Fifteen novel 5-substituted-2-(pyridyl)benzothiazole compounds were designed and synthesized by simple hydrolization and condensation reaction of the 2-amino-5-substituent benzothiazole. Activities of these synthesized compounds were evaluated on Bcap-37, HCT-15 and HepG2 tumor cells in vitro by standard MTT assay. 5-Fluorouracil (5-FU) was used as the positive control. The results revealed that most of the new compounds had potent effects on Bcap-37, HCT-15 and HepG2 tumor cells, and had no or less effect on 293T and L02 normal cells. Particularly, compounds 1c and 2e exhibited better activities on HCT-15 and HepG2 cells with IC50 values of 41.59 and 38.65 micromol x L(-1), and 1i showed excellent activities on Bcap-37 and HepG2 cells with IC50 values of 46.63 and 23.51 micromol x L(-1), respectively. The structure-activity relationship of 5-substituted-2-(pyridyl)benzothiazole compounds were also discussed preliminarily.

To explore novel coumarin derivatives with more potent anti-proliferative activity, a series of novel compounds were designed and synthesized by linking Schiff base and N, N-bis (2-chloroethyl) amine pharmacophore of nitrogen mustards to the coumarin's framework. Their structures were confirmed by 1H NMR, MS and element analysis techniques. In vitro anti-proliferative activities were evaluated against HepG2, DU145 and MCF7 cell lines by the standard MTT assay. The results showed that some of the target compounds exhibited strong anti-proliferative activities against selected tumor cells, and compounds 7c, 7f, 7g, 7h and 7q were better than or equal to the activities of positive control, they deserved further development.

Twenty-four novel benzothiazole derivatives containing arylpiperazine were designed and synthesized by bioisosterism principle. Anti-proliferative effect of these synthesized compounds against four cancer cell and two normal cell lines were evaluated in vitro by the standard MTT assay. Pharmacological test showed that most of the compounds exhibited potent antitumor activity. Some of the compounds (II2, II3, II6, II7) showed strong anti-proliferation activities against HepG2 and HeLa229 cell lines with the IC 50 values of 1.6-4.5 micromol x L(-1) and 2.5-5.3 micromol x L(-1), respectively, and compounds having cyan in p-substituted benzene ring (I4, I8, I12, II4, II8 and II12) were found to have better antitumor activities against AsPC-1 cell lines with the IC50 values of 5.2-11.3 micromol x L(-1). The structure-activity relationship of benzothiazole derivatives containing arylpiperazine was also discussed preliminarily.

Objective To explore the impact of calciotropic hormones,such as parathyroid hormone (PTH)and vitamin D,on bone mineral density(BMD)in the old men with type 2-Diabetes.Methods Sixty elderly men with type 2-Diabetes were submitted to dual-energy X-ray absorptiometry to evaluate the BMD at lumbar spine and hip.Fasting blood samples were collected to evaluate the indexes of bone metablism and blood glucose.PTH and 25-(OH)-Vitamin D3 were measured and analyzed for their correlation with BMD at different sites.Results In all patients,the percentage of osteoporosis and osteopenia accounted for 20.0％ and 53.3％ of the patients according to BMD at lumbar or hip.Compared with the patient group with normal BMD,serum PTH was significantly higher in the patient group with osteopenia or osteoporsis([44.87 ± 10.62]μg/L vs[36.96 ±12.36]μg/L,P ＜ 0.05 ;[50.24 ± 20.32]μg/L vs[36.96 ± 12.36]μg/L,P ＜ 0.05).But there was no difference in 25-(OH)-Vitamin D3 levels between all groups.PTH was correlated negatively with BMD at hip (r =-0.224,P ＜ 0.05),but not significantly correlated with BMD at lumbar(r =-0.187,P ＞ 0.05)Conclusions Serum PTH was correlated negatively with BMD at hip in elderly man with type 2-Diabetes.

Objective To realize the clinical characteristics of fungemia in premature infants.Methods Clinical characteristics of fungemia in premature infants in the intensive care unit of a children''s hospital between January 2011 and December 2015 were analyzed retrospectively, general condition of premature infants, laboratory-related indicators, and antimicrobial susceptibility testing results were compared.Results From January 2011 to December 2015, 42 premature infants with confirmed fungemia were treated in this hospital, 22 (52.38％) of whom were with fungemia caused by Candida albicans(C.albicans), 13 (30.95％) by Candida parapsilosis (C.parapsilosis), 3 by Candida krusei (C.krusei), and 4 by other fungi.Patients were grouped according to the main pathogens causing infection: C.parapsilosis group and C.albicans group.Maternal genitourinary tract infection rate and incidence of fungal meningitis in C.albicans group were both higher than C.parapsilosis group(27.27％ vs 7.69％, 27.27％ vs 0.00％ respectively), peripherally inserted central catheter (PICC) rate in C.albicans group was lower than that in C.parapsilosis group(22.73％ vs 69.23％), platelet count in C.parapsilosis group was lower than C.albicans group, differences were all statistically significant (all P<0.05).Conclusion The major fungi causing fungemia in premature infants were C.parapsilosis and C.albicans, maternal reproductive system infection during pregnancy can easily lead to candidemia, premature infants with candidemia are more vulnerable to developing fungal meningitis;PICC is more likely to lead to C.parapsilosis fungemia, and platelet decline is more obvious.

Objective To explore the possible risk factors that influence bone mineral density (BMD) in the elderly man with type-2 diabetes.Methods Sixty elderly man with type-2 diabetes were subjected to dual-energy X-ray absorptiometry to evaluate the BMD at lumbar spine ( LS),and femoral neck (FN).Fasting blood and urine samples were taken to check the biochemical levels about bone metablism and blood sugar.The correlations between BMD and other factors were analyzed.Results In this group of patients,the percentage of osteoporosis and osteoponia was 20％ and 53.3％ in LS or FN site,respectively.Age,Weight,and HbA1c were correlated with BMD.Weight of them had the best correlation with BMD at LS( r =0.254,P ＜0.01 ),whereas,HbA1c had the best correlation with BMD at FN( r =-0.224,P ＜0.01 ).Conclusions Age,Weight,and HbAlc c were correlated with BMD of elderly man with type-2 diabetes.

Objective To observe the effect of shock lymph drainage on multiple organ injury of rats with traumatic hemorrhagic shock (THS) and discuss the relating mechanism. Methods Male Wistar rats were divided into control group, lymph drainage group and lymph return group. The THS model was established in lymph drainage group and lymph return group, when the shock mesenteric lymph was drained in lymph drainage group. The change of the mean arterial pressure ( MAP), the biochemical indices of liver, kidney, myocardium and acid-base, the morphology, ATP contents and ATPase activities of lung, kidney, liver and myocardium were observed. Results The MAP at multiple time points after 80 minutes of infusion, the ATP contents and ATPase activities of multiple organs in lymph drainage group were higher than those in lymph return group. Multiple biochemical indices in lymph drainage group were superior to those in lymph return group, with statistical difference. The inflammation, congestion, degeneration and necrosis were found in organs of lymph return group, but only mild lesions could be seen in lymph drainage group. Conclusions The shock lymph drainage can alleviate multiple organ injury of THS rats, mechanism of which is correlated with improvement of the energy metabolism and maintenance of MAP and acid-base status.

Objective To explore the value of prenatal echocardiography in diagnosis of fetal ventricular septal defect (VSD).Methods Prenatal echocardiography was performed on 3 826 fetuses,and the results were compared with those of postnatal echocardiography or autopsy findings.The diagnostic accuracy,misdiagnosis rate and missed diagnosis rate of prenatal echocardiography for VSD were calculated.Results Among 3 826 fetuses,VSD was found in 61 fetuses (61/3 826,1.59％) with prenatal echocardiography,including simple VSD in 36 fetuses (36/3 826,0.94％) and VSD complicated with other heart malformations in 25 fetuses (25/3 826,0.65 ％).According to the results of autopsy and postnatal echocardiography,the final diagnosis of VSD was found in 76 cases (76/3 826,1.99％),of which simple VSD was found in 51 cases (51/3 826,1.33 ％),VSD complicated with other heart malformations were found in 25 fetuses (25/3 826,0.65％).The diagnostic accuracy,missed diagnosis rate and misdiagnosis rate of simple VSD with prenatal echocardiography was 58.82％ (30/51),41.18％ (21/51) and 1.06‰ (4/3 775),respectively.The diagnostic accuracy,missed diagnosis rate and misdiagnosis rate of VSD complicated with other heart malformations with prenatal echocardiography was 96.00％ (24/25),4.00％ (1/25) and 0.26‰ (1/3 801),respectively.Conclusion Echocardiography has important clinical value in prenatal diagnosis of fetal VSD,which can provide important references for treatment plan and prognosis evaluation.

Objective To study the transport risk and factors that influence deaths of very low birth weight (VLBW) and extremely low birth weight (ELBW) infants.Method All infants transferred to our neonatal intensive care unit (NICU) by our hospital transport team or local hospital transport team from January 2014 to December 2015 were included in our study.Their clinical data were retrospectively studied.The risks of transport between hospitals were analyzed.The risk factors of deaths within and after 7 days of admission were further analyzed by multivariate Logistic regression analysis.The receiver operation characteristic (ROC) curve was used to assess the sensitivity and specificity of mortality index for neonatal transportation (MINT),transport related mortality score (TREMS),transport risk index of physiologic stability (TRIPS) for predicting mortality of preterm infants.Result (1) A total of 527 cases of ELBW/VLBW infants were included in our study.There were no deaths during transport.There were 10.2％ (54/527) died within and 8.9％ (42/473) died after 7 days of hospitalization.(2) Multivariate Logistic regression analysis showed that scleredema of newborn,secondary transport,gastrointestinal malformations,metabolic acidosis,high TREMS score,and high MINT score were risk factors of mortality within 7 days of admission for ELBW/VLBW infants;necrotizing enterocolitis,intraventricular hemorrhage ≥ three degree,high MINT score and low admission weight were risk factors of mortality after 7 days of admission.(3) The area under the ROC curve for MINT,TREMS,and TRIPS score were 0.672,0.655 and 0.665,respectively.The cut-off values for MINT score (cut-off 8,sensitivity 0.444,specificity 0.829),for TREMS score (cut-off 2,sensitivity 0.500,specificity 0.757,for TRIPS score (cut-off 20,sensitivity 0.444,specificity O.829) were selected to predict mortality within 7 days of admission.Conclusion (1) Secondary transport is the transport-related risk factor of mortality within 7 days of admission for ELBW/VLBW infants.(2) High MINT score is the risk factor of mortality within and after 7 days of admission.(3) If MINT ≥ 8,TREMS ≥2,or TRIPS ≥20,it might significantly increase the risk of mortality of ELBW/ VLBW infants within 7 days of admission after transport.

Objective To study the occurrence of bronchopulmonary dysplasia (BPD) in extremely low birth weight (ELBW) infants and to determine the risk factors of severe BPD.Method From January 2007 to January 2017,ELBW infants admitted to neonatal intensive care unit (NICU) in Hunan Children's Hospital were retrospectively analyzed.They were assigned into severe and mild/moderate groups based on the severity of BPD.The general condition,maternal status,prenatal and delivery room treatment,transportation,clinical courses,therapy and outcome in NICU of the two groups were compared,and the risk factors of severe BPD were analyzed.Result A total of 367 cases were hospitalized during the 10 years.281 ELBW infants with complete medical records survived longer than 28 days were enrolled in this study.Among them,233 had BPD.Among BPD infants,116 cases were in the severe BPD group,47 cases (40.5％) died.117 cases were in the mild/moderate BPD group and 1 case (0.9％) died.The difference between the two groups was statistically significant (P ＜ 0.05).Multivariate Logistic regression analysis showed that the risk factors of severe BPD were duration of mechanical ventilation ≥ 7 days (OR =7.518,95 ％ CI 3.197 ～ 17.676),ventilator-associated pneumonia (OR =3.047,95 ％ CI 1.436 ～ 6.464),1 min Apgar score ≤7 (OR =2.341,95 ％ CI 1.142 ～ 4.796) and patent ductus arteriosus (OR =2.223,95 ％ CI 1.079 ～4.582).Conclusion The incidence and mortality of BPD,especially severe BPD,are high in ELBW infants.Avoiding asphyxia,shortening the time of mechanical ventilation,preventing infection and closing ductus arteriosus are important measures to reduce the severity of BPD.