A series of 4-(2-acetoxybenzoylamino) butyrate derivatives were designed and synthesized. All of the novel 12 compounds (7a-7k) were synthesized from gamma-aminobutyric acid (1) as starting material, and their structures were confirmed with IR, 1H NMR, EI-MS and elemental analysis. Preliminary pharmacological test in vitro showed that most of these title compounds possessed antiepileptic activity. Compounds 7i-7k displayed strong antiepileptic activity and are worth for further development. Compounds 4, 7d-7h showed moderate antiepileptic activity. The structure-activity relationship of 4-(2-acetoxybenzoylamino) butyrate derivatives is also discussed preliminarily.

Animals ; Dentistry ; Swine ; Swine, Miniature

BACKGROUND:Mesenchymal stem cel s are multipotent progenitor cel s that can be isolated from the bone marrow, adipose tissue, umbilical cord blood and so on. Mesenchymal stem cel s possess strong immunosuppressive effects on both innate and adaptive immunity.
OBJECTIVE:To summarize the immunomodulatory properties of mesenchymal stem cel s for T lymphocytes, B lymphocytes, natural kil er cel s and dentritic cel s and prospect its therapeutic implication.
METHODS:PubMed and CNKI databases were searched for relevant literatures published from 2000 to 2015. The key words were“mesenchymal stem cel s, immunomodulator, T cel s, B cel s, NK cel s, dendriticc cel s”in Chinese and English, respectively. Then, 61 papers were included and further analyzed.
RESULTS AND CONCLUSION:The immunomodulatory effects of MSCs on lymphocytes, B lymphocytes, natural kil er cel s and dentritic cel s were elicited by cel-cel contact and soluble cytokines. But mesenchymal stem cel s from different sources hold different immunomodulatory effect on immune cel s. When we use mesenchymal stem cel s in clinic, some important factors, such as isolation methods, cel sources, colonization sites, should be taken into account. In order to ensure the clinical safety and effectiveness, there are stil many problems to be further studied before mesenchymal stem cel s can be widely used in clinic.

A series of 4-(2-acetoxybenzoylamino) butyrate derivatives were designed and synthesized. All of the novel 12 compounds (7a-7k) were synthesized from gamma-aminobutyric acid (1) as starting material, and their structures were confirmed with IR, 1H NMR, EI-MS and elemental analysis. Preliminary pharmacological test in vitro showed that most of these title compounds possessed antiepileptic activity. Compounds 7i-7k displayed strong antiepileptic activity and are worth for further development. Compounds 4, 7d-7h showed moderate antiepileptic activity. The structure-activity relationship of 4-(2-acetoxybenzoylamino) butyrate derivatives is also discussed preliminarily.
4-Aminopyridine ; Animals ; Anticonvulsants ; chemical synthesis ; chemistry ; therapeutic use ; Butyrates ; chemical synthesis ; chemistry ; therapeutic use ; Drug Design ; Epilepsy ; chemically induced ; drug therapy ; Female ; Lethal Dose 50 ; Male ; Mice ; Molecular Structure ; Random Allocation ; Structure-Activity Relationship ; gamma-Aminobutyric Acid ; chemistry

AIMTo establish a solid phase extraction-high performance liquid chromatographic (SPE-HPLC) method for determining plasma scutellarin concentration, and study its pharmacokinetics after i.v. breviscapine in rabbits.

METHODSMethanol-water-phosphoric acid (50:50:0.5) mixture was used as mobile phase, Nucleosil C18 column (250 mm x 4.6 mm ID) was selected. The wavelength of UV detection was 335 nm. Fifteen rabbits, randomized into 3 groups, were given breviscapine i.v. at the dose of 10, 20 and 40 mg.kg-1. Scutellarin in plasma was determined by SPE-HPLC method.

RESULTSLinearity was obtained over the range of 0.02-10.0 mg.L-1 of scutellarin. The method recovery was 96.15%-99.31%; the within-day and between-day RSDs were all below 10%. After i.v. 10, 20 and 40 mg.kg-1 of breviscapine to rabbits, the concentration-time curve of scutellarin fitted to a three compartment model. The main pharmacokinetic parameters showed no significant difference between low and medium doses, but the difference was significant between high dose and other doses.

CONCLUSIONThis assay method was accurate, sensitive, simple and suitable for the measurement of plasma scutellarin concentration. The pharmacokinetic characteristics were found to fit a three-compartment model following i.v. injection of breviscapine to rabbits. The changes of drug concentration in vivo exhibited linear kinetics ove the dosage range of 10-20 mg.kg-1, but when the dosage was 40 mg.kg-1, the linear kinetic properties disappeared.

Animals ; Apigenin ; Area Under Curve ; Chromatography, High Pressure Liquid ; methods ; Flavonoids ; blood ; pharmacokinetics ; Male ; Rabbits

Objective To observe the levels of alanine aminotransferase(ALT), total bilirubin(TBIL), hyaluronic acid (HA), procollagen type Ⅲ aminoterminal peptide (P Ⅲ NP) and larninin (LN) in the sera of rats infected with Clonorchis sinensis (C. sinensis) after treatment of albendazole combined with milkvetch root. Methods Thirty-two healthy adult Wistar rats were randomly divided into four groups with 8 in each based on body mass: control group, non-treatment group, Albendazole group(ALB group) and albendazole combined with milkvetch root group(ALB+MR group). The rats in non-treatmen, ALB and ALB+MR groups were infected orally with metacercariae of C. sinensis 50 per rat. The rats in control group were mock-infected with saline. The rats in ALB group were treated to each rat with 50 mg/kg alhendazole for 5 days, and ALB+MR groups were given to same treat with albendazole, meanwhile each rat injected with 800 mg/kg milkvetch root intraperitoneally for 30 days. All rats were killed after infestation 14 weeks and their sera samples were collected to detect ALT, TBIL, HA, PⅢNP, LN. Results There were statistically significant differences in the levels of ALT and LN in the sera of rats between groups(F=31.40,11.82, P<0.01). Compared with control[ (47.88±4.88)U/L, (51.20±4.12)μg/L], the levels of ALT and LN in rats in non-treatment group [(85.50±9.65)U/L, (64.20±4.18) μg/L] and ALB group [(65.29± 7.78) U/L, (58.23±2.55) μg/L] were significantly increased (P<0.05). Compared with non-treatment group, the levels of ALT and LN in rats in ALB group and ALB+MR groups[(50.25±9.29)U/L, (53.68±5.63)μg/L] were significantly decreased(P<0.05), and they decreased more obviously in ALB+MR group (P<0.05). There were statistically significant differences in the levels of TBIL, PⅢNP and HA in the sera of rats between groups (χ2=15.309,21.418,19.759, P<0.01). Compared with control[(0.700±0.350)μmol/L, (26.085±4.075)μg/L, (81.935±42.550)μg/L], the levels of TBIL, PⅢNP and HA in rats in non-treatment group(2.400 μmol/L, 46.220 μg/L,310.885 μg/L) and ALT group(1.200 μmol/L,36.540 μg/L, 178.010 μg/L) were significantly increased(P<0.05). Compared with non-treatment group, the level of TBIL in ALT+MR group(0.750 μmol/L), the levels of pⅢNP and HA in ALT and ALT+MR group(30.470,100.240 μg/L) were significantly decreased(P< 0.05). The levels of TBIL, PⅢNP and HA decreased more obviously in ALB+MR group(P<0.05). Conclusions The liver function in rats infected with C. sinensis is abnormal. The liver function and fibrosis are improved after treatment with albendazole or albendazole combined with milkvetch root. The treatment of albendazole combined with milkvetch root is more effective.

OBJECTIVE To study the effect of polygonatum polysaccharide on zebrafish with Alzheimer disease. METHODS Zebrafish were trained in T maze for 7 d. The 40 zebrafish successfully trained were divided into 4 groups:blank group, model group, positive group and polygonatum polysaccharide group. Model group, positive group and polygonatum polysaccharide group were put in AlCl3100μg·L-1 for 6 d. The positive group was exposed to Huperzine A solution 4μg·L-1, and the polygonatum polysaccharide group was exposed to polygonatum polysaccharide solution 6 g·L-1 for 6 d. The model group was not treated, and the blank group was not treated. Each stage of zebrafish was recorded by video, and the time of each group in the EC region was analyzed. After administration, the brain tissue was taken out and the expression of N-cadherin, P38 and p-P38 protein factors was determined by Western blotting. RESULTS In behavior, the analysis of the time spent in the EC area, the blank group, the positive group and the polygonatum polysac?charide group were compared with the model group, respectively, there were statistically significant differences (P<0.05). At the protein level, compared with the model group, the P38 and p-P38 proteins in the positive group and the polygonatum polysaccharide group were down-regulated, while the N-cadherin protein was up-regulated, with statistical difference (P<0.05). CONCLUSION Polygonatum polysaccharide can improve the learning and memory ability of zebrafish with Alzheimer disease by up regulating the protein level of N-cadherin and hindering P38 phosphorylation.

OBJECTIVE: To seek simple and cost-effective extraction technique to improve multiplex STR amplification from minimal oral epithelial cell samples. METHODS: One hundred DNA samples of oral epithelial cells extracted by mini system Chelex-100 method were quantitated by ABI 7500 Real Time System and were then typed with Identifiler system in ABI 3130 Genetic Analyzer. RESULTS: The DNA contents of different categories of samples were as followings: suck pipes (0.72-116.78 ng), cup edges (2.15-142.5 ng), mouths of drink bottle (1-34.65 ng), chopsticks (3.35-26.6 ng), fruit cores (0.294-21.4 ng), and poultry bones (0.88-5.88 ng). The mean successful typing rate for gender and more than 9 STR loci was about 59.38%. Except the addition or no addition of proteinase K to the samples, all other factors-C users' variation, sample extraction methods, and qualities and properties of the samples had considerable effects on the contents of extracted DNA. CONCLUSION Successful STR typing can be achieved in about 60% minimal oral epithelial cell DNA samples extracted by mini Chelex system.
DNA/analysis* ; Epithelial Cells/metabolism* ; Forensic Medicine/methods* ; Humans ; Microsatellite Repeats ; Mouth Mucosa/cytology* ; Polymerase Chain Reaction

OBJECTIVESTo investigate the techniques of posterior lumbar interbody fusion and pedicle screws in the treatment of degenerative scoliosis and evaluate their clinical significance.

METHODSTwenty five patients with degenerative scoliosis were treated operatively during 1997 - 2002. Among the 25 patients, 13 patients were treated with Brantigan I/F carbon cages in 28 intervertebral spaces, 7 patients were treated with Prospace cages in 15 spaces, 1 patient was treated with CONTACT cages in 2 spaces. The correcting effects, complications and follow-up results were analyzed retrospectively.

RESULTSThe average correction rate of scoliosis was 59% and the rate of pain relief was 88%. There was a case of pseudoarthritis and a case of embolism. During follow-up, correction rate and height of disc spaces were not lost nor shift of interbody cages.

CONCLUSIONPosterior pedicle screws combined with interbody fusion is a safe and effective treatment for degenerative scoliosis.

Adult ; Aged ; Bone Screws ; Female ; Humans ; Internal Fixators ; Male ; Middle Aged ; Retrospective Studies ; Scoliosis ; surgery ; Spinal Fusion

Objective To observe the absorption, excretion and retention of fluoride and aluminum after drinking brick tea in healthy adults. Methods The study was conducted in ten healthy volunteers by drinking brick tea solution in which the fluoride and aluminum concentrations were 5.97, 7.53 mg/L, respectively. The concentrations of fluoride and aluminum were determined in serum samples collected before and at 0.5,1.0,2.0,3.0,and 24.0 h, and in urine samples collected before and during the periods 1.0,2.0,4.0, ＞ 4.0 - ＜ 24.0 h and 24 h after drinking brick tea solution by ion-selective electrode, inductively coupled plasma atomic emission spectrometry (ICP-AES) and inductively coupled plasma atomic mess spectrometry. The total amounts of intake and excretion of fluoride and aluminum in healthy volunteers during 24.0 h were calculated from their corresponding fluoride and aluminum ingesting from brick tea and excreting from urine. Results Before and during the periods 1.0,2.0,4.0,＞ 4.0 - ＜ 24.0 h and 24.0 h after drinking brick tea solution, the urinary fluoride concentrations were (0.50 ±0.14), (2.14 ± 0.90), (1.57 ± 0.93), (2.43 ± 1.49), (1.91 ± 0.69), (0.58 ± 0.20)mg/L, respectively, and the aluminum concentrations in the urine samples were (0.35 ± 0.15), (0.65 ± 0.37), (0.50 ± 0.25), (0.52 ± 0.21 ),(0.50 ± 0.23), (0,46 ± 0.27)mg/L, respectively; the 24.0 h excreting rates of fluoride and aluminum from urine were 52.90%(4.64/8.77) and 12.38% (1.37/11.07), respectively. The fluoride concentrations in serum samples collected before and at 0.5,1.0,2.0,3.0,24.0 h after drinking brick tea solution were (0.06 ± 0.02), (0.14 ± 0.01 ), (0.21 ±0.04), (0.17 ± 0.04), (0.10 ± 0.03), (0.04 ± 0.01 )mg/L, respectively, and aluminum in those were (0.30 ± 0.05),(0.27 ± 0.01 ), (0.30 ± 0.12), (0.34 ± 0.19), (0.30 ± 0.10), (0.27 ± 0.09)mg/L, respectively. Conclusions Fluoride in brick tea is easyly to be absorbed and excreted through kidney, and the kidney excretory capacity of aluminum in brick tea is limited. Levels of fluoride and aluminum in urine could be taken as the indicators for monitoring the prevalent extent and evaluating preventive experiment's effect on the brick tea fluoride-aluminum toxicity; and fasting serum fluoride and aluminum levels could be taken as indicators for estimating the toxic condition of the brick tea fluoride-aluminum toxicity.