To compare the anxiolytic effects of reduced metabolite of progesterone and benzodiazepine.Methods　The effects of allopregnanolone and diazepam on spontaneous locomotor activity and on exploration in the elevated plus-maze were studied in C57 mice 20 min after vehicle or drug intraperitoneal administration.Results Allopregnanolone (0.1 mg.kg-1,ip) elicited marked anxiolytic effects in terms of significantly reducing the latency to enter the open arm from (31.30±8.39)s to (8.80±6.00)s,(P<0.001),and significantly increasing both the number of open arm entries from 1.20 ± 0.42 to 4.80 ±1.75,(P<0.001) and the proportion of total time spent on the open arm from 7.13％ to 32.50％,(P<0.001).Meanwhile,the diazepam (0.25 mg·kg-1) produced a lower anxiolytic effect comparing to that of the allopregnanolone.Analysis of spontaneous locomotor activity showed while 0.5 mg·kg-1 of diazepam decreased the locomotor activity (P<0.01),neither 0.1 mg·kg-1 of allopregnanolone nor 0.25 mg·kg-1 of diazepam affect the locomotor activity score.Conclusion Together,these results provide evidence for differential behavioral actions of the neurosteroids and benzodiazepines.Since the allopregnanolone produce a selective anxiolytic effect without affecting the spontaneous locomotor activity,the allopregnanolone may be a better alternative for diazepam in treating anxiety.

Ten compounds were isolated from the 70% ethanol extract of linseed meal (Linum usitatissimum L) through a combination of various chromatographic techniques, including silica gel, macroporous adsorbent resin, Sephadex LH-20, and preparative HPLC. On the basis of spectroscopic data analysis, they were elucidated as 1-methylethyl-2-O-beta-D-glucopyranosyl-(1" --> 6')-beta-D-glucopyanoside (1), linustatin (2), neolinustatin (3), lotaustralin (4), linamarin (5), deoxyguanosine (6), deoxyadenosine (7), (+)-pinoresinol-4'-O-beta-D-glucopyranoside (8), 4-O-beta-D-glucopyranosylvanillyl alcohol (9) and tachioside (10), separately. Among them, compound 1 is a new compound, and compounds 6, 8 and 10 were isolated from the linseed meal for the first time.

Aim To compare the anxiolytic effects of reduced metabolite of progesterone and benzodiazepine.Methods The effects of allopregnanolone and diazepam on spontaneous locomotor activity and on exploration in the elevated plus_maze were studied in C57 mice 20 min after vehicle or drug intraperitoneal administration. Results Allopregnanolone (0.1 mg?kg-1, ip) elicited marked anxiolytic effects in terms of significantly reducing the latency to enter the open arm from (31.30?8.39)s to (8.80?6.00)s, (P

Objective To observe the expression law of cytokine signaling suppressors (SOCSs) mRNA in burn rats with Staphylococcus aureus sepsis and investigate their potential role in the pathogenesis of postburn sepsis. Methods Wistar rats were inflicted with 20% TBSA Ⅲ? scald, followed by Staphylococcus aureus challenge. Then, the expressions of SOCS1, SOCS2 and SOCS3 mRNA and interferon-? (IFN-?) levels in the liver and lungs were determined. Results With Staphylococcus aureus challenge after burn, IFN-? levels in the liver and lungs were significantly elevated and reached peak at the 0.5th and 6th hours, respectively (P

AIM: To investigate the role of staphylococcal enterotoxin B (SEB) in early intestinal injury in scald rats with Staphylococcus aureus sepsis. METHODS: 86 male Wistar rats were randomly divided into four groups as follows: normal controls ( n= 10), scald control group( n= 10), postburn sepsis group( n= 50) and SEB monoclonal antibody (MAb)treatment group ( n= 16). Plasma samples were collected to determine SEB, endotoxin, tumor necrosis factor-? (TNF-?) and interferon-? (IFN-?). RESULTS: After scald injury followed by Staphylococcus aureus challenge, the levels of SEB, TNF-? and IFN-? in plasma were significantly higher than those of normal controls, peaking at 2-6 h ( P

A new animal model of multiple system organ failure (MSOF) in rabbits is used in this experiment. The purpose of the current study is to observe dynamically the changes in the intestinal flora, the relationship between the changes and bacterial translocation to various organs and endotoxemia. The results show that there is no obvious alteration in population of Bacteroides, but a significant increase in enteric bacilli population in the contents of the ileocecum is found. Changes in the intestinal micro-flora correlate to the positive bacterial culture of the blood, viscera, and the level of endotoxin in the plasma. The results of our work suggest that ecological imbalance in the intestinal flora may promote-the gut-derived septic process and the development of MSOF.

Objective To test the hypothesis that in a rat model of acute intestinal ischemia/reperfusion injury, endotoxemia from the gastrointestinal tract would play a role in mediating tumor necrosis factor (TNF) response and remote organ dysfunction. Methods Wistar rats underwent 45 minutes of superior mesenteric artery occlusion followed by 6 hours of reperfusion. The rats were treated intravenously with either TNF monoclonal antibody (MoAb) or saline solution 90 minutes prior to the onset of ischemia. Results Significant elevation of plasma TNF level in both portal and systemic circulation was detected immediately after the onset of reperfusion. The level peaked at two hours after reperfusion (P<0.01). Similarly, a remarkable TNF mRNA expression in the intestine in controls was detected at 0.5 hour post-reperfusion, and sustained a marked elevation throughout the observation period (P<0.05-0.01). TNF elevation was found associated with gut-origin endotoxemia, and the maximal TNF response occurred approximately 0.5-2 hours after the initial appearance of endotoxin in the portal vein. Concomitantly, multiple organ dysfunction in response to local ischemic insult was also observed in untreated controls upon reperfusion, but it was significantly attenuated by pretreatment with MoAb against TNF. Conclusions Intestinal injury can result in the gut becoming a cytokine-liberating organ. The escape of endotoxin and bacteria from the gut may be responsible for the TNF expression and release, which would be an important mechanism underlying pathophysiological alterations associated with intestinal ischemia/reperfusion injury.

Objective:To investigate the correlation between plasma homocysteine (Hcy) concentration and transient ischemic attack (TIA) and traditional vascular risk factors.Methods:The plasma Hcy concentrations of 112 patients with TIA and 62 controls were measured by fluorescenee polarization immunoassay.Hcy concentrations and related risk factors were analyzed.Results:The risk of TIA was increased significantly in plasma Hcy concentration 10.0 to 14.9 μmol/L group(OR=2.450,95% CI 1.091 to 5.502) and≥15.0 μmol/L group(OR=5.169,95% CI 2.096 to 12.746) compared with plasma Hcy concentration＜10.0 μmol/L group.Using TIA as the dependent wariable,various vascular risk factors (including plasma Hcy concentration) as the independent variable,logistic regression was analyzed.The result showed that the risk of TIA was increased significantly in plasma Hcy concentration＞10.0 μmol/L group compared with plasma Hcy concentration＜10.0 μmol/L group(OR=3.150,95% CI 1.380 to 7.192).Conclusions:Plasma Hcy concentration is an independent risk factor for TIA.

AIMTo synthesizs of derivatives of (9S)-12-methylene erythromycin possessed potent antibacterial activity.

METHODSUsing erythromycin A as a starting material, via two intermediate compounds protected 12,21-dehydroerythromycin A and 6,7: 12,21-didehydro erythromycin A, several 9-O, 11-O-ethylidene compounds were obtained. During this process, benzyl and isopropyl have been selected as the protecting group. The structures of compounds obtained were confirmed with 13C NMR and MS-FAB. Their antibacterial activity in vitro was tested.

RESULTSEleven derivatives of erythromycin were synthesized. Five of them were unknown compounds.

CONCLUSIONThe preliminary biological test showed that two target compounds exhibited less potent antibacterial activity in vitro.

Anti-Bacterial Agents ; chemical synthesis ; pharmacology ; Erythromycin ; analogs & derivatives ; chemical synthesis ; pharmacology ; Microbial Sensitivity Tests ; Staphylococcus aureus ; drug effects ; Staphylococcus epidermidis ; Streptococcus pneumoniae ; drug effects

OBJECTIVETo explore clinical effects of suturing-assisted locking plate in treating elderly proximal humeral fractures.

METHODSFrom January 2005 to January 2013, 55 elderly patients with three- and four-part fractures of proximal humeral fractures were divided into treatment group and control group. In treatment group, there were 31 patients including 12 males, and 19 females aged from 65 to 85 with an average of (74.00±5.42) years old, and treated with suturing-assisted locking plates; 19 patients were Neer 3-part fractures, and 12 patients were Neer 4-part fractures of proximal humerus; 23 patients were suffered from low-energy injuries and 8 patients were caused by high-energy injuries. In control group, there were 24 patients including 7 males, and 17 females aged from 65 to 85 with an average of (72.79±5.34) years old, and treated with locking plates; 16 patients were Neer 3-part fractures, and 8 patients were Neer 4-part fractures of proximal humerus; 17 patients were suffered from low-energy injuries and 7 patients were caused by high-energy injuries. Operative time, blood loss during operation, and bone healing time between two groups were observed and compared. Postoperative Neer scoring were used to evaluate recovery of shoulder joint function.

RESULTSAll patients were followed up from 6 to 24 months with an average of 16.1 months. In treatment group, blood loss was (495.806±143.150) ml, function of Neer scoring was 22.645±2.443, range of action was 18.194±2.613, anatomy was 7.935±1.504 and total score of Neer scoring was 77.161±8.335; while in control group, blood loss was (641.667±169.851) ml, function of Neer scoring was 13.958±1.989, range of action was 13.083±2.165, anatomy was 5.500±1.978 and total score of Neer scoring was 58.792±7.313. There were sigificant difference between two groups in these indexes.

CONCLUSIONSuturing-assisted locking plate for the treatment of proximal humerus fractures in elderly, has advantages of less blood loss, simple fracture reduction and rapid recovery of shoulder joint, and is a effective method.

Aged ; Aged, 80 and over ; Bone Plates ; Case-Control Studies ; Female ; Humans ; Male ; Recovery of Function ; Shoulder Fractures ; physiopathology ; surgery ; Shoulder Joint ; physiopathology ; Sutures