Objective To investigate the rat bone structural changes of lower limb following lumbar nerve dorsal roots section.Methods Forty-eight mature female Wistar rats were divided into posterior radi- cotomy(PR)and comtrol groups randomly.The bilateral femoral bone mineral density(BMD)and biome- chanics characteristics were analyzed 2,4 and 8 weeks after the radicotomy.The same operation except the radicotomy was done in the sham group.Results In PR group,2,4,and 8 weeks after the radicotomy,the BMD of femur was(0.221?0.008)g/cm~3,(0.213?0.015)g/cm~3 ,and(0.216?0.105)g/cm~3 ,respective- ly;while that was(0.223?0.005)g/cm~3,(0.218?0.014)g/cm~3 ,and(0.208?0.111)g/cm~3 in control group.No significant difference was observed between the two groups(P＞0.05).In PR group,2,4,and 8 weeks after the operation,the mean maximum load in three-point bending test of femun midshaft was(93.64?8.76)N,(89.77?11.18)N and(93.21?8.74)N,respectively,and was lower than the values of the con- trol group at the same time point(95.94?6.29)N,(91.63?9.43)N,(95.57?8.64)N,However,there was no significant difference between the two groups(P＞0.05).Accordingly,there was no significant difference in the energy absorption in femun midshaft between the two groups(P＞0.05).Conclusion The selective rhizotomies of part lumbar never dorsal roots might not cause the loss of the femur BMD and the change of bio- mechanics property significantly in short period.

Cerebrospinal Fluid Rhinorrhea ; diagnosis ; etiology ; Chondrosarcoma ; surgery ; Endoscopy ; Enterococcus ; pathogenicity ; Humans ; Male ; Meningitis ; diagnosis ; microbiology ; Middle Aged ; Skull Base ; pathology ; surgery

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OBJECTIVETo build 3D-pharmacophore model of epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors using distance comparisons method and design novel EGFR inhibitors.

METHODSThirteen typical EGFR inhibitors were selected, and their biologically active conformations were obtained by using DOCK5.0 program, then 3D-pharmacophore model of EGFR inhibitors was built using distance comparisons method.

RESULTSValidation of the 3D-pharmacophore model was carried out and novel structures with potential inhibitory activity were selected by means of 3D-searching and docking method.

CONCLUSIONThis method can improve hit rate of lead compounds discovery and can be used to design novel EGFR inhibitors.

Drug Design ; Enzyme Inhibitors ; Epidermal Growth Factor ; metabolism ; Models, Chemical ; Protein-Tyrosine Kinases ; antagonists & inhibitors ; chemistry ; pharmacology ; Receptor, Epidermal Growth Factor ; antagonists & inhibitors ; chemistry ; Structure-Activity Relationship

Objective To explore acute toxicity of succimer on mice.Methods Twenty Kunming mice(10 males and 10 females) weighting approximately (21.2?2.3)g were acclimatized for 3 days prior to dosing,then were divided into control group and experiment group with 10 mice in each group according to body weight.Fasted for 12 hours,the mice in experiment group received intragastric administration of 160mg DMSA in deionized water in 24 hours,and the control group received the same volume of deionized water,and then they were observed for 7 days.Blood was collected into heparinized-tubes by removal of eyeball.All mice were sacrificed and brain,heart,liver and kidney were removed and washed with normal saline.The activity or amount of BUN,Scr,AST,ALT,SOD, GSH-PX and MDA were analyzed.Results (1)Given 160rag DMSA in 24 hours,gastrointestinal symptoms were main side effects.During the observation,experiment group lost weight due to the decrease of food-intake ,and some mice had slight hydroabdomen.(2)High dose of DMSA caused a significant inhibition of GSH-PX(P0.05).The hepatic cell was damaged accord- ing to the significant raise of MDA in liver(P0.05),which was related to acute toxicity on liver.Conclusion Succimer could inhibit the antioxidarrt systems and could do damage to liver and kidney.

AIMDesign, synthesis and evaluation of a series of 7-imidazolylalkanamido-1-carboxylalkylbenzodiazepine farnesyltransferase (FTase) inhibitors.

METHODS AND RESULTSCoupling of imidazolylalkylcarboxylic acids and 1-substituted 7-aminobenzodiazepines (5a-5c) yielded 10 new compounds (6-12, 16-18) which were biologically tested against FTase using scintillation proximity assay method.

CONCLUSIONFive target compounds were found to be potential farnesyltransferase inhibitors.

Alkyl and Aryl Transferases ; antagonists & inhibitors ; drug effects ; Benzodiazepines ; chemical synthesis ; chemistry ; pharmacology ; Farnesyltranstransferase ; Imidazoles ; chemical synthesis ; chemistry ; pharmacology ; Inhibitory Concentration 50 ; Molecular Conformation ; Molecular Structure ; Structure-Activity Relationship

Adult ; Aged ; Female ; Humans ; Hypertension, Portal ; etiology ; surgery ; Liver Cirrhosis ; complications ; surgery ; Male ; Middle Aged ; Portasystemic Shunt, Transjugular Intrahepatic ; methods

AIMTo investigate the in vitro and in vivo stability of 9-nitrocamptothecin lactone form in rat plasma.

METHODSThe specific and accurate HPLC method was developed for quantifying 9-nitrocamptothecin lactone form and the total lactone and carboxylate forms simultaneously. By using of this method, the ratios of lactone form to the total in rat plasma at different time were determined in vitro and in vivo. The results were compared to determine which was the main factor influencing the stability of 9-nitrocamptothecin lactone form in rat plasma in vivo.

RESULTSThe stability of lactone form in rat plasma was much higher in vivo than that in vitro.

CONCLUSIONBlood cells help to increase the stability of 9-nitrocamptothecin lactone form. Clearance from blood in vivo is the primary factor which influences the plasma stability of 9-nitrocamptothecin lactone form. The kinetic process of 9-nitrocamptothecin lactone form and total drug in rats were both best fitted to a two-compartment model. However, the process of 9-nitrocamptothecin carboxylate form in vivo was best fitted to a one-compartment model.

Animals ; Antineoplastic Agents ; blood ; pharmacokinetics ; Area Under Curve ; Camptothecin ; analogs & derivatives ; blood ; pharmacokinetics ; Carboxylic Acids ; blood ; pharmacokinetics ; Chromatography, High Pressure Liquid ; methods ; Drug Stability ; Lactones ; blood ; pharmacokinetics ; Male ; Rats ; Rats, Sprague-Dawley

Female ; Humans ; Middle Aged ; Neuroma, Acoustic ; complications ; Subarachnoid Hemorrhage ; etiology

OBJECTIVETo investigate the feasibility of removing extracranial trigeminal schwannomas located in the infratemporal fossa by using a purely endoscopic endonasal approach.

METHODSFrom November 2004 to July 2009, 8 patients with extracranial trigeminal schwannomas located in the infratemporal fossa (4 male patients and 4 female patients, age ranged 31 - 62 years) were surgically treated by using a purely endoscopic endonasal approach.

RESULTSThe maximum diameters of the tumors ranged from 3 to 7 cm. All tumors were completely removed. The operation time was 40 to 120 min, blood loss was 300 to 1500 ml. The clinical symptoms of some patients were relieved or improved. There were no intraoperative and postoperative complications, no deaths in this series. No relapse happened during the follow-up.

CONCLUSIONSThe purely endoscopic endonasal approach may provide a minimally invasive and safe approach to remove extracranial trigeminal schwannomas extending into the infratemporal fossa. Radical resection is associated with an excellent long-term outcome in this series.

Adult ; Endoscopy ; methods ; Feasibility Studies ; Female ; Follow-Up Studies ; Humans ; Male ; Middle Aged ; Neurilemmoma ; surgery ; Nose ; surgery ; Trigeminal Nerve