AIM　A series of 4-piperidinylthioether and sulfone derivatives of 4-［1-hydroxy-1-(2,3-dimethoxyphenyl) methyl］-N-2-(4-fluorophenylethyl) piperidine (MDL 100907) were synthesized in order to find new 5-HT2A selective ligands. METHODS　Title compounds 2a-2c were synthesized from 2,3-dimethoxythiophenol and tested for their affinities to 5-HT2A, 5-HT2C, 5-HT6 and 5-HT7 receptors and some other nervous transmitter receptors in vitro. RESULTS　Compounds 2a-2c are new compounds. The results of the binding assay demonstrated that they have relatively high selectivity for 5-HT2A receptor in vitro. CONCLUSION　Some sulfur containing analogues of MDL 100907 showed selective affinity to 5-HT2A receptor and are worth further study.

BACKGROUND: Long-term utilization of steroid hormone easily induces avascular necrosis of the femoral head (ANFH). Cornu Cervi Pantotrichum possesses bone growth factor and can promote wound healing and tissue repairing, which may has effect on treatment of ANFH. OBJECTIVE: To investigate therapeutic effect of antler powder on ANFH induced by corticosteroids in rats. METHODS: Totally 42 male wistar rats were randomly divided into the blank control, model and high-, moderate- and low-dose treatment groups. Exception those in the blank control group, all rats were intragluteally injected with dexamethasone at 30 mg/kg twice per week for 6 weeks to induce ANFH. Then the rats were treated with antler powder by oral gavage at 200, 400 and 800 mg/kg dosage, once per day for 60 days. Same volume of physiological saline was gavaged in the blank control and model groups. Serum lipid level and bone mineral density (BMD) of femur were measured, pathological change and expression of vascular endothelial growth factor (VEGF) were investigated. RESULTS AND CONCLUSION: Steroid hormone intervention resulted in obviously ANFH in rats. After treatment with antler powder, the degree of necrosis was significant reduced. Compared with the model group, BMD were increased, total cholesterol, triacylglycerol, and low density lipoprotein levels were decreased, and the VEGF expression increased in the treatment groups. The results suggest that antler powder has a positive curative effect on ANFH by promoting bone formation, fat metabolism and increasing VEGF expression.

Objective To analyze the features of intracrayze the features of intracranial cystic diseases on ~1H MRS,and to evaluate the applicable value of ~1H MRS.Methods Fifty-two patients were examinated by single voxel ~1H MRS,included Ⅰ-Ⅱ graded astrocytomas(n=8),glioblastomas(n=9),metastasis(n=13),brain abscesses(n=10),epidermoids(n=4),anachnoid cysts(n=5),brain Cysticerciasis(n=3).Results(1)There was only Lac in Ⅰ-Ⅱ graded astrocytomas.But in glioblastomas,as were as all showed Lac,4 cases showed low Cho and NAA and 2 cases Lip.(2) In(13 metastasis) patients,7 cases only presented Lac,6 cases showed Cho,3 cases showed low NAA and(6 ones) Lip.(3) In brain abscesses,all showed Lac,9 cases displayed AA,6 cases showed Ace,5 cases appeared Suc and Ala,2 cases had Lip.(4) Four cases of epidermoid showed Lac,one showed Lip.In(4 arachnoid) cysts,2 cases had low Lac,one showed Lip.Three cases of cysticerciasis showed Lac,Ace,Suc,Ala and no AA,Cho,NAA.Conclusion Lac is the most common resonance peak on ~1H MRS in intracranial cystic diseases and for no diagnostic specificity.AA combined Ace,Suc,and Ala are highly specificity for brain abscess.Ace,Suc and Ala appearance cues the the possible existence of cysticerciasis.~1H MRS is helpful for the qualitative diagnosis of intracranial disease.

Objective To explore the efficacy difference of biliary stent combined with 125I seed intracavity irradiation and palliative biliary drainage in the treatment of obstructive jaundice caused by pancreatic head cancer. Methods The clinic date of 95 patients with pancreatic head cancer who underwent palliative surgery from June 2010 to June 2015 were analyzed retrospectively. 46 of the cases were treated with percutaneous biliary metal stent implantation combined with 125I seed intracavity irradiation (stent group), and the other 49 cases were treated with palliative biliary enterostomy (surgery group). The levels of jaundice, liver function, tumor size, survival time and hospitalization cost were compared between the patients before and after treatment. Paired t-test was applied for statistical analysis. Results Both the two treatment coulel effectively relieve jaundice and improve liver function. The mean TBIL of surgery group and stent group was (29.4±9.6) and (21.0±8.0)μmol/L after three months treanment, (40.3±11.0) and (24.4±9.6)μmol/L after six months treatment, respectively. Tumor maximum diameter of the two groups were (37.9 ± 4.5) mm and (33.5 ± 6.0)mm after three months treatment, (45.9 ± 5.0) mm and (37.0 ± 6.5) mm after six months, respectively. Each time point between them had statistical significance (t=-4.235,-5.476,-3.654,-6.702, P<0.05). The mean survival time was (12.83 ± 0.80) months in the stent group and (9.06±0.49) months in the surgery group, the difference was statistically significant (t=-3.49, P<0.01). The mean hospitalization cost of the stent group was (38 453.0 ± 7 282.0) yuan and the surgery group was (43 057.0 ± 7 667.4) yuan, the difference was statistically significant (t= 2.759, P<0.05). Conclusion For inoperable pancreatic head cancer patients, compared with palliative biliary enteric drainage, percutaneous biliary stent placement combined with 125I seed intracavity irradiation can effectively relieve biliary obstruction, improve liver function, inhibit tumor growth and prolong survival time.

Objective To summarize and evaluate the clinical features,therapeutic methods and prognosis of 197 cases with eating crayfish caused rhabdomyolysis in our hospital within July,2016 to August,2016.Methods Using retrospective method,197 rhabdomyolysis cases induced by eating crayfish were admitted into study.Data of epidemiological character,clinical features,therapy protocol and prognosis were collected and analyzed.Results All the patients had the experience of eating crayfish within 12h before the onset.Patients in this cohort had the common symptoms but varying degrees of myalgia,fatigue of the whole body muscles,and urine color change.Laboratory tests revealed:On day 1 of onset,serum myoglobin level had raised up to the peak with average level at (2 135 ± 1 547) μg/L (0-46 μg/L).Creatine kinase with average level at (4 657 ± 2 178) U/L (25-190 U/L);Aspartate transaminase with average level at 264 ± 83 U/L (10-45 U/L);Lactate dehydrogenase with average level at (1 457 ± 673) U/L (313-618 U/L),all these three markers reached peak on day 2,then gradually declined.All the patients recovered and discharged after relaxation,fluid infusion,alkalization of urine and dealing with the complications.Conclusion Timely diagnosis and treatment of the rhabdomyolysis syndrome induced by eating crayfish could indicate favorable prognosis in these patients from July,2016 to August,2016.

Objective To analyze the DWI characteristics of intracranial epidermoid cyst (ECs),and to evaluate “T2 shine-through” effect. Methods There were 15 cases of ECs confirmed by pathology, in which 3 cases had the residual tumor after surgery. The ADC value was measured in ECs,deep white matter and CSF,and the comparison was made between DWI and FLAIR in showing the tumors. Results (1) The lesions in 15 cases were high intensity on DWI, their ADC value was from 0.80?10 -3mm2/s to 1.23?10 -3mm2/s, the average was (1.05?0.14)?10 -3mm2/s. But the ADC value of deep white matter was from 0.74?10 -3mm2/s to 1.09?10 -3mm2/s, the mean was (0.88?0.09)?10 -3mm2/s. The ADC value of CSF was from 2.98?10 -3mm2/s to 3.78?10 -3mm2/s,the mean was (3.31?0.21)?10 -3mm2/s. The ADC value of ECs was significant lower than that of CSF ( P

BACKGROUND: In recent years, ultrasound microbubble gene transfer system has been applied for gene transfection in many parts of the body, but it has been seldom reported to be used for gene transfection in bone parts. OBJECTIVE: To investigate the efficiency and feasibility of ultrasound-targeted microbubble destruction applied for transfection of enhanced green fluorescent protein plasmid into the femoral head of rabbits.METHODS: Japanese big-ear rabbits were randomly divided into five groups: bare transfection, pre-irradiation + bare transfection, ultrasound transfection, pre-irradiation+ultrasound transfection, and repeatable transfection. In the first two groups, ultrasound-targeted gene transfection and irradiation was not used, but in the latter three groups, ultrasound-targeted microbubble destruction was used to transfect enhanced green fluorescent protein (EGFP) plasmid into the femoral head of rabbits. At 1 week after transfection, EGFP expression in femoral head was observed under the fluorescence microscope. RESULTS AND CONCLUSION: EGFP expression appeared in the ultrasound transfection, pre-irradiation + ultrasound transfection and repeatable transfection. The transfection efficiency of EGFP plasmid was significantly higher in the repeatable transfection group than in the other groups (P < 0.01). Obvious injury loci were not observed in the soft tissue and bone tissue slices of ultrasonic irradiation parts in the ultrasound transfection, pre-irradiation + ultrasound transfection and repeatable transfection groups. These results confirm that ultrasound-targeted microbubble destruction is a safe and effective method to transfect EGFP plasmid into the femoral head of rabbits.

Objective: To explore the correlation of plasma level N-terminal pro-B-type natriuretic peptide (NT-proBNP) in patients with non-diabetic acute myocardial infarction (AMI) combining stress hyperglycemia.
Methods: A total of 327 non-diabetic AMI patients treated in our hospital from 2012-02 to 2014-05 were studied. The patients were divided into 2 groups according to fasting blood glucose level:Stress group, the patients with blood glucose≥7.0 mmol/L, n=182 and Non-stress group, the patients with blood glucose<7.0 mmol/L, n=145. The basic clinical condition, laboratory tests within 24 hours of onsets, echocardiography and 24 h dynamic electrocardiogram were examined;the incidence of major adverse cardiovascular events (MACE) including arrhythmia, heart failure, cardiac shock and sudden cardiac death in 2 weeks of onsets were analyzed and compared between 2 groups.
Results: The patients’ age, gender, history of hypertension, smoking, drinking, and blood levels of TC, TG, HDL-C, LDL-C were similar between 2 groups, P>0.05. Plasma levels of NT-proBNP, CK-MB, MYO, ultra-TnI, ALT, AST and blood glucose level were signiifcantly different between 2 groups P<0.01. NT-proBNP level was positively related to
ultra-TnI (r2=0.811, r=0.901, P<0.01). Stress group presented obviously higher incidence of MACE (P<0.05), lower LVEF (P<0.01), and signiifcantly increased left ventricular end diastolic diameter, left ventricular end systolic diameter (P<0.01) than those in Non-stress group.
Conclusion: Plasma levels of NT-proBNP may judge the severity and evaluate recent prognosis in patients with non-diabetic AMI combining stress hyperglycemia, it could be used as a risk indicator for relevant patients in clinical practice.

Objective To investigate the clinical features of patients with recurrent epithelial ovarian cancer (EOC),and explore the factors that can prolong the disease-free interval(DFI) after primary treatment.Methods We retrospectively reviewed the medical records of 54 patients with recurrent EOC and analyzed the clinical stage,histological subtypes,primary treatments,DFI,recurrent site,secondary treatment,and the response after secondary treatment.By Mann-Whitney test and T test,factors influent the DFI were analyzed,the relationship between DFI and the response after secondary treatment were analyzed also.Results The mean DFI for all 54 patients was 19.07 months.The DFI of patients received optimal cytoreductive surgery was longer than those received non-optimal cytoreductive surgery [(32 ± 19.10) months vs (18.77 ± 7.80) months,P ＜ 0.01];The DFI of patients with serous,mucous and clear cell tumor was [(20.16 ± 14.63) months,(14.00 ± 4.73) months and (16.67 ± 13.03) months,respectively],suggesting patients with mucous tumor might have shorter DFI.The DFI of patients with low tumor grade was longer than those with high tumor grade [(28.18 ± 16.97) months vs (16.52 ±9.46) months,respectively];The DFI of patients with stage Ⅰ and Ⅱ disease was [(19.60 ± 12.89)months],was compared to the DFI of patients with stage Ⅲ,stage Ⅳ disease,which was [(19.22 ± 12.38) months] and [(11.67 ±5.39) months],respectively.When disease recurred,the most frequent recurrent site was pelvic (50％,n =27),with upper abdominal (29.6％) and lymph node(29.6％) followed.When recurrence was found in lymph node,the most frequent site was pelvic and para-arotic lymph node.In our study,when disease recurred,response of the tumor after the secondary treatment has no relationship with the DFI.Conclusions Patients received optimal cytoreductive surgery,patients with low tumor grade and early stage have longer DFI.Retroperitoneal lymphadenectomy might be chosen during the primary cytoreductive surgery in some selected patients.

OBJECTIVE To investigate the ?-lactamase genes in 4 kinds of nonfermenting Gram-negative bacilli isolated from the 98th Hospital of PLA. METHODS Sixty strains of Acinetobacter baumannii,30 strains of Pseudomonas aeruginosa,19 strains of Stenotrophomonas maltophilia,and 15 strains of Flavobacterium were isolated from hospitalized patients.Nine kinds of ?-lactamases genes of TEM,SHV,OXA,CTX-M,PER,VEB,IMP,VIM and GES were analyzed by PCR and verified by DNA sequencing. RESULTS In A.baumannii and(P.aeruginosa),the positive rates of gene of TEM were 100.0% and 66.7%,respectively.SHV gene was positive in 18 of 60 strains of A.baumannii tested,17 of which were SHV-12 subtype ESBLs.The other was a new SHV type ?-lactamase nominated SHV-48.OXA gene was positive in 1 of 30 strains of P.aeruginosa tested,it was an OXA-10 subtype ESBLs.But the rest of genes were all negative. CONCLUSIONS There exist 4 kinds of(?-lactamase) genes at least in nonfermenting Gram-negative bacilli including TEM-1,SHV-12,SHV-48,and(OXA-10.)