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1.
Acta Pharmaceutica Sinica ; (12): 256-262, 2018.
Article Dans Chinois | WPRIM | ID: wpr-779871

Résumé

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.

2.
Journal of Zhejiang University. Science. B ; (12): 313-318, 2008.
Article Dans Anglais | WPRIM | ID: wpr-359427

Résumé

<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>


Sujets)
Humains , Lignée cellulaire , Noyau de la cellule , Métabolisme , Cytoplasme , Métabolisme , Régulation négative , Régulation de l'expression des gènes , Luciferases , Métabolisme , Microscopie confocale , Modèles biologiques , Plasmides , Métabolisme , Régions promotrices (génétique) , Récepteur à l'insuline , Génétique , Résistine , Pharmacologie , Transcription génétique , Transfection
3.
Journal of Zhejiang University. Medical sciences ; (6): 588-591, 2007.
Article Dans Chinois | WPRIM | ID: wpr-344394

Résumé

<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>


Sujets)
Humains , Séquence nucléotidique , Clonage moléculaire , Gènes de synthèse , Vecteurs génétiques , Données de séquences moléculaires , Réaction de polymérisation en chaîne , Méthodes , Protéines recombinantes , Génétique , Métabolisme , Résistine , Génétique , Métabolisme
4.
Journal of Zhejiang University. Science. B ; (12): 875-880, 2007.
Article Dans Anglais | WPRIM | ID: wpr-277304

Résumé

<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>


Sujets)
Femelle , Humains , Mâle , Adulte d'âge moyen , Syndrome coronarien aigu , Sang , Angine de poitrine , Sang , Infarctus du myocarde , Sang , Résistine , Sang
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