In this study,a series of new sildenafil analogues 11-27 possessing a guanidine group were synthesized to investigate their PDE5 inhibitory activity and selectivity using[~3H]cGMP SPA kit in vitro and efficacy in the rat model of erection.Most of the compounds showed potent activity against PDE5,and more importantly,several compounds exhibited higher PDE5 selectivity over PDE6 than that of sildenafil.Structure-activity relationship of these sildenafil analogues was also discussed.Within this series of compounds,compound 15(IC_(50) =1.7 nmol/L)not only exhibited more potent PDE5 inhibitory activity than that of sildenafil (IC_(50) = 6.5 nmol/L),but also showed functional efficacy in the rat model of erection.

With the constant rise of energy price,it has a great practical meaning of using lignocellulose to produce ethanol.Xylose is a kind of monosaccharide whose content is only less than glucose in most lignocellulosic hydrolysates.There is some difficulty of producing ethanol from lignocellulose by the traditional ethanol production strain Saccharomyces cerevisiae,because it cannot metabolize xylose.People have tried to use genetic engineering technology and cell fusion method to modify Saccharomyces cerevisiae to make it metabolize xylose and produce ethanol for many years.This review indroduced the progress in this field.

In this study,we discussed the way of imparting the microbial knowledge and elevating non-biological student's science in public optional course "Microbes and Man" from the teaching practice.During the course,we first chose the material according to students' characteristic,and then introduced several methods like lecturing on subject,visiting factories and making microbial experiments in order to inter-est students in microbiology and get better in teaching effects.

Objective To study the characteristics of dynamic susceptibility-contrast(DSC)MR perfusion curves,color images and perfusion values in pre-operative brain metastasis.Methods Twenty- eight brain metastases underwent DSC MR perfusion imaging by using a first-pass T_2~* echo-planar sequence. The patients' data were transferred to on-line workstation.Time-signal intensity curves,color perfusion maps and rCBV,rMTT values in both tumor parenchyma and peri-tumor edema were analyzed,and independent t- test was used and P0.05).Conclusion Different originated brain metastases have nearly same characteristics in DSC MR perfusion imaging.

OBJECTIVETo understand the exposed positions and levels of indium and its compounds in manufacture of liquid crystal displays, and to evaluate the degree of occupational hazard from indium and its compounds.

METHODSOn-site investigation of occupational health, occupational hazard monitoring, and occupational health examination were used to evaluate the degree of occupational hazard from indium and its compounds in three manufacturers of liquid crystal display panel in Shenzhen, Guangdong, China.

RESULTSThe time-weighted average (TWA) and short-term exposure limit (STEL) concentrations of indium and its compounds to which sputtering machine operating positions were exposed were less than 0.002~0.004 mg/m³ and 0.006~0.007 mg/m³, respectively, both of which complied with the National Hygienic Standard (PC-TWA = 0.1 mg/m³; PC-STEL = 0.3 mg/m³); the TWA and STEL concentrations of indium and its compounds to which grinding positions were exposed were 0.114~2.98 mg/m³ and 0.31~10.02 mg/m³, respectively, both of which exceeded the National Hygienic Standard with the highest concentration 33-fold higher than the standard. No significant health damages were found in exposed workers according to the results of occupational health examination.

CONCLUSIONThe grinding positions are the key to the control of occupational hazard from indium and its compounds in manufacture of liquid crystal display panel. The workers should be equipped with the anti-particulate full-face respirator, which is an effective way to prevent occupational hazard from indium and its compounds.

Air Pollutants, Occupational ; toxicity ; China ; Data Display ; Humans ; Indium ; toxicity ; Liquid Crystals ; Occupational Exposure ; analysis ; Occupational Health ; Risk Assessment ; Threshold Limit Values

OBJECTIVETo study the effect of Jinguo Weikang Capsule [see text] on the gene expression of H-ras, epidermal growth factor receptor (EGFR), P53 and C-myc of the gastric mucosa in rats with gastric precancerous lesions, and to investigate the action mechanism of JWC on gastric precancerous lesions.

METHODSA rat model with paratypical proliferation of the gastric epithelium mucosa was established by using 60Co irradiation. Rats were divided into the normal group, model group, high-, medium-, low-dose JWC treatment groups, and the vitacoenzyme control group, and were treated for 30 days. The expression of H-ras, EGFR, P53 and C-myc genes of the gastric mucosa was detected by using immunohistochemical methods.

RESULTSThe expression and over-expression rates of H-ras, EGFR, P53 and C-myc gene in the high-and medium-dose JWC treatment groups were significantly lower (P<0.05) as compared with those of the model group.

CONCLUSIONJWC can inhibit the expression of the H-ras, EGFR, P53 and C-myc genes expression of the gastric mucosa in rats, which may be one of mechanisms involved in suppressing or reversing gastric carcinogenesis.

Animals ; Drugs, Chinese Herbal ; pharmacology ; Gastric Mucosa ; drug effects ; metabolism ; pathology ; Gene Expression Regulation, Neoplastic ; drug effects ; Immunohistochemistry ; Oncogene Proteins ; metabolism ; Precancerous Conditions ; metabolism ; pathology ; Proto-Oncogene Proteins ; metabolism ; Proto-Oncogene Proteins c-myc ; metabolism ; Rats ; Rats, Sprague-Dawley ; Receptor, Epidermal Growth Factor ; metabolism ; Tumor Suppressor Protein p53 ; metabolism ; ras Proteins ; metabolism

BACKGROUNDContrast-enhanced fluid-attenuated inversion-recovery (FLAIR) magnetic resonance imaging (MRI) has been reported to have higher sensitivity for detecting leptomeningeal disease compared with contrast-enhanced T1-weighted MRI (CE T1WI). However, currently there are no studies showing the potential value of clinical applications of contrast-enhanced FLAIR (CE FLAIR) sequence in diagnosing intracranial tumors in a larger group of patients. The purpose of this study was to evaluate the diagnostic value of CE FLAIR in comparison with CE T1WI for intracranial tumors and to provide more information for clinical diagnosis and therapy.

METHODSOne hundred and four consecutive cases of intracranial tumors referred for CE brain MRI were analyzed with regard to FLAIR and T1WI pre- and post-administration of Gd-DTPA. The CE FLAIR and CE T1WI were evaluated independently by two radiologists for the number of examinations with one or more enhanced lesions, the number and location of enhanced lesions per examination, signal-to-noise ratio (SNR) and contrast-enhancement ratio (CER) of lesions, as well as the size and extent of the enhanced lesions.

RESULTSIn 98 of 104 cases, enhanced lesions were seen both on the FLAIR and T1W images. More lesions were seen on CE T1WI (n = 120) than those on CE FLAIR sequence (n = 117), but no differences of statistical significance were found between the two sequences (P > 0.05). Four lesions were revealed only on the CE FLAIR images whereas 7 lesions were only found on CE T1WI. Enhanced lesions located in the cerebral hemisphere or the forth ventricle were revealed much more on CE T1WI than on CE FLAIR images. However, CE FLAIR images may be useful in showing superficial abnormalities and those located in the sulcus or lateral ventricle. The CER and contrast-to-noise ratio (CNR) on CE T1WI was significantly higher (t = 7.10, P = 0.00; t = 9.67, P = 0.00, respectively), but grey matter/white matter contrast was lower (t = 2.46, P = 0.02) than those on CE FLAIR images. The SNR did not show any statistically significant difference between the two sequences (t = 1.1, P = 0.27). The size and extent of lesions on the CE FLAIR images were significantly larger than those on CE T1WI (t = 4.13, P = 0.00).

CONCLUSIONSCE FLAIR and CE T1WI may complement each other in showing intracranial tumors and the CE FLAIR sequence should be selected as a routine MRI sequence.

Adolescent ; Adult ; Aged ; Brain Neoplasms ; diagnosis ; pathology ; Child ; Child, Preschool ; Contrast Media ; Female ; Gadolinium DTPA ; Humans ; Image Enhancement ; Magnetic Resonance Imaging ; methods ; Male ; Middle Aged

OBJECTIVETo compare oncologic outcomes between doublet and triplet adjuvant chemotherapy for gastric cancer patients undergoing radical resection.

METHODSPatients with gastric cancer receiving adjuvant chemotherapy after radical resection from January 2004 to December 2008 were included. Doublet was defined as 5-FU 750 mg/m² (days 1-5) or capecitabine 1000 mg/m² (days 1-14) plus cisplatin 60 mg/m² (day 1) or oxaliplatin 130 mg/m² (day 1), while triplets had epirubicin 50 mg/m² (day 1) added. Chemotherapy was initiated 4-6 weeks after surgery, repeated every three weeks for 6 cycles. Patients were followed-up in the outpatient clinic until death or the most recent follow up(April 30, 2010). Cox proportional- hazard model and Chi-square test were used to test statistical difference.

RESULTSA total of 316 patients (210 received doublets, 106 received triplets) had a median follow-up time of 47 months. Seventy-seven patients died at the end of the follow-up. Two groups were comparable except for age (median age of 57 in doublets, 51 in triplets, P<0.01). The two groups had similar disease-free survival (16 months vs. 23 months, P=0.656) and 3-year overall survival(59.6% vs. 64.8%, P=0.293). There was no significant difference in severe adverse side effects between the two groups (21.9% vs. 30.2%, P=0.107).

CONCLUSIONTriplet adjuvant chemotherapy appears not to be associated with superior efficacy than doublet regimen for patients with gastric cancer after radical resection.

Capecitabine ; Chemotherapy, Adjuvant ; Cisplatin ; administration & dosage ; Deoxycytidine ; administration & dosage ; analogs & derivatives ; Female ; Fluorouracil ; administration & dosage ; analogs & derivatives ; Humans ; Male ; Middle Aged ; Postoperative Care ; Prognosis ; Retrospective Studies ; Stomach Neoplasms ; drug therapy

OBJECTIVETo evaluate the oncologic safety, indications and aesthetic results for skin-sparing mastectomy (SSM) and immediate breast reconstruction (IBR).

METHODOne hundred and twenty-nine breast cancer patients treated by SSM + IBR from October 1999 to May 2007 were reviewed. Reconstructive techniques included latissimus dorsi flaps (38 patients), implants only (2 patients), latissimus dorsi flaps plus implants (61 patients), pedicled transverse rectus abdominis myocutaneous (TRAM) flaps (25 patients) and deep inferior epigastric artery perforator (DIEP) flaps (3 patients). Aesthetic results were judged by patients' self-evaluation.

RESULTSMean duration of hospitalization was 18.6 days. Time of first chemotherapy was 5.2 days after operation. Eleven patients (11/63, 17.5%) developed capsular contracture and 24 patients (24/99, 24.2%) developed seroma in the donor site. Nine patients (9/28, 32.1%) developed partial fat necrosis in TRAM and DIEP flaps. The satisfaction with the aesthetic results of the reconstructive breast was significantly lower in irradiated patients than non-irradiated ones. Median follow-up time was 11 months. Five patients developed local recurrence and 7 patients with metastasis.

CONCLUSIONSSSM with IBR can be used for the 0 to II a stage breast cancer patients, with surgical oncologic and aesthetic satisfaction. Radiotherapy has an adverse effect on the reconstructive breast. Delayed or delayed-immediate reconstructions are recommended for patients indicated to postoperative radiotherapy.

Adult ; Breast Neoplasms ; surgery ; Female ; Follow-Up Studies ; Humans ; Mammaplasty ; methods ; Mastectomy, Subcutaneous ; Middle Aged ; Retrospective Studies ; Surgical Flaps ; Treatment Outcome

OBJECTIVETo evaluate the efficacy and safety of neoadjuvant chemotherapy in patients with locally advanced gastric cancer, and to analyze the relevant factors of recurrent death of gastric cancer after adjuvant chemotherapy.

METHODSClinical data of 49 patients who underwent neoadjuvant chemotherapy for locally advanced gastric cancer between July 2007 and June 2011 were reviewed. Preoperative staging was determined by endoscopic ultrasonography and abdominal computer tomography (CT) or magnetic resonance imaging (MRI). Chemotherapy was administered for regimen of two or three drugs. Prognostic factors were analyzed by univariate and multivariate analysis with Cox proportional hazard model.

RESULTSThe response rate was 33.3% (16/48) and disease control rate was 93.8% (45/48). Forty-four (89.8%, 44/49) patients received curative resection after neoadjuvant chemotherapy, among whom 90.9% (40/44) underwent D2 lymphadenctomy. Thirty-two cases had pathological response and 2 patients had pathological complete response. The average hospital stay was 11.6 days and 2 patients had longer hospitalization because of postoperative pancreatic complications. The toxicities were most in grade 1-2. All the patients were followed up postoperatively and the median follow-up was 21.6 months. Median progression-free survival was 29.6 (95%CI:24.0-35.2) months and median overall survival was 34.6 months (95%CI:29.8-39.4). Imaging response (P=0.038, RR=0.168, 95%CI:0.031-0.904) and pathological response (P=0.007, RR=0.203, 95%CI:0.064-0.642) were identified as independent prognostic factors with COX multivariate analysis.

CONCLUSIONSNeoadjuvant chemotherapy has quite high disease control rate and R0 resecting rate for patients with locally advanced gastric cancer. Imaging response and pathological response are most important prognostic factors in those patients.

Adult ; Aged ; Antineoplastic Combined Chemotherapy Protocols ; therapeutic use ; Chemotherapy, Adjuvant ; Female ; Humans ; Male ; Middle Aged ; Neoadjuvant Therapy ; methods ; Preoperative Care ; Proportional Hazards Models ; Retrospective Studies ; Stomach Neoplasms ; drug therapy ; surgery ; Treatment Outcome