Objective To investigate the prognositic factors of small intestine stromal tumors after radical resection.Methods The clinicopathological data of 41 patients with small intestine stromal tumors admitted between January 2005 and December 2010 in Henan Tumor Hospital were analyzed restrospectively.Kaplan-Meier survival rate and COX regression were used to evaluate the prognostic factors.Results There were 22 males and 19 females.The age ranged from 22 to 78 years old (median,55years).Location of tumor included duodenum (n =12),jejunum and ileum (n =29).The 3-year survival rate was 22％ in those 16 cases who reported preoperative gastrointestinal bleeding and 65％ in those without GIT bleeding,the difference was statistically significant (P =0.0012).COX model showed that tumor size,the tumor location,recurrence and metastasis were independent risk factors associated with the prognosis in small intestine stromal patients (P ＜ 0.05).Conclusions The most common clinical presentation of these tumors was gastrointestinal bleeding.The tumor location,recurrence and metastasis and gastrointestinal bleeding was independent risk factors associated with the prognosis of small intestine stromal tumor patients.

Objective Monitoring the thyroid hormone levels in patients before and after renal transplantation to realize the relationship between thyroid hormones and renal function.Methods Fifty-seven patients were subdivided into stabled graft function group (50 cases) and delayed graft function (DGF) group (7 cases).Thirty healthy men served as control group.Serum triiodothyronine (T3),thyroxine (T4),thyroid-stimulating hormone (TSH) and serum creatinine (Scr) were determined respectably before transplantation and on different days after transplantation.Correlations between thyroid hormones and Scr at 10th day after transplantation were analyzed.Results Serum T3 and T4 levels before transplantation in the two groups were significantly lower than those in the control group (P＜0.01).These four parameters levels had no significant difference between stabled graft function group and DGF group (P＞0.05).In stabled graft function group:T3 level was decreased obviously by 30％ in the 1st day after transplantation,which was higher than the others,elevated at the 1st week post-transplantation,reached the normal range.at the 2nd week post-operation,and higher than pre-transplantation (P ＜ 0.01) at 3rd week; T4 revealed a decrease trend after transplantation and was elevated at 10th day post-transplantation,returned to the pre-transplantation level at 3rd week; TSH had slight decrease after operation,and had no significant difference among every period in comparing with pre-transplantation; Scr revealed a decrease trend continuously and returned to the normal level at the 7th day post-transplantation.In DGF group,Hormones levels were obviously decreased as compared with stabled graft function group; T3 reached the normal range at the 3rd week post-transplantation,whereas T4 returned to pre-transplantation levels at the 30th day; TSH had a significant decrease at the 5th day,and began to increase at the 10th day post-operation; Scr retuned to the normal range at the 30th day post-operation.The correlation coefficients between Scr and T3,T4 were 0.546 and 0.423 respectively.Conclusion There is a significant correlation between thyroid hormones and renal function (T3,T4).Monitoring the thyroid hormones,specially T3,can diagnose renal function change.

To discover novel fluoroquinolone lead compounds as possible anti-infective or/and antitumor chemotherapies, combination principle of pharmacophore-based drug design, a series of novel tricyclic fluoroquinolone title compounds, [1,2,4]triazino[3,4-h][1,8]naphthyridine-8-one-7-carboxylic acid derivatives ( 5a-5p), were designed and synthesized with a fused [1,2,4]-triazine ring unit. Their structures were characterized by spectral data and elemental analysis and the in vitro antibacterial and anti-cell proliferation activities were also evaluated. The results showed that the titled compounds exhibited more significant inhibitory activities against drug-resistant bacteria (Methicillin-resistant Staphylococcus aureus and multi drug-resistant Escherichia coli strains) and three tested cancer cell lines (human hepatoma SMMC-7721, murine leukemia L1210 and human murine leukemia HL60 cells). Interestingly, SAR showed that compounds with electron-donating groups attached to benzene ring had stronger antibacterial activity than antitumor activity, but electron-withdrawing compounds displayed more potential antitumor activity than antibacterial activity, especially antitumor activity of nitro compounds was comparable to comparison doxorubicin. Thus, novel triazine-fused tricyclic fluoroquinolones as potent anti-infective or/and antitumor lead compounds are valuable to pay attention and for further development.
Animals ; Anti-Bacterial Agents ; chemical synthesis ; chemistry ; Antineoplastic Agents ; chemical synthesis ; chemistry ; Carboxylic Acids ; Carcinoma, Hepatocellular ; Cell Line ; Cell Proliferation ; Drug Design ; Escherichia coli ; drug effects ; Fluoroquinolones ; chemical synthesis ; chemistry ; HL-60 Cells ; Humans ; Leukemia L1210 ; Liver Neoplasms ; Methicillin-Resistant Staphylococcus aureus ; drug effects ; Mice ; Naphthyridines ; Triazines

To explore an efficient strategy for the conversion of antibacterial fluoroquinolones into antitumor fluoroquinolones, an azole heterocyclic ring of oxadiazole instead of the C-3 carboxylic acid group with a functionalized hydrazone group as a modified side-chain, fifteen novel 2-(fluoroquinolon-3-yl)-oxadiazole-5- sulfanylacetylhydrazone derivatives 7a-7o were designed and synthesized on the basis of the pharmacophore hybridization principle from pefloxacin, separately. The structures for fifteen title compounds were characterized by elemental analysis, 1H NMR and MS, and their in vitro antitumor activity against Hep-3B cell line was evaluated by a MTT assay. The results showed that the title compounds exhibited more significantly inhibitory activity than that of the parent pefloxacin, in which compounds with electron-withdrawing group attached on aryl ring had more potency than that of compounds with electron donating group, especially compounds with a carboxylic substituent were comparable to comparison doxorubicin. It suggests that it is favorable for an improvement of antitumor activity to remain a carboxylic acid unit at the aromatic ring.
Antineoplastic Agents ; chemical synthesis ; chemistry ; Cell Line, Tumor ; Fluoroquinolones ; chemistry ; Humans ; Oxadiazoles ; chemistry ; Structure-Activity Relationship

OBJECTIVETo investigate midterm follow-up results on Asian femoral intramedullary nail in treating segmental and comminuted femoral fractures.

METHODSBetween June 2011 and October 2012,16 patients with segmental and comminuted femoral fractures were treated with minimally invasive reset and Asian femoral intramedullary nail under extension table. Among them, there were 10 males and 6 females aged from 21 to 49 years old with an average of 34.5 years old; the time from injury to operation ranged from 3 to 24 d with an average of 9.1 d. There were 6 cases were type C1,2 cases were type C2 and 8 cases were type C3 according to AO classification. X-ray of femoral segment at 3,6 and 12 months after operation were applied for evaluating fracture healing. Harris score of hip joint and HSS score of knee joint were used to evaluate postoperative function.

RESULTSAll patients were followed up from 24 to 36 months with an average of 28.4 months. Operative time was from 88 to 112 min with an average of 90.7 min; blood loss ranged from 150 to 200 ml with an average of 188.75 ml; the time of fracture healing was from 5 to 9 months with an average of 5.4 months. All incision were healed at stage I. No loosening, breakage of internal fixation and displacement of fracture were occurred. There were no significant differences in Harris score of hip joint at 3, 6 and 12 months after operation (F = 0.07, P = 0.893 > 0.05), 10 cases obtained excellent results, 5 good and 1 moderate. There was no obvious meaning in HSS score of knee joint (F = 0.08,P = 0.876 > 0.05), 9 cases obtained excellent results, 6 good and 1 poor.

CONCLUSIONAsian femoral intramedullary nail could treat segmental and comminuted femoral fractures by using variety of less invasive ways,which has advantages of less trauma, quick recovery of function and satisfied midterm following-up results. But long term following-up effects remains to be seen.

Adult ; Bone Nails ; Female ; Femoral Fractures ; surgery ; Femur ; injuries ; surgery ; Follow-Up Studies ; Fracture Fixation, Intramedullary ; Fractures, Comminuted ; surgery ; Humans ; Male ; Middle Aged ; Treatment Outcome ; Young Adult

To discover an efficient strategy for the conversion of the antibacterial activity of fluoroquinolones into the antitumor activity, the three series of C-3 s-triazole-based derivatives including sulfide ketones (6a-6g), thiosemicarbazones (7a-7g) and fused heterocyclic thiazolotriazoles (8a-8g) were synthesized from ciprofloxacin (1), respectively. The structures were characterized by elemental analysis and spectral data. The antitumor activity was tested against three tumor cell lines (Hep-3B, Capan-1 and HL60) using the MTT assay. The three types of compounds all exhibited stronger anti-proliferative activities than ciprofloxacin in the test. The order of their activities was in compounds 7>8>6, and the order of selectivity against cancer cell lines was Capan-1, Hep-3B and HL60. Meanwhile, the SAR revealed that some compounds with electron-drawing group substituted such as fluoro- and nitro-phenyl compounds (6f, 7f, 8f) and (6g, 7g, 8g) displayed more significant activity than the control compounds, especially the IC50 values of thiosemicarbazone compounds 7f and 7g against Capan-1 was comparable to doxorubicin. Thus, a five-membered triazole as the C-3 bioisostere modified with the functionalized side-chain of sulfide-ketone thiosemicarbazone warrants special attention and further investigation.

To search for fluoroquinolones(FQs)with antitumor activity;the C-3 carboxylic acid group of peflox-acin (1)was replaced by fused heterocyclic core;and twelve novel thiazolo[3;2-b][1;2;4]triazole heterocycles(6a-6l)were designed and synthesized.The structures of target compounds were characterized by elemental anal-ysis and spectral data.The results of the in vitro antiproliferative effect on SMMC-7721;L1210 and HL60 cell lines showed that the title compounds exhibited more significant antitumor activity than both of the pefloxacin and the corresponding opening-ring intermediates(5 a-5 l).Among them;the target compounds which possess a ben-zene ring bearing a hydroxyl group (6e)or a fluorine atom (6j)exhibited more potent antiproliferative effect on SMMC-7721 cells than other compounds.Therefore;the antitumor fluoroquinolones can be designed by replacing the C-3 carboxylic acid group of fluoroquinolones with the thiazolo[3;2-b][1;2;4]triazole moiety.

To discover novel antitumor rhodanine unsaturated ketones, a series of fluoroquinolone (rhodanine α, β-unsaturated ketone) amine derivatives (5a-5r) were designed and synthesized with fluoroquinolone amide scaffold as a carrier. The structures of eighteen title compounds were characterized by elemental analysis, 1H NMR and MS. The in vitro anti-proliferative activity against Hep-3B, Capan-1 and HL60 cells was evaluated by MTT assay. The results showed that the title compounds not only had more significant anti-proliferative activity against three tested cancer cell lines than that of the parent ciprofloxacin 1, but also exhibited the highest activity against Capan-1 cells. The SAR revealed that some compounds carrying aromatic heterocyclic rings or phenyl attached to an electron-withdrawing carboxyl or sulfonamide substituent were comparable to or better than comparison doxorubicin against Capan-1 cells. As such, it suggests that fluoroquinolone (rhodanine α, β-unsaturated ketone) amines are promising leads for the development of novel antitumor fluoroquinolones or rhodanine analogues.

Objective To investigate the association between catechol-O-methyltransferase (COMT) Val158Met polymorphism and the memery function of schizophrenia treated with Aripiprazole.Methods Schizophrenic patients were diagnosed in according to Diagnostic and Statistical Manual of Mental Disorders-IV (DSM-IV).A total of 78 Chinese Han subjects were involved in this study.The polymerase chain reaction-restriction fragment length polymorphism(PCR-RFLP) was used to identify COMT genotypes.The Chinese revised version of Wechsler Memory Scale (WMS-RC) was used twice to evaluate the memory function of patients treated with Aripiprazole alone before and after drug treatment for 8 weeks.ANOVA,rank sum test and t-test were used to statistical analysis.Results There was statistical difference of cumulative memory among the three groups (F=12.371,P=0.002),and Met/Met genotype showed much poorer cumulative memory than Val/Met and Val/Val genotypes (Z=-3.168,-2.641 ; P=0.002,0.008,respectively) Memory function was significantly improved after patients been treated with Aripiprazole except the associative memory(P＜0.05).Met/Met genotype showed more improvement of cumulative memory than other genotypes after Aripiprazole treatment (t=4.203,P＜0.01 ; t=3.024,P ＜0.01,respectively).Conclusions There may be a relationship between COMT Val158Met polymorphism and the memory function of schizophrenia in Aripiprazole treatment.Met/Met genotype of schizophrenia showed worst cumulative memory but best responsiveness in Aripiprazole treatment.

Background lnterleuldn-18(IL- 18) plays a key role in the development,progression and outcome of coronary artery disease and its complications.However,its variability relation to the characterization of atherosclerotic plaque and percutaneous coronary intervention are still unknown.Methods Fifty four patients with coronary artery disease [22 patients with stable angina (SA) and 32 patients with acute coronary syndrome (ACS)] were enrolled in this study.All patients underwent percutaneous coronary intervention (PCI).The stability of the plaques at the criminal vessels was assessed with analogical IVUS.Serum IL-18 levels were measured at the time points of 5 rain before PCI,and Oh,6h,24h and lmonth after PCI in all patients.Results ACS group consisted mainly of lipidic unstable plaques while SA group of fibrous stable plaques.Moreover,compared with those in SA group,eccentricity index (EI) and remodeling index (RI) were significantly higher in ACS group.Positive remodeling was seen in ACS group while negative or no remodeling in SA group.Further,serum IL-18 levels were significantly elevated in patients with ACS than those in SA group before PCI,increased at Oh,6h,24h after PCI (P＜0.05)and were not significant different at 1 month after PCI from those before PCI.Conclusions There is significant difference in the composition and structural characteristics of atherosclerotic plaques between ACS and UA groups.PCI triggersd and enhances the inflammatory response in a short time.Serum levels of IL- 18 are the predictors of progression of unstable plaque in atherosclerosis.Post-operative complications of PCI might be reduced by inhibiting IL- 18.(J Geriatr Cardiol 2008;5:21-24)