To investigate the anticancer effects of ring C in 18β-glycyrrhetinic acid (GA), a series of GA derivatives featured with 9(11)-ene moiety in ring C were designed and synthesized. The structures were confirmed by IR, LC-MS and 1H NMR. Their inhibitory effects towards human prostate cancer PC-3 and leukemia HL-60 cell lines were determined. Most of the derivatives displayed stronger antiproliferative activities than GA. Particularly, compound 14 showed promising anticancer activity with the GI50 values of 4.48 µmol · L(-1) and 1.2 µmol · L(-1) against PC-3 and HL-60 cells respectively, which is worth further study.
Antineoplastic Agents ; chemistry ; pharmacology ; Cell Line, Tumor ; drug effects ; Cell Proliferation ; drug effects ; Drug Design ; Glycyrrhetinic Acid ; analogs & derivatives ; chemistry ; HL-60 Cells ; drug effects ; Humans ; Male ; Prostatic Neoplasms ; pathology

Objective To study the technique and clinical significance of percutaneous biopsy of transplanted liver guided by CT.Methods 19 transplanted liver were undergone 25 times of percutaneous biopsy and the pathomorphologic changes were demonstrated by HE staining.Results The successful rate of the percutaneous biopsy was 100% for all the 25 times of this procedure,including acute rejection on 9 episodes,preservation perfusion retrauma in 6,bile duct strictures in 4,drug-induced injury in 4,chronic rejection in 1 and acute hepatic necrosis in 1.Conclusions CT-guided percutaneous biopsy is an important method for diagnosing transplanted liver injury and providing great value for distinguishment of the causes for transplanted liver injury.(J Intervent Radiol,2007,16:855-857)

Objective To investigate the effect ofYindanxinnaotong (YDXNT) capsule on learning and memory abilities, super oxide dismutase (SOD) activity and malondialdehyde (MDA) content in the hippocampus of rat models of vascular dementia (VD). Methods Animals were randomly divided into sham-operated group,VD vehicle group (Group VD) and YDXNT treatment group (Group VD+YDXNT); the 4-vessel occlusion was employed to establish the VD rat models in the Group VD and Group VD+YDXNT,while rats in the sham-operated group were not performed occlusion of the bilateral common carotid artery.Rats of the Group VD+YDXNT were given 1 mL liquid (9 granules of YDXNT into 360 mL normal saline) through intragastric administration 3 times daily for a consecutive 4 weeks; and rats of the other 2 groups were given the same volume of saline.The changes of learning and memory abilities were observed by Morris water maze test; the activity of SOD and the content of MDA in the hippocampus were measured. Results As compared with those in rats of the Group VD, the learning and memory abilities in rats of the Group VD+YDXNT were significantly improved (P＜0.05):time in finding the platform was obviously decreased and swimming distance in finding the platform was obviously shortened in rats of Group VD+YDXNT.As compared with those in rats of the Group VD,the activity of SOD in the hippocampus was significantly increased and the content of MDA was obviously decreased in rats of the Group VD+YDXNT (P＜0.05). Conclusion YDXNT could increase oxygen radical metabolism to improve the learning and memory abilities of rats with VD.

OBJECTIVETo describe the prevalence trend and epidemiological characteristics of neural tube defects (NTDs) in perinatal in Zhengzhou city from 1996 to 2005.

METHODSData collected from hospital were used to depict the epidemiology of NTDs in Zhengzhou. All perinatal fetuses born in hospitals had an access within 7 days after delivery. The prevalence were calculated by perinatal'year, sex, birth area (urban versus rural) and maternal age. All monitored perinatal (162,074) accounted for 32.66% from totals (496,203).

RESULTSAll 238 cases were found NTDs, and the overall prevalence rate was 14.68/10,000. The annual prevalence rate presented a decreasing trend during that period. The rates in rural and urban area, in male and female birth were 29.28/10,000 and 9.63/10,000, 11.42/10,000 and 17.74/10,000 respectively. There were significant differences among maternal-age-specific prevalence rates (chi2 = 22.952, P = 0.000). The rates of <20 years group(53.76/10,000) and >35 years group(21.74/10,000) were higher than others.

CONCLUSIONThe prevalence rates of NTDs in rural area is higher than that in urban, female's is higher than male's in Zhengzhou. The annual prevalence rates of NTDs presents a decreasing trend in the past ten years.

China ; epidemiology ; Female ; Humans ; Infant, Newborn ; Male ; Neural Tube Defects ; epidemiology ; Pregnancy ; Pregnancy Trimester, Second ; Pregnancy Trimester, Third ; Prevalence ; Rural Population ; Sex Distribution ; Urban Population

OBJECTIVETo study effective active constituents of Cayratia japonica,a genuine herbal medicine from Fujian.

METHODSuch chromatographic methods as Macroporous, Sephadex LH-20, ODS and normal phase silica gel column chromatography were adopted to separate the chemical components of C. japonica.

RESULTThirteen compounds were obtained, and their structures were identified by analyzing multiple spectral data as luteolin(1), apigenin(2), triethyl citrate-(3), 3-formylindole(4), esculetin(5), bis(2-ethylhexyl)-phthalate(6), calendin(7), ethyl-trans-3,4-dihydr-oxycinnamate(8), luteolin7-O-D-glucoside(9),5-hydroxy-3,4-dimethyl-5-pentyl-2(5H-furanone(10),ethyl-3,4-dihydroxybenzoate(11), eriodictyol(12) and daucosterol(13).

CONCLUSIONAmong them, compounds 3-8 and 10-12 were separated from the plant for the first time.

Nuclear Magnetic Resonance, Biomolecular ; Plants, Medicinal ; chemistry ; Vitaceae ; chemistry

OBJECTIVETo evaluate the therapeutic efficacy and safety of lamivudine treatment in late pregnancy by analyzing the maternal-fetal outcomes of chronic hepatitis B (CHB) mothers featuring hepatitis B e antigen (HBeAg)-positivity and highly viremic status.

METHODSA total of 256 pregnant women in the second or third trimester with monoinfected CHB, HBeAg-positivity, and HBV DNA more than 6 log10 copies/mL were divided into two groups: lamivudine (lam) treatment (n=164) or no treatment (controls; n=92). All infants were treated with hepatitis B immune globin (HBIg; 200 IU) within 12 hrs of birth and 15 days later, and were given the recombinant HBV vaccine (20 mug) at 0, 1 and 6 months. All infants were followed-up to at least seven months and hepatitis B surface antigen (HBsAg) and HBV DNA levels were used to determine perinatal transmission (PT) rates. The mothers' data from routine blood analysis, tests of hepatic and renal function, detection of HBV markers and HBV DNA were retrospectively analyzed to determine changes associated with the lam treatment. Correlations of lam treatment with HBV PT rate, alanine aminotransferase (ALT) normalization, adverse reactions, pregnancy complications, congenital deformities, and infants' growth/development were determined by statistical analyses.

RESULTSPrior to delivery, the lam-treated mothers had significantly lower HBV DNA levels (3.72+/-1.78 vs. controls: 7.83+/-0.67 log10 c/ml; t=-22.359, P less than 0.001). The rate of virological response in the lam-treated group was 97.56% (160/164). The lam-treated group had significantly higher ALT normalization rate (90.20% vs. controls: 55.88%; X2=13.349, P less than 0.001) and significantly lower HBeAg titer (957.73+/-458.42 vs. controls: 1296.35+/-383.14 S/CO; t=-5.410, P less than 0.001). At birth, the infants from lam-treated mothers had significantly lower HBsAg-positivity (15.24% (25/164) vs. controls: 30.43% (28/92); X2=8.284, P=0.004). By 7-12 months after birth, none of the infants born to lam-treated mothers tested positive for HBsAg, compared to 8.70% (8/92) of the infants born to mothers in the control group (X2=14.721, P less than 0.001). None of the lam-treated mothers required treatment discontinuation due to adverse events or lam-resistance. No congenital deformities were observed during the study and follow-up periods. There were no differences between the lam-treated and control groups for postpartum hemorrhage, gestational age, infants' height/weight or Apgar scores.

CONCLUSIONIn highly viremic HBsAg+ mothers with CHB, lam treatment in the second or third trimester of pregnancy is safe and effective for reducing HBV maternal-neonatal transmission.

Adult ; Antiviral Agents ; therapeutic use ; DNA, Viral ; blood ; Female ; Hepatitis B, Chronic ; drug therapy ; transmission ; Humans ; Infant ; Infectious Disease Transmission, Vertical ; prevention & control ; Lamivudine ; therapeutic use ; Mothers ; Pregnancy ; Pregnancy Complications, Infectious ; drug therapy ; virology ; Pregnancy Outcome ; Pregnancy Trimester, Third ; Treatment Outcome ; Young Adult

OBJECTIVETo study the effect of cinobufagin (CBG) on HeLa cell proliferation, and to analyze its mechanism.

METHODSProliferation inhibition in vitro was evaluated by MTT and Sulforhodamine B (SRB) assays in several human tumor cell lines, including Bel-7402, HeLa, MCF-7, BGC-823 and HL60. The cycle of HeLa cells was analyzed by flow cytometry. Two-dimensional electrophoresis was applied to analyze the influence of CBG on HeLa cell proteomics.

RESULTSCBG had inhibitory effects on proliferation of five human cancer cell lines, and the IC(50) values were 0.011 micromol/L (Bel-7402), 0.019 micromol/L (HeLa), 0.116 micromol/L (MCF-7), 0.149 micromol/L (BGC-823) and 1.369 micromol/L (HL60), respectively. HeLa and Bel-7402 cells were among the most sensitive. Flow cytometry assay indicated that the treatment of HeLa cells with various concentrations of CBG for 72 h was able to increase the cell number at G(2)/M phase, from 17.3% up to 35.6%. The results of two-dimensional electrophoresis showed that treatment of HeLa cells with 0.02 micromol/L CBG for 48 h resulted in apparent changes of certain small molecular weight (30,000 - 90,000) acidic proteins (pH 4 - 6).

CONCLUSIONCinobufagin has significant inhibitory effect on growth of five human cancer cells in vitro. It may lead to cell cycle arrest of HeLa cells at G(2)/M phase. It can also change the expression of some small molecular acidic proteins in HeLa cells.

Antineoplastic Agents ; pharmacology ; Bufanolides ; pharmacology ; Cell Cycle ; drug effects ; Cell Proliferation ; drug effects ; Dose-Response Relationship, Drug ; Drugs, Chinese Herbal ; pharmacology ; HeLa Cells ; Humans ; Materia Medica ; Pilot Projects

OBJECTIVETo evaluate the efficacy of combined vaccination with 200IU dose of HBIG and 20 μg of anti-HBV vaccine for the prevention of HBV vertical transmission in babies delivered by HBeAg + and highly viremic mothers and the HBV markers' dynamic changes in babies during follow-up.

METHODSHBeAg + mothers with HBV DNA ≥ to 1.0 × 6 log(10) copies/ml were enrolled and their babies were followed up until 12 months old. The infants received HBIG 200 IU IM in 24 hrs and on day 15, and 20 μg recombinant anti-HBV vaccine at 0, 1 and 6 months. The HBV markers and HBV DNA were tested at birth day, and 1, 7, 12 months after birth respectively. The vertical transmission rate at birth and intrauterine infection rate, the HBsAb positive rate and the HBV markers' dynamic changes during follow up were evaluated.

RESULTS(1) 29 out of 127 infants with HBsAg (+) at birth, 11 of which were HBV DNA (+), HBV perinatal transmission rate was 22.83%. 2 infants' HBsAg were positive at month 1 and became negative at month 7 and 10 infants were still HBsAg (+) and HBV DNA (+). HBV intrauterine infection rate was 7.87%. (2) The positive rate of HBeAg and HBcAb in uninfected infants were 96.58% and 98.29% respectively, which declined gradually to undetectable level after immunization. No infants were HBeAb (+). (3) Infants uninfected produced effective HBsAb after vaccination. The level of HBsAb elevated gradually, and the level of HBeAg decreased quickly even to undetectable.

CONCLUSIONThe combination vaccination of 200 IU HBIG with 20 μg recombinant anti-HBV vaccine in the Infants delivered by HBeAg (+) and highly viremic mothers reduced obviously the rate of perinatal transmission of HBV, enhanced largely the production of antibody against HBV surface antigen and dropped the maternal HBeAg and HBcAb in infants or even to negative.

Adult ; DNA, Viral ; blood ; Female ; Follow-Up Studies ; Hepatitis Antibodies ; administration & dosage ; Hepatitis B ; prevention & control ; Hepatitis B Surface Antigens ; blood ; Hepatitis B Vaccines ; Hepatitis B e Antigens ; blood ; Humans ; Immunization ; Infant ; Infant, Newborn ; Infectious Disease Transmission, Vertical ; prevention & control ; Pregnancy ; Young Adult

Objective To systemically evaluate the efficacy and safety of azithromycin eye drops in treatment of bacterial conjunctivitis.Methods Databases including PubMed, EmBase, the Cochrane Library, CNKI, VIP and WanFang were searched to identify randomized controlled trials (RCT) of azithromycin eye drops in treatment of bacterial conjunctivitis up to December, 2018. Two researchers independently screened the articles, extracted data and assessed the trials qualities. The Meta-analysis was performed using RevMan 5. 3 software to evaluate the clinical cure, bacteriological resolution, and adverse reaction of two treatment groups. Results A total of 6 RCTs (2874 patients) were eligible. The results of Meta-analysis showed that azithromycin eye drops was non-inferior to tobramycin eye drops in both clinical cure (87. 6％vs. 85. 6％, P> 0. 05) and bacteriological resolution rates (91. 9％ vs.92. 7％, P> 0. 05) , while azithromycin showed obvious superiority to tobramycin in the earlier clinical cure rate (35. 8％ vs. 22. 2％, P < 0. 001) . There was no significant difference in the adverse reaction rate (1. 7％ vs. 2. 3％, P> 0. 05) . Compared with placebo, azithromycinshowed advantages in both clinical cure and bacteriological resolution (P < 0. 05, P < 0. 001) . Conclusion Azithromycin eye drops have favorable efficacy, good safety profile and superior earlier effectiveness in treatment of bacterial conjunctivitis, however further RCTs of higher quality are needed to validate it.

Objective To look into effect of health failure mode and effects analysis in reducing the risk of errors in intravenous infusion of inpatients in HIS system.Methods HFMEA was used to assess the procedure of intravenous infusion of inpatients in HIS system,in order to analyze the failure mode and the causes of potential risks.Risk priority number (RPN) was calculated and effective precautionary measures were formulated and implemented.Results After the intervention,the incidence rate of errors in medication had been reduced from 5.13‰ to 1.69‰,and the difference was statistically significant (x2 =208.50,P ＜ 0.01).Conclusions HFMEA is effective in reducing the events of errors in intravenous infusion of inpatients in HIS system,so as to guarantee the safety of the clinical medication of inpatients.