Nucleotide binding oligomerization domain (NOD)-like receptor protein 3, NLRP3) inflammasomes regulate the secretion of caspase-1, interleukin-18 (IL-18), IL-1β, and other cytokines, and participates in aging. In recent years, it has been found that NLRP3 inflammasomes are abnormally activated in aging heart and vessels, and inhibition of NLRP3 inflammasomes can alleviate heart aging and vascular aging. This review summarizes the research of NLRP3 inflammasome in heart and vascular aging, and the related drugs to promote the discovery of the mechanism of NLRP3 inflammasome in heart and vascular aging and the development of related drugs.

Humans ; Mouth Diseases ; drug therapy ; Mouth Mucosa ; pathology ; Thalidomide ; therapeutic use

Contraindications ; Humans ; Infant ; Infant, Newborn ; Promethazine ; adverse effects

Poly(ADP-ribose)polymerase-1 (PARP-1) plays a significant role in the DNA repair process by catalyzing the transfer of ADP-ribose from NAD+ to its receptors. It is a promising anticancer drug target and many PARP-1 inhibitors have been developed and used in the clinical trial. In this work, a series of 3-(2-oxo-2-substituted acetamido)benzamides have been synthesized and their inhibitory activities against PARP-1 were evaluated. Of all the tested compounds, six compounds displayed inhibitory activities with IC50 values ranging from 0.23 to 5.78 µmol.L-1 . The binding pose of compound 5a was predicted using molecular docking to facilitate further structural modification.

Objective To determine the safety and clinical value of secondary ERCP to a failed intubation procedure.Methods A total of 212 patients with difficult intubation during ERCP procedures were enrolled.Patients with failed conventional intubation accepted precut sphincterotomy.The operation stopped after one hour of effort.A secondary selective ERCP was performed at a appropriate time.The operation success rate and complication rate of first ERCP and secondary ERCP were compared.Results The success rate of first ERCP was 67.0％ (142/212),and the total success rate was 90.6％ (192/212).The total success rate is significantly higher than that of first ERCP operation(x2 =35.263,P ＜0.05).The complication rate of first ERCP,secondary ERCP and total complication rate was 8.96％ (19/212),4.29％ (3/70),10.38％ (22/212),respectively.Complication rates of total ERCP and secondary ERCP were not significantly different from the first ERCP (P ＞ 0.05).Conclusion It is safe and effective for patients with failed ERCP intubations after precut to receive a secondary ERCP at a appropriate time.

Objective To assess the effects of fluvastatin retard tablets on the elder patients of acute coronary syndrome(ACS) complicated with diabetes mellitus(DM) undergoing percutaneous coronary intervention (PCI) and the safety of drugs.Methods From December 2009 to December 2011,78 elderly patients (age≥65 years) of ACS complicated with DM who underwent PCI were enrolled in this study.They were all treated by drug elution stents.They were divided into group A(fluvastatin retard tablets 80 mg/d) and group B (fluvastatin retard tablets 160 mg/d) with 39 cases each by random digits table method.The plasma levels of high sensitivity C reactive protein (hs-CRP),matrix metalloproteinase proteinase 9 (MMP-9),monocyte chemoattractant protein 1 (MCP-1) and lipid levels were measured before and after treatment of 24 h,7 d and 180 d.All the patients were followed up for 180 d,and the adverse reaction of drug and the incidence of cardiovascular event were detected.Results Blood lipid levels had no significant changes in the two groups before and after treatment (P ＞ 0.05).The plasma levels of hs-CRP,MCP-1,MMP-9 were higher after treatment of 24 h than those before treatment in two groups [group A:(12.14 ± 2.71)mg/L vs.(8.76 ±2.25) mg/L,(491.75 ± 19.29) ng/L vs.(440.56 ± 13.15) ng/L,(449.6 ±11.8) μmol/L vs.(353.8 ± 16.0) μ mol/L;group B:(11.39 ± 2.38) mg/L vs.(9.30 ± 1.99) mg/L,(488.56 ± 17.61) ng/L vs.(436.06 ± 15.36) ng/L,(444.9 ± 19.1) μ mol/L vs.(349.8 ± 13.6) μmol/L],and there were significant differences (P ＜ 0.05).The plasma levels of hs-CRP,MCP-1,MMP-9 decreased significantly after treatment of 7,180 d compared with that after treatment of 24 h in two groups (P ＜ 0.05).Compared with those in group A,the plasma levels of hs-CRP,MCP-1,MMP-9 decreased even lower in group B[after 7 d:(4.51 ±1.16) mg/L vs.(5.43 ± 1.44) mg/L,(306.06 ± 18.49) ng/L vs.(384.64 ± 13.23) ng/L,(206.2 ± 16.8)μ mol/L vs.(263.4 ± 15.4)μ mol/L;after 180 d:(4.23 ± 1.08) mg/L vs.(4.68 ± 1.46) mg/L,(280.16 ± 14.54) ng/L vs.(354.64 ± 11.32) ng/L,(187.2 ± 14.2)μ mol/L vs.(225.4 ± 12.7) μ mol/L],and there were significant differences (P ＜ 0.05).After followed up for 180 d,there was no serious adverse reaction in two groups,and the total incidence of cardiovascular event in group B was lower than that in group A [7.7％(3/39) vs.25.6％ (10/39)],and there was significant difference (P ＜ 0.05).Conclusion Intensive lipid lowering therapy can reduce the level of inflammatory factors and cardiovascular event of the elder patients of ACS complicated with DM undergoing PCI and has good security.

The progress in integrative medicine (IM) of coronary heart disease (CHD) in 2013 was summarized in this paper. Gratifying progress has taken place both in clinical studies and basic research of IM on CHD during 2013. We got some innovation in Chinese medical etiologies and pathogeneses of CHD. We also got some improvement in researches on Chinese medical syndromes in various fields. Many clinical studies have proved Chinese medicine and pharmacy is playing a role in preventing and improving CHD patients. In-depth basic researches on preventing and treating CHD by IM are gradually undergoing. Acting targets and mechanism are further clarified. Besides, we also pointed out the developing tendency of CHD researches and the current deficiency in CHD researches, hoping to provide reference for further studies in this field.
Coronary Disease ; drug therapy ; Drugs, Chinese Herbal ; therapeutic use ; Humans ; Integrative Medicine

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.

Objective To analyze the mechanism of fentanyl combines midazolam,by comparison with some of the commonly used anesthetic method to determine in the ethical advantages of anesthesia.Methods 45 rats were randomly divided into three groups,Group A:1％ anesthetized by intraperitoneal injection of sodium pentobarbital 40 mg/kg; Group B:5 ％ ketamine 120 mg/kg intraperitoneal injection; Group C:midazolam 5 mg/kg + fentanyl 0.05 mg/kg Last intravenous anesthesia.Observe the effects of anesthesia.Results The rats which are used of fentanyl conbines midazolam anesthesia,the onset of anesthesia time:0.02 ± 0.03 min,maintenance of anesthesia time:89.73 ± 22.59 min,the the narcotic operation time:1.51 ± 0.30 min,the success of anesthesia cases:15 cases.Conclusions Fentanyl combines midazolam compared with the currently used method of anesthesia,the advantages of the more prominent,it has significant improvement and protection about the security,utilization and recovery ethics in experimental rats.

Objective To evaluate the clinical utility of SpyGlass single-operator ERCP-guided cholangiopancreatoscopy system for the diagnosis and treatment of bile duct disorders.Methods A total of 9 patients with biliary diseases were treated with SpyGlass single-operator ERCP-guided cholangiopancreatoscopy system.Four patients with large bile duct stones accepted laser lithotripsy,and stones were removed by ERCP.Five patients with indeterminate bile duct stricture accepted cholangioscopy-guided sampling.All patients underwent ENBD,routine blood test,blood amylase test,oral food and water restriction,acid suppression and prophylactic antibiotics.Results SpyGlass was successful in all patients with a manipulating time of 21.2min and total procedure time of 46.2min.Complete stone clearance was achieved in all 4 patients with large biliary stones.Sample quality was adequate in all patients with bile duct stricture with 2 patients diagnosed as having malignant biliary tumor and 3 as inflammatory bile duct stenosis.Post-ERCP complications including mild pancreatitis in 2 patients,and the patients recovered gradually after corresponding treatment.Conclusion ERCP-guided cholangiopancreatoscopy with the SpyGlass system is technically feasible and can be successfully and safely performed in patients with biliary disorders.