1.Design, synthesis and biological evaluation of novel 4-substituted-3-nitrobenzamide derivatives.
Qifeng ZHU ; Yongxiang GONG ; Jinqing ZHONG ; Lifei LIU ; Xufei LI ; Xuyang ZHAO
Acta Pharmaceutica Sinica 2014;49(8):1143-9
A series of novel 4-substituted-3-nitrobenzamide derivatives were designed and synthesized. The structures of the target compounds were confirmed with 1H NMR, 13C NMR, MS and element analysis. Anti-tumor activities against HCT-116, MDA-MB435 and HL-60 cell lines in vitro were evaluated by SRB assay. The results indicated most of the target compounds exhibited potent anti-tumor activity. Compound 4a showed the most potent inhibitory activities against three cancer cell lines with the GI50 values of 1.904-2.111 micromol x L(-1). Compounds 4g, 41-4n exhibited more potent inhibitory activities against MDA-MB435 and HL-60 cell lines with the GI50 values of 1.008-3.586 micromol x L(-1) and 1.993-3.778 micromol x L(-1), respectively. The structure-activity relationship of these compounds is discussed preliminarily.
2.Design, synthesis and biological evaluation of novel 1,3 dioxolo 4,5-fisoindolone derivatives.
Yongxiang GONG ; Qifeng ZHU ; Jinqing ZHONG ; Lifei LIU ; Xufei LI ; Xiaohe ZHENG ; Hongying LUO ; Xuyang ZHAO
Acta Pharmaceutica Sinica 2015;50(2):191-8
A series of [1,3]dioxolo[4,5-f]isoindolone derivatives were designed, synthesized and evaluated as inhibitors of acetylcholinesterases (AChE). Furthermore, their effects on memory impairment of mice induced by scopolamine were investigated with step-through test. The results suggested that most of the target compounds exhibited potential inhibition on AChE with IC50 values at micromolar range. Compounds I1 (IC50 value of 0.086 μmol · L(-1)) and I2 (IC50 value of 0.080 μmol · L(-1)) showed the strongest AChE inhibitory activity, which are equipotent to donepezil (IC50 value of 0.094 μmol · L(-1)). Moreover, compounds I1-I4 could improve the memory impairment induced by scopolamine in mice.
3.The diagnosis and treatment of hepatic focal nodular hyperplasia
Rongping GUO ; Chong ZHONG ; Ming SHI ; Yun ZHENG ; Wei WEI ; Xiaojun LIN ; Minshan CHEN ; Yaqi ZHANG ; Jinqing LI ; Guohui LI
Chinese Journal of General Surgery 2001;0(08):-
Objective To explore the clinical diagnosis and management of focal nodular hyperplasia (FNH) of the liver. Methods Forty-two FNH cases treated in the past 9 years were studied retrospectively. The clinical and pathologic data were reviewed. Results Preoperative liver function test and AFP were normal. The preoperative radiography in FNH was usually not specific, with less than 50% cases were suggestive of FNH of the liver. Surgical resection resulted in a permanent cure with no significant postoperative complications. More than one year follow-up found recurrence in one case. Conclusion Clinical, laboratory and radiological findings when combined could help in establishing tentative diagnosis of FNH. Surgery is recommended in cases with equivocal diagnosis or in fear of hepatocellular carcinoma.
4.Study of reactive oxygen species and adiponectin for chronic HBV infection combined with nonalcoholic fatty liver diseases
Liang XU ; Yan ZHONG ; Shuting SU ; Yonggang LIU ; Feinan LYU ; Xiaoli ZHOU ; Jinqing REN ; Ping LI ; Ruifang SHI ; Yong JIANG ; Jiangao FAN ; Yuqiang MI
Chinese Journal of Hepatology 2020;28(3):247-253
Objective:To investigate the application value of reactive oxygen species (ROS) and adiponectin (ADPN) in the judgment of liver inflammation in chronic hepatitis B virus infection combined with nonalcoholic fatty liver disease (NAFLD).Methods:A total of 159 cases with NAFLD (21 cases), chronic hepatitis B virus infection (57 cases), and chronic hepatitis B virus infection combined with NAFLD (81 cases) were collected between June 2016 to December 2018, and the visited patients diagnosis were confirmed by histopathological examination of the liver. ROS and ADPN level retained in serum was determined by enzyme-linked immunosorbent assay. Histopathological examination of liver tissue was used as the gold standard to discuss the diagnostic value of the serum in patients with chronic hepatitis B virus infection combined with NAFLD for the occurrence of nonalcoholic steatohepatitis. One-way analysis of variance was used for the comparison among multiple groups, and LSD-t test was used for pairwise comparison between groups. Measurement data for non-normal distributions were expressed as M (P25, P75). Comparisons between groups were performed using the Mann-Whitney U or Kruskal-Wallis H test. Chi-square test was used to compare the count data between groups. Correlation analysis was performed using Spearman correlation analysis. Histopathological grouping of liver tissue was used as the gold standard, and the area under the receiver operating characteristic curve was used to evaluate the diagnostic efficacy of the regression formula.Results:(1) In patients with chronic hepatitis B virus infection combined with NAFLD, the levels of ROS in the non-hepatic steatosis group and the mild hepatic steatosis group were significantly lower than those in the moderate and severe hepatic steatosis group, while the ADPN level in the non-hepatic steatosis group was significantly higher than liver steatosis group, P < 0.05. (2) The results of correlation analysis showed that ROS was significantly correlated with NAS score, change in the degree of fatty liver and lobular inflammation (all P < 0.05).There was a significant negative correlation between ADPN and the change in the degree of fatty liver ( P < 0.05). (3) Logistic regression analysis results showed that the diagnostic formula for chronic hepatitis B virus infection combined with nonalcoholic steatohepatitis was 0.02 × controlled attenuation index + 0.584 × white blood cells/10 9 + 0.587 × ROS-10.982. The area under receiver operating characteristic curve of the subject was = 0.896. The sensitivity, specificity, positive and negative predictive value were 97.1%, 71.2%, 64.2%, and 97.9%. Conclusion:ADPN and ROS have certain reference value in differentiating the change in the degree of fatty liver and inflammation in chronic hepatitis B virus infection combined with NAFLD and the diagnostic formula has higher application value in the diagnosis and exclusion of chronic hepatitis B virus infection combined with nonalcoholic steatohepatitis.