AIMTo study the synthesis and antibacterial activity of pyridonecarboxylic acid derivatives containing 2-methyl-5-nitroimidazol.

METHODSPyridonecarboxylic acid derivatives containing 2-methyl-5-nitroimidazol were synthesized primarily from 2-methyl-5-nitroimidazol, norfloxacin, ciprofloxacin, enoxacin via nucleophilic substitution and esterification. The antibacterial activity of the nine target compounds were tested.

RESULTSNine new compounds were synthesized (IIa-c and IIIa-f). The structure of the title compounds were identified by 1HNMR, MS as well as elementary analysis.

CONCLUSIONCompounds IIa, IIb and IIc showed antibacterial activity, and were worth further studying.

Animals ; Anti-Infective Agents ; chemical synthesis ; chemistry ; pharmacology ; Ciprofloxacin ; antagonists & inhibitors ; chemical synthesis ; pharmacology ; Combinatorial Chemistry Techniques ; methods ; Enoxacin ; antagonists & inhibitors ; chemical synthesis ; pharmacology ; Escherichia coli ; drug effects ; Female ; Mice ; Microbial Sensitivity Tests ; Molecular Structure ; Nitroimidazoles ; chemistry ; Norfloxacin ; antagonists & inhibitors ; chemical synthesis ; pharmacology

Objective The aim of this study is to investigate the role of angiotensin-converting enzyme (ACE)gene susceptibility to systemic lupus erythematosus(SLE)by familial studies.Methods PCR-based re- striction fragment length polymorphism(RFLP)was applied to genotype single nucleotide polymorphism(SNP) G261T of the ACE gene.A total of 119 patients with SLE from 119 families were recruited.In addition,316 family members of these patients were also genotyped.A family-based association study was carried out to ex- plore the association between gene polymorphism and SLE.We studied the SNP encoding non-synonymous substitution in the ACE gene with respect to genetic susceptibility to SLE.Results Among 119 SLE patients. the frequency of ACEG261TG,T alleles was 44.8%.55.2% respectively,the frequency of ACEG261T GG,GT and TT genotypes was 13.9%,62.0%,24.1% respectively,Univariate(single-marker)family-based association test(FBAT)demonstrated that variant alleles at the SNP,rs4303,exon 5 of ACE gene were significantly asso- ciated with genetic susceptibility to SLE in Additive Model(Z=2.877,P=0.004),Dominant Model(Z=2.557, P=0.011).Recessive Model(Z=2.202,P=0.028).Transmission-disequilibrium test(TDT)and sib transmission -disequilibrium test(STDT)showed an excess of the allele of T from heterozygous parents to affected offspring or higher frequency of the allele of T in the patients than their normal siblings(X~2=11.66,P=0.001).Conclu- sion Our findings suggest that the ACE gene may he the susceptible gene to SLE in Chinese population,and the individuals carrying ACE-261T allele is significantly associated with susceptibility to SLE.

AIMTo study the synthesis and antibacterial activity of ciprofloxacin derivatives.

METHODSCiprofloxacin derivatives were synthesized primarily from 2-methyl-5-nitroimidazol and ciprofloxacin through nucleophilic substitution. The antibacterial activity of the synthesized compounds were tested.

RESULTSNine new compounds were synthesized. The structure of the title compounds were confirmed by 1H NMR, MS and element analysis.

CONCLUSIONCompounds II, IVC and IVD showed appreciable antibacterial activity, and were worth further studying.

Animals ; Anti-Infective Agents ; chemical synthesis ; chemistry ; pharmacology ; Ciprofloxacin ; analogs & derivatives ; chemical synthesis ; chemistry ; pharmacology ; Escherichia coli ; drug effects ; Female ; Mice ; Molecular Structure ; Nitroimidazoles

OBJECTIVETo develop a rapid test kit for antibody to HIV by nano immunomagnetic lateral flow method.

METHODSA rapid test kit was developed by conjugation of the HIV antigen gp41 and gp36 to 200nm super paramagnetic particles by carbodiimide (EDC) and coating of the HIV antigen gp41 and gp36 to nitrocellulose membrane. Then the kit was evaluated with serials of experiments.

RESULTSThe kit was qualified with examination of national reference panel of anti-HIV antibody for colloidal gold diagnostic kit. The sensitivity was 100% by tested with 20 HIV antibody positive sera, the specificity was 98.5% by tested with 600 HIV antibody negative sera, respectively. The stability of the kit was over 12 month by storage at room temperature.

CONCLUSIONA diagnostic kit for antibody to HIV was developed with the advantages of convenience, rapid test, good stability and point of care.

Antibodies, Anti-Idiotypic ; immunology ; Gold Colloid ; chemistry ; HIV ; immunology ; isolation & purification ; HIV Antibodies ; HIV Envelope Protein gp41 ; HIV Infections ; diagnosis ; HIV Seropositivity ; blood ; HIV-1 ; immunology ; isolation & purification ; Immunomagnetic Separation ; methods ; Molecular Biology ; methods ; Nanotechnology ; Reagent Kits, Diagnostic

OBJECTIVETo evaluate the value of deep small-bowel endoscopy (DSBE) in the diagnosis of Crohns disease (CD).

METHODSThe endoscopic and clinical data of 54 patients with CD receiving capsule endoscopy (CE) and double-balloon enteroscopy (DBE) between January, 2004 and December, 2008 were summarized and analyzed retrospectively.

RESULTSThe main indications for DSBE in our series were suspected CD (42.6%) and obscure gastrointestinal bleeding (25.9%). DSBE was obviously superior to barium imaging. The detection rate of CD was significantly higher with DSBE (92.6%) than with ileocolonoscopy (75.9%, P=0.017), and DSBE provides much more detailed descriptions of specific endoscopic features such as segmental distribution and lumen changes. DSBE significantly improve the diagnostic efficiency, giving priority to offer a guide and raise suspected diagnosis for CD.

CONCLUSIONDSBE is a valuable modality for detecting CD lesions in the jejunum and ileum and for evaluating lesion involvement and severity. The combination with a comprehensive analysis of routine imaging findings, gastro endoscopy, and clinical data can further enhance the diagnostic efficiency of DSBE.

Adolescent ; Adult ; Capsule Endoscopy ; Crohn Disease ; diagnosis ; pathology ; Double-Balloon Enteroscopy ; Female ; Humans ; Intestine, Small ; pathology ; Male ; Retrospective Studies ; Young Adult

AIMTo study the chemical constituents of the stems and leaves of Aconitum coreanum (Lèvl.) Rapaics.

METHODSThe constituents of Aconitum coreanum were isolated by using various kinds of modern chromatographic methods. The new alkaloid was identified on the basis of spectral analysis.

RESULTSTwo compounds were isolated and identified as: 13-dehydro-1beta-acetyl-2alpha,6beta-dihydroxyhetisine (I) and Guanfu base G (II).

CONCLUSIONCompound I is a new alkaloid.

Aconitum ; chemistry ; Diterpenes ; Heterocyclic Compounds, Bridged-Ring ; chemistry ; isolation & purification ; Molecular Conformation ; Molecular Structure ; Plant Leaves ; chemistry ; Plant Stems ; chemistry ; Plants, Medicinal ; chemistry

OBJECTIVETo investigate the role of FCGR3A gene in susceptibility to systemic lupus erythematosus (SLE) using family based studies.

METHODSA total of 119 patients from 95 nuclear families, with SLE according to the American College of Rheumatology 1997 criteria were recruited. In addition, 316 family members of these patients were also genotyped. A family-based association study was used to explore the association between gene polymorphism and SLE. The authors studied the single nucleotide polymorphisms (SNP) encoding non-synonymous substitution in the cFCGR3A gene with respect to genetic susceptibility to SLE. The FCGR3A gene was genotyped with RFLP.

RESULTSAmong 119 SLE patients, the frequency of FCGR3A-72R/S, R and S allele were 39.4% and 60.6%; the frequency of FCGR3A R/S RR, RS and SS genotypes were 9.1%, 60.6% and 30.3%, respectively. Univariate (single marker) family-based association tests (FBATs) demonstrated that variant allele at the SNP(rs403016) in exon 3 of FCGR3A gene was significantly associated with genetic susceptibility to SLE in Additive Model(Z=2.544, P =0.01097) and Recessive Model(Z = 2.198, P = 0.02795). TDT analysis showed an excess of the allele of R from heterozygous parents to affected offspring (chi square was 9.30, P=0.0032).

CONCLUSIONThe findings suggest that the FCGR3A gene may be the susceptible gene of SLE in Chinese population, and that the individual carrying FCGR3A 72R allele was significantly associated with increase of susceptibility to SLE.

Adult ; Family ; Female ; Genetic Predisposition to Disease ; Genome-Wide Association Study ; Genotype ; Humans ; Lupus Erythematosus, Systemic ; genetics ; Male ; Polymorphism, Single Nucleotide ; Receptors, IgG ; genetics

Objectve: To investigate the feasibility of establishing xenografted leukemia model by zebrafish, so as to provide the more direct model in vitro and experimental evidence for study of acute myeloid leukemia and screening of the drugs for targeting therapy.

METHODSAcute myeloid leukemia cell line KG-1a was labeled with red fluorescent dye-MitoRed, then the labeled cells were injected into the yolk sac of zebrafish embryos. Morphological observation, cell count and histopathological detection were used to analyse the infiltration and metastasis of KG-1a cells in zebrafish.

RESULTSKG1a cells could proliferate and gradually spread to the entire abdominal cavity of the zebrafish after KG-1a cells were injected into the yolk sac during 1-7, the results of cell counting in vitro also proved a significant proliferation of KG-1a cells in zebrafish, suggesting that the implanted leukemia stem cells could survive, proliferate and spread in zebrafish. Further study showed that the implanted cells could be transfered to the liver of zebrafish, these cells displayed the signature of KG-1a cells by hematoxylin-eosin(HE) staining.

CONCLUSIONSHuman acute myeloid leukemia cells KG1a can survive, proliferate and migrate in zebrafish, suggesting xenografted leukemia model of zebrafish has been successfully established. This model may be benefitcial for the study of acute myeloid leukemia and the screening of the drugs for targeting therapy of acute myeloid leukemia.

During the treatment of non-small cell lung cancer ( NSCLC) , many patients have developed drug resistance due to the use of targeted EGFR inhibitors. The main reasons for drug resistance are EGFR site mutations and bypass activation. Activation of ALK pathway is one of the major types of bypass activation. A recent authoritative study indicates that ALK is closely related to immunotherapy. This article reviews the treatment of ALK in tumors from three aspects: the structure and physiological function of ALK, the small molecule inhibitor of ALK, the biological function of ALK and its related treatment methods for NSCLC, and prospects future directions for better application of ALK in the treatment of NSCLC.