Synthesis and anti-inflammatory activity of novel isobutyl benzophenone derivatives / 药学学报

Twenty target compounds were synthesized by the reduction reaction of HUANG Minglong and Friedel-Crafts acylation reaction in this study. The inhibitory effects of the new compounds were tested on NO production in LPS-induced mouse macrophage RAW264.7 cells, a cellular inflammation model. The structure-activity relationships were discussed. The structures of target compounds were confirmed by ESI-MS, 1H NMR and 13C NMR. In vitro activity experiments showed that 18 compounds had certain anti-inflammatory effects at the concentration of 40 μmol·L-1, of which 9a, 8b, 7c and 9c showed strong anti-inflammatory activities, and IC50 of 7c and 9c were comparable to the positive control drug ibuprofen.

Resistin does not down-regulate the transcription of insulin receptor promoter / 浙江大学学报（英文版）（B辑：生物医学和生物技术）

<p><b>OBJECTIVE</b>To detect the effect of resistin on the transcription of insulin receptor promoter.</p><p><b>METHODS</b>Luciferase reporter gene was fused downstream of human insulin receptor promoter and the enzymatic activity of luciferase was determined in the presence or absence of resistin. The resistin expressed with plasmid was stained with antibody against Myc tag which was in frame fused with resistin coding sequence, and then imaged with confocal microscopy.</p><p><b>RESULTS</b>The treatment of pIRP-LUC transfected cells with recombinant resistin did not result in significant difference in the enzymatic activity of luciferase compared to the untreated cells. Cell staining showed that green fluorescence could be observed in the cytoplasm, but not in the nucleus.</p><p><b>CONCLUSION</b>The results suggest that the endogenous resistin may functionally locate in the cytoplasm, but does not enter the nucleus and not down-regulate the transcription of insulin receptor promoter.</p>

Assembly of full-length human resistin gene in vitro and construction of its eukaryotic expression vector / 浙江大学学报·医学版

<p><b>OBJECTIVE</b>To assemble the full-length of human resistin gene in vitro by using oligonucleotides and to construct its eukaryotic expression vector.</p><p><b>METHODS</b>According to the gene sequence of resistin (GenBank: AF323081), 10 oligonucleotides were designed and synthesized, followed by a touch down PCR to assemble the full-length gene. The PCR products were cloned into pSecTag2B vector and confirmed by sequencing.</p><p><b>RESULTS</b>The band of PCR products and gene sequencing showed the insert fragment in pSecTag2B vector was identical to that as designed.</p><p><b>CONCLUSION</b>The full-length of human resistin coding sequence was successfully assembled and amplified by touch down PCR, and a resistin-expressing eukaryotic vector was constructed.</p>

Relationship between resistin level in serum and acute coronary syndrome or stable angina pectoris / 浙江大学学报（英文版）（B辑：生物医学和生物技术）

<p><b>OBJECTIVE</b>To investigate the relationship between serum resistin level and acute coronary syndrome (ACS) or stable angina pectoris (SAP).</p><p><b>METHODS</b>Sixty-five patients, with coronary artery disease, were enrolled and divided into three subgroups: acute myocardial infarction (AMI), unstable angina pectoris (UAP) and SAP, and 26 healthy people were recruited as controls in the cross-sectional study. Serum resistin levels were determined by ELISA (enzyme-linked immunosorbent assay), and WBC (white blood cell count), hsCRP (high sensitive C-reaction protein), CK(max) (maximum of creatinkinase), CK-MB(max) (maximum of isozyme of creatinkinase) and cTnI(max) (maximum of troponin) were measured by standard laboratory methods.</p><p><b>RESULTS</b>The serum resistin levels were 4 folds higher in AMI patients, 2.43 folds in UAP patients and 1.12 folds in SAP patients than in the healthy controls (P<0.05). The resistin levels were also significantly different between AMI [(8.16+/-0.79) ng/ml], UAP [(5.59+/-0.75) ng/ml] and SAP [(3.45+/-0.56) ng/ml] groups (P<0.01); WBC, hsCRP, CK(max), CK-MB(max) and cTnI(max) were significantly increased in AMI patients over UAP and SAP patients. Spearman analysis showed that serum resistin levels were positively correlated with WBC (r=0.412, P=0.046), hsCRP (r=0.427, P=0.037), CK(max), CK-MB(max) and cTnI(max) (r=0.731, 0.678, 0.656; P<0.01).</p><p><b>CONCLUSION</b>Serum resistin levels increased with inflammatory factors and myocardial impairment. The results suggest that human resistin might play an important role in the pathogenesis of atherosclerosis and AMI as an inflammatory factor.</p>