Kinetically Controlled Stereoselective Synthesis of 2-Oxo-2-aryl-1,3,2-dioxaphosphorinane Derivatives via a Palladium-Catalyzed Reaction.

Chiral phosphonate esters have been widely applied in the fields of organic chemistry, medicine, and photoelectric materials. However, it requires the challenging enantioselective synthesis of cyclic phosphonate esters with the desired chiral configuration. The two epimers of 2-oxo-2H-1,3,2-dioxaphosphorinane derivatives should have different reactivities in Pd-catalyzed coupling reactions, which could lead to an effective methodology for the asymmetric synthesis of 2-oxo-2-aryl-1,3,2-dioxaphosphorinane derivatives. A thorough investigation of the coupling reactions both computationally and experimentally led to the stereoselective synthesis of chiral cyclic phosphonate esters. The axial isomer of products can be obtained with both high diastereoselectivity and good chemical yields from the mixture of 2-oxo-2H-1,3,2-dioxaphosphorinane derivatives under kinetically controlled conditions.

Effect of natriuretic peptide on vascular endothelial function and inflammatory factors of patients with heart failure complicating myocardial infarction / 药物评价研究

Objective To investigate the effect of natriuretic peptide on vascular endothelial function and inflammatory factors of patients with heart failure complicating myocardial infarction.Methods Two hundred and twenty-six patients with heart failure complicating myocardial infarction admitted into Hanzhong Central Hospital from March 2012 to March 2016 were randomly divided into experimental group (n =138) and control group (n =128).Patients in control group were treated with conventional drug,and patients in experimental group were treated with natriuretic peptide based on conventional drug treatment.The vascular endothelial function,contents of NO and eddthelin 1,and inflammatory factors including CRP,IL-6,and TNF-α were detected.Results After 2 weeks of treatment,the flow-mediated vasodilation (FMD) and NO in experimental group were remarkably higher than those in control group,and eddthelin 1 was significantly lower than those of control group (P ＜ 0.05).Additionally,CRP,IL-6,and TNF-α in experimental group were significantly lower than those in control group after treatment for 5 d (P ＜ 0.05).Conclusion Natriuretic peptide could improve the vascular endothelial function of patients with heart failure complicating myocardial infarction via increasing the content of NO and decreasing content of eddthelin 1,and was benefit to cardiac function by inhibiting release of inflammatory factors.

Effect of bazedoxifene on endometriosis in a rat model / 中华妇产科杂志

Objective To investigate the therapeutic mechanism of bazedoxifene, the third-generation selective ER modulator (SERM), on endometriosis lesions in a rat model. Methods Endometriosis was induced by transplanting pieces of endometrium from other syngeneic rats that were as donors onto the subcutaneous of other unmated female rats. The rats with successful ectopic implants were divided into two groups:control group (n=10) and bazedoxifene group (n=10). The macroscopic morphology, volume, histopathology of ectopic implant and rats uterine wet weight were determined before and after the treatment. Expression of proliferation cell nuclear antigen (PCNA), ER and PR in the eutopic endometrium and endometriosis lesions detected by immunohistochemistry in the two groups. Results (1) The gross morphology and histological changes of endometriosis lesions in rats after treatment: compared with the control group, it was obviously depauperated and had more less glands and blood vessels in the stroma. (2) The change of rats′weight, the volume of endometriosis lesion before and after treatment and rats uterine wet weigh after treatment respectively in the control group and the bazedoxifene group:rats′ weight were respectively before treatment: (201±17) g, (202±18) g, that were respectively after treatment: (266±16) g, (261±16) g, which showed no significant difference between two groups before and after treatment (P>0.05). The volume of ectopic implant before treatment were respectively (85±17) mm3, (85±12) mm3, and showed no significant difference between two groups;that were respectively (48±11) mm3, (24±9) mm3 afte rtreatment, which was significantly decreased compared with the control group (P0.05). Conclusion Bazedoxifene could obviously reduce the size of endometriosis lesions, the mechanism may be related with suppressing estrogen-induced proliferation, the expression of ER and direct ER antagonism by this SERM.

The clinical observation of GnRHa and addback therapy for 153 cases of severe endometriosis after laparoscopic surgery / 实用医学杂志

Objective To investigate the clinical effect of Gonadotropin-releasing hormone agonist (GnRHa) combined with addback therapy after laparoscopic surgery on 153 cases with severe endometriosis patients. Methods 153 cases with severe endometriosis patients who underwent laparoscopic surgery from 2011 to 2013 were retrospectively analyzed in the Second Affiliated Hospital of Zhengzhou University. According to GnRHa or addback therapy three groups were divided:GnRHa group,GnRHa and addback therapy group, control group. The curative effects of different treatment group, adverse reactions, recurrence rates, and fertility were analyzed. The follow-up time was 6-24 months with an average time of 17.15 months. Results 51 patients suffered from obvious menopausal symptoms and received addback therapy (Progynova,0.5~1 mg/d). The VAS score and Kupperman score in GnRHa group,GnRHa and addback therapy group were significantly superior to the control group (P 0.05). The VAS scores in the GnRHa group and addback therapy group were 2.14±2.02 and 1.73±2.17 , respectively (P > 0.05). The main side effect of GnRHa group is hot flashes, diaphores, insomnia, sexual dysfunction, etc. The incidences were higher in the GnRHa group than that in the addback therapy group. But the addback therapy can significantly relieve the symptoms of low estrogen introduced by the application of GnRHa (P<0.05). Conclusions Laparoscopic combined with GnRHa treatment can significantly improve clinical curative effect of endometriosis. Addback therapy could abate the side reaction of GnRHa and do not affect the clinical curative effect. The clinical curative effect in the GnRHa and addbacktherapy group were superior to the GnRHa group.

Six-month angiographic and one-year clinical outcomes of polymer free paclitaxel-eluting stent in patients with ST-segment elevation myocardial infarction: a comparison with permanent polymer sirolimus-eluting stent / 中华医学杂志(英文版)

<p><b>BACKGROUND</b>Since permanent polymer is implicated in adverse events associated with delayed vessel healing after drug eluting stents (DES) implantation, great efforts have been made to develop more biocompatible DES with biodegradable polymer or without polymer. The present study aimed to evaluate the safety and efficacy of polymer free paclitaxel-eluting stents (PF-PES) in comparison with permanent polymer sirolimus-eluting stents (PP-SES) in patients with acute ST-segment elevation myocardial infarction (STEMI).</p><p><b>METHODS</b>Patients with STEMI were randomly assigned to receive PP-SES (n = 55), and PF-PES (n = 50). The 6-month angiographic and 1-year clinical outcomes were compared between the two groups. Target lesion failure (TLF) was defined as the composite of cardiac death, recurrent nonfatal myocardial infarction (Re-MI), or target lesion revascularization (TLR).</p><p><b>RESULTS</b>Follow-up angiography at six months was performed in 72.7% of the PP-SES group and 70.0% of the PF-PES group (P = 0.757). The two groups had comparable angiographic outcomes including minimal luminal diameter, diameter stenosis, late loss and binary restenosis. All patients were clinically followed up to one year. The two groups had similar clinical outcomes with relatively low rates of target lesion failure (10.9% PP-SES vs. 12.0% PF-PES, P = 0.861) and definite or probable stent thrombosis (1.8% PP-SES vs. 2.0% PF-PES, P = 1.000) at one year.</p><p><b>CONCLUSIONS</b>The present study suggests that the safety and efficacy of PF-PES in the setting of STEMI are comparable to PP-SES. Further randomized trials with larger study populations are needed to get definite conclusions.</p>

Retrospective analysis of drug treatment on inpatients with chronic heart failure / 中华流行病学杂志

<p><b>OBJECTIVE</b>To investigate drug treatment of inpatients with chronic heart failure(CHF) during the past 30 years in some areas and to provide more information on the treatment strategy of CHF.</p><p><b>METHODS</b>In two centers a retrospective study was conducted. All data were taken from the hospitalized cases with chronic heart failure. The medication distributions in different decade, gender, age heart function grade and etiology were analyzed.</p><p><b>RESULTS</b>5189 cases were enrolled with the ratio of male to female as 1:1.02. The mean age was (62.93 +/- 13.49) years old. The general causes of chronic heart failure were as follows: coronary heart disease (44.2%), rheumatic heart disease (24.1% ) , pulmonary heart disease (19.0%) and cardiomyopathy (4.8%). The admission cardiac function was mostly seen as grade NYHA IlI and IV, and their proportions were 40.6% and 44.5%. Major medication would include nitride (80.0%), diuretics (71.8% ), digitalis (68.1% ), angiotensin conversion enzyme inhibitors (ACEI) (52.2% ) and beta-blockers (19.5% ) etc. Moreover the frequency of above used medication was essentially increasing decade by decade. The major drug treatment of pulmonary heart disease also included diuretics, nitride, digitalis. ACEI was more commonly used in male than in female cases. The frequency of ACEI and ARB were more commonly used in the group > or = 60 years old than that in the group < 60 years old. The administration frequency of beta- blockers had no significant difference among different age and sexes.</p><p><b>CONCLUSION</b>The conventional drugs such as nitride, diuretics, digitalis were still dominated the treatment of CHF. Although the administration frequency of ACEI and beta-blockers increased quickly, there had been a great gap between the optimal medical strategy and clinical practice in the management of CHF. Data showed the treatment strategy was changing.</p>

Retrospective Analysis of Hospitalized Cases with Chronic Heart Failure Complicated with Atrial Fibrillation in Single-central Hospital / 中国慢性病预防与控制

Objective To understand the trend of the constituent ratio of atrial fibrillation(AF)and primary etiology in hospitalized cases with chronic heart failure(CHF)and complicated with AF in late 20 years.Methods 1 180 patients with CHF(thereinto,440 complicated with AF)were selected from the hospitalized cases during the past 20 years(1983—2002),and a retrospective analysis was performed with every 5 years interval.Results The constituent ratio of AF in the general cases with CHF was 37.3%,and it was higher in females than in males(41.3% vs 33.4%,P

Intravascular ultrasound study of coronary remodeling and determination of matrix metalloproteinase and hypersensitive C-reactive protein / 中华心血管病杂志

<p><b>OBJECTIVE</b>To investigate remodeling characteristics of coronary lesions in patients with acute coronary syndromes (ACS) versus stable angina pectoris (SA) using intravascular ultrasound (IVUS), and to explore the relationship between arterial remodeling and clinical presentation or matrix metalloproteinase (MMPs) or hyper-sensitive C-reactive protein (hs-CRP).</p><p><b>METHODS</b>We studied culprit lesions of 38 patients with ACS and 18 patients with SA using IVUS before coronary intervention. The lesion site and a proximal or distal reference site including the external elastic membrane (EEM) area and lumen area were analyzed. Plaque area and remodeling index (RI) were calculated, and directions of arterial remodeling were determined. Positive remodeling was defined as RI > 1.05 and negative remodeling as RI < 0.95. We analyzed the culprit lesion qualitatively, identified high risk plaque and compared them in each group. The blood level of MMP-2, MMP-9 and hs-CRP in each group were also determined.</p><p><b>RESULTS</b>The plaque area at culprit lesions in patients with ACS was significantly larger (11.94 +/- 4.90 versus 9.17 +/- 3.36 mm2; P = 0.035), and also the RI in ACS group was significantly greater than that of patients with SA (0.972 +/- 0.222 versus 0.796 +/- 0.130; P = 0.003). The distribution of remodeling in these two groups was different: positive remodeling was more frequent in ACS group than in SA group (34.2% versus 5.6%, P = 0.047), whereas negative remodeling was more frequent in SA group (52.6% versus 88.9%, P = 0.003). There was higher incidence of high risk plaque in ACS group compared to SA (76.3% versus 50.0%, P = 0.040). The level of serum MMP-2 in ACS group was higher than that of SA group (250.65 +/- 47.97 microg/L versus 214.21 +/- 47.20 microg/L, P = 0.029). The same applied for plasma MMP-9 (84.26 +/- 9.78 microg/L versus 68.46 +/- 22.82 microg/L, P = 0.038) and serum hs-CRP (3.62 +/- 3.37 mg/L versus 1.48 +/- 1.52 mg/L, P = 0.041).</p><p><b>CONCLUSIONS</b>Positive remodeling, larger plaque area and higher incidence of high risk plaque are associated with ACS, whereas negative remodeling is more common in patients with SA. This association between the extent of remodeling and clinical presentation may reflect a greater tendency that plaques with positive remodeling can cause ACS. The change of level of MMP-2, MMP-9 and hs-CRP in ACS patients may be helpful in investigating vulnerable plaques.</p>

The relationship of beta-fibrinogen gene polymorphisms and ischaemic cardiocerebral vascular disease / 中华血液学杂志

<p><b>OBJECTIVE</b>To analyze the frequency of beta-fibrinogen (beta-Fg) gene -455G/A, -148C/T and 448G/A polymorphism, fibrinogen molecular reactivity and their association with plasma fibrinogen levels in health adults, myocardial infarction and cerebral infarction disease.</p><p><b>METHODS</b>The beta-Fg gene -455G/A, -148C/T and 448G/A polymorphisms were analyzed by restriction fragment length polymorphism (RFLP). Fibrinogen molecular reactivity was analyzed for the conversion kinetics of fibrinogen into fibrin by a computer assistant procedure. Plasma fibrinogen levels were determined by Clauss method.</p><p><b>RESULTS</b>The frequencies of -455A, -148T, 448A allele in health adults were 0.185, 0.194 and 0.192, in myocardial infarction disease 0.295, 0.318 and 0.307, in cerebral infarction disease 0.177, 0.193 and 0.182, respectively. The frequencies of -455A, -148T, 448A alleles in myocardial infarction disease were apparently higher than that of health adults. There were close linkage between -455G, -148C and 448G or -455A, -148T and 448A, the correspondence was over 98%. There are no differences in the plasma fibrinogen levels of the three polymorphisms in two genotype groups. The fibrinogen molecular reactivity was significantly increased in cardiocerebral vascular disease and related with plasma fibrinogen level.</p><p><b>CONCLUSION</b>The three polymorphisms loci are strong linkage disequilibrium. There are no significant differences in the plasma fibrinogen levels of the three polymorphisms in two genotype groups. The frequencies of -455A, -148T, 448A alleles in myocardial infarction disease were apparently higher than that of health adults. It suggest that there was no association between beta-Fg gene -455G/A, -148C/T and 448G/A polymorphisms and plasma fibrinogen levels, but did in myocardial infarction disease. The fibrinogen molecular reactivity was significantly increased in cardiocerebral vascular disease and related with plasma fibrinogen level.</p>

Immediate and Follow-up Results of Stenting for the Small Coronary Artery Disease

BACKGROUND: Intracoronary stenting in large coronary artery with diameters >3 mm has been shown to be beneficial in the treatment of acute or threatened closures complicating balloon angioplasty and in the prevention of restenosis. However, whether equally favorable results are afforded by stent placement in small vessels (<3 mm) remains unclear. Accordingly, we evaluated the safety and feasibility of intracoronary stenting in native coronary vessels less than 2.75 mm in size. METHODS: Between January 1997 and July 1998, seventy eight patients with 81 lesions were treated with 83 stents, regardless of clinical setting. The angiographic criteria for enrollment included at least 70% stenosis and a vessel that reference diameter was less than 2.75 mm. Every patients received aspirin (300 mg qd, indefinitely) and ticlopidine (250 mg bid, one month) and was given a bolus dose of 10,000 U heparin during procedure. RESULTS: Angiographic success was achieved in 80 of 81 attempts (98%). There was one in-hospital death because of pump failure in AMI patient. There was no acute stent thrombosis. At 6 month follow-up, event free survival was achieved in 90% of patients and angiographic restenosis was found in 28% of patients (9/32). CONCLUSION: The present observational study demonstrates that angiography-guided stent placement in coronary artery < 2.75 mm in diameter is safe and effective in conjunction with current stent deplyment technique and antiplatelet protocol.

A Case of Transcatheter Alcohol Ablation of the Septum in a Patient of Hypertrophic Obstructive Cardiomyopathy

Hypertrophic obstructive cardiomyopathy (HOCM) is characterized by inappropriate myocardial hypertrophy that occurred in the absence of an obvious cause for the hypertrophy and dynamic left ventricular outflow tract obstruction, caused by asymmetrical septal hypertrophy and systolic anterior motion of the anterior mitral leaflet. The pathophysiological abnormality in HOCM is diastolic dysfunction, abnormal stiffness of the left ventricle with resultant impaired ventricular filling and impaired vasodilator reserve (perhaps related to the thickened and narrowed small intramural coronary arteries found in HOCM). During the early course of this progressive disease, treatment consists of negative inotropic drugs. Surgery has been the only therapeutic option in patients with hypertrophic cardiomyopathy who are resistant to drug treatment and sequential pacemaker therapy. We describe a novel catheter-based technique that may replace surgical myocardial reduction. The technique is interventional infarction of a portion of the interventricular septum by the infusion of alcohol into a selectively catheterized septal artery.

Coronary angioplasty in the elderly patients with coronary heart disease / 中国介入心脏病学杂志

Objective Summarize the lesion characters, procedure results and clinical follow up results of the elderly patients with coronary heart disease who underwent coronary angioplasty Methods 53 cases of coronary heart disease patients undergoing PTCA and stenting were ≥65 years old 35 were male, 18 were female 33 patients were diagnosed acute Q wave myocardial infarction, 2 patients acute non Q wave myocardial infarction, 14 patients unstable angina pectoris, and 4 patients coronary heart disease with severe heart failure PTCA and stenting were performed with conventional method, and temporary pacemakers were used if necessary Heparin was used if target vessel were involved in small vessels or the patients had multivessel diffuse lesions or PTCA was performed in more than one vessel Results Multivessel diffuse severe atherosclerosis was common in elderly patients The lesions were complex, and the procedures were difficult The success rate was 98% and the mortality was 11% during hospitalization 30 patients were follow up in 8 7?5 4 months, during which 11 (36%) patients had angina, 1 (3 5%) patients suffered acute myocardium infarction, 1 (3 5%) patient died of cerebral infarction, and the other 17 patients were asymptomatic Conclusion PTCA for the elderly patients is feasible The lesions in elderly patients with coronary heart disease are complex, the procedures are difficult and the mortality in hospitalization and the recurrent of ischemic chest pain are higher However, if we sufficiently estimate the lesion′s characters, PTCA can be safely performed in the elderly patients, and PTCA is the better method for elderly patients than medicine treatment