Animals ; Animals, Newborn ; Female ; Hyperbaric Oxygenation ; Hypoxia-Ischemia, Brain ; physiopathology ; therapy ; Nerve Growth Factor ; pharmacology ; Nerve Regeneration ; drug effects ; physiology ; Rats ; Rats, Wistar

Bioimprinting is a new developed technique to improve the characteristics of enzymes.Bioimprinting by lauric acid was conducted to improve the esterification activity of lipase PS in sol-gel immobilization process with methyltrimethoxysila(MTMS) and tetramethoxysila(TMOS) as the precursors.Results generated by checking the esterification activity and scanning electron microscope showed that bioimprinting can enhance the specific activity and thermal stability of lipase PS.The bioimprinting system was optimized by orthogonal experiment,and the optimal condition for lipase bioimprinting is water/silane molar ration(R) 12,polyethylene glycol(PEG) 120?l,and lauric acid 0.15 mmol.Compared with the free enzyme and the non-imprinted enzymes,the specific activity of imprinted enzymes has been improved 44.3 fold and 2.4 fold,respectively.Imprinted lipase show better thermal stability,and the relative activity is 58% after incubated in 80 ℃ for 0.5 h,while no activity was detected for the free enzyme.

Objective To investigate the influence of exogenous basic fibroblast growth factor(bFGF) on glial fibrillary acidic protein(GFAP) expression in neonatal rats with hypoxic-ischemic brain damage(HIBD).Methods Eighty HIBD models of neonatal Wistar rats were made by shearing right arteria carotis communis and then breathing 8% oxygen and 92% nitrogen for 2 hours.The models were divided into 2 groups randomly: trial group of bFGF and control group of normal sodium.The other 40 rats were taken into the sham(ope-)ration group.Expressions of GFAP were examined with immunohistochemical staining and image quantitative analysis at the 4~(th),7~(th),10~(th),17~(th) and 24~(th) days after operation.Results The expression of GFAP in hippocampal CA1 region of rats in sham operation group reached peak at the 7~(th) day after(ope-)ration.The expression of GFAP in control group increased and reached peak at the 10~(th) day after(ope-)ration,which GFAP-positive cells mainly appeared in hippocampal CA1 region and CA3 region.The expression of GFAP in hippocampal CA1 region of rats of trial group was higher than those of sham operation group and control group,which reached peak at the 10~(th) day after the operation,there was significant difference in 3 groups at the 4~(th),10~(th) and 17~(th) days after operation(all P

Developmental changes in children can affect drug disposition and clinical effects. A physiologically-based pharmacokinetic (PBPK) model is a mathematical model that can be used to predict blood drug concentrations in children and gain insight into age-dependent physiological differences in drug disposition impact. Pediatric PBPK (P-PBPK) models have attracted attention over the past decade. With the concerted efforts of academia, pharmaceutical companies, and regulatory agencies, there are more and more examples of pediatric clinical studies using PBPK models. Nevertheless, the number of P-PBPK models and their predictive performance still lag behind adult models. By referring to the literature, we study the process of children adapting to adult absorption, distribution, metabolism, and excretion (ADME) parameters and analyze the general principles of P-PBPK model establishment. In addition, we summarize the functions and application examples of commonly used P-PBPK modeling software to provide a basis for the rational application of modeling software.

Adult ; Air Pollutants, Occupational ; adverse effects ; Chemical Industry ; Female ; Humans ; Insecticides ; adverse effects ; Male ; Maximum Allowable Concentration ; Middle Aged ; Occupational Diseases ; chemically induced ; diagnosis ; Organothiophosphorus Compounds ; adverse effects ; Phosphorus Compounds ; adverse effects ; Sulfides ; adverse effects

In this paper, fourteen new L-proline derivatives were designed and synthesized, and their acetlcholinesterase (AChE) inhibitory activities were also investigated in vitro. New L-proline derivatives were prepared from substituted 2-bromo-1-acetophenones through four-step reaction; and their bioactivities as AChE inhibitors were measured by Ellman spectrophotometry. The results showed that the target compounds had a certain AChE inhibitory activity to in vitro. The bioactivity of compound 8b was the best of them, and its IC50 value was 5.45 µmol.L-1, which was better than that of rivastigmine. So the acetylcholinesterase inhibitory activities of new L-proline derivatives were worth to be further studied.
Acetylcholinesterase ; Cholinesterase Inhibitors ; chemical synthesis ; chemistry ; Drug Design ; Proline ; analogs & derivatives ; Rivastigmine ; chemistry ; Structure-Activity Relationship

OBJECTIVETo explore the effects of S-adenosyl-L-methionine (SAM) on blood lead concentration and oxidative stress of tissue in prenatal and postnatal lead-exposed rats, and evaluate the potential reparation exerted by SAM on paired-pulse facilitation (PPF) and long-term potentiation (LTP) in lead-exposed rat.

METHODSPregnant Wistar rats were randomly divided into three groups: control, lead-exposed and lead-exposed with SAM treatment groups. Lead-exposed rats drank 1.5 g/L lead acetate solution through pregnancy until weaning and then the pups received 20 mg/kg SAM or saline daily intraperitoneally depending on their group. Control group rats drank tap water throughout the experiment. At the postnatal 44-60 days, all the pup rats were given an extracellular recording measured in dentate gyrus (DG) area of hippocampus. The blood lead concentration and oxidative stress in liver, brain and hippocampus were also detected.

RESULTSThe blood lead concentration in lead-exposed group was higher (159. 3 +/- 10. 9 microg/L) in comparing with those of control group (27.5 +/-3.8 microg/L) and lead +SAM group (33.1 +/-9.5 microg/L) (F=213.5, P<0.01). A significant recovery of liver, brain glutathione (GSH) and malondialdehyde (MDA) level was clearly produced in lead-exposed rats after SAM treatment (P <0.05). Chronic lead exposure during development impaired LTP measured on field excitatory postsynaptic potential (EPSP) [(112 +/-2.1)%] compared with control rats [(131+/-4.5)%] and the impaired LTP could be significantly increased by SAM treatment [(120 +/- 2.6)%] (F = 26. 1, P <0. 05).

CONCLUSIONSAM might be beneficial for treatment of lead intoxication, especially in the rescue of learning and memory impairment induced by lead and should deserve more detailed research.

Animals ; Brain ; metabolism ; Female ; Glutathione ; biosynthesis ; Lead ; blood ; Lead Poisoning ; prevention & control ; Long-Term Potentiation ; drug effects ; Male ; Maternal Exposure ; prevention & control ; Pregnancy ; Rats ; Rats, Wistar ; S-Adenosylmethionine ; pharmacology

The target compounds were prepared from 5-aminobenzimidazolone by two steps reaction, and their AChE inhibitory activities were measured by Ellman method in vitro. The AChE inhibitory activity of compound 4d is the best of them, and its IC50 value is equal to 7.2 μmol·L(-1), which is better than that of rivastigmine; moreover the 4d had no inhibitory activities to BuChE. Therefore, the inhibitory activities of 5-aminobenzimidazolone derivatives to acetylcholinesterase are worth further researching.
Acetylcholinesterase ; metabolism ; Benzimidazoles ; chemical synthesis ; chemistry ; Cholinesterase Inhibitors ; chemical synthesis ; chemistry ; Drug Design ; Phenylcarbamates ; chemistry ; Rivastigmine ; Structure-Activity Relationship

Objective To investigate the value of three-dimensional speckle tracking imaging (3D-STI) in assessment of left ventricular (LV) strains. Methods Thirty healthy young adults examined by two-dimensional speckle tracking imaging (2D-STI) and 3D-STI. And the results of LV measurements were compared, which included mean peak systolic longitudinal strains, radial strains and circumferential strains. Also, the time consumption of these two methods was compared. Results The time needed for 3D-STI in acquisition and analysis of the images were (309.3±23.4)s, (305.5±11.2)s, while the time for 2D-STI were (490.6±14.4)s, (1261.4±39.9)s. The differences were signiifcant(t=-21.81, 69.94, both P<0.01). The global mean peak systolic radial strains was (48.59±7.68)%by 3D-STI and (33.25±7.27)%by 2D-STI. The difference was signiifcant(t=9.16, P<0.01). The global mean peak systolic longitudinal and circumferential strains were (-17.66±3.14)%, (-17.13±2.29)% by 3D-STI and (-21.35±2.46)%, (-21.97±3.84)% by 2D-STI. The differences were signiifcant(t=5.33, 5.99, both P < 0.01). The 3D-STI strains were different at different levels of LV. The longitudinal, circumferential and radial 3D-STI strains were largest at middle levels. However, 2D-STI strains didn′ t show such trend. Peak strains measured by 3D-STI and 2D-STI showed high inter-observer and intra-observer agreement in Bland-Altman chart. Conclusion 3D-STI is a novel, convenient and reproducible method to evaluate the strains of LV.

Adult ; Endoscopy ; Female ; Hemangioma, Cavernous ; surgery ; Humans ; Orbital Neoplasms ; surgery ; Otorhinolaryngologic Surgical Procedures ; methods