A series of quinoline-polyamine conjugates (8a-8n) were designed, synthesized and evaluated as inhibitors of cholinesterases (ChEs). Some of these compounds had potent ChEs inhibitory activity with IC50 values at micromolar range. Compound 8n exhibited the strongest inhibition on acetylcholinesterase (AChE) with an IC50 value of 8.78 micromol x L(-1), and compound 8i showed the most potent inhibition on butyrylcholinesterase (BChE) with IC50 value of 1.60 micromol x L(-1) which was slightly better than rivastigmine. The structure-activity relationship revealed that the chain length of polyamine and linker played important roles for inhibitory activity. Molecular modeling studies showed that 8i targeted both the catalytic active site (CAS) and the peripheral anionic site (PAS) of cholinesterases.

Objective To observe the effect of polyethylene terephthalates (PET) coated with 58S bioactive glass on graft-bone healing.Methods The PET coated with 58S bioactive glass was used in experimental group,and uncoated PET was used as a control.The coating solution was made of 20％ bioactive glass powder and 80％ gelatin powder (by weight).In our vitro study,4×104/ml MT3T3-E1 cells were cultured in 24-well plates with the coated or uncoated PET,and the MTT and ALP were tested at 1,3,5 days to show the proliferation and the activity of the cells.The SEM and the X-ray photoelectron spectrometer were adopted to analyze the surface characteristics of the fiber.In our vivo study,24 skeletally mature New Zealand white rabbits were randomly divided into two groups,the 58S-PET group and the PET group.Both groups underwent a surgical procedure to establish a tibia-articular tendon-bone healing model.Mechanical examination and histological assay were taken to verify the coating effect in vivo.Results The 58S-PET group showed significantly differences in both the MTT and ALP tests at each time point (3,5 days) compared with the PET group.In the animal experiments,the maximum load increased by time in both groups.At 6 weeks,the load-to-failure was significantly higher in the 58S-PET group [(61.70±6.95) N]than that of the PET group [(45.21±9.78) N].At 12 weeks,the load-to-failure was also significantly higher in the 58S-PET group [(89.25±9.50) N]than that of the PET group [(71.38±6.26) N].In the histological assay,it was found that there was new bone formation in the indistinct interface between the graft and the host bone in both groups at 6,12 weeks,and a stronger binding was seen in the 58S-PET group than in the PET group.Conclusion The 58S-PET could enhance the proliferation and activity of the osteoblast and therefore promote the new bone formation and subsequently leads to a positive effect on tendon-bone healing.

The G protein-coupled estrogen receptor (GPER), also known as G protein-coupled receptor 30 (GPR30), was identified in the recent years as a functional membrane receptor different from the classical nuclear estrogen receptors. This receptor is widely expressed in the cortex, cerebellum, hippocampus, heart, lung, liver, skeletal muscle, and the urogenital system. It is responsible for the mediation of nongenomic effects associated with estrogen and its derivatives, participating in the physiological activities of the body. The present study reviews the molecular structure, subcellular localization, signaling pathways, distribution, and function of GPER in the male reproductive system.
Estrogens ; metabolism ; Genitalia, Male ; metabolism ; Humans ; Male ; Molecular Structure ; Organ Specificity ; Receptors, Estrogen ; chemistry ; physiology ; Receptors, G-Protein-Coupled ; chemistry ; physiology ; Reproduction ; physiology ; Signal Transduction

Objective To observe the effect of spleen-strengthening and kidney-reinforcing method on leukopenia in patients with malignant tumor after chemotherapy.Methods Seventy-one patients with malignant tumor were randomly allocated to Group A(n=37) and Group B (n=34).Group A was treated with spleen-strengthening and kidney-reinforcing herbal medicine and chemotherapy and Group B with chemotherapy only. The treatment course lasted 28 days.Blood routine examination was carried out before chemotherapy and on 7 th,9 th,12 th,15 th,18 th and 21 st day of chemotherapy.Results In Group A,5 cases of leukopenia were found, 3 in degree Ⅰ, 1 in degree Ⅱ and 1 in degree Ⅲ,the incidence being 13.5%; In Group B,25 cases of leukopenia were found, 3 in degree Ⅰ,13 in degree Ⅱ,8 in degree Ⅲ and 1 in degree Ⅳ, the incidence being 73.5%. There was significant difference between the two groups (P

Dental Materials ; Dental Porcelain ; Humans

Ammonium perchlorate (AP), mainly used as solid propellants, was reported to interfere with homeostasis via competitive inhibition of iodide uptake. However, detailed mechanisms remain to be elucidated. In this study, AP was administered at 0, 130, 260 and 520 mg/kg every day to 24 male SD rats for 13 weeks. The concentrations of iodine in urine, serum thyroid hormones levels, total iodine, relative iodine and total protein, and malondialdehyde (MDA), superoxide dismutase (SOD) and catalase (CAT) activity in thyroid tissues were measured, respectively. Our results showed that high-dose perchlorate induced a significant increase in urinary iodine and serum thyroid stimulating hormone (TSH), with a decrease of total iodine and relative iodine content. Meanwhile, free thyroxine (FT4) was decreased and CAT activity was remarkably increased. Particularly, the CAT activity was increased in a dose-dependent manner. These results suggested that CAT might be enhanced to promote the synthesis of iodine, resulting in elevated urinary iodine level. Furthermore, these findings suggested that iodine in the urine and CAT activity in the thyroid might be used as biomarkers for exposure to AP, associated with thyroid hormone indicators such as TSH, FT4.

Objective To investigate the clinical significance of retinal binding protein (RBP) and Cystatin C in blood and urine in patients with chronic kidney disease (CKD).Methods One hundred and twenty-one patients with CKD in Nephrology Laboratory of The People's Hospital of Xinjiang Uygur Autonomous Region from Aug.2012 to Jan.2013 were served as the case group.Sixty healthy check-up people were considered as control group.Enzyme linked immunosorbent assay was used to detect RBP and Cystatin C in urine,and the immune turbidimetry testing was applied to detect RBP and Cystatin C in blood.The receiveroperating characteristic (ROC) curve and area under curve (AUC) were applied to evaluate the sensibility and diagnostic value of indexes in CKD.Results The positive rate of RBP,Cystatin C in urine and blood were 89.6％,92.6％,52.5％,59.5％ respectively of 12 patients in case group,higher than those in control group (all value were 0,P ＜0.001).ROC curve showed that the sensitivity of urine RBP and Cystatin C were higher than that in blood of case group.AUC of RBP,Cystatin C level in urine and blood were 0.915,0.974,.655,and 0.623 respectively.And 95％ confidence interval were 0.877-0.954,0.956-0.992,0.575-0.736,0.543-0.702 respectively,and the differences are statistically significant (P ＜ 0.001).Conclusion The sensitivity of urine cystatin C and RBP are significantly higher than that in blood,which might be served as a diagnostic marker of CKD and can provide important basis for clinical diagnosis.

OBJECTIVETo apply single nucleotide polymorphism (SNP) microarray for delineation of small supernumerary marker chromosome (sSMC) in two newborns.

METHODChromosome karyotyping was performed on newborns who were born in Jan. 2013 and Jan. 2014 in Haidian Maternal and Child Health Hospital because of the abnormalities found in pregnancy checkups. SNP microarray analysis was carried out on 2 newborns with de novo sSMCs (one was mos 47,XY, + mar[45]/46,XY[5] and the other was mos 47, XY, + mar [30]/46, XY [20]), which could not be determined by conventional banding techniques. Genomic DNA was extracted from cord blood samples, amplified, tagged and hybridized following the manufacturer' s protocol. Data were collected and analyzed.

RESULTThere was a 78. 6 Mb duplication in chromosome 8 for Newborn A, which was associated with 8p22 duplication syndrome; and a 32. 7 Mb duplication in chromosome 13 for Newborn B, which was not yet reported definitely as pathogenic. The newborn A was identified with agenesis of the corpus callosum, obvious right eyelid drooping, the onset of low muscle tone and mental developmental lag behind their peers, while the newborn B had normal findings on physical and mental evaluation.

CONCLUSIONSNP-array can identify sSMCs of newborns at the DNA level, and can be used as an important supplement to the conventional karyotype analysis, but the pathogenicity of positive outputs need further verification.

To examine the role of ultrasound in gene delivery in vitro, three cells lines were exposed to the low-frequency ultrasound of varying intensities and for different durations to evaluate their effect on gene transfection and cell viability of the cells. Microbubble (MB), Optison (10%), was also used to observe the role of the microbubbles in gene transfection. The results demonstrated that as the ultrasound intensity and the exposure time increased, the gene transfer rate increased and the cell viability decreased, but at high energy intensities, the cell viability decreased dramatically, which caused the transfer rate to decrease. The most efficient ultrasound intensity for inducing gene transfer was 1 W/cm(2) with duration being 20 s. At the same energy intensity, higher ultrasound intensity could achieve maximal gene transfer rate earlier. Microbubbles could increase ultrasound-induced cell gene transfer rate by about 2 to 3 times mainly at lower energy intensities. Moreover, microbubbles could raise the maximum gene transfer rate mediated by ultrasound. It is concluded that the low-frequency ultrasound can induce cell gene transfer and the cell gene transfer rate and viability are correlated with not only the ultrasound energy intensity but also the ultrasound intensity, the higher ultrasound intensity achieves its maximal transfer rate more quickly and the ultrasound intensity that can induce optimal gene transfer is 1 W/cm(2) with duration being 20 s, and microbubbles can significantly increase the maximal gene transfer rate in vitro.
3T3 Cells ; CHO Cells ; Cell Line ; Cell Survival/*genetics ; Contrast Media/metabolism ; Cricetinae ; Cricetulus ; Microbubbles ; Transfection/*methods ; Ultrasonics

Objective To evaluate the CT and MRI characteristics of Primary Central Nervous System Lymphoma(PCNSL)in immunocompetent patients,and enhance its diagnosis level.Methods CT and MRI data of 20 patients with PCNSL confirmed by histo-pathology were analyzed retrospectively.MRI scans were performed with and without Gadolinium contrast.Two of them had contrast-enhanced CT scan;six had CT scan without contrast administration;1 had CT scan with both non-contrast and contrast enhancement.Re- suits Totally,38 lesions were found in all patients:14 lesions of them were single and 24 lesions were found in 6 patients.Generally,the lesions were located in the surface and/or midline of the brain.The signal features and density were similar to meningioma,and strongly enhancing after contrast administration.Thirty-six of the 38 lesions had spicular sign peripheral to the lesion.Conclusion Although the manifestations of the PCNSL are variety,there are still many characteristics in the medical imaging,especially in the locations,the signal features,and spicular sign in the edge of the lesions after contrast material injection.