OBJECTIVETo investigate the situation of antibiotic resistance of Streptococcus pneumoniae (Sp) and Hemophilus influenzae (Hi) clinical isolates from children in Guangzhou area.

METHODSThe authors cultured, isolated and identified the Sp and Hi strains from nasopharyngeal secretion of patients who visited Guangzhou Children's Hospital for upper respiratory tract infection between 2003 and 2004. K-B disc diffusion and E-test for antibiotic susceptibility were performed for these clinical isolates.

RESULTSTotally 172 and 484 strains of Sp and Hi were respectively isolated from nasopharyngeal secretions in the hospital. For Sp strains, the rates of resistance to penicillin, amoxicillin/clavulanic acid, ceftriaxone, cefuroxime, cefaclor, erythromycin, tetracycline, chloramphenicol, sulfamethoxazole/trimethoprim (SMZ/TMP), clindamycin and ofloxacin were 32.0%, 11.1%, 32.6%, 18.1%, 39.5%, 82.6%, 78.5%, 24.4%, 87.2%, 69.2% and 3.1%, respectively. The penicillin non-susceptible Sp (PNSSP) isolates showed higher rates of resistance to other antimicrobial agents such as other beta-lactam antimicrobial agents, erythromycin, and SMZ/TMP than those of penicillin susceptible Sp (PSSP) isolates. More than 90% of PNSSP were multidrug resistant strains. The average rate of beta-lactamase production among 484 strains of Hi was 29.5% (143/484). For Hi isolates, the rates of resistance to ampicillin, amoxicillin/clavulanic acid, ceftriaxone, cefuroxime, cefaclor, SMZ/TMP, tetracycline, chloramphenicol, azithromycin, and ofloxacin were 40.1%, 3.4%, 4.1%, 1.9%, 5.6%, 56.2%, 52.1%, 17.4%, 2.1%, and 0.6%, respectively.

CONCLUSIONThe antimicrobials resistant Sp and Hi isolated from children with respiratory tract infection in the area have become a severe problem. The rate of resistance to penicillin of Sp had been decreased compared with the last three years, but the rate of resistance to ceftriaxone of Sp increased, and the multidrug resistance rates of PNSSP was rather high. PNSSP was characterized by a multidrug-resistance to erythromycin, tetracycline and SMZ/TMP. beta-lactamase production and ampicillin resistance among the Hi isolates from children in the area had increased generally during the period 2003 - 2004. The Hi isolates were more susceptible to the second and the third generation cephalosporins, amoxicillin/clavulanic acid and azithromycin.

Anti-Bacterial Agents ; pharmacology ; Child, Preschool ; China ; Drug Resistance, Bacterial ; Female ; Haemophilus Infections ; drug therapy ; microbiology ; Haemophilus influenzae ; drug effects ; isolation & purification ; Humans ; Infant ; Infant, Newborn ; Male ; Microbial Sensitivity Tests ; Nasopharynx ; microbiology ; Pneumonia, Pneumococcal ; drug therapy ; microbiology ; Respiratory Tract Infections ; drug therapy ; microbiology ; Streptococcus pneumoniae ; drug effects ; isolation & purification

OBJECTIVETo explore the analgesia of oxymatrine (OMT) affecting high voltage-dependent calcium channels (HVDCCs) and GABA release under neuropathic pain condition.

METHODSTotally 66 C57BL/6 mice were randomly divided into the sham-operation group, the model group, and the OMT group, 22 in each group. Neuropathic pain models were established by partial sciatic nerve ligation (PSNL). Hind paw plantar mechanical response threshold (MWT) was measured by up-and-down method with Von-Frey filament. mRNA expression of HVDCCs in brains and spinal cords was detected with Real-time PCR and concentration of GABA was determined using ELISA kit.

RESULTSCompared with day 0, the left hind paw MWTwas decreased on day 7, 10, and 14 in the model group (P < 0.05). Compared with the sham-operation group, the left hind paw MWT was significantly reduced in the model group on day 7 (P < 0.05). The MWT of PSNL ipsilateral hind paw was decreased on day 7 before OMT administration, when compared with day 0 (P < 0.05), and increased after OMT administration (P < 0.05). Compared with the sham-operation group, mRNA levels of Cav1.2, Cav1.3, Cav2.1, and Cav2.3 in brain tissues were increased and those of Cav2.2 were decreased significantly in the model group (P < 0.05). In spinal cord tissues, mRNA levels of Cav1.2 and Cav1.3 were increased, but those of Cav2.1, Cav2.2, and Cav2. 3 were decreased significantly in the model group, when compared with those of the sham-operation group (P < 0.05). Compared with the model group, mRNA levels of Cavl.2, Cavl.3, Cav2.1, and Cav2. 3 in brain tissues were decreased, and those of Cav2.2 were increased significantly in the OMT group (P < 0.05). In spinal cord tissues of the OMT group, mRNA levels of Cav1.3 decreased and those of Cav2.1, Cav2.2, and Cav2.3 increased significantly with statistical difference, when compared with those of the model group (P < 0.05). Compared with the sham-operation group, GABA levels in brain tissues decreased in the model group (P < 0.05). Compared with the model group, GABA levels in brain tissues increased in the OMT group (P < 0.05). There was no statistical difference in GABA levels of spinal cord tissues among these groups (P > 0.05).

CONCLUSIONSOMT had analgesic effect on neuropathic pain, which might be probably related to HVDDCs. Cav2.2 might directly affect GABA release.

Alkaloids ; pharmacology ; therapeutic use ; Analgesia ; methods ; Animals ; Calcium ; Calcium Channels ; drug effects ; metabolism ; Disease Models, Animal ; Mice ; Mice, Inbred C57BL ; Neuralgia ; drug therapy ; Pain Management ; Quinolizines ; pharmacology ; therapeutic use ; Spinal Cord ; metabolism ; gamma-Aminobutyric Acid

OBJECTIVETo study the distribution and antibiotic resistance of the isolated pathogens from children with infectious diarrhea in Guangzhou.

METHODSThe fecal samples of 2 409 children with infectious diarrhea between January 2006 and December 2007 were collected and cultured. Pathogenic bacterium were isolated and identified by biochemical and serological methods. The antibiotic susceptibilities were tested by the Kirby-Bauer method.

RESULTSA total of 448 isolates of pathogenic bacterium (18.6%) were obtained, including Shigella (n=159), enteropathogenic Escherichia coli (n=141), Salmonella (n=76), Vibrion (n=11), fungus (n=41), and C jejuni (n=20). All of isolates of the three major pathogenic bacterium, Shigella, enteropathogenic Escherichia coli and Salmonella, were susceptible to imipenem and less than 10% of the isolates were resistant to the third generation cephalosporins and beta-lactamase inhibitors. However, the isolates showed a high resistance to ampicillin and sulfamethoxazole/trimethoprim (>75%).

CONCLUSIONSShigella, enteropathogenic Escherichia coli and Salmonella were major pathogenic bacterium of diarrhea in children from Guangzhou. The major isolates were susceptible to imipenem, the third generation cephalosporins and beta -lactamase inhibitors, but were resistant to ampicillin and sulfamethoxazole/trimethoprim.

Adolescent ; Bacteria ; drug effects ; isolation & purification ; Child ; Child, Preschool ; Diarrhea ; drug therapy ; microbiology ; Drug Resistance, Microbial ; Female ; Fungi ; drug effects ; isolation & purification ; Humans ; Infant ; Male

OBJECTIVETo investigate the antimicrobial resistance and penicillin resistance-associated genes (TEM and pbp2B) of Streptococcus pneumoniae (S. pneumoniae) isolated from sputum specimens of Guangzhou children with respiratory tract infection.

METHODSE-test and Kirby-Bauer methods were applied to detect the antibiotic susceptibility of 44 strains of S. pneumoniae. PCR was used to detect resistance genes pbp2B and TEM, followed by DNA sequence analysis of pbp2B gene. The sequence results were compared to those of penicillin-susceptible S. pneumoniae R6.

RESULTSOf the 44 isolates of S. pneumoniae, only 5 (11.4%) were susceptible to penicillin. All strains were resistant to erythromycin but susceptible to ofloxacin and vancomycin. The resistance rate of the isolates to clindamycin and trimoxazole was more than 90%. The S. pneumoniae isolates showed a high susceptibility to amoxicillin, imipenem and ceftriaxone, with a resistance rate of 0, 2.6% and 3.9%, respectively. The sequence analysis showed that more than 99% nucleotide sequence of pbp2B gene of five penicillin-susceptible isolates was the same as penicillin-susceptible S. pneumoniae R6, without any amino acid replacement. Site mutation was found in the remaining 39 penicillin-nonsusceptible isolates with a nucleotide mutation rate ranging from 13.2% to 23.1% and amino acid replacement rate from 6.5% to 10.9%. The 39 penicillin-nonsusceptible isolates were classified into 4 types according to the mutation site between Ser391 and Thr492 of pbp2B: type I (n=30), type II (n=7), type III (n=1) and type IV (n=1). No TEM gene was detected in all the 44 S. pneumoniae isolates.

CONCLUSIONSThe S.pneumoniae isolates from Guangzhou children with respiratory tract infection are resistant to penicillin and erythromycin. Amoxicillin and the third generation cephalosporin may be recommended for treating S. pneumoniae infection. The mutation of pbp2B gene plays an important role in the development of S. pneumoniae resistance to penicillin.

Aminoacyltransferases ; genetics ; Child, Preschool ; Drug Resistance, Bacterial ; genetics ; Female ; Humans ; Infant ; Male ; Microbial Sensitivity Tests ; Penicillin Resistance ; genetics ; Penicillin-Binding Proteins ; genetics ; Respiratory Tract Infections ; microbiology ; Streptococcus pneumoniae ; drug effects ; genetics ; beta-Lactamases ; genetics

Objective To evaluate the feasibility of 3-(4-~(18)F-fluorobenzyl)-8,9-dimethoxy-1,2,3,4-tetrahydrochromeno [3,4-c]pyridin-5-one ( is F-FDTP) as a potential dopamine D4 receptor PET imaging agent.Methods ~(18)F-FDTP solution in ethanol-physiological saline was incubated with calf serum to test its in vitro stability through the determination of radiochemical purity.Normal rats were injected intravenously with ~(18)F-FDTP and then sacrificed at 2,5,10,15,30,60 and 120 min after anesthesia.Blood,organs and brain tissue samples were collected.All samples were weighed and measured for radioactivity.The uptake of samples was expressed as percentage activity of injection dose per gram of tissue ( % ID/g).Results The stability of ~(18)F-FDTP was satisfactory and its radiochemical purity was above 95% after incubation 120 min at 37℃ in calf serum.The biodistribution showed that ~(18)F-FDTP could penetrate through the blood-brain barrier and selectively accumulate in striatum,hypothalamus,frontal certex,hippocampus,cerebellum,where the D_4 receptor was reportedly located.The radioactivities in hippocampus,hypothalamus,striatum,frontal cortex,cerebellum,pons were (0.42±0.03),(0.46±0.05),(0.54±0.04),(0.39±0.04),(0.45±0.06),(0.35±0.04) %ID/g,respectively,2 min post injection.And there was difference between the normal biodistribution results and the blocking experimental results:(0.36 ±0.05),( 0.33±0.05 ),(0.55±0.05 ),(0.30±0.07 ),(0.34±0.07 ) and (0.32±0.04) % ID/g in hippocampus,hypothalamus,striatum,frontal cortex,cerebellum and pons,respectively.Conclusions ~(18)F-FDTP can penetrate through the blood-brain barrier and selectively accumulate in striatum,hypothalamus,frontal cortex,hippocampus,cerebellum,where the D_4 receptor was known to concentrate.These preliminary results suggest that ~(18)F-FDTP is a potential dopamine D_4 receptor imaging agent and further studies are needed.

OBJECTIVETo investigate the incidence of campylobacter jejuni (CJ) infection and the drug resistance of CJ in children with diarrhea in Guangzhou.

METHODSThe fecal samples of 3,351 children with diarrhea between July 2005 and June 2008 were collected for CJ culture. The species of CJ strains were identified by Lior methods. The drug susceptibility tests were performed by the Kirby-Bauer method.

RESULTSTwo hundred and sixty-seven CJ strains (8.0%) were isolated from 3,351 samples. The children at age of 1 month to 1 year were susceptible to CJ, accounting for 91.0%. A higher incidence of CJ infection (76.8%) was found in summer and autumn. The CJ strains were susceptible to imipenem, amikacin, cefoperazone/sulbactam, chloramphenicol, macrolides and lincomycins. Parts of CJ strains (20%-40%) were resistant to ampicillin, quinolones and ambramycin. All CJ strains were resistant to sulfamethoxazole/trimethoprim and cefditoren. Two hundred and one strains (75.3%) were CJ biotype I.

CONCLUSIONSCJ is an important pathogen of diarrhea in children from Guangzhou. CJ is resistant to some antibiotics used often in clinical practice, and so it is thus important to use antibiotics based on the results of drug susceptibility tests in children with CJ infection.

Campylobacter Infections ; microbiology ; Campylobacter jejuni ; classification ; drug effects ; isolation & purification ; Child, Preschool ; Diarrhea ; microbiology ; Female ; Humans ; Infant ; Male ; Microbial Sensitivity Tests

OBJECTIVETo explore optimal choice of surgical treatment and operative approach for closed complex tibial plateau fractures and its influencing factors.

METHODSFrom January 2003 to January 2011, 95 patients with closed complex tibial plateau fractures were estimated Schatzker V and Vl, and treated with three different surgical methods. The methods included single plate through anterolateral incision (Group A, 22 cases), double plates through inside and outside incisions (Group B, 36 cases), and double plates through antero-midline incisions (Group C, 37 cases). There were 56 males and 39 females, ranged the age from 19 to 57 years (averaged, 36.3 years), 50 cases in left, 45 cases in right. According to Schatzker classification, 51 cases were type V, 44 cases were VI. The data of operation time, intraoperative blood loss, complications (infectious of wound, necrosis, bad incision, collapse fracture, loosen of internal fixation, fracture failure)and recovery of function of lower limb joint were collected.

RESULTSThere were no significant difference among three groups in operation time (P > 0.05); blood loss in group A was obvious better than other groups (P < 0.05); collapse of joint surface and failure rate of internal fixation in group A was higher than other groups (P > 0.05); Merchant score after 1 year were higher in group B, C than group A. For lower limb function, 10 cases got excellent results, 5 good, 4 fair and 3 poor in group A; 21 cases got excellent results, 11 good, 3 fair and 1 poor in group B; 23 cases got excellent results, 11 good,2 fair and 1 poor in group C.

CONCLUSIONThe blood loss in group A was least, but fracture exposure and joint surface was not satisfactory, and stable fixation could not be achieved, the long-term result was not good. For fractures with double condyles and dislocated involved, double plates through inside and outside incisions or double plates through antero-midline incisions was suggested,which benefit good reduction of joint surface, stable fixation, and erlier exercise.

Adult ; Bone Plates ; Case-Control Studies ; Female ; Fracture Fixation ; adverse effects ; methods ; Fractures, Closed ; surgery ; Humans ; Male ; Middle Aged ; Tibial Fractures ; surgery

Kinases play crucial roles in the life of cell. Their functional abnormity usually leads to many human major diseases including tumors. The prospecting of ATP-competitive small-molecule kinase inhibitors targeting kinases of therapeutic interest has become the focus of researches. Due to the high conservation of the catalytic domain of kinases, the selectivity of kinase inhibitors is poor in general. However, along with the development of structural biology and computer-aided drug design, great progress in the research of selective, ATP-competitive kinase inhibitors has been achieved in recent years. In this account, the review has been made on the development of the design of selective kinase inhibitors.
Adenosine Triphosphate ; chemistry ; Binding, Competitive ; Drug Design ; Molecular Structure ; Protein Binding ; Protein Kinase Inhibitors ; chemical synthesis ; chemistry ; pharmacology

OBJECTIVETo investigate CT and MRI characteristics of primary spinal large B cell lymphoma.

METHODSCT and MRI data of 23 patients with primary spinal large B cell lymphoma confirmed by histopathology were retrospectively analyzed from March 2011 to August 2015. Among them, including 14 males and 9 females aged from 28 to 70 years old with an average of 53.4 years old. The clinical manifestation mainly focus on pain around spinal and minority peripheral nerve symptom. The courses of disease ranged from 2 weeks to 3 months with an average of 9 weeks. Nine patients underwent CT plain scan, 8 patients underwent plain and enhanced CT; 21 patients underwent MRI plain scan and enhanced; 15 patients underwent CT and MRI examination. The location, bone changes, shape, density, signal intensity and enhancement characteristics of lesions were observed and compared with pathology.

RESULTSLocation and size of lesion showed cervical vertebrae in 1 case, thoracic vertebrae in 16 cases, lumbar vertebrae in 2 cases, and sacral vertebrae in 4 cases. Mass was larger, the largest cross-sectional size of group was up to 73 mm× 125 mm. CT examination showed that 11 cases with "cloud and mist" shape change, 6 cases with compression fractures, and with "floating ice" shape change, 9 cases with "oversleeve" shape change, 11 cases with spinal stenosis; enhancement scan showed obvious reinforcement. MRI showed slightly low signal on T1WI and T2WI were slightly high signal, and signal was uneven, and enhancement scan showed obvious reinforcement, 13 of 16 cases with spinal canal stenosis changed like "oversleeve", intervertebral space showed no significant stenosis. Comparison of CT and MRI showed the manifestation of bone destruction by CT was superior than that of MRI, but the range of lesion, and related surrounding structures were not better than MRI. MRI displayed the range of lesion usually bigger than CT. Pathology results showed that 23 patients were all primary spinal large B cell lymphoma.

CONCLUSIONSPrimary spinal large B cell lymphoma has certain features in age, location and imaging findings. The "cloud and mist", "floating ice" and "oversleeve" shape bony destruction by CT and MRI has certain significance to diagnosis of primary spinal large B cell lymphoma.

Adrenomedullin ; Animals ; Endothelin-1 ; blood ; Liver Cirrhosis, Experimental ; physiopathology ; Nitric Oxide ; blood ; Peptides ; blood ; pharmacology ; Portal Pressure ; drug effects ; Rats ; Rats, Wistar