Synthesis and cytotoxic activity of 3, 4, 11-trihydroxyl modified derivatives of bergenin / 中国天然药物

To synthesize a series of 3-, 4-, and/or 11-trihydroxy modified bergenin derivatives and evaluated their cytotoxic activity in vitro. The phenolic hydroxyl groups of bergenin were protected by benzyl groups with benzyl bromide. Treatment of dibenzyl bergenin with the corresponding acid in the presence of EDC·HCl and DMAP in CH2Cl2, followed by hydrogenation over Pd/C catalysts, afforded derivatives of bergenin esters. All of the target compounds were identified by IR, MS, and (1)H NMR. Twenty-six novel and three known derivatives of bergenin esters were synthesized. Their cytotoxicity values were evaluated by the MTT assay on the inhibition of DU-145 and BGC-823 cells in vitro. Several triply-substituted (3a, 4a, 5a, 6a, 7a) and doubly-substituted (8b, 9b) bergenin derivatives exhibited higher cytotoxic activity than bergenin. The result showed that the size of substituents and the lipophilicity of the bergenin esters displayed an important role on their cytotoxic activity.

Effect and safety of the therapies for acute myocardial infarction patients with failed thrombolytic therapy: a systematic review / 南方医科大学学报

<p><b>OBJECTIVE</b>To assess the effect and safety of therapies in common use for acute myocardial infarction (AMI) patients with failed thrombolytic therapy.</p><p><b>METHODS</b>We searched the Cochrane Central Register of Controlled Trials (CENTRAL, Issue 2, 2006), MEDLINE (1966 to July 2006), EMBASE (1984 to July 2006), China National Knowledge Infrastructure (CNKI, 1994 to July 2006), China Biomedicine Database disc (CBMdisc, 1980 to July 2006). We also searched several key Chinese journals in the field of cardiovascular diseases. The language was limited to Chinese and English. We included all the randomized controlled trials (RCTs) for acute myocardial infarction patients with failed thrombolytic therapy. Two authors independently assessed the methodological quality of the included studies, the data were analyzed by RevMan 4.2.8 from the Cochrane Collaboration.</p><p><b>RESULTS</b>Nine RCTs met the inclusion criteria. A significant difference was found between the rescue percutaneous coronary intervention (PCI) group and conventional treatment group in the mortality rate at the end of the follow-up [RR=0.64, 95%CI (0.41, 0.98)]. Thromboembolic stroke and bleeding in rescue PCI group were significantly higher than that in conventional treatment group [RR=4.39, 95%CI (1.14, 16.87), and RR=2.79, 95%CI (1.55, 5.02), respectively]. Compared with conventional therapy, rescue thrombolytic treatment was associated with a significantly higher reperfusion rate [RR=2.92, 95%CI (1.75, 4.85)]. Comparison between rescue PCI with rescue thrombolytic treatment revealed that the revascularization rate in rescue PCI group was significantly lower than that in rescue thrombolytic group [RR=0.57, 95%CI (0.34, 0.95)], and the incidence of bleeding was significantly higher in rescue PCI group [RR=2.15, 95%CI (1.27, 3.63)]. Comparison of glycoprotein (GP)IIb/IIIa receptor antagonists with standard treatment showed no significant difference between them in the mortality rate and bleeding rate at the end of the follow-up.</p><p><b>CONCLUSION</b>Current evidence does not confirm the effect or safety of the therapies for AMI patients with failed thrombolytic therapy, nor support the routine use of these therapies in clinical practice except for rescue PCI that reduces mortality compared with traditional treatment. Further high-quality randomized controlled trials are needed to provide reliable evidence for the treatments of AMI patients with failed thrombolytic therapy.</p>

Prevalence and correlation factors of carotid atherosclerosis among the middle and old aged workers in an Iron and Steel corporation, Chongqing / 中华流行病学杂志

Objective To investigate the prevalence and correlation factors of carotid atherosclerosis (CAS) among workers of Chongqing Iron and Steel Corporation, and to offer information for the development of prevention program for cerebro-vascular disease. Methods 512 asymptomatic individuals (mean age 56.8 years, ranged from 45 to 80) from the subsidiary workshop of Chongqing Iron and Steel Corporation were recruited. Demographic data and serum were collected and the internal-media thickness (IMT) of the CAS and the extent of plaque formation were evaluated by B-mode ultrasound. Logistic regression analysis was used to estimate the correlation factors of CAS. Results (1) The overall prevalence of carotid atherosclerosis among the iron and steel workers was 37.6%. IMT was found as 10.2% , with the prevalence rates of nonstenotic plaque and stenotic plaque were 25.0% and 2.4% respectively. (2)It was shown by logistic regression analysis that age (0R=1.289, 95%CI: 1.014-1.568, P<0.001 ), smoking (0R=1.420, 95%C1: 0.802-3.872, P<0.001 ), hypertension (0R=4.530, 95%CI: 3.952-6.753, P<0.001), diabetes mellitus (0R=2.285, 95%C1: 1.008-5.057, P<0.001 ), HsCRP(0R= 1.273, 95%C1: 0.479-2.889, P=0.037), TC (0R= 1.032,95%C1: 0.320-1.882,P=0.047) and LDL-C (0R=2.313, 95% CI:1.237-4.331, P=0.008) were significantly associated with the severity of CAS. (3)Prevalence of the CAS increased with the increasing number of correlation factors. Conclusion The prevalence of CAS among the iron and steel workers was higher than those in ordinary people of the same age. Age, smoking, hypertension, diabetes mellitus, HsCRP, TC and LDL-C were independent risk factors related to CAS. The prevalence of CAS was increasing parallel to the number of correlation factors.

The Application of Transcranial Color-Coded Sonography in Cerebrovascular Diseases / 国际脑血管病杂志

Transcranial Doppler combined with flow imaging technique can conveniently,nonin- vasively and accurately detect the blood flow in large intracranial vessels.It has practical signifi- cance in the diagnosis and treatment of cerebrovascular diseases.This article reviews the appli- cation of transcranial color-coded sonography(TCCS)in cerebrovascular diseases.