OBJECTIVE:To evaluation of the efficacy and safety of azithromycin in the treatment of acute infections METHODS:A randomized controlled multicenter clinical study was used to compare the clinical efficacy of azithromycin(200mg q d for 3～5 days) with erythromycin(500mg b i d for 5 days) RESULTS:The cure rate,effective rate,and bacterial clearance rate were 76 7%,95 0%,and 94 3% respectively for azithromycin group and were 48 3%,76 7%,and 77 4% respectively for erythromycin group with a side-effect incidence of 10 0% for azithromycin group and 39 3% for erythromycin group CONCLUSION:Azithromycin is superior to erythromycin in clinical efficacy,safety and side-effect incidence

Objective To investigate the association between peripheral white blood cell (WBC) count and the carotid intimal-medial thickness (cIMT) in middle-aged and elderly Chinese of suburban area of Shanghai.Methods A total of 2 519 subjects aged 40 years or older from Jiading District,Shanghai were recruited to undergo questionnaire interview,anthropometric measurements,fasting blood sampling,and carotid B-mode ultrasonography.After excluding subjects with biochemical index missing,WBC count ＞ 10× 109/L as well as those with known myocardial infarction,cerebral infarction,coronary heart disease,and those taking lipid-lowing agents,2 239subjects were included in this analysis.Results Increased WBC count was associated with more unfavorable metabolic risk profiles.With the increasing quartiles of WBC count,cIMT were 0.558,0.570,0.573,and 0.587mm respectively(P for trend ＜ 0.01).As compared with participants in the first WBC quartile,the risks of cIMT thickening were increased by 79％,109％ in males and 29％ in females (P＞ 0.05 in females).Multiple linear regression model showed that peripheral WBC count was an independent risk marker for cIMT thickening,especially for neutrophil and monocyte count.Conclusion A high-normal WBC count was significantly associated with cIMT thickening in middle-aged and elderly Chinese of suburban area of Shanghai,especially in males.

Objective To investigate the clinical application of a new thermosensitive embolic agent in interventional arterial embolization treatment, and to evaluate its effectiveness and safety in treating inoperable advanced hepatocellular carcinoma (HCC). Methods Prospective, open and single center clinical study of a new thermosensitive embolic agent was conducted. A total of 10 patients with clinically confirmed inoperable advanced HCC were treated with percutaneous arterial embolization using thermosensitive embolic agent; a maximum of 4 therapeutic cycles were performed until the disease progressed. Objective effect was evaluated at (30 ±7) days after the treatment according to mRECIST standard; the progression free survival (PFS) time and the survival period (OS) were recorded. The adverse reactions and adverse events were determined by NCI-CTC 3.0 version standard. Results Ten patients (23 target lesions in total) were enrolled in this study. After the treatment, complete remission (CR) was obtained in one patient, partial remission (PR) in 3 patients, stable disease (SD) in 5 patients, and progress disease (PD) in one patient. The objective response rate (CR+PR) was 40%, and the disease control rate (CR+PR+SD) was 90%. The PFS of hepatic lesions was 18.4 weeks (95%CI:14.15-22.65), the cumulated median survival period was 46.2 weeks (95%CI:38.18-54.22). The most common adverse reactions included pain, fever, hepatic function damage, small amount of ascites, diarrhea, etc. Conclusion The new thermosensitive embolic agent is not sticky to vessel and is visible under X-ray; it has reliable embolization effect, and the therapeutic results can be easily evaluated. This embolic agent is not perfect, and it has some limitations in clinical use. The adverse reactions are mild, which can be easily tolerated by the patients. It is worth trying to carry out large sample and randomized controlled studies in order to open up more areas for arterial chemoembolization therapy of tumors.

Poly(ADP-ribose) polymerase-1 (PARP-1) has emerged as a promising anticancer drug target due to its key role in the DNA repair process. It can polymerize ADP-ribose units on its substrate proteins which are involved in the regulation of DNA repair. In this work, a novel series of para-substituted 1-benzyl-quinazoline-2, 4 (1H, 3H)-diones was designed and synthesized, and the inhibitory activities against PARP-1 of compounds 7a-7e, 8a-8f, 9a-9c and 10a-10c were evaluated. Of all the tested compounds, nine compounds displayed inhibitory activities with IC50 values ranging from 4.6 to 39.2 micromol x L(-1). In order to predict the binding modes of the potent molecules, molecular docking was performed using CDOCKER algorithm, and that will facilitate to further develop more potent PARP-1 inhibitors with a quinazolinedione scaffold.
Antineoplastic Agents ; chemical synthesis ; chemistry ; pharmacology ; Drug Design ; Enzyme Inhibitors ; chemical synthesis ; chemistry ; pharmacology ; Molecular Docking Simulation ; Molecular Structure ; Poly (ADP-Ribose) Polymerase-1 ; Poly(ADP-ribose) Polymerases ; Quinazolinones ; chemical synthesis ; chemistry ; pharmacology ; Structure-Activity Relationship

PARP [poly(ADP-ribose)polymerase] represents a novel potential target in cancer therapy. It is involved in a DNA repair process by catalyzing the transfer of ADP-ribose units from NAD to a number of its substrate proteins. In this work, a series of novel azaindole derivatives was designed and synthesized. Moreover, 16 target molecules were screened and 8 compounds displayed inhibitory activity against PARP-1. It has been demonstrated that these azaindoles bearing cycloamine substituents at 2-position were active to both PARP-1 and PARP-2.
Antineoplastic Agents ; chemical synthesis ; chemistry ; pharmacology ; Aza Compounds ; chemical synthesis ; chemistry ; pharmacology ; Indoles ; chemical synthesis ; chemistry ; pharmacology ; Poly (ADP-Ribose) Polymerase-1 ; Poly(ADP-ribose) Polymerases ; metabolism

Objective To explore the difference of four calculating methods used to determine the obesity. Methods Two thousand four hundred and forty six (2446) men and three hundred and seventy nine (379) women were measured height and body mass, Standard body mass, BMI, body fat ratio and obesity index(OI) were calculated with formula. According to the BMI≥ 25 kg/m2 , BMI ≥ 27 kg/m2 and BMI≥28 kg/m2, the obese adults were 1419,680 and 435 respectively;there were 649 adults that their body mass was over 20％standard body mass; there were 639 adults that their body fat ratio was over 25％(male)and 33％(female). Results For obesity determination, the adults who were 20％overweight and over standard body fat ratio were significantly different from those whose BMI were over 25 kg/m2 ( P＜0. 05 ) ;Those who were 20％overweight and over standard body fat ratio were not significantly different from those whose BMI were over 27 kg/m2 ( P＞0.05 ) ; Those who were 20％overweight and over standard body fat ratio were significantly different from those whose BMI were over 28 kg/m2 ( P＜0. 05 ). Conclusion Determining obesity with BMI≥27 kg/m2 is feasible and rational.

Objective To establish a method for isolation and cultivation of human invasive pituitary adenoma-derived fibroblast in vitro and explore their biological properties in order to investigate the role of the fibroblasts in the invasive growth of the pituitary adenoma.Methods The fibroblasts were isolated from hu- man invasive pituitary adenoma tissue by different rate of adhesion.Primary culture and passage culture were carried out,and growth characteristics of fibroblasts were observed under phase-contrast microscope in primary and passage culture.Immunohistochemical technique was used to identify the fibroblasts.The cell growth curve was measured by MTT method.The ultrastructure was observed under electronmicroscope.Results The cultured invasive pituitary adenoma-derived fibroblasts showed active proliferative ability.The cell bodies was bigger than other tissue fibroblasts,and the cell shape was irregular.The rough endoplasmic reticulum, Golgi complex and ribosome were profuse in the cytoplasm.The positive expression rate of collagen[and vi- mentin of the fibroblasts were above 95%.Conclusion The method of different rate of adhesion is success- fully utilized to culture human invasive pituitary adenoma-derived fibroblasts.These cells showed active prolif- erative ability,and maybe have an importent function in the invasive growth of the pituitary adenoma.

Objective To investigate the association between essential hypertension(EH)and nonalcoholic fatty liver(NAFL).Methods Four hundred and nine patients of EH underwent liver uhrasonographic examina- tion during 2006-2007 year were enrolled.Patients were categorized as MS(n=312)or non-MS(n=97)ac- cording to the criteria by CDA.Body mass index(BMI),blood pressure,the profiles of blood lipid,liver func- tion,renal function,plasma sugar were determined.Results 1)The prevalence of fatty liver in EH+MS group (66.0%)was significantly higher than that of EH without MS group(41.2%,P

Objective To accurately judge the tumor-feeding artery is the most important basis for a successful treatment of hepatocellular carcinoma (HCC) with super-selective hepatic arterial chemoembo lization therapy. This study aims to assess the clinical value of cone-beam CT hepatic arteriography (CBCT-HA) in detecting tumor-feeding arteries during the performance of conventional transarterial chemoembo lization (TACE), and to compare the diagnostic effects between CBCT-HA and non-selective hepatic DSA. Methods Twenty-three consecutive patients with inoperable HCC were enrolled in this study. TACE was carried out in all patients. During the performance of TACE, the DSA-HA, CBCT-HA, Lipiodol-TACE and Lipiodol-CBCT were performed separately. The imaging materials, including DSA-HA and CBCT-HA, were analyzed by two experienced interventional physicians together to judge the tumor-feeding arteries. Statistic analysis was conducted by using chi square test. Results Tumor stain and lipiodol accumulation were regarded as the “gold standard” of the presence of tumor-feeding artery, based on which the tumor-feeding artery was confirmed in 75 lesions. DSA-HA demonstrated positive tumor-feeding artery in 40 lesions, among which true-positive tumor-feeding artery was seen in 32 and false-positive one in 8. CBCT-HA showed positive tumor-feeding artery in 72 lesions, which included true-positive tumor-feeding artery in 68 and false-positive one in 4. The sensitivity of CBCT-HA in judging tumor-feeding artery was 90.7% (68/75), which was much higher than that of DSA-HA (42.6%, 32/75), the difference was statistically significant(P<0.001). The positive predictive value of CBCT-HA in detecting tumor-feeding artery was also higher than that of DSA-HA (94.4% vs. 80.0%; P=0.040). Conclusion Cone-beam CT hepatic arteriography is obviously superior to DSA hepatic arteriography in identifying tumor-feeding arteries, which is very helpful in guiding super-selective TACE for HCC.