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A novel series of bis-nicotine derivatives (3a-3i) were designed, synthesized and evaluated as bivalent anti-Alzheimer's disease agents. The pharmacological results indicated that compounds 3e-3i inhibited both acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) in the micromolar range (IC50, 2.28-117.86 micromol x L(-1) for AChE and 1.67-125 micromol x L(-1) for BChE), which was at the same potency as rivastigmine. A Lineweaver-Burk plot and molecular modeling study showed that these derivatives targeted both the catalytic active site (CAS) and the peripheral anionic site (PAS) of AChE. Besides, these compounds could significantly inhibit the self-induced Abeta aggregation with inhibition activity (11.85%-62.14%) at the concentration of 20 micromol x L(-1).

Adolescent ; Anal Canal ; physiopathology ; Child ; Constipation ; physiopathology ; Female ; Gastrointestinal Motility ; physiology ; Humans ; Male ; Rectum ; physiopathology

Aim To explore the protective effect of Sertoli cells on the co-transplanted allogeneic renal cells in male and female recipient rats. Methods Testicular Sertoli cells were prepared by digestion with trypsin， collagenase and DNase， while renal cells were prepared by digestion with trypsin alone. FasL and Fas expressions were detected respectively by FCM before transplantation. About 106 cells were injected into the allogeneic renal subcapsule. In order to demonstrate the survival of renal cells， the expression of g-PG in graft was examined by SABC method. Apoptosis of the lymphocytes surrounding the graft was observed by TUNEL(terminal deoxynucleotidyl transferase-mediated X-dUTP nick end labeling). Results The grafts were analyzed histologically 20 days after transplantation. The renal cells transplanted alone were all rejected, while the survival rates of the mixed cell transplantation were 87.5％ and 77.8％ in male and female recipients respectively. When the renal cells co-transplanted with Sertoli cells treated by anti-FasL mAb， only 30.0％ grafts were survived. Apoptosis of lymphocytes surrounding the graft were quite evident. Conclusion Sertoli cells expressing FasL can protect renal cells from allograft rejection by inducing apoptosis of Fas expressing T cells surrounding the grafts.

Objective:To investigate frequencies of microsatellite instability(MSI)and loss of heterozygosity(LOH)in renal ceil carcinoma(RCC),and to discuss the relationship of clinicopathological characteristics of RCC with MSI and LOH. Methods:Twelve microsatellite markers located at chromosomes 3p,9p and 14q were selected to investigate microsatellite alterations(MSI and LOH)in 31 RCC specimens and their paired metastasis specimens by polymerase chain reaction- polyacrylamide gel elect rophoresis-ethylene dibromide(PCR-PAGE-EB)staining and sequencing.Results:The frequency of MSI could reached 61.3% and that of LOH could reach 54.8%.The highest frequency of MSI was at locus of D9S168(32.3%);the highest frequency of LOH was at locus of D3S1289(21.4%).No correlation was found between MSI or LOH and the patients' age,sex,pathology type and metastastis,except that MSI was correlated with TNM stage of RCC(P

Abstract: Objective　A survey on the plague foci in Qiaojia County of Jinsha River Basin was conducted to understand the composition of plague host vectors and the prevalence of plague among animals, to explore the occurrence and epidemic risk of plague, and to provide scientific basis for plague monitoring and control in this area. Methods　Seven villages and towns in Qiaojia County were selected as the research areas, and the cage night method and the clamp line method were used to investigate the small mammals and their surface parasitic fleas. The host animal organs, serum and surface parasitic flea's samples were collected. The plague indicator animal serum was collected simultaneously on the spot, and the collected host animal organs and flea's samples were cultured and detected for Yersinia pestis. The indirect hemagglutination test (IHA) was used to detect the fraction 1 capsular antigen (F1) antibody of the host animal and the indicator animal serum samples. Results　A total of 525 small mammals belonging to 3 orders, 6 families, 12 genera and 23 species were captured. The dominant species in farming areas were Apodemus chevrieri (31.05%), Niviventer confucianus (13.90%) and Anourosorex squamipes Milne-Edwards (11.43%). The dominant species in residential areas were Rattus norvegicus (66.67%) and Rattus tanezumi (20.00%). The rat densities in agricultural and residential areas were 20.98% and 1.00%, respectively. A total of 277 external parasitic fleas belonging to 15 species, 13 genera, 5 families were collected. The dominant species were Palaeopsylla remota (22.02%), Neopsylla specialis specialis (20.58%), Frontopsylla diqingensis (18.77%) and Ctenophthalmus (Sinoctenophthalmus) quadratus (11.55%), and the rat fleas index was 0.53. No Yersinia pestis was isolated from all rodent organs and flea samples. A total of 167 serum samples from dogs and 15 serum samples from rats were collected, and plague F1 antibody was detected by IHA. IHA detection of plague F1 antibody were negative. Conclusions　Qiaojia County has the distribution of the main host and main vector of plague, and the rat density is high, but the rat body flea index is low. There is no positive detection of plague host animals, vector fleas and indicator animals. It can be considered that the risk of plague occurrence and epidemic in the region is not high in the near future. It is necessary to further strengthen the monitoring and control of plague and other rodent-borne diseases in the region.

Objective To evaluate the chnical features and prognosis of traumatic benign paroxysmal positional vertigo (t-BPPV).Methods By retrospectively analyzing the results of clinical features and prognosis in 19 patients with t-BPPV from January 2003 to September 2006,the results were compared with 51 patients with idiopathic benign paroxysmal positional vertigo (i-BPPV).Results The mean ages were (51.3?19.1) years in t-BPPV group and (63.2?16.5) years in i-BPPV group,the difference was significant (t=2.57,P0.05).The one-stage success rates were 62.5% in t-BPPV group and 83.6% in i-BPPV group,the difference was significant (x~2=4.94,P

Objective To study the expression and significance of Ezrin in triple negative breast cancer tissues .Methods We selected 102 cases ,including 24 ones of triple negative breast cancer ,58 ones of non‐triple negative breast cancer ,and 20 of benign breast disease .The expression of Ezrin in all the specimens was detected by SP immunohistochemistry .We observed whether there was any difference between the positive expression rates of Ezrin in the three groups . We also analyzed the correlation between Ezrin expression and clinicopathologic parameters of triple negative breast cancer .Results The positive expression rate of Ezrin in groups of triple negative breast cancer , non‐triple negative breast cancer , and benign breast disease was 15 .00% ,48 .28% and 75 .00% ,respectively . The difference between the three groups differed significantly ( P < 0 .01 ) . The high expression of Ezrin in triple negative breast cancer had relationship with histological grading and clinical TNM staging (P< 0 .05 ) , but not with patients' age , tumor size , or axillary lymph node metastasis ( P > 0 .05 ) . Conclusion Ezrin is highly expressed in triple negative breast cancer tissues ;therefore , it can be used as an important indicator of poor prognosis of triple negative breast cancer .

Objective To investigate and report a group of patients with cutaneous nocardiosis occurring in China.Methods The skin lesion of twenty-three patients were examined and the pathogen was identified.The possible cause of this disease was also investigated.Results All the twenty-three patients belon g to a same village in a province.Skin lesions on buttoc ks manifested as nodules and abscesses whereas some other lesions as ulcers and draining sinuses,occurring 2-10mo nths after intramuscular injection.The pathogens were identified as Nocardia asteroides.Conclusion Twenty-three patients of cutaneous nocardiosis were related to intramu scular injection.

Objective To observe the effect of CO2 pneumoperitoneum combined with position changes on the stability of cardiac electrophysiology in gynecological laparoscopy. Methods The gynecological laparoscopy was performed for 30 patients to undergo elective gynecological laparoscopy under general anesthesia ,with the pneumoperitoneum pressure of 12 mmHg and the Trendelenburg positionat 15° . The observations and analyses were done over the basic monitoring index and the QT interval (QT),T peak tend interval (Tp-e),heart rate corrected QT interval(QTc),QT dispersion(QTd),Tp-e/QT before anesthesia(T0),after anesthesia(T1),1 min after pneumoperitoneum (T2),30 min after pneumoperitoneum and head-down tilt (T3),30 min after deflation and supine position(T4). Results Compared with the time point of T0,QTd increased significantly at T1(P<0.05) and so it was with QT,QTc,QTd,Tp-e,Tp-e/QT at T2,T3,and T4(P<0.05). Compared with the time point of T2,QTc,QTd,Tp-e,Tp-e/QT significantly increased at T3(P < 0.05). Conclusions CO2 pneumoperitoneum combined with Trendelenburg position can prolong ventricular repolarization duration and destroy the stability of cardiac electrophysiology so it may increase the incidence of cardiovascular events.