To explore new agents of gamma-aminobutyric acid (GABA) derivatives with more potent antiepileptic activity, a series of 4-(2-acetoxybenzoylamino) butyramide derivatives were designed and synthesized. All of the novel compounds (5a-51) were synthesized from GABA as starting material, and their structures were confirmed with IR, 1H NMR, EI-MS and elemental analysis. Preliminary pharmacological test in vitro showed that all target compounds displayed strong antiepileptic activities and were worth for further study. The structure-activity relationship of 4-(2-acetoxybenzoylamino) butyramide derivatives was also discussed preliminarily.

Accidents, Occupational ; Humans ; Hydrogen Sulfide ; poisoning

Coccidioides ; Coccidioidomycosis ; pathology ; Humans ; Infant ; Male

Adult ; Female ; Humans ; Insecticides ; poisoning ; Ivermectin ; analogs & derivatives ; poisoning ; Male ; Middle Aged

Objective To investigate the clinical efficacy of nephrotic syndrome in children adjunctively treated by underatured lactalbumin.Methods Thirty-six cases of nephrotic syndrome were studied for about 1 year.The changes in red blood cells of reduced glutathione(GSH) were analyzed in 18 cases of underatured lactalbumin treatment group and 18 cases of control group.The clinical presentations were observed in both groups.Results GSH levels increased in underatured lactalbumin treatment group when compared with control group.The frequency of relapse and upper respiratory tract infection in underatured lactalbumin treatment group were significantly reduced compared with control group.Conclusion Underatured lactalbumin can provide support for the potential use of an antioxidant therapy in these patients.

OBJECTIVEThe present study was undertaken to design antisense oligodeoxynucleotides (AS-ODNs) of glial glutamate transporter-la (GLT-1a) and to evaluate the effectiveness of the designed AS-ODNs on the expression of GLT-1a.

METHODSFive sequences of GLT-1a AS-ODNs were designed according to the C terminus specific sequences of GLT-1a mRNA using antisense design software of IDT Com- pany. Western blot analysis was used to evaluate the inhibition effects of the five GLT-1a AS-ODNs on the expression of GLT-la.

RESULTSThe sequence of GLT-1a AS-ODNs with sequence of 5'-GGTTCTTCCTCAACACTGCA-3' could specifically inhibit the expression of GLT-1a in the hippocampal CA1 subfield of rats, while it had no effect on the expression of GLT-1b. This sequence showed similar inhibition on the expression of GLT-la in sham and ceftriaxone (Cef)-treated rats. It could also significantly inhibit the cerebral ischemic preconditioning (CIP)-induced up-regulation in the expression of GLT-1a. The magnitude of the inhibition in sham, Cef- or CIP-treated rats was similar by more than 60%.

CONCLUSIONFrom the designed five sequences of GLT-1a AS-ODNs, we obtained an effective sequence which can specifically inhibit the expression of GLT-1a.

Animals ; CA1 Region, Hippocampal ; metabolism ; Excitatory Amino Acid Transporter 2 ; antagonists & inhibitors ; metabolism ; Ischemic Preconditioning ; Oligonucleotides, Antisense ; genetics ; RNA, Messenger ; Rats ; Up-Regulation

To evaluate the regulating effect of Buyang Huanwu decoction and its simple prescription (Naojian tablet) on CDK4/Cyclin D1 expression in hippocampus tissues of rats with cerebral ischemia, SD rats were divided into the sham-operation group, the model group, the Buyang Huanwu decoction group (ig, 3.15 g · kg⁻¹) and the simple prescription group (ig, 2.41 g · kg⁻¹). Each group was further divided into five subgroups based on time points after the administration, i. e. 1 d, 3 d, 7 d, 14 d and 28 d, respectively. CDK4/Cyclin D1 expressions of the group at different time points were examined by using immunohistochemistry and real-time qPCR. According to the results, the cerebral ischemia model group showed higher CDK4/Cyclin D1 expression than the sham-operation groups (P < 0.05), suggesting that the cell cycle signal pathway would be activated by the cerebral ischemic injury. Both Buyang Huanwu decoction and simple prescription groups showed significantly lower cyclin expression than the model group at 3 d, 7 d, 14 d, 28 d (P < 0.05), indicating both Buyang Huanwu decoction and its simple prescription could play the neuroprotective effect through the cell cycle signal pathway.
Animals ; Brain Ischemia ; drug therapy ; genetics ; metabolism ; physiopathology ; Cell Cycle ; drug effects ; Cyclin D1 ; genetics ; metabolism ; Cyclin-Dependent Kinase 4 ; genetics ; metabolism ; Drugs, Chinese Herbal ; administration & dosage ; Humans ; Male ; Rats ; Rats, Sprague-Dawley

Objective To compare the efficacy of thrombus aspiration catheter combined with intracoronary tirofiban and nitroglycerol injection through the aspiration catheter versus the guiding catheter during primary percutaneous coronary intervention (PCI) in patients with acute ST-segment elevation myocardial infarction (STEMI).Methods Thirty-four patients with STEMI undergoing primary PCI and receiving thrombus aspiration catheter combined with intracoronary tirofiban and nitroglyeerol injection through the aspiration catheter were enrolled as the aspiration group (n =34),and those who had similar coronary angiography results and basic characteristics but receiving thrombus aspiration catheter combined with intracoronary tirofiban and nitroglycerol injection through the guiding catheter were served as the guiding group ( n =33 ).The outcomes of the two groups were observed and compared.Results There was no significant change of blood pressure between before and after injection in the aspiration group ( P ＞ 0.05 ),but the change of blood pressure was significant after injection compared with before injection in the guiding group ( P ＜ 0.01 ).The cTn-I,BNP,peak-value of CK-MB,peak-time of CK-MB,TIMI grade 3 flow,slow-reflow in IRA after PCI in the aspiration group were superior to those in the guiding group ( t =3.92,P ＜ 0.01 ;t =4.70,P ＜ 0.01 ; t =3.39,P ＜ 0.01 ; t =7.17,P ＜0.01 ; x2 =3.877,P ＜ 0.05 ; x2 =3.876,P ＜ 0.05 ).LVEF,LVEDd and LVESd after 1 month in the aspiration group were superior to those in the guiding group (t =5.99,P ＜ 0.01 ;t =4.53,P ＜ 0.01 ;t =8.12,P ＜ 0.01 ),but no significant differences of LVEF,LVEDd,LVESd were found after 1 week resolution of sum of ST-segment elevation and the MACE rates after PCI were found between the two group ( P ＞ 0.05 ).Conclusion Application of thrombus aspiration catheter combined with intracoronary tirofiban injection through the aspiration catheter is more effective than through the guiding catheter in patients with Acute ST-segment elevation myocardial infarction,which could decrease slow-reflow phenomenon and improve re-perfusion and left ventricular function with better clinical outcomes.

Objective To develop a multiplex PCR-based reverse line blot(mPCR/RLB) hybridization assay to detect,simultaneously,seven genes encoding AR-erm(A/TR),erm(B),mef(A/ E),tet(M),tet(O),aphA-3,aad-6 and two AR-related genes,int-Tn and mreA in group B streptococcus.Methods Nine pairs of specific primers and Oligonucleotide probes targeting erm(A/TR), erm(B),mef(A/E),tet(M),tet(O),aphA-3,aad-6 int-Tn and mreA respectively were modified according to former studies or designed in this study.The primers and probes were labeled with biotin and amino,respectively.The nine genes were amplified simultaneously in the same tube.PCR product hybridized with the probes labeled in the BiodyneC nylon membrane to detect the nine genes.To detect the sensitivity and specificity of the method developed,PCR with single pair of primer targeting each gene were tested in 318 isolates tested and the results were compared with the one abtained by RLB.Results The nine resistance-related genes could be successfully detected by mPCR/RLB assay developed in this study.Based on sequencing,21 of 22 isolates with mef had mef(E)and eight of 353 with int-Tn had an atypical sequence.Except for the above 29 genes,all the others corresponded well with the results obtained by single pair primer PCR.Conclusion The mPCR/RLB assay developed in this study is simple,rapid and suitable for surveillance of antibiotic resistance in GBS.