OBJECTIVE：To investigate the use of micellar paper chromatography on the isolation and identification of flavonoids and their soluble derivatives.METHOD:Quercetin,Genistein and their sulphate derivatives were separated and identified by SDS solution above critical micelle concentration (CMC) on paper chromatography.The concentration of SDS,ratio of organic modifier and their concentration,fluorescence were investigated.RESULTS:The best concentration of SDS micelle was 0.01～0.02mol*L-1,and the spot effects of micellar chromatography could be improved by adding 2%～4% isopropanol (or n-amyl alcohol)into the mobile phase.CONCLUSION:The simple,rapid,accurate and qualitative method could be used to analyze and isolate flavonoids and their soluble derivatives.

Object To prepare the water soluble quercetin arginine complex (QAC) and widen the administration path of quercetin (QUE). Methods Definite QUE and L arginine were refluxed in alcohol to prepare QAC. The QAC structure was identified by micellar paper chromatography, UV spectrometry, IR spectrometry, and X ray diffraction. Results QAC was prepared from QUE and L arginine in molar ratio 1∶1. The inhibitory activity of QAC that existed stably in room temperature on cancer cell growth was as strong as that of QUE, and the solubility of QAC in water was remarkably enhanced. Conclusion The above preparation method is simple and available, and it is suitable to improve the bioavailability.

AIMTo design and synthesize compounds with insulin-sensitizing activity.

METHODSUsing association principle of drug design, ten title compounds were designed and synthesized on the basis of known compounds with insulin-sensitizing activity, and their insulin-sensitizing activity were evaluated on 3T3-L1 pre-adipocyte cells.

RESULTSOne of the synthesized compounds showed strong insulin-sensitizing activity in vitro.

CONCLUSIONThis compound may possess good sugar-lowering activity, and will be chosen for further hypoglycemic evaluation in vivo.

3T3-L1 Cells ; metabolism ; Adipocytes ; drug effects ; Animals ; Drug Design ; Hypoglycemic Agents ; chemical synthesis ; pharmacology ; Indoles ; chemical synthesis ; pharmacology ; Insulin ; pharmacology ; Mice ; Triglycerides ; metabolism

Objective To investigate the value of high-resolution magnetic resonance imaging (HRMRI)in diagnosis of extramural vascular invasion (EMVI)of rectal cancer.Methods 33 patients with rectal cancer were reviewed preoperatively.The MRI findings of EMVI of all cases were scored and compared with the postoperative pathological results.Results The MRI EMVI scores were consistent with histopathology findings (k=0.324,P=0.039).The accuracy rate of MRI in diagnosis of EMVI was 66.7% (22/33).The MRI EMVI scores rose up with increased pT stage,meanwhile there was a high correlation between both (r=0.546).The percentage of MRI EMVI positive number was increased with elevated pT stage,and there was also a high correlation between both (r=0.469). ROC curve showed that MRI EMVI scoring was an effective method in diagnosis of rectal cancer EMVI (AUC=0.757).Conclusion HRMRI is a valuable method in diagnosis of EMVI of rectal cancer.

Objective To observe the anti-tumor action of Chang'aishu and its influence on the expression of the Ki67 and PCNA. Methods Forty Balb/c mice with CT-26 colorectal cancer were randomly divided into four groups, including the control group (normal saline, 0.6 mL), the chemotherapy group (Xeloda 205.5 mg/kg), the high dose group (Chang'aishu 51.38 g/kg) and the low dose group (Chang'aishu 17.13 g/kg). Each group of mice was treated with intragastric administration every two days. After 15 days, the anti-tumor rate was calculated and the expression of Ki67 and PCNA were analyzed by immunohistochemistry. Results Compared with the control group, inhibitive rate of the chemotherapy group, the high dose group and the low dose group was 43.35%, 29.48% and 13.30%, respectively. Compared with the control group, the treatment group showed statistical significant difference in Ki67 and PCNA (P<0.05, P<0.01). Conclusion Chang'aishu had inhibition effect on the growth of colorectal cancer, which may be related to down-regulating the expression of Ki67 and PCNA.

Brassinosteroids, a group of plant steroid hormones, regulate many aspects of plant growth and development. We and other have previously solved the crystal structures of BRI1(LRR) in complex with brassinolide, the most active brassinosteroid identified thus far. Although these studies provide a structural basis for the recognition of brassinolide by its receptor BRI1, it still remains poorly understood how the hormone differentiates among its conserved receptors. Here we present the crystal structure of the BRI1 homolog BRL1 in complex with brassinolide. The structure shows that subtle differences around the brassinolide binding site can generate a striking effect on its recognition by the BRI1 family of receptors. Structural comparison of BRL1 and BRI1 in their brassinolide-bound forms reveals the molecular basis for differential binding of brassinolide to its different receptors, which can be used for more efficient design of plant growth regulators for agricultural practice. On the basis of our structural studies and others' data, we also suggest possible mechanisms for the activation of BRI1 family receptors.
Amino Acid Sequence ; Arabidopsis ; metabolism ; Arabidopsis Proteins ; chemistry ; metabolism ; Binding Sites ; Brassinosteroids ; chemistry ; Crystallography, X-Ray ; Molecular Sequence Data ; Protein Kinases ; chemistry ; metabolism ; Protein Structure, Tertiary ; Recombinant Proteins ; genetics ; Sequence Alignment ; Steroids, Heterocyclic ; chemistry

Objective To evaluate the value of percutaneous hyperthermia-chemotherapy (PHC)under CT guided in treating original and secondary hepatic and pulmonary malignant tumor.Methods Percutaneous hyperthermia and chemotherapy under CT guided was performed for 21 patient with original and secondary hepatic and pulmonary malignant tumor.Chemical drugs against tumors were warmed to 55～60℃ and injected into the tumors.Injected volume was according to:V=4/3 ?(r+0.5 cm) 3.Observation depends upon attenuation changes of CT scanning and biochemical index(AFP)The therapeutic effect was classified into Ⅰ～Ⅴgrade.Results The period of observation was 36 monthes,In 20 cases,survival period was 8～22 monthes,average survival period was 16 monthes.A patient had treated with PHC and transcatheter arterial embolization and was alive for 28 monthes.Total effective rate was 95.2%.Conclusion PHC under CT guidence is an effective method in treating hepatic and pulmonary malignant tumors.especially for unresected tumors.Cooperating transcatheter arterial embolization(TAE)can raise curative effect.

Objective:To explore the category,prevalence and related factors of comorbidities associated with Tourette syndrome.Methods:125 patients with TS according to CCMD-3(Chinese Classification of Mental Disorders,3rd edition)were assessed with a self-designed family circumstance questionnaire,YGTSS,CBCL,Leyton obsessive-compulsive scale,and Conner's Child Behavior Checklist.Results:Of 125 TS patients,the comorbidities included attention deficit and hyperactivity disorder(ADHD,41.6%),obsessive-compulsive disorder(OCD,25.6%), anxiety disorders(8.0%),depressive disorders(4.8%),conduct disorders(8.0%),self-injurious behavior(3.2%),and sleep disorder(2.4%).Conclusion:There are many kinds of comorbid disorders at high prevalence in TS patients. These comorbidities adversely influence the therapy and prognosis of TS and are taken as the possible reasons for social function deficit.

OBJECTIVETo develop a simple method for genotyping of hepatitis E virus (HEV) and to investigate HEV genotype distribution in Nanjing area.

METHODSTwenty-seven full HEV sequences currently-available in GenBank were analyzed with MegAlign and MapDraw programs of DNA STAR software. Degenerate primers were designed and applied to amplify a fragment in HEV ORF1 region. HEV genotypes were determined by the size of the PCR products and by single restriction endonuclease analysis.

RESULTSThe PCR products of HEV genotype 1 and 2 were 275 bp and 269 bp in size. Distinctively, the PCR products of genotype 3 and 4 were 317 bp and 314 bp in size. Moreover, the PCR products of genotype 1 could be digested by Nae 1, but the products of genotype 2 could not. Distinctively, the PCR products of HEV genotype 3 could be digested by Not 1, but the products of genotype 4 could not. Six HEV reference strains standing for different HEV genotypes were clustered into their own types as predicted. Within 43 HEV IgM-positive clinical specimens collected in Nanjing, 19 were HEV PCR-positive and identified as genotype 4.

CONCLUSIONA simple method of PCR combined with single restriction endonuclease analysis is developed for HEV genotyping. This assay allows rapid identification of a large number of HEV isolates directly from clinical specimens. Among patients with hepatitis E in Nanjing, most were infected with HEV genotype 4.

DNA Restriction Enzymes ; metabolism ; DNA, Complementary ; genetics ; metabolism ; Deoxyribonucleases, Type II Site-Specific ; metabolism ; Genotype ; Hepatitis E ; blood ; genetics ; immunology ; Hepatitis E virus ; genetics ; Humans ; Polymerase Chain Reaction ; methods ; RNA, Viral ; genetics ; Reverse Transcriptase Polymerase Chain Reaction

Ten novel compounds were designed and synthesized on the basis of compound 1, their insulin-sensitizing activities were evaluated in 3T3-L1 cells. Results showed that compound 10 exhibited strong differentiation-stimulating activity on 3T3-L1 cells model, which indicated that compound 10 may possess well insulin-sensitizing activity.
3T3-L1 Cells ; Animals ; Benzopyrans ; chemical synthesis ; pharmacology ; Drug Design ; Hypoglycemic Agents ; chemical synthesis ; pharmacology ; Insulin ; pharmacology ; Mice