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141.
Preclinical Research
A series of phosphate and thiophosphate flavone derivatives were synthesized and biologically evaluated in vitro for inhibition of steroid sulfatase (STS) activity. The described synthesis includes the straightforward preparation of 7‐hydroxy‐2‐phenyl‐4H‐chromen‐4‐one 3a, 2‐(4‐fluorophenyl)‐7‐hydroxy‐4H‐chromen‐4‐one 3b, 7‐hydroxy‐2‐(4‐(trifluoromethyl)phenyl)‐4H‐chromen‐4‐one 3c, 7‐hydroxy‐2‐(p‐tolyl)‐4H‐chromen‐4‐one 3d modified with different phosphate or thiophosphate moieties. The inhibitory properties of the synthesized compounds were tested against human placenta STS. Some of the novel STS inhibitors had good activities against STS. In particular, the bis‐(4‐oxo‐2‐(p‐tolyl)‐4H‐chromen‐7‐yl) hydrogenthiophosphate, 6i had the most potent inhibitory effect with an IC50 value of 3.25 µM as compared to an IC50 value of 8.50 µM for the 2‐(4‐trifluoromethylphenyl)‐chromen‐4‐one‐7‐O‐sulfamate used as a reference. Drug Dev Res 76 : 450–462, 2015. © 2015 Wiley Periodicals, Inc.  相似文献   
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A 65 year old man with low grade malignant B cell lymphoma developed bilateral chylothorax, which reached the volume of 52.1. Chylothorax arised most probably as a result of pleural infiltration in the course of the disease. Chemotherapy and repeated drainage of chylus was successful. The resolution of massive bilateral chylothorax in our patient shows, that conservative measures (chemotherapy and repeated pleural drainage) should be tried even in very extensive chylothorax in the course of neoplastic disease.  相似文献   
145.
BACKGROUND: Modern therapy of acute myocardial infarction (AMI) is aimed at rapid and persisting restoration of blood flow in an infarct-related artery (IRA). However, in some patients myocardial reperfusion is not achieved in spite of effective IRA recanalisation. Myocardial Blush Grade (MBG) is one of the angiographic markers useful for the detection of this phenomenon. AIM: To assess the prognostic value of MBG in patients with anterior AMI treated with primary angioplasty. METHODS: The study group consisted of 104 patients (74 males, 30 females, mean age 62+/-13 years) treated with primary angioplasty due to anterior ST-segment elevation AMI. MBG was assessed after the procedure. The mortality and major cardiovascular event (MACE) rates were analysed one and six months after AMI. RESULTS: Patients with preserved myocardial reperfusion following angioplasty (MBG 2-3, n=64 (61.5%)) had a trend towards lower one-month mortality and significantly reduced six-month mortality compared with 40 (38.5%) patients with an impaired (MBG 0-1) myocardial reperfusion (3% vs 12.5%, NS; and 6.25% vs 20%, p<0.05, respectively). The rate of MACE was significantly lower in patients with rather than without reperfusion both after one and six months of follow-up (9.4% vs 27.5%, p=0.027 and 12.5% vs 42.5%, p<0.001, respectively). Compared with patients with a high MBG score, patients with altered reperfusion more frequently had diabetes (30% vs 12.5%, p=0.04), hypertension (67.5% vs 45%, p=0.043), longer time from the onset of symptoms to balloon inflation (355.9+/-199 min vs 215.5+/-113 min, p<0.001) and lower left ventricular ejection fraction, measured 3 days after AMI (43.3%+/-8 vs 47.4%+/-9, p=0.02). CONCLUSIONS: MBG has a significant prognostic value in patients with anterior AMI treated with primary angioplasty. Diabetes, hypertension and long delay of treatment are associated with the impairment of myocardial reperfusion.  相似文献   
146.
BACKGROUND: Subacute stent thrombosis was a significant complication in the early years of coronary stenting, often leading to myocardial infarction, need for urgent surgery or even death. The introduction of intracoronary ultrasound enabled the identification and proper treatment of the main causes of stent thrombosis, reducing the rate of this complication to 1%. AIM: To identify risk factors of subacute stent thrombosis. METHODS: Data concerning 845 procedures with a single stent implantation in patients with stable or unstable angina, undergoing this procedure between 1998 and 2000, were analysed. RESULTS: Subacute stent thrombosis occurred in 13 (1.54%) patients. Risk factors for this complication included urgent procedures (so-called bailout stenting), improper pre-treatment with drugs ("ad hoc" procedures), dissection uncovered by stent, and poor final result of procedure (higher degree of residual stenosis). The majority of these patients developed myocardial infarction in spite of the fact that the patency of stented vessel was quickly achieved in all but one patient. CONCLUSIONS: Urgent stenting, improper drug pre-treatment and suboptimal result of the procedure are the risk factors of subacute stent thrombosis.  相似文献   
147.
We report a case of Fabry's disease, diagnosed in a 39-year-old patient treated for 4 years because of glomerulonephritis. The disease manifested itself by the presence of typical petechiae-like skin lesions in the bathing trunk area (angiokeratoma), eye changes, paresthesia, and--in additional investigations--mild proteinuria, lowered creatinine clearance, along with changes in the central nervous system. A biopsy of the kidney revealed the presence of foamy cells in all glomeruli, and in electron microscopy multilamellar bodies (zebra bodies). The diagnose of the disease was confirmed by a marked decrease in leucocyte alpha-galactosidase activity. An early diagnosis of non-inflammatory character of Fabry's disease allows to avoid an unnecessary immunosuppressive treatment.  相似文献   
148.
Pregnancy is considered a factor of vulvovaginal mycosis. Secretion of hydrolases is an important determinant of Candida virulence. Thus, the aim of the study was to found the relationship between activity of 19 hydrolases in fungi isolated from vagina of pregnant women and symptoms of mycosis. 251 pregnant women were examined. Samples were collected from vagina and cultured on Sabouraud media. Activity of hydrolytic enzymes was evaluated using API ZYM (bioMerieux) test Fungi were found in 20.1% of vaginal samples. Symptoms were detected in 45.8% of women. Only 32.1% of women with discharge and 26.4% with pruritus had mycosis. Out of the 19 examined hydrolazes, 13 active enzymes were detected in fungal strains. We found for the first time the relationship between activity of fungal esterase lipase and the presence of vaginal discharge in pregnant women.  相似文献   
149.
We studied the selenium (Se) concentration in whole blood and plasma, glutathione peroxidase (GSH-Px) activity in red blood cells and plasma, as well as both of these parameters in cancerous and tumor-free lung tissue of lung cancer patients. Blood samples were taken from 84 cancer patients and 61 healthy controls. Normal and neoplastic lung tissues were obtained from 57 patients at the time of surgery. Se concentrations in whole blood and palsma were lower by 23% (p < 0.001) in patients compared with controls. GSH-Px activity in red cells was lower by 20.2% (p < 0.004) and in plasma by 11.7% (p < 0.05) in patients than in the control group. On the other hand, the tumor Se level was higher by 66.6% (p < 0.0001) and GSH Px activity by 49.5% (p < 0.0001) than in adjacent tumor-free tissue. No differences in Se concentrations and GSH-Px activities were found between squamous cell carcinoma and adenocarcinoma nor among the clinical stages of the disease. In the whole blood and plasma of cancer patients significantly lower Se concentrations were found in smokers than in nonsmokers. Significantly lower Se concentrations were also found among cancer patients who were smokers compared with controls. These findings show that in the blood of cancer the antioxidant ability, as measured by Se and GSH-Px, is reduced significantly. The cause of increased Se and GSH-Px in the malignant part of the lung is not understood and requires further studies. Accepted for publication: 17 April 1997  相似文献   
150.
Cytokines and heart rate variability in patients with chronic heart failure   总被引:3,自引:0,他引:3  
INTRODUCTION: Heart rate variability (HRV) analysis is a non-invasive method of assessment of the autonomic nervous system's effects on heart function. In chronic heart failure (CHF), decreased HRV correlates with the progression of the disease. It is also known that in CHF increased levels of proinflammatory cytokines are present. Because these molecules are believed to influence the nervous system at both the central and peripheral levels, their potential role in HRV reduction in the course of CHF has been proposed. AIM: The study was designed to verify potential relations between cytokines and HRV parameters in CHF patients. The concept of the study was driven by the recognition of controversies in this field and the paucity of published reports. METHODS: Forty-four patients with CHF and stable NYHA class I-IV symptoms and 15 healthy controls were enrolled in the study. Time-domain HRV analysis was performed based on of 24-hour Holter ECG monitoring. Plasma concentrations of soluble TNFalpha receptors sTNF-RI and sTNF-RII and interleukin 6 (IL-6) were measured using commercially available ELISA kits (Quantikine, RD Systems). RESULTS: In patients with CHF, HRV indices included in the analysis were significantly decreased, and the levels of cytokines increased in comparison with the control group. In the whole study population, both in the CHF patients and the control group, significant negative correlations were observed between sTNF-RI level and long-term HRV indices such as SDNN (r=-0.44; p=0.0006), SDANN (r=-0.44; p=0.0005) and short-time index SDNNI (r=-0.37; p=0.004). Similar negative correlations were found between sTNF-RII level and SDNN (r=-0.35; p=0.007), SDANN (r=-0.34; p=0.01), and SDNNI (r=-0.31; p=0.02), as well as between IL-6 level and SDNN (r=-0.41; p=0.001), SDANN (r=-0.44; p=0.0005) and SDNNI (r=-0.34; p=0.009). CONCLUSIONS: Significant negative correlations between TNF-alpha soluble receptors sTNF-RI, sTNF-RII and IL-6 levels and time-domain HRV parameters were observed in the study. Because the results of investigations conducted so far do not elucidate the cause-effect relationship, further studies are needed to clarify the mechanisms of HRV depression in CHF and the role of cytokines in this severe clinical condition.  相似文献   
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