1.Study on Purification of Swertiaman from Swertia pesudochinensis Hara. with Macroporous Adsorbent Resin
Dacheng ZHOU ; He MENG ; Rongsheng LI
Chinese Journal of Information on Traditional Chinese Medicine 2006;0(07):-
Objective To explore the suitable type of macroporous adsorbent resin to purity swertiaman from Swertia pesudochinensis Hara., and determine the parameters and conditions for its purification procedures. Method Purification effect of 8 types of macroporous resins used to purify the Swertia pesudochinensis Hara. were inspected, with the content of swertiaman as index. Result HPD-100 type resin showed better effect than others, it had optimum adsorption and elution parameters with its dynamic saturated adsorption ratio was 70.48 mg/g. After eluted with 2 BV of distilled water, 4 BV 30% ethanol and collected, the content of swertiaman in the spray dried powder was 52.29%. Conclusion HPD-100 types macroporous resin showed a better comprehensive adsorption property and can be used to enrich and purify the swertiaman included active fraction of iridoid glycosides for industrialization.
2.Prenatal screening and diagnosis of fetal abnormal chromosome and nervous tube defect: report of 7698 cases
Ruiping HUANG ; Hong ZHOU ; Zhiying DI ; Yaying ZHANG ; Dacheng SUN
Chinese Journal of General Practitioners 2008;7(1):65-67
This study was to explore the value of maternal serum screen in identification of fetal abnormal chromosome and neural tube defect(NTD). By using time-distinguished fluorescence immunoassay, serum levels of free-β-HCG and alpha fetal protein(AFP)were obtained in 7698 pregnant women at 15~20 +6weeks. and 483 were found at a higher risk of fetal abnormal chromosome. Based on amniotic fluid examination or cord blood testing on 344 high. Risk participants. Fetal abnormal chromosome was found in 18 women with a positive rate of 5. 2%. Twenty-five pregnant women were NTD high-risk, and their positive rate was 0. 3%. B-mode ultrasound identified 6 fetal malformations and 2 fetal deaths ( positive rate of 32. 0%). In high-risk or low-risk group, there were 25. 6%and 7. 7%subjects developed adverse outcome, respectively(P<0. 05). Our findings suggested that maternal serum screen is an effective prediction factor for fetal abnormal chromosome and NTD.
3.Synthesis and investigation on antidiabetic activity of 4-(1-aryl-3-oxo-5-phenylpentylamino) benzenesulfonamide.
Dacheng YANG ; Jufang YAN ; Jin XU ; Fei YE ; Zuwen ZHOU ; Weiyu ZHANG ; Li FAN ; Xin CHEN
Acta Pharmaceutica Sinica 2010;45(1):66-71
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.
4.Correlation between internal thyroid function and intrahepatic cholestasis in pregnancy
Hong ZHOU ; Qiuwei WANG ; Fang CAO ; Ruiping HUANG ; Ziqiang ZHU ; Dacheng SUN ; Bin YU
Chinese Journal of General Practitioners 2011;10(6):417-419
A total of 166 women with intrahepatic cholestasis in pregnancy (ICP) participated in the study. Serum levels of thyroid stimulating hormone (TSH), free thyroxine 4 (FT4) and thyroid peroxidase antibody (TPOAb) were quantified for all of them with electrochemiluminescence (ECL) technique, and compared with those in normal pregnant women. Results showed that serum TSH and TPOAb [22. 9%(38/166)] increased significantly, but no significant change in serum level of FT4 was observed in women with ICP, as compared to those in normal pregnant women. Overall prevalence of thyroid diseases in ICP women was 35.5% (59/166), significantly higher than that in normal population screened for thyroid disease (17. 1%, 143/837) at the same time period. It suggests that thyroid dysfunction may be involved in pathogenesis of ICP.
5.Synthesis of novel beta-aminoalcohols containing nabumetone moiety with potential antidiabetic activity.
Kun ZHANG ; Jufang YAN ; Xuemei TANG ; Hongping LIU ; Li FAN ; Guangming ZHOU ; Dacheng YANG
Acta Pharmaceutica Sinica 2011;46(4):412-21
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.
6.Design, synthesis and PPAR agonist activities of novel L-tyrosine derivatives containing phenoxyacetyl moiety.
Lijiang ZHOU ; Jufang YAN ; Kun ZHANG ; Li FAN ; Xin CHEN ; Dacheng YANG
Acta Pharmaceutica Sinica 2013;48(10):1570-8
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.
7.Detection of the diagnosis about primary hepatocellular carcinoma with the AFP-IgM immune complexes in serum
Jingting JIANG ; Changping WU ; Jun WU ; Xihu QIN ; Dacheng SUN ; Mei JI ; Bin XU ; Haifeng DENG ; Mingyang LU ; Guoping ZHOU ; Min LI ; Xiao ZHENG ; Jian LIU ; Liangrong SHI ; Xu NING ; Nilssonehle PETER
Chinese Journal of Laboratory Medicine 2008;31(7):789-792
Objective To evaluate the significance of AFP-IgM, this is one of new tumor markers, in the diagnosis of primary hepatocellular carcinoma (PHC). Methods The contents of AFP-IgM and AFP in serum of 103 healthy subjects, 74 patients suffered primary hepatic carcinoma, 27 patients affected by liver cirrhosis and 63 patients affected by chronic hepatitis were detected by means of enzyme linked immunosorbent assay and electrochemiluminescence. No-PHC is comprised of liver cirrhosis,chronic hepatitis and health subjects as control group. Results The area under ROC curve of AFP was larger than that of AFP-IgM (0.85 vs 0.72, Z=3.21) and the best cut-off value of AFP-IgM and AFP was 3×105-AU/L and 10 ug/L respectively, which was determined by ROC curve. Under the cut-off value, the sensitivity of AFP- lgM and AFP for PHC were 64.9% and 79.7%, and the specificity were 75.6% and 80.3%, yet their efficacies were similar. However, for early diagnosis of liver cancer (stage Ⅰ and Ⅱ), the area under ROC curve of AFP-IgM was larger than that of AFP (0.91 vs 0.82,Z=1.73). The sensitivity of AFP-IgM andAFP were 94.4% and 72. 2%, and the specificity were 81.9% and 79.9%. The differences of AFP-IgMand AFP for early diagnosis of liver cancer were statistically significant. When both of the test results combined AFP-IgM with AFP are positive, it can be diagnosed as liver cancer. The specificity of combineddetermination of the two forms was 89.1%, and the efficacy was 79. 0%. Conclusions Both of thesensitivity and specificity of the AFP-IgM test were higher than that of the AFP for early diagnosis of livercancer. We also found that combined determination of the two forms significantly increased the specificityand the positive predictive value for the diagnosis of PHC, thus AFP-IgM was of especially significance forearly diagnosis of liver cancer.