1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine ; Animals ; Female ; MPTP Poisoning ; drug therapy ; pathology ; physiopathology ; Male ; Materia Medica ; therapeutic use ; Mice ; Mice, Inbred C57BL ; Microglia ; drug effects ; pathology ; Parkinson Disease, Secondary ; chemically induced ; drug therapy ; physiopathology ; Scorpion Venoms ; chemistry

The effect of tranilast on the down- regulation of beta- adrenoceptor agonist was investigated. Male guinea pigs were divided into 3 groups, one group is control. Others were received injection of terbutaline or terbutaline plus tranilast for successive 5 days. The radioli-gand binding assays for beta-adrenoceptors in the lung membranes of the guinea pigs were per-formed. The results showed the numbers of maximal binding sites (Bmax) of beta-adrenoceptors in terbutaline group was significantly less than that in control group ( P 0. 05).The affinity ( Kd) of beta-adrenoceptors both in terbutaline group and in terbutaline plus tranilast group was higher than that in control (P

Connexin 43 ; genetics ; Connexins ; genetics ; Heart Defects, Congenital ; genetics ; Homeobox Protein Nkx-2.5 ; Homeodomain Proteins ; genetics ; Humans ; Infant ; Infant, Newborn ; Mutation ; genetics ; Myocardium ; metabolism ; Transcription Factors ; genetics

Objective To investigate the minimal and optimal concentration of ropivacain for epidural anesthesia in patients with breast cancer.Methods 103 patients with breast cancer ASA Ⅰ-Ⅱ undergoing elective radical mastectomy were conducted with epidural anesthesia.T2-3 were selected as a puncture site.A catheter was inserted into the epidural space in a cephalic direction for 3.5-4.0 cm.The concentration of ropivacain was produced by the test of up-down sequential allocation technique.20-25 ml of 0.20 ％ ropivacaine was given after a test of 0.20 ％ 5 ml ropivacaine.If the anesthesia was effective (VAS≤3),the next concentration was down 0.01％,while the VAS was more than 5,the next concentration was up 0.01％.The anesthesia effect and segments of block were measured with acupuncture.Blood pressure (NIBP),heart rates(HR),blood oxygen saturation (SPO2),blood gas and VAS were monitored during operation.Nasal catheter oxygen inhalation was used in routine method.Results The median effective concentration (EC50) of ropivacaine was 0.10 ％ determined by the formula of dixon and massey.The 95 ％ confidence intervals was 0.1022 ％-0.1065 ％.The least and the best analgesic concentration of ropivacaine for the upper thoracic epidural block was 0.14 ％ and 0.17 ％-0.18 ％ respectively.Conclusion The minimal and the optimal analgesic concentration of ropivacaine for the upper thoracic epidural block are 0.14 ％ and 0.17 ％-0.18 ％respectively,and which provides a safe and rational use of ropivacaine for the clinic.

Aim To investigate the effect of asiatic acid on apoptosis and autophagy in human glioblastoma T98G cells. Methods MTT colorimetry was employed to assay the cellular proliferating activity. The fluores-cence microscope and Hoechst 33258 staining were used to detect the morphological changes. The cell ap-optosis and autophagy were analyzed by flow cytometry with Annexin-V/7-AAD and MDC staining respective-ly. The expressions of associated proteins were detected by Western blot to analyze the mechanism of apoptosis and autophagy. Results MTT assay showed that the growth of T 9 8 G cells was inhibited by asiatic acid ( IC50 =46. 3 μmol · L-1 ) . Annexin V/7-AAD stai-ning and Western blot revealed that asiatic acid in-duced apoptosis in T98 G cells by reducing the expres-sion of Akt, decreasing the mitochondrial membrane potential, and increasing the expression of Caspase-3. MDC staining and Western blot showed that the per-centage of MDC-positive cells was decreased and the expressions of Beclin-1 , LC3-II and Atgs were inhibi-ted by asiatic acid treatment. 5 μmol·L-1 chloroquine was used to up-regulate the expressions of LC3-Ⅱand Beclin-1 . Asiatic acid-inhibited autophagy was blocked and the total apoptotic rate was reduced remarkably. Conclusion Asiatic acid suppresses T98 G cells pro-liferation by inducing apoptosis and inhibiting cell au-tophagy, and the very role of inhibiting autophagy could promote apoptosis to a certain extent.

Thorough excavation and artful utilization of various kinds concrete and invisible learning resources contribute to the cultivation of excellent postgraduates.In postgraduate education of anesthesiology Xuzhou Medical College utilizes time,network,technique platform,research outcome,self-potentiality and clinical patients resources,which produces an active effect and has important instructional significance.

This research aims to construct a lentiviral expression vector carrying the extracelluar domain (ED) of human hepatocyte growth factor receptor (C-Met), and to express it in transfected 293T cells. The extracellular domain of C-Met was amplified by RT-PCR, ligated with lentiviral expression vector p RRL-CMV-ED, and then expressed in 293T cell line. The expressed protein was purified and identified by RT-PCR and Western blot. The enzyme digestion and sequence analysis showed that the lentiviral expression vector p RRL-CMV-ED was constructed correctly. The size of amplified genes was about 2 700 bp. The purified protein with Ni-affinity column was about 105 kD analyzed by SDS-PAGE. The Western blot and ELISA results showed that the expressed protein which could bind to HGF specifically was the extracelluar domain of human hepatocyte growth factor receptor. This research may lay a foundation for further study of anti-C-MET monoclonal antibody and neutralizing antibody.
Genetic Vectors ; HEK293 Cells ; Humans ; Lentivirus ; Proto-Oncogene Proteins c-met ; genetics ; metabolism ; Transfection

Poly(ADP-ribose)polymerase-1 (PARP-1) plays a significant role in the DNA repair process by catalyzing the transfer of ADP-ribose from NAD+ to its receptors. It is a promising anticancer drug target and many PARP-1 inhibitors have been developed and used in the clinical trial. In this work, a series of 3-(2-oxo-2-substituted acetamido)benzamides have been synthesized and their inhibitory activities against PARP-1 were evaluated. Of all the tested compounds, six compounds displayed inhibitory activities with IC50 values ranging from 0.23 to 5.78 µmol.L-1 . The binding pose of compound 5a was predicted using molecular docking to facilitate further structural modification.
Antineoplastic Agents ; Benzamides ; chemistry ; DNA Repair ; Drug Design ; Humans ; Molecular Docking Simulation ; Poly(ADP-ribose) Polymerase Inhibitors ; chemical synthesis ; chemistry ; Poly(ADP-ribose) Polymerases

The compatibility of traditional Chinese medicines (TCMs) formulae containing enormous information, is a complex component system. Applications of mathematical statistics methods on the compatibility researches of traditional Chinese medicines formulae have great significance for promoting the modernization of traditional Chinese medicines and improving clinical efficacies and optimizations of formulae. As a tool for quantitative analysis, data inference and exploring inherent rules of substances, the mathematical statistics method can be used to reveal the working mechanisms of the compatibility of traditional Chinese medicines formulae in qualitatively and quantitatively. By reviewing studies based on the applications of mathematical statistics methods, this paper were summarized from perspective of dosages optimization, efficacies and changes of chemical components as well as the rules of incompatibility and contraindication of formulae, will provide the references for further studying and revealing the working mechanisms and the connotations of traditional Chinese medicines.
Chemistry, Pharmaceutical ; statistics & numerical data ; Data Interpretation, Statistical ; Drug Incompatibility ; Drugs, Chinese Herbal ; analysis ; Medicine, Chinese Traditional

Objective To study the clinical value of transcervical resection under hysteroscope in treatment of placental remnants.Methods From March 2003 to April 2006,14 cases of placental remnants were treated with transcervical resection under hysteroscope.They included 3 cases of term birth,and 11 cases of midtrimester induction of labor.Drug pretreatment was performed for those who had more than 80 U/L of blood beta-human chorionic gonadotropin (?-hCG) level,including mifepristone (RU486), Chinese herbs and methotrexate(MTX).RU486 was taken orally at 25 mg,three times daily and misoprostol was given 600 ?g at one dose on the third day.MTX was given by deep intramuscular injection at 1 mg/m~2 if ?-hCG was higher than 150 U/L.Bipolar evaporation was used in the operation with alternation of resection and forceps holder under ultrasonographic supervision.After operation a circular contraceptive device was placed followed by hormone periodic treatment such as estradiol valerate for 2-4 months.Results Under the monitoring by ultrasonography,14 operations were all performed smoothly.The follow-up was from 6 months to 2 years.Menstruations in almost all the cases were recovered,and 3 cases of those were pregnant and delivered smoothly 4,6 and 7 months after operation.Conclusion The transcervical resection under hysteroscope is useful in treatment of placental remnants with obvious effects,little trauma and few complications.