A series of isoindoline derivatives were designed, synthesized, and evaluated for their double inhibitory activities. All of them were new compounds, and their structures were confirmed by 1H NMR and HR-MS. Preliminary in vitro pharmacological tests showed that all compounds exhibited 5-HT or NE reuptake inhibition activity. Among the tested compounds, compound I-3 exhibited potent inhibitory activity against 5-HT and NE reuptake in vitro, and exhibited potent antidepressant activity in vivo. These compounds designed can be further optimized for finding more potent 5-HT/NE dual reuptake inhibitors and antidepressant candidates as well.
Antidepressive Agents ; chemical synthesis ; chemistry ; Biological Transport ; Drug Design ; Isoindoles ; chemical synthesis ; chemistry ; Serotonin Uptake Inhibitors ; chemical synthesis ; chemistry ; Structure-Activity Relationship

Adolescent ; Anemia, Aplastic ; complications ; Humans ; Leukemia, Myeloid, Acute ; etiology ; Male

Objective To study the effects of pulsed electromagnetic fields(PEMFs)of 15Hz and lmT on osteoblast differentiation of bone marrow mesenchymal stem cells.Methods The bone marrow mesenchymal stem cells were isolated and cultured in vitro,the third passage cells were harvested and half of them was exposed to PEMFs,another half exposed to sham PEMFs served as the control.The activity of ALP was measured.And the ex- pression of osteoblast and adipogenesis was measured with the semi-quantitative RT-PCR,adipogenic differentiation was observed with the Oil Red O Staining.Results When compared with the control,PEMFs of 15 Hz and 1 mT significantly increased the activity of ALP(P

A study was made on the pharmacokinetic regularity of effective components salvianolic acid B and ferulic acid in Salviae Miltiorrhizae Radix et Rhizoma (SMRR) and Chuanxiong Rhizoma(CR) in rats, so as to discuss the compatibility mechanism of Salviae Miltiorrhizae Radix et Rhizoma and Chuanxiong Rhizoma. Rats were randomly divided into three groups and intravenously injected with 50 mg x kg(-1) salvianolic acid B for the single SMRR extracts group, 0.5 mg x kg(-1) ferulic acid for the single CR extracts group and 50 mg x kg(-1) salvianolic acid B + 0.5 mg x kg(-1) ferulic acid for the SMRR and CR combination group. The blood samples were collected at different time points and purified by liquid-liquid extraction with ethyl acetate. With chloramphenicol as internal standard (IS), UPLC was adopted to determine concentrations of salvianolic acid B and ferulic acid. The pharmacokinetic parameters of salvianolic acid B and ferulic acid were calculated with WinNonlin 6.2 software and analyzed by SPSS 19.0 statistical software. The UPLC analysis method was adopted to determine salvianolic acid B and ferulic acid in rat plasma, including linear equation, stability, repeatability, precision and recovery. The established sample processing and analysis methods were stable and reliable, with significant differences in major pharmacokinetic parameters, e.g., area under the curve (AUC), mean residence time (MRT) and terminal half-life (t(1/2)). According to the experimental results, the combined application of SMRR and CR can significantly impact the pharmacokinetic process of their effective components in rats and promote the wide distribution, shorten the action time and prolong the in vivo action time of salvianolic acid B and increase the blood drug concentration and accelerate the clearance of ferulic acid in vivo.
Animals ; Apiaceae ; chemistry ; Benzofurans ; blood ; pharmacokinetics ; Coumaric Acids ; blood ; pharmacology ; Drug Interactions ; Drugs, Chinese Herbal ; analysis ; pharmacokinetics ; Male ; Rats ; Rats, Sprague-Dawley ; Rhizome ; chemistry ; Salvia miltiorrhiza ; chemistry

So far there exists no corresponding quality test procedures and grading standards for the seed of Prunus humilis, which is one of the important source of base of semen pruni. Therefor we set up test procedures that are adapt to characteristics of the P. humilis seed through the study of the test of sampling, seed purity, thousand-grain weight, seed moisture, seed viability and germination percentage. 50 cases of seed specimens of P. humilis tested. The related data were analyzed by cluster analysis. Through this research, the seed quality test procedure was developed, and the seed quality grading standard was formulated. The seed quality of each grade should meet the following requirements: for first grade seeds, germination percentage ≥ 68%, thousand-grain weight 383 g, purity ≥ 93%, seed moisture ≤ 5%; for second grade seeds, germination percentage ≥ 26%, thousand-grain weight ≥ 266 g, purity ≥ 73%, seed moisture ≤9%; for third grade seeds, germination percentage ≥ 10%, purity ≥ 50%, thousand-grain weight ≥ 08 g, seed moisture ≤ 13%.
Cluster Analysis ; Germination ; Prunus ; growth & development ; Seeds ; physiology

OBJECTIVETo investigate the inhibitory effect of bone marrow mesenchymal stem cells (BMSCs) on E coliinduced prostatitis in rats.

METHODSBMSCs were isolated, cultured and amplified by the attached choice method. Fifty SD rats were randomized into five groups of equal number: normal control, acute bacterial prostatitis (ABP) , chronic bacterial prostatitis (CBP), ABP + BMSCs, and CBP + BMSCs, and the animals in the latter four groups were injected with E. coli into both sides of the prostate under ultrasound guidance for 1 - 14 days to induce ABP and for 4 - 12 weeks to induce CBP. The control rats were injected with the same amount of PBS. Two weeks after injection of BMSCs into the prostates, pathomorphological changes in the prostate were observed under the light microscope and the mRNA and protein levels of IL-1β and TNF-α determined by RT-PCR and ELISA, respectively, followed by statistical analysis with SPSS 18.0.

RESULTSHistopathological evaluation showed typical pathological inflammatory changes in the prostates of the rats in the ABP and CBP groups, including glandular structural changes, interstitial edema, inflammatory cell infiltration, and fibrous hyperplasia, which were all remarkably relieved after treated with BMSCs. The mRNA and protein levels of IL-β ([0.829 ± 0.121] and [271.75 ± 90.59] pg/ml) and TNF-α ([0.913 ± 0. 094] and [105.78 ± 19. 05] pg/ml) in the ABP and those of IL-1β ([0. 975 ± 0. 114] and [265. 31 ± 71. 34] pg/ml) and TNF-α ([0. 886 ± 0. 084] and [107. 45 ± 26. 11 ] pg/ml) in the CBP groups were significantly higher than those in the control rats ([0. 342 ± 0.087] and [45.76 17. 99] pg/ml, P <0. 05); ([0.247 ± 0.054] and ([19.42 ± 7. 75] pg/ml, P <0. 01) as well as than those in the ABP + BMSCs ([0. 433 ± 0. 072] and [51. 34 ± 22. 13] pg/ml, P < 0. 05 ) ; ( [0. 313 ± 0. 076] and [28. 38 ± 8. 78] pg/ml, P < 0. 01) and the CBP + BMSCs group ([0.396 ± 0.064] and [56.37 ± 21.22] pg/ml, P <0.05); ([0.417 ± 0.068] and [29.21 ± 10.22] pg/ml, P <0.01).

CONCLUSIONInjection of BMSCs can reduce E coli-induced prostatic inflammation reaction, which.may be associated with its reduction of inflammatory cell infiltration and the expressions of IL-1β and TNF-α in the prostate tissue.

Acute Disease ; Animals ; Bone Marrow Cells ; physiology ; Chronic Disease ; Escherichia coli Infections ; therapy ; Humans ; Interleukin-1beta ; genetics ; Male ; Mesenchymal Stromal Cells ; physiology ; Prostate ; metabolism ; Prostatitis ; metabolism ; microbiology ; therapy ; RNA, Messenger ; Random Allocation ; Rats ; Rats, Sprague-Dawley ; Tumor Necrosis Factor-alpha ; genetics ; metabolism

OBJECTIVETo investigate the feasibility of reducing THM precursors and controlling bromate taste and odor in drinking water taken from the Yellow River by an ozonation combined system.

METHODSThe appropriate ozone dosage was determined, and then the changes of TOC, UV254 and THM formation potential (THMFP) in the combined system were evaluated.

RESULTSOne mg/L ozone could effectively remove taste and odor and meet the maximum allowable bromate level in drinking water. The pre-ozonation increased THMFP, but the conventional treatment system could effectively reduce the odor. The bio-ceramic filter could partly reduce CHCl3FP, but sometimes might increase CHCl2BrFP and CHClBr2FP. The biological activated carbon (BAC) filter could effectively reduce CHCl3FP and CHCl2BrFP, but increase CHClBr2FP. Compared with other filters, the fresh activated carbon (FAC) filter performed better in reducing THMFP and even reduced CHClBr2FP.

CONCLUSIONThe combined system can effectively reduce taste, odor, CHCl3FP, and CHCl2BrFP and also bring bromate under control.

Bromates ; chemistry ; isolation & purification ; China ; Chlorine ; Humans ; Odorants ; analysis ; prevention & control ; Ozone ; chemistry ; pharmacology ; Rivers ; chemistry ; Taste ; Trihalomethanes ; chemistry ; isolation & purification ; Water Supply ; analysis ; standards

OBJECTIVETo investigate the reduction of chlorination by-products (CBPs) precursors using the fluidized-bed biofilm reactor (FBBR).

METHODSReduction of total organic carbon (TOC), ultraviolet absorbance (UV254), trihalomethane (THM) formation potential (THMFP), haloacetic acid (HAA) formation potential (HAAFP), and ammonia in FBBR were evaluated in detail. Results The reduction of TOC or UV254 was low, on average 12.6% and 4.7%, respectively, while the reduction of THMFP and HAAFP was significant. The reduction of ammonia was 30%-40% even below 3 degrees C, however, it could quickly rise to over 50% above 3degrees C. Conclusions The FBBR effectively reduces CBPs and ammonia in drinking water even at low temperature and seems to be a very promising and competitive drinking water reactor for polluted surface source waters, especially in China.

Biofilms ; Chlorine ; Water Purification

Objective To investigate a shorter and safer route for contralateral C_7 nerve root transfer. Methods Eight male patients were treated from Dec2005 to Nov.2006Their range of age was from 22 to 43 years with an average of 30 yearsFive cases had total brachial plexus avulsion.The operative delay was from 2 to 6 months(mean:4 months).The sealenus anterior muscle was transected before a prespinaJ & ret- ropharyngeal tunnel was madeThe contralateral C_7 nerve root was used to repair the upper trunk or the infra- clavicular lateral cord and posterior cord of injured side via this routeusing direct anastomosis or nerve graft- ing.Results The length of the harvested contralateral C_7 nerve root was(4.67?0.52em in the early 5 casesThe nerve graft was6.25?0.35)em long for repairing supraclavicular brachial plexus and(8.56?0.45cm long for repairing infraclavicular brachial plexusThe length of the harvested contralateral C_7 nerve root averaged 6.85cm in the other 3 cases2 of which had direct anastomosis to the residual nerve C_5 and C_6 nerve roots and the other used nerve graft of 3 cm in lengthTransient contralateral sensory symptoms were re- ported in most patientsAt 3 months followups6 patients had tingling sensation on the contralateral fingers with percussion on the injured cervical areaIpsilateral SSEP could be recorded by stimulating at 2 cm above sternoclavicular joint on the injured sideAt 7 months follow ups of 5 patientsCMAP could be recorded in bi- cepsdeltoids and infraspinatus or triceps with stimulation at Erb's pointHoweverno clinical movements was noticedAt 12 months follow ups of 3 patientswe could observe early motor and sensory function recovery of those patients to different extent.Conclusion Transection of anterior scalenus muscle shortens the length of the transfer route and allows more efficient neurotizationThe procedure is convenient and safeprovided certain precautions being usedThe principal of contralateral C_7 nerve transfer are reconstruct the anterior divi- sions of upper trunkposterior divisions of upper trunk and suprascapular nerve when repairing the supraclavic- ula brachial plexusReconstruct the lateral cord and posterior cord when repairing the infraclavicula brachial plexusPostsurgical fasting for 4 days included foods and liquids will benefit of healing of anastomosed nerves and regenerationaud avoid complications.

AIMTo clone and analyse the coding cDNA sequence of alpha1, beta2 and gamma2 subunit of GABAA receptor in American king Pigeon.

METHODSWithdrew total RNA from the American king pigeon brain, reverse transcribing general primers to acquire a gene set cDNA. Designing specific primers of three subunit mRNA of the GABAA receptor, by RT-PCR respectively expanded the conservative gene of al subunit, beta2 subunit and gamma2 subunit of GABAA receptor, and carried on clone, plastid identification and the sequence measurese of three genes.

RESULTSThe experiment on sequence measures has succeeded that sequence analysis indicated that lengths of the conservative gene of alpha1 subunit, beta2 subunit and gamma2 subunit of GABAA receptor was respectively 899 bp, 597 bp and 563 bp, homology on reference sequence was respectively 94.99%, 94.64% and 96.28%.

CONCLUSIONHomology is high on the conservative gene of alpha1 subunit, beta2 subunit and gamma2 subunit of GABAA receptor of brain tissue of pigeon and chicken but there is a discriminating characteristic in different kinds of animals.

Animals ; Brain ; metabolism ; Cloning, Molecular ; Columbidae ; DNA, Complementary ; genetics ; RNA, Messenger ; genetics ; Receptors, GABA-A ; classification ; genetics ; Sequence Analysis, DNA