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Background: Anthranilic diamide derivatives are among the most important classes of synthetic insecticides. Moreover, the 1,2,4-oxadiazole heterocycle, a bioisostere of amide, has been extensively used in pesticides. In order to discover novel molecules with high insecticidal activities, a series of anthranilic diamide analogues containing 1,2,4-oxadiazole rings were designed and synthesised., Results: A series of novel anthranilic diamide derivatives containing 1,2,4-oxadiazole were obtained, and confirmed by 1 H and 13 C nuclear magnetic resonance and high-resolution mass spectrometry. The structure of 3-bromo-N-(4-chloro-2-methyl-6-{3-[(methylsulphonyl)methyl]-1,2,4-oxadiazol-5-yl}phenyl)-1-(3-chloropyridin-2-yl)-1H-pyrazole-5-carboxamide was further characterised by X-ray diffraction analysis. In addition, bioassays showed that most of the newly synthesised compounds displayed 100% mortality against Plutella xylostella at 100 mg L -1 , and compound 3IIl showed 90% larvicidal activities at a concentration of 0.5 mg L -1 . The LC 50 value of 3IIl was 0.20 mg L -1 , which indicated that it may be used as a potential leading compound for further structural optimisation. Furthermore, brief comparative molecular field analysis (CoMFA) models were established to study the structure-activity relationships (SARs) of the title compounds., Conclusion: Compound 3IIl may be used as a potential leading compound for further structural optimisation, and SARs and CoMFA models could provide reliable clues for further structural optimisation. © 2016 Society of Chemical Industry., (© 2016 Society of Chemical Industry.)

Human corneal endothelial cells are a non-proliferative cell type. As a result of the increase in corneal endothelium disease, increasing numbers of studies have been conducted in order to promote corneal endothelial cell proliferation. The aim of the present study was to investigate the proliferative effects of Rho-associated protein kinase inhibitor, Y-27632, on rabbit corneal endothelial cells (rCECs). Y-27632 (1, 10 or 30 μM) was added at two different time points to two groups of rCECs. The first group received Y-27632 when rCECs were initially plated, and the second following 72 h of cell growth. Cell morphology and cell adhesion ratios were subsequently observed using light microscopy. A cell counting kit was used to measure the number of viable cells that adhered to culture plates. Cell cycle transitions and levels of Annexin V-positive apoptotic cells were detected using flow cytometry. Cells treated with 1 μM Y-27632 and 10 μM Y-27632 retained their cell shape. At a concentration of 30 μM Y-27632, the cell shape became irregular. Cell adhesion ratios, in 1 μM Y-27632 (36.84%), 10 μM Y-27632 (84.21%) and 30 μM Y-27632 (84.21%) were higher than the adhesion ratio in the control group (P<0.01). The optical densities of rCECs treated with 10 μM or 30 μM Y-27632 following 72 h of cell growth was less than that of the control cells (P<0.01), but higher than that of cells which received Y-27632 at the time of plating (P<0.01). Flow cytometry results also demonstrated that there was a delay in G1 to S phase cell cycle progression in rCECs following administration of 10 μM Y-27632 (P<0.01). Cell apoptosis was inhibited when 10 μM Y-27632 was added, at the time of cell plating, as well as when added following 72 h of cell growth (P<0.01). At a concentration of 10 μM Y-27632, there was an improvement in cell adhesion and an inhibition of the cell cycle in rabbit corneal endothelial cells. In conclusion, Y-27632 has different effects on rCECs when administered at varying concentrations and at particular stages of cell growth.

The aim of this study was to evaluate the feasibility and safety of porcine Descemet's membrane (DM) as a carrier for the generation of tissue-engineered corneal endothelium by analyzing porcine endogenous retroviruses (PERVs) and the α-gal epitope. The morphology of porcine and human DM was observed by hematoxylin and eosin staining and scanning electron microscopy. Immunohistochemical staining was used to investigate the location of α-gal epitopes on porcine DM used for xenotransplantation. The porcine DM was treated with ethylene glycol diglycidyl ether (EDGE) for 2 weeks, and then the PERV gene sequences in porcine DM and DM-EDGE were detected by polymerase chain reaction (PCR) and real-time PCR, respectively. The porcine DM had tight basement membrane morphology, which was similar to human DM in terms of thickness. No positive immunohistochemical staining of the α-gal epitope was detected in porcine DM. PERV expression of pol, gag, env-A and env-B was noted in porcine DM, but in DM-EDGE it was completely degraded. Based on structural, immunological and etiological studies, porcine DM may be an ideal and viable carrier for the generation of tissue-engineered corneal endothelium.

We previously reported that daucosterol (a sterolin) up-regulates the expression of insulin-like growth factor I (IGF1)(1) protein in neural stem cells. In this study, we investigated the effects of daucosterol on the survival of cultured cortical neurons after neurons were subjected to oxygen and glucose deprivation and simulated reperfusion (OGD/R)(2), and determined the corresponding molecular mechanism. The results showed that post-treatment of daucosterol significantly reduced neuronal loss, as well as apoptotic rate and caspase-3 activity, displaying the neuroprotective activity. We also found that daucosterol increased the expression level of IGF1 protein, diminished the down-regulation of p-AKT(3) and p-GSK-3β(4), thus activating the AKT(5) signal pathway. Additionally, it diminished the down-regulation of the anti-apoptotic proteins Mcl-1(6) and Bcl-2(7), and decreased the expression level of the pro-apoptotic protein Bax(8), thus raising the ratio of Bcl-2/Bax. The neuroprotective effect of daucosterol was inhibited in the presence of picropodophyllin (PPP)(9), the inhibitor of insulin-like growth factor I receptors (IGF1R)(10). Our study provided information about daucosterol as an efficient and inexpensive neuroprotectants, to which the IGF1-like activity of daucosterol contributes. Daucosterol could be potentially developed as a medicine for ischemic stroke treatment., (Copyright © 2015 Elsevier Ltd. All rights reserved.)

Purpose: the study aimed to compare the quality of life (QOL) and radiotherapy complications among Chinese nasopharyngeal carcinoma (NPC) patients at different 3-dimensional conformal radiotherapy (3DCRT) stages adjusting for other variables., Methods: 511 NPC patients at different 3DCRT stages were enrolled. They were interviewed regarding SF-36, complications and socio-demographic variables and cancer- or treatment- related variables. Analysis of covariance (ANCOVA) based on SF-36, complications scores as dependent variables, 3DCRT stages as independent variables, and other variables as covariate were established., Results: The influencing factors of PCS included 3DCRT stages and age group. The influencing factors of MCS included 3DCRT stages and income. Most QOL scores of NPC patients were significantly associated with 3DCRT stage, after accounting for other variables. QOL scores of the patients receiving 3DCRT were the lowest, QOL scores of people after 3DCRT gradually increased. PCS scores of people greater than 5 years after 3DCRT was improved to or even better than the level before 3DCRT. The complications with significantly different scores of patients at different 3DCRT status included xerostomia, throat ache, hypogeusia, caries, hearing loss, snuffles., Conclusions: Clinicians should pay more attention to older NPC patients and patients with lower income. When patients receive 3DCRT, measures should be taken to reduce radiation injury to improve the patients' QOL.

Objective: To clone and express S-dsRNA gene of Cryptosporidium parvum virus, and investigate the reactogenicity of the recombinant., Methods: Total RNA was extracted from Cryptosporidium parvum and S-dsRNA gene was amplified by RT-PCR. The PCR product was cloned into pET-28a(+) expression vector. The recombinant plasmid pET-28a(+)-S was transformed into E. coli BL21 (DE3) and induced with IPTG. The expression situation of recombinant protein was analyzed by SDS-PAGE. Its reactogenicity was examined by Western blotting analysis., Results: pET-28a (+)-S was identified by PCR and double endonuclease digestion. SDS-PAGE result showed that the recombinant protein (M, 37,000) was expressed in the form of inclusion body. High level expression of recombinant protein was found at 1 mmol/L IPTG condition after incubation at 37 degrees C for 4 h and reached up to 72.6% of the total protein. The protein was recognized by the antisera from mice immunized with antigens from Cryptosporidium parvum oocysts., Conclusion: The S-dsRNA gene of Cryptosporidium parvum virus has been expressed with adequate reactogenicity.

Aim: To investigate whether there was a dominant sacral root for the motive function of rectum and anal sphincter, and to provide an experimental basis for sacral root electrically stimulated defecation in spinal cord injuries., Methods: Eleven spinal cord injured mongrel dogs were included in the study. After L4-L7 laminectomy, the bilateral L7-S3 roots were electrostimulated separately and rectal and sphincter pressure were recorded synchronously. Four animals were implanted electrodes on bilateral S2 roots., Results: For rectal motorial innervation, S2 was the most dominant (mean 15.2 kPa, 37.7% of total pressure), S1 (11.3 kPa, 27.6%) and S3 (10.9 kPa, 26.7%) contributed to a smaller part. For external anal sphincter, S3 (mean 17.2 kPa, 33.7%) was the most dominant, S2 (16.2 kPa, 31.6%) and S1 (14.3 kPa, 27.9%) contributed to a lesser but still a significant part. Above 85% L7 roots provided some functional contribution to rectum and anal sphincter. For both rectum and sphincter, the right sacral roots provided more contribution than the left roots. Postoperatively, the 4 dogs had electrically stimulated defecation and micturition under the control of the neuroprosthetic device., Conclusion: S2 root is the most dominant contributor to rectal pressure in dogs. Stimulation of bilateral S2 with implanted electrodes contributes to good micturition and defecation in dogs.

Objective: To evaluate the results of a self-designed bladder controller for restoring micturition function in paraplegic dogs., Methods: The spinal cords of 4 dogs were transected above the cone. Electrodes were implanted in S2 bilaterally and connected to the subcutaneous receivers for external activation. Microsurgical technique was employed to perform dorsal rhizotomy of S1-3 intradurally. The dogs were stimulated daily to observe micturition. Urodynamic testing and vesicography were performed., Results: All the dogs acquired micturition under the control of electric stimulation, with urine volume 80-140 ml per time. The mode of micturition was post-stimulus voiding. Vesicography revealed that the bladder was filled well and the bladder neck was open in the micturition course of electric stimulation. Residual urine volume was 15-20 ml. Urodynamic testing found that the bladder pressure and intraurethral pressure increased simultaneously, but when the intraurethral pressure was greater than the bladder pressure, no micturition occurred. The pressure decreased to baseline rapidly and the bladder pressure decreased slowly between two bursts. Micturition occurred when the bladder pressure was greater than the intraurethral pressure., Conclusions: The self-designed bladder controller together with a sacral deafferentation procedure can restore micturition function of paraplegic dogs.