Diversity-oriented synthesis (DOS) aims to efficiently generate collections of small molecules with diverse appendages, functional groups, stereochemistry and skeletons, thus yielding diverse biological activities capable of modulating a wide variety of biological processes. In this review, we discussed the common strategies employed in DOS with specific examples from recent literature, including reagent-based approach, substrate-based approach, build-couple-pair strategy and privileged substructure-based DOS. The application of some DOS libraries in drug discovery is also presented.

OBJECTIVE To study the feasibility and security of parotidectomy for parotid benign tumor by tracing cervical branch to expose facial nerve. METHODS Parotid benign tumor of 87 patients were studied.We exposed facial nerve by tracing main facial nerve branch、buccal branch、marginal mandibular branch and cervical branch in parotidectomy for parotid benign tumor and observed the function of facial nerve after operation.RESULTS The number of patients traced by main facial nerve branch- buccal branch、marginal mandibular branch and cervical branch group were 10、8、28 and 41 respctively,and the percentage of facial nerve injury after operation were 30%、37.5%、46.4%and 24.3%.The percentage of facial nerve injury was statistically different between the marginal mandibular branch group and the cervical branch group(P

Objective To understand the expression of heat shock protein(HSP70)mRNA induced by chlorpyrifos in the hepatic tissue of rats.Methods Wistar rats aged 6 weeks were divided into 4 groups,12 in each including 6 male and 6 female,the rats in the experimental groups were treated with chlorpyrifos by gavage once a day at the doses of 17 mg/kg?bw,8.5 mg/kg?bw and 4.25 mg/kg?bw respectively for 14 consecutive days,one group was the negative control.After the exposure,the hepatic tissue was sampled to examine the expression of HSP70 mRNA by polymerase chain reaction(PCR).Results The expression of HSP70 mRNA in the hepatic tissue in the groups of 17 mg/kg?bw,8.5 mg/kg.bw was significantly up-regulated with a dose-response relationship compared with the negative control group.Conclusion The expression of HSP70 mRNA is a sensitive parameter for early exposure assessment of chlorpyrifos.

Objective:To study behavior problems,family factors an d parental rearing styles in students with poor academic achievement.Meth od:Through stratified cluster sampling,488 primary or middle school studen t s were identified as study group(below 5th percentile in their classes),while th e controls were 599 students whose academic achievement were above 95th percent ile in their classes.All subjects completed EMBU,CBCL(children behavior checkli st).Results:Higher boy/girl ratio was pound in study group(326/162) than in control(291/308,? 2=36.4,p

In recent studies,obesity is a risk factor for a variety of cancers,including breast cancer and colorectal cancer.Obesity can regulate the tumorigenesis and development of cancer by some factors,such as insulin and insulin-like growth factor-1 (IGF-1),leptin,fat cytokines and hormones.Understanding the relationship between obesity and cancer can provide a new perspective for the prevention and treatment of cancer.

Objective: To explore the prevalence of depression in junior school students and its relationship with potential psychological and environmental factors. Method:Depressive symptoms, self-esteem, life events, social support, family cohesion and conflict were investigated with self-report questionnaire in 300 junior school students, the relationship between depression and other psychological or environmental factors were analyzed through stepwise regression. Results:The prevalence of depression in junior high school students was 11%. Among the 5 investigated psychological and environmental factors, self-esteem and social support were negatively related with depression (standardized regression coefficient were -0.59 and -0.14), while life events positively related with it(standardized regression coefficient was 0.26). Only "academic pressure" and another factors covering the item "do not want to go to school" showed a negative association with the students' self-esteem among the 6 factors included in the life events questionnaire (standardized regression coefficient were -0.149 and -0.13).Conclusion: Depression is common among junior school students. Poor self-esteem, lack of social support and negative life events are currently related with the development of adolescent depression. The pressure and failing experiences coming from academic activities are the most influential life events to the development of adolescents' self-esteem.

Objective To study the effects of organ dose modulation (ODM) technique on dose reduction of the breasts and the related thoracic image quality in female chest CT.Methods One hundred and twelve female patients with chest CT were enrolled in this study and divided into two groups according to the order:control group (n =56,using conventional scan) and experimental group (n =56,using ODM technique).The tube currents in different directions (A/L/P/R) were analyzed in the two groups.The effects of ODM on the radiation dosage and image quality were assessed.Results The tubc currents in anterior and posterior direction were both (128 ± 43)mA in the control group.However,the tube current in the anterior was lower than that in the posterior in experimental group (t =-18.701,P ＜0.01).The tube currents in all direction in the experimental group were all lower than those in the control group (t =11.71-20.22,P ＜0.01).The CTDIvol and E in the experimental group were lower than those in the control group(t=3.58,3.55,P ＜0.05).There were no significant differences for the objective and the subjective scores between two groups (P ＞ 0.05).Conclusions ODM technique could protect the female breasts by reducing the radiation dose without image quality degrading during chest CT scan.

The objectives of this study are to prepare resveratrol loaded mixed micelles composed of poloxamer 403 and poloxamer 407, and optimize the formulation in order to achieve higher drug solubility and sustained drug release. Firstly, a thin-film hydration method was utilized to prepare the micelles. By using drug-loading, encapsulation yield and particle size of the micelles as criteria, influence of three variables, namely poloxamer 407 mass fraction, amount of water and feeding of resveratrol, on the quality of the micelles was optimized with a central composite design method. Steady fluorescence measurement was carried out to evaluate the critical micelle concentration of the carriers. Micelle stability upon dilution with simulated gastric fluid and simulated intestinal fluid was investigated. The in vitro release of resveratrol from the mixed micelles was monitored by dialysis method. It was observed that the particle size of the optimized micelle formulation was 24 nm, with drug-loading 11.78%, and encapsulation yield 82.51%. The mixed micelles increased the solubility of resveratrol for about 197 times. Moreover, the mixed micelles had a low critical micelle concentration of 0.05 mg · mL(-1) in water and no apparent changes in particle size and drug content were observed upon micelles dilution, indicating improved kinetic stability. Resveratrol was released from the micelles in a controlled manner for over 20 h, and the release process can be well described by Higuchi equation. Therefore, resveratrol-loaded poloxamer 403/407 mixed micelles could improve the solubility of resveratrol significantly and sustained drug release behavior can be achieved.

Objective To compare the anti-tumor activity and antioxidant activity of ethanol extracts of F.veluties and A.auricula.Methods Three human carcinoma cell lines, including MCF-7, HeLa and A375 were assessed by MTT assay to measure cell viability.The antioxidant activity was detected with a DPPH and RFAP assays.Results Two domestic fungus have different anti-tumor activity on the inhibition of MCF-7, HeLa and A375 cells at 25-400μg/mL concentration rage.F.velutipes was better than the A.auricula.The difference was statistically significant ( P<0.05 ).Compared with the control group, the inhibition of F.velutipes were 48.20%, 52.61%and 50.58%at the concentration of 400μg/mL, respectively (P<0.01).At the same concentration, the inhibition of A.auricula were 37.62%、50.21%and 41.59%, respectively (P<0.01).The ethanol extracts of two domestic fungus have significant antioxidant activity.F.velutipes was better than the A.auricula.The difference was statistically significant ( P<0.01 ).Compared with the control group, the scavenging radical capacities on DPPH of ethanol extracts of F.velutipes and A.auricula were 60.30%and 40.43%at the concentration of 1.6 mg/mL, respectively (P<0.01).At the same concentration FRAP value were 9.5 and 7.0 mmol/mL(P<0.01).Conclusion The F.velutipes and A.auricula both have strong anti-tumor and antioxidant activities, F.velutipes is better than A.auricula.

Objective To analyse the etiology and clinical characteristics of 26 critically ill children with severe hand foot and mouth disease (HFMD) of Shanxi province in 2010.Methods We retrospectively analysed the clinical data of 26 children with severe HFMD from Mar to Sep 2010.Nucleic acid of enterovirus 71 ( EV71 ) and Coxsackie virus A 16 ( CoxA16) were detected in 20 out of 26 children with HFMD by reversed real time polymerase chain reaction (rRT-PCR),and the whole VP1 gene of EV71 deriving from 6 different areas of Shanxi province was amplified,sequenced,and compared with strains from other areas in china.Results EV71 nucleic acid were positive in 18 out of 20 children,while the other two were negative for EV71 and CoxAl6.Among all the critical cases,20 cases (76.9％) occurred in Weinan area,four in Xianyang area,and two in Xi'an urban area.Compared with those of Fuyang Anhui,Hong Kong China,Guangzhou,Shenzhen,Shandong,Beijing,the homology of the whole VP1 gene sequence from 6 strains of Shanxi area was 96％ ～ 100％.Most of the critical children were under 3-year-old,and the incidence rate of male children was higher than that of female children.All affected children had persisted fever,poor energy,hyperarousal,hypersomnia,and limb shaking.Meanwhile their peripheral blood leukocytes,C-reactive protein and blood glucose were markedly increased,but renal injuries were rare.Eighteen children clinically recovered on discharge,among which 2 cases had sequelae of limb activity obstacle,and 8 cases died.Conclusion Weinan is the area with the highest incidence rate of critical HFMD cases in Shanxi Province,and the major etiological organism is EV71,which is highly homologous to EV71 found in other regions of mainland China.As many cases are in dangerous condition,thus early identification and intervention could inhibit the disease progression,and play a key role in reducing the mortality.