabetic activity / 药学学报

Twenty five new beta-aminoalcohols containing nabumetone moiety were prepared via the reduction of potassium borohydride with a convenient and efficient procedure, starting from beta-aminoketones that have been synthesized by our group. Their chemical structures were determined by IR, MS, 1H NMR, 13C NMR, HR-MS and antidiabetic activities were screened in vitro. Preliminary results revealed that the antidiabetic activity of most beta-aminoalcohols were better than that of the corresponding beta-aminoketones. Although most compounds showed weak antidiabetic activity, the alpha-glucosidase inhibitory activity of compounds 5hd(1) and 5id(2) reached 74.37% and 90.15%, respectively, which were superior to the positive control. The relative peroxisome proliferator-activated receptor response element (PPRE) activity of five compounds were more than 60%, among them compound 5ca possessed the highest activity (112.59%). As lead molecules of antidiabetic agents, compounds 5hd(1), 5id(2) and 5ca deserve further study.

Synthesis and investigation on antidiabetic activity of 4-(1-aryl-3-oxo-5-phenylpentylamino) benzenesulfonamide / 药学学报

Searching for new antidiabetic lead compound, 4-(1-aryl-3-oxo-5-phenylpentylamino) benzenesulfonamides were designed and synthesized directly by three component one-pot condensation of 4-phenyl-2-butanone and sulfanilamide with some aromatic aldehydes at an yield of 23%-97%. The chemical structures of the twelve new Mannich bases were confirmed by 1H NMR, 13C NMR, FTIR, ESI-MS and HR-MS. The screening results of antidiabetic activity indicated that most of these title compounds possess alpha-glucosidase inhibitory activity, among which compound le is the strongest one. And compound 11 possesses good peroxisome proliferator-activated receptor response element (PPRE) agonist activity. The structure-activity relationship of these new beta-amino ketones containing benzenesulfonamide unit was also discussed preliminarily.

Study on Contamination Level of Polychlorinated Biphenyls in Retail Livestock Food in a City / 环境与健康杂志

Objective To investitgate the level of polychlorinated biphenyls in retail livestock meat.Methods Totally 28 samples of three kinds of meat including of beef,pork and mutton were collected during Aug-Dec.,2008.Twelve dioxin-like polychlorinated biphenyls(DL-PCBs) and six marker PCBs were extracted by Soxhlet extractor,cleaned up by FMS and qualitative and quantitative analyzedsis by isotope dilution high-resolution gas chromatography/high resolution mass spectrometry(HRGC/ HRMS).Results Levels of total 18 compounds including of 12 DL-PCBs and indicator PCBs in beef,pork and mutton were 1 607.60 pg/g fat,435.82 pg/ g fat,and 505.17 pg/g fat respectively,DL-PCBs concentration were 456.19 pg/g fat,46.37 pg/g fat and 77.50 pg/g fat respectively.Maker-PCBs concentration were 1 151.41 pg/g fat,389.45pg/g fat and 427.67 pg/g fat respectively.The levels of PCB toxicity equivalent(TEQ)(the median value)were:0.84 pg/g fat in beef,0.15 pg/g fat in pork,0.28 pg/g fat in mutton respectively.The TEQ concentration of PCB(median value) was lower than the EU action level limit value.In all samples,PCB118 was the greatest contributor to the total contaminated concentration,and PCB126 was the dominant contributor to toxicity equivalent(TEQ).Six of 28 samples exceeded the limit value of the EU action level.Conclusion The results show that PCBs contamination exists in a city from the six samples exceeding the EU standard limit.It should take measures to explore the cause of contamination of PCBs compounds and control the pollution in order to guarantee food safety effectively.