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Electrophoretic, antioxidant, and FTIR profiles of some varieties of amaranth, quinoa, and buckwheat seeds and their by products were compared. Water extracts of these products were evaluated by the Folin-Ciocalteau method in order to determine total phenolic content. The antioxidant activities were determined by 2,2'-azobis-2-methyl-propanimidamide, ferric-reducing/antioxidant power, and cupric reducing antioxidant capacity radical scavenging assays. FTIR spectra showed the secondary structure of pseudocereals in the ranges of amides I, II, and III shifts. Results of evaluated methods could be used to control several products (seeds, flours, extracts, flakes, roasting) with high phenolic content and antioxidant activity suitable for supplementation in food applications. Graphical Abstract ᅟ.

Background: The biodegradable polymer drug-eluting stents have been proposed as an alternative to durable polymer DES, theoretically improving vessel healing and reducing the need for prolonged double anti platelet therapy (DAPT), however clinical significance of this technology is under debate. Therefore, we sought to compare the clinical outcomes of two Paclitaxel eluting stents (PES) containing different polymer-based eluting matrices., Methods: In this multicenter registry of 392 consecutive patients who underwent PCI between June 2006 and September 2008, we included patients with stable angina or NSTE-ACS displaying at least one significant lesion (>50% diameter stenosis) in native coronary arteries., Results: Biodegradable polymer PES (BP-PES, LUC Chopin(2) , Balton, Poland) was implanted in 206 patients, whereas durable polymer PES (DP-PES, Taxus, Boston Scientific, USA) was implanted in 186 patients. There were no significant differences in baseline characteristics between groups with the exception of increased diabetes and number of lesions for BP-PES. In risk-unadjusted analysis at 1-year follow-up, there were no significant differences in TLR (BP-PES: 8.4% vs., Dp-Pes: 6%; P = 0.36), TVR (BP-PES: 11.1% vs., Dp-Pes: 8.4%; P = 0.36) and incidence of stent thromboses (BP-PES: 2.15% vs., Dp-Pes: 3.4%; P = 0.42) between groups. There was also no difference in MACCE between groups (17.6% vs. 14.4%, P = 0.49). The mean dual antiplatelet therapy (DAPT) compliance at 1 year was 77% for BP-PES versus 92% for DP-PES (P = 0.03). Kaplan-Meier analysis showed a significantly higher long-term stroke free survival in BP-PES (P = 0.04). After adjustment, this was sustained with an additional tendency toward higher MI free survival for BP-PES (P = 0.059)., Conclusions: In this observational analysis, BP-PES were comparable to DP-PES, with regard to incidence of repeated revascularizations, stent thromboses and MACCE despite earlier DAPT discontinuation., (Copyright © 2012 Wiley Periodicals, Inc.)

Objective: To assess the influence of two persimmon cultivars on some atherosclerosis indices in rats fed cholesterol (Chol)-containing diets., Methods: Persimmon cultivars "Fuyu" and "Jiro" as supplementation to rats' diets were investigated in vitro to compare the contents of their bioactive compounds (polyphenols, flavonoids, flavanols, tannins, carotenoids, and ascorbic acid) and antioxidant potentials. In the in vivo investigation, 36 male Wistar rats were randomly divided into six diet groups, each with six rats: control, control/Fuyu, control/Jiro, Chol, Chol/Fuyu, and Chol/Jiro. During a period of 47 d (42 d of feeding and 5-d adaptation before the experiment) of the trial, rats in the control group were fed a basal diet and two additional control groups (control/Fuyu and control/Jiro) a basal diet plus 5% of lyophilized Fuyu and Jiro, respectively. The Chol, Chol/Fuyu, and Chol/Jiro rat groups were fed a basal diet supplemented with 1% Chol (Chol group) and 1% Chol plus 5% lyophilized Fuyu (Chol/Fuyu group) and plus 5% lyophilized Jiro (Chol/Jiro group), respectively. After completion of the experiment, the rats were anesthetized using Narcotan (halothane) and sacrificed and the atherosclerotic lesions in the aorta were assessed. The obtained results of the investigation of all six groups were compared. Testing of total cholesterol, low-density lipoprotein cholesterol, high-density lipoprotein cholesterol, triacylglycerols, total cholesterol in the liver, electrophoretic patterns of liver tissue, and three-dimensional fluorescence of serum protein fractions was performed., Results: The polyphenols and tannins were significantly higher in the Fuyu cultivar (P<0.05). The antioxidant potential of persimmon Fuyu was higher than in the Jiro cultivar, but the difference was significant only according to the 2,2-azino-bis (3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) assay (P<0.05). Supplementation of diets with 5% of the lyophilized Fuyu and Jiro hindered the increase in plasma lipids versus the Chol group (total cholesterol 19.4% and 9.5%, low-density lipoprotein cholesterol 25.6% and 13.1%, respectively, P<0.05) and hindered the decrease in plasma antioxidant activity versus the Chol group by 40.0% and 16.8% and by 39.6% and 11.3% for the ABTS and 1,1-diphenyl-2-picrylhydrazyl assays, respectively. The atherosclerotic lesions in the aortas of the Chol/Fuyu and Chol/Jiro groups were significantly less than in the Chol group (P<0.05). Electrophoresis of the proteins from rats' liver tissue showed changes in 14-kDa bands after persimmon supplementation. A shift in maximum wavelengths in three-dimensional fluorescence of serum protein fractions after persimmon supplementation was found in comparison with the control group and an increase in fluorescence intensity compared with the Chol groups., Conclusion: The contents of polyphenols and tannins were significantly higher in the Fuyu cultivar (P<0.05). The antioxidant potentials of Fuyu were higher than those of the Jiro cultivar, but the difference was significant only according to the ABTS assay (P<0.05). Supplementation of 5% lyophilized Fuyu and Jiro to diets of rats fed Chol-containing diets 1) hindered the increase in plasma lipids levels and the decrease in plasma antioxidant activity and 2) significantly decreased the atherosclerotic lesions in the aorta (P<0.05). Electrophoretic patterns of liver tissue and fluorescence spectra can be used as additional biomarkers for determination of atherosclerosis indices., (Copyright © 2011 Elsevier Inc. All rights reserved.)

Objectives: We sought to determine the frequency of left ventricular remodeling in the 6-month follow-up after anterior ST elevation myocardial infarction and the value of quantitative parameters of perfusion contrast echocardiography for prognosis of left ventricular remodeling against other established risk., Methods: A total of 60 patients with anterior ST elevation myocardial infarction treated by primary percutaneous intervention were examined. In 28 patients, thromboaspiration was performed before stent implantation with Driver catheter. Before and after successful angioplasty, perfusion in myocardial blush grade (MBG) scale was assessed. Various electrocardiogram parameters were analyzed. Resting perfusion with myocardial contrast echocardiography was performed., Results: Logistic regression has permitted one to conclude that higher value of MBG, higher left ventricular ejection fraction at discharge, and higher value of parameter A at quantitative echocardiography in dysfunctional segments were prognostic for lack of remodeling over 6 months. The receiver operating characteristics curves for parameters of quantitative perfusion echocardiography (A, β, A×β) allowed us to conclude that value A>1.96 dB, value β>0.155 s, and value A×β>0.57 dB/s are optimal cut-off points prognostic for remodeling. Area under the curve was 0.8 for A and 0.85 for β., Conclusion: The best predictors of remodeling in 6 months' observation have appeared to be lower left ventricular ejection fraction at discharge, poorer perfusion assessed angiographically (MBG scale), and the rate of signal intensity increase reflecting the mean bubble velocity of the myocardium by contrast as assessed by contrast echocardiography. Quantitative perfusion angiography independently has high predictive value for the development of remodeling in long-term follow-up.

Aims: We report here the final 5-year follow-up results from the ENDEAVOR II trial, which was the first randomised trial evaluating the Endeavor(tm) zotarolimus-eluting stent (ZES) compared with a bare metal stent (BMS) in patients with single, de novo coronary artery lesions., Methods and Results: Eligible patients were randomised 1:1 to receive ZES or BMS and were followed by telephone or clinic visit up to five years. We evaluated TVF and its components (target vessel revascularisation [TVR], Q-wave or non Q-wave myocardial infarction, or cardiac death attributed to the target vessel) at five years. Additionally, we report rates of MACE, TLR, and stent thrombosis (protocol- and ARC-defined) through five years. ENDEAVOR II enrolled 1,197 patients (598 ZES, 599 BMS). At five years of follow-up, the rates of TVF (15.4% vs 24.4%), TVR (10.7% vs 20.1%), MACE (15.4% vs 24.6%), and TLR (7.5% vs 16.3%) remained significantly lower in ZES patients compared with BMS patients. ARC definite and probable very late (>1 year) stent thrombosis remained low (0.2% ZES and 0.3% BMS) through five years., Conclusions: After five years of follow-up, ZES demonstrated significantly improved clinical outcomes with sustained safety compared with BMS in patients with obstructive coronary artery disease.

Breathalysing and blood analysis is the basic instrument of measuring the level of intoxication. Prior to collecting a blood sample, an individual suspected of being under the influence of alcohol is examined by a physician, who fills out the "protocol of obtaining a blood sample". This work aims at evaluating the applicability of the described examination in measuring the level of intoxication. In order to do so, our team analyzed 352 "protocols of obtaining blood sample" referred to the Forensic Laboratory KWP in Bydgoszcz, Poland, and compared them with the results of blood analysis. The results of the above analysis point to the fact that the elements of medical examination constituting "the protocol of obtaining a blood sample" are of a minor usefulness in determining the degree of intoxication with ethyl alcohol. The smell from the mouth and the conclusions formulated the examining physician prove to be the most useful. The summary usage of deviations from the norm does not seem to increase the usefulness of methods used within "the protocol of obtaining a blood sample" in evaluating the degree of intoxication.

We describe a novel series of potent inhibitors of the kinase activity of mTOR. The compounds display good selectivity relative to other PI3K-related kinase family members and, in cellular assays, inhibit both mTORC1 and mTORC2 complexes and exhibit good antiproliferative activity.

The aim of this investigation was to examine the influence of extrusion on the bioactive compounds and the antioxidant capacity of bean/corn mixtures. Whole bean flour and nixtamalized corn were mixed in a 60:40 proportion and extrusion was performed in different moisture (14.5%, 15.4%, 17.1% and 18.0%) and temperature (150°C, 160°C, 170°C, 180°C and 190°C) conditions in order to find the optimal extrusion conditions. According to their functional properties and antioxidant status, the mixtures 142°C/16.3% H, 170°C/16.3% H and 198°C/16.3% H were defined as optimal, moderate and bad, respectively. Total polyphenols and flavonoids in the mixture of 142°C/16.3% H (15.09±1.7 mg gallic acid equivalent [GAE]/g dry weight [DW] and 1.57±0.2 mg catechin equivalent [CE]/g DW) were significantly higher (P<0.05) than in the sample 170°C/16.3% H (9.42±1.1 mg GAE/g DW and 1.4±0.1 mg CE/g DW) and the mixture 198°C/16.3% H (6.46±0.8 mg GAE/g DW and 0.78±0.1 mg CE/g DW). The antioxidant activity (37.02±3.8 and 25.01±2.5 µM Trolox equivalent [TE]/g DW) of mixture 142°C/16.3% H, determined by the cupric reducing antioxidant capacity with Trolox equivalent antioxidant capacity and β-carotene-linoleic acid (β-carotene,% of inhibition) assays, was significantly higher (P<0.05) than in 170°C/16.3% H (25.69±2.8 and 17.02±1.8 µM TE/g DW) and in mixture 198°C/16.3% H (13.93±1.5 and 8.94±0.9 µM TE/g DW), respectively. The free polyphenols, flavonoids and the antioxidant activities showed lower results than the hydrolyzed ones. The correlation coefficients between polyphenols, flavonoids, and cupric reducing antioxidant capacity capacities were between 0.93 and 0.99. In cereal proteins extracted and separated by electrophoresis, some differences were found in the sodium dodecyl sulfate-protein bands in the region from 36 to 45 kDa for 142°C/16.3% H, in comparison with other samples. Therefore, there is a need to find such conditions for the extrusion procedures that would take into consideration the contents of the bioactive compounds and the antioxidant capacity in the end product.

Aims: The aim of this analysis was to examine the influence of different in-cath-lab antiplatelet regimens for the primary percutaneous coronary intervention (PCI) on all-cause mortality., Methods and Results: The study group consisted of 7193 patients (pts) undergoing primary PCI in 38 centres in 2003 in Poland. All patients received pretreatment with 300 mg of aspirin, 992 pts (14%) received glycoprotein (GP) IIb/IIIa inhibitors, 2690 pts (37%) were treated with 300 mg loading dose of clopidogrel, and 1566 (22%) received combined antiplatelet treatment with both GP IIb/IIIa inhibitors and clopidogrel. Remaining 1945 patients (27%) did not receive GP IIb/IIIa inhibitors or clopidogrel. Primary endpoint of the study was all-cause mortality up to 1 year from ST-segment elevation myocardial infarction (STEMI). One year mortality rates in the four groups were: 10.4%, 9.0%, 9.7%, and 15.3%, respectively. Propensity-adjusted survival analysis showed significant reduction of mortality for combination therapy with GP IIb/IIIa inhibitors and clopidogrel, clopidogrel alone, and GP IIb/IIIa inhibitors alone over aspirin alone. No additive effect on survival was seen for a combination therapy with GP IIb/IIIa inhibitors and clopidogrel in comparison to treatment with clopidogrel alone., Conclusion: In this large cohort, multicentre STEMI registry in-cath-lab use of GP IIb/IIIa inhibitors and clopidogrel alone or in combination was associated with the reduction of 1 year all-cause mortality in the setting of primary PCI in comparison with aspirin only. However, the use of GP IIb/IIIa inhibitors on top of 300 mg loading dose of clopidogrel did not further reduce mortality.

The influence of diets supplemented with mussels, from polluted (MPoll) and non-polluted (MNPoll) areas, on some atherosclerosis indices in rats fed cholesterol (Chol) were studied. According to the results of our investigation in vitro, mussels from polluted areas had higher contents of proteins, metals and antioxidant compounds, mostly phenolics and higher antioxidant capacities. 28 male Wistar rats were divided into 4 groups of 7 and named Control, Chol, Chol/MPoll and Chol/MNPoll. The rats of the Control group received basal diet (BD) only, and the diets of the other 3 groups were supplemented with 1% of non-oxidized cholesterol (NOC), 1% of NOC and 5.6% of mussel dry matter (DM) from polluted and 1% of NOC and 5.6% of mussel DM from non-polluted areas for Chol, Chol/MPoll and Chol/MNPoll, respectively. The histology of the aorta and brain in rats fed cholesterol did not show any signs of atherosclerosis. Some differences were registered in the electrophoretic protein patterns of plasma in rats, with mussel-supplemented diets. In full plasma electrophoretic patterns of the Chol/MPoll diet group more proteins were detected than in both Chol and Control groups, and the differences were significant. In conclusion, in groups of rats fed cholesterol with mussels supplementation, a significant hindering in the rise of plasma lipid levels and also hindering in the decrease of plasma antioxidant activity were registered., (Copyright © 2008 Elsevier Ltd. All rights reserved.)

Poly(ADP-ribose) polymerase activation is an immediate cellular response to metabolic-, chemical-, or ionizing radiation-induced DNA damage and represents a new target for cancer therapy. In this article, we disclose a novel series of substituted 4-benzyl-2 H-phthalazin-1-ones that possess high inhibitory enzyme and cellular potency for both PARP-1 and PARP-2. Optimized compounds from the series also demonstrate good pharmacokinetic profiles, oral bioavailability, and activity in vivo in an SW620 colorectal cancer xenograft model. 4-[3-(4-Cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2 H-phthalazin-1-one (KU-0059436, AZD2281) 47 is a single digit nanomolar inhibitor of both PARP-1 and PARP-2 that shows standalone activity against BRCA1-deficient breast cancer cell lines. Compound 47 is currently undergoing clinical development for the treatment of BRCA1- and BRCA2-defective cancers.

The antioxidant activities of different durian cultivars at the same stage of ripening (Mon Thong, Chani, Kan Yao, Pung Manee and Kradum) were compared in order to choose the best as a supplement in the human diet. Total polyphenols (mg gallic acid equivalent/100 g fresh weight (FW)) and flavonoids (mg catechin equivalent (CE)/100 g FW) in Mon Thong (361.4+/-23.2 and 93.9+/-7.4) were significantly higher (P<0.05) than in Kradum (271.5+/-11.2 and 69.2+/-5.3) and Kan Yao (283.2+/-16.5 and 72.1+/-6.8). The free polyphenols and flavonoids showed lower results than the hydrolyzed ones. Anthocyanins (microg cyanidin-3-glucoside equivalent/100 g FW) and flavanols (microg CE/100 g FW) were significantly higher in Mon Thong (427.3+/-23.8 and 171.4+/-16.3) than in Kradum (320.2+/-12.1 and 128.6+/-9.7) and Kan Yao (335.3+/-14.1 and 134.4+/-11.7). Ultraviolet spectroscopy and high-performance liquid chromatography/diode array detection analyses showed that caffeic acid and quercetin were the dominant bioactive substances in Mon Thong cultivar. The antioxidant activity (microM trolox equivalent/100 g FW) of Mon Thong cultivar (260.8+/-20.2, 1,075.6+/-81.4 and 2,352.7+/-124.2) determined by ferric-reducing/antioxidant power (FRAP), cupric reducing antioxidant capacity (CUPRAC) and 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) with Trolox equivalent antioxidant capacity (TEAC) assays was significantly higher (P<0.05) than in Kradum (197.4+/-8.9, 806.5+/-31.2 and 1,773.2+/-102.5) and in Kan Yao (204.7+/-9.7, 845.5+/-48.6 and 1,843.6+/-107.5). The correlation coefficients between polyphenols, flavonoids, flavanols and FRAP, CUPRAC and TEAC capacities were between 0.89 and 0.98. In extracted and separated by electrophoresis durian proteins, some differences were found in the sodium dodecyl sulfate-protein bands in the region of 16 and 68 kDa for Kradum, 45 kDa for Mon Thong and three bands for Kan Yao. Antioxidants and proteins can be used for characterization of the quality of durian cultivars. In conclusion, the bioactivity of durian cultivars Mon Thong, Chani and Pung Manee was high and the total polyphenols were the main contributors to the overall antioxidant capacity. The results of our investigation in vitro are comparable with other fruits that widely used in human diets. Therefore, Durian can be used as a supplement for nutritional and healthy purposes, especially Durian Mon Thong, Chani and Pung Manee.

We have previously described poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors based on a substituted benzyl-phthalazinone scaffold. As an alternative chemical template, a novel series of alkoxybenzamides were developed with restricted conformation through intramolecular hydrogen bond formation; the compounds exhibit low nM enzyme and cellular activity as PARP-1 inhibitors.

Polish garlic and white and red onions were subjected to blanching, boiling, frying, and microwaving for different periods of time, and then their bioactive compounds (polyphenols, flavonoids, flavanols, anthocyanins, tannins, and ascorbic acid) and antioxidant activities were determined. It was found that blanching and frying and then microwaving of garlic and onions did not decrease significantly the amounts of their bioactive compounds and the level of antioxidant activities ( P > 0.05). The HPLC profiles of free and soluble ester- and glycoside-bound phenolic acids showed that trans-hydroxycinnamic acids (caffeic, p-coumaric, ferulic, and sinapic) were as much as twice higher in garlic than in onions. Quercetin quantity was the highest in red onion among the studied vegetables. The electrophoretic separation of nonreduced garlic and onion proteins after boiling demonstrated their degradation in the range from 50 to 112 kDa.

The properties of Mon Thong, Chani and Kan Yao durian (Durio zibethinus Murr.) cultivars were compared in vitro and in vivo studies in order to find the best one as a supplement to antiatherosclerotic diet. Total polyphenols (361.4+/-35.3 mgGAE/100g FW), flavonoids (93.9+/-8.9 mgCE/100g FW) and total antioxidant capacity determined by DPPH and beta-carotene-linoleic acid assays (261.3+/-25.3 microMTE/100g FW and 77.8+/-7.8% of inhibition) were maximal in Mon Thong in comparison with Chani and Kan Yao and showed a good correlation between these three variables (R(2)=0.9859). Five groups of rats were fed diets supplemented with cholesterol and different durian cultivars. Diets supplemented with Mon Thong and to a lesser degree with Chani and Kan Yao significantly hindered the rise in the plasma lipids (TC - 8.7%, 16.1% and 10.3% and (b) LDL-C - 20.1%, 31.3% and 23.5% for the Chol/Kan Yao, Chol/Mon Thong and Chol/Chani, respectively) and the decrease in plasma antioxidant activity (P<0.05). Nitrogen retention remained significantly higher in Chol/Mon Thong than in other diet groups. Diet supplemented with Mon Thong affected the composition of plasma fibrinogen in rats and showed more intensity in protein bands around 47 kDa. No lesions were found in the examined tissue of heart and brains. Mon Thong cultivar is preferable for the supplementation of the diet as positively influenced the lipid, antioxidant, protein and metabolic status. The durian fruit till now was not investigated extensively, therefore based on the results of this study durian cultivars can be used as a relatively new source of antioxidants.

Late loss has been used as a reliable surrogate end point for evaluation and differentiation of short-term performance of drug-eluting stents. This study investigated the consistency between angiographic and intravascular ultrasound (IVUS) outcomes of late lumen loss (late loss) and neointimal growth to measure restenotic plaque load in TAXUS and bare metal stents. The randomized TAXUS II trial evaluates the polymer-based paclitaxel-eluting TAXUS stent in slow- and moderate-release formulations. Serial angiographic and IVUS analyses were available in 155 event-free patients (bare metal stent, 74; TAXUS stent, 81) after the procedure, at 6 months, and at 2 years. For this subanalysis, quantitative coronary angiographic (QCA) and IVUS measurements were used to derive late loss and neointimal volume. From after the procedure to 6 months, quantitative coronary angiography and IVUS showed matching results for the 2 groups with significant decreases in late loss and neointimal volume in the TAXUS versus the control group. From 6 months to 2 years, QCA and IVUS measurements also showed results similar to those in the control group, demonstrating neointimal compaction over time. However, in the TAXUS group, QCA late loss showed a nonsignificant decrease from 6 months to 2 years, whereas IVUS neointimal volume increased. In conclusion, although QCA and IVUS results were similar over the first 6 months, long-term assessment of changes in restenotic plaque load showed discrepant findings for the TAXUS. These findings suggest the need for critical reevaluation of current end points and the use of more precise techniques to detect lumen and stent boundaries.

The aim of this investigation was to assess the nutritional and health properties of Mon Thong durian cultivar at different stages of ripening. The assessment was carried out in vitro and in vivo. The contents of dietary fibers, minerals and trace metals at different stages of ripening were comparable. Total polyphenols (mgGAE/100 g FW) and flavonoids (mg CE/100 gFW) in ripe durian (358.8 +/- 31.4 and 95.4 +/- 9.3) were significantly higher (p < 0.05) than in mature (216.1 +/- 1 and 39.9 +/- 3.8) and overripe (283.3 +/- 26.2 and 53.5 +/- 4.9). Antioxidant capacity (muMTE/100 g FW) in total polyphenol extracts of ripe durian measured by 1,1-diphenyl-2-picrylhydrazyl radical (DPPH) and [2,2'-azinobis (3-ethylbenzothiazoline-6-sulfonic acid)] (ABTS) assays (259.4 +/- 23.6 and 2341.8 +/- 93.2) were significantly higher (p < 0.05) than that of mature (151.6 +/- 15.2 and 1394.6 +/- 41.5) and overripe (201.7 +/- 19.4 and 1812.2 +/- 61.4) samples. The correlation coefficients between the bioactive compounds in different stages of ripening and their antioxidant capacities were high (R;{2} = 0.99). Then 35 male Wistar rats were divided into 5 dietary groups each of 7 and named Control, Chol, Chol/Mature, Chol/Ripe and Chol/Overripe. During 30 days of the experiment the rats of all 5 groups were fed basal diet (BD), which included wheat starch, casein, soybean oil, vitamin and mineral mixtures. The rats of the Control group were fed a BD only. To the BD of the Chol group was added 1% of cholesterol. The BD of the Chol/Mature, Chol/Ripe and Chol/Overripe groups was supplemented with 1% of cholesterol and 5% of the mature, ripe and overripe durian as freeze-dried powder, respectively. Diets containing ripe and to a lesser degree mature and overripe durian significantly hindered the rise in plasma lipids and also hindered a decrease in plasma antioxidant activity. The nitrogen retention in rats of the Chol/Ripe group was significantly higher (63.6%, P < 0.05) than in other diet groups and the level of the plasma glucose remained normal. A decrease in fibrinogen fraction with ripe durian included in rat's diets was shown by electrophoretic separation. These changes were detected mostly in the low molecular weight proteins of rat's serum. Histological examination of aorta showed only slight differences in the tissue. In conclusion, ripe durian contains higher quantity of bioactive compounds, has higher antioxidant capacity and nutritional value. It positively affects the plasma lipid profile, the plasma glucose and the antioxidant activity in rats fed cholesterol enriched diets. Therefore, the ripe durian supplemented diet could be beneficial for patient suffering from hypercholesterolemia and diabetes mellitus. <

The aim of this investigation was to evaluate the dose-dependent influence of commercial garlic on rats fed cholesterol-containing diets. It was found that commercial garlic contains high concentrations of dietary fibers, microelements, and total polyphenols, and its total antioxidant capacity as determined by two independent assays [1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2'-azinobis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS)] was similar to that of the original garlic samples. Wistar rats (35) were randomly divided into five diet groups, named control, Chol, Garlic500, Garlic750, and Garlic1000. Control rats were fed basal diet (BD), which included wheat starch, casein, soybean oil, and vitamin and mineral mixtures. To the BD of the Chol group was added 1% of cholesterol. To the BD of the other three groups (Garlic500, Garlic750, and Garlic1000) were added 1% of cholesterol and commercial garlic equal to 500, 750, and 1000 mg of raw garlic per kilogram of animal weight. After 4 weeks of the experiment only in rats from the Garlic500 group were a significant hindering in the rise in plasma lipids and also a significant hindering in a decrease of plasma antioxidant activity registered. A significant decrease in plasma circulating fibrinogen and an increase in the clotting time were found in the same group of rats (P < 0.05 in both cases). The fibrinogenolytic effect of garlic diets was visualized by sodium dodecyl sulfate-polyacrylamide gel electrophoresis. In the fibrinogen fraction of Garlic500 the 66, 24, and 14 kDa protein bands were detected with weaker protein intensity than in the corresponding ones in the Garlic750 and Garlic1000 diet groups. In conclusion, the positive influences of commercial garlic on plasma lipids, proteins, antioxidant activity, and some indices of blood coagulation are dose-dependent. Therefore, commercial garlic (Elena, Zelazków, Poland) could be a valuable component of atherosclerosis-preventing diets only in optimal doses.

We have previously described the discovery of poly(ADP-ribose)polymerase-1 (PARP-1) inhibitors based on a phthalazinone scaffold. Subsequent optimisation of inhibitory activity, metabolic stability and pharmacokinetic parameters has led to a novel series of meta-substituted 4-benzyl-2H-phthalazin-1-one PARP-1 inhibitors which retain low nM cellular activity and show good stability in vivo and efficacy in cell based models.

The main aim of the present study was the evaluation of proteins and antioxidant potential in ethylene-treated kiwifruit during the first 10 days of ripening. Kiwifruit samples were randomly divided into two groups: treated and untreated. Flesh firmness, sensory value, visual score, free sugars, soluble solids, ethylene biosynthesis, proteins, dietary fibers, total polyphenols and antioxidant potential were determined in both groups. Ethylene (100 ppm) at 20 degrees C for 24 h was used in the treated group. The flesh firmness and acidity in treated samples decreased significantly in the early stage of ripening simultaneously with significant increase in the contents of free sugars, soluble solids, endogenous ethylene production, sensory value, 1-aminocyclopropane-1-carboxylic acid (ACC) content, ACC synthase and ACC oxidase activities, total polyphenols and related antioxidant potential, and was significantly higher than in untreated samples (P < 0.05). Proteins were extracted from kiwifruit and separated by modified sodium dodecyl sulphate polyacrylamide gel electrophoresis. The separation was resolved into 14 protein bands. Some minor quality changes were found only in the 32 kDa band, which was more pronounced in the treated samples. In conclusion, ethylene treatment of kiwifruits leads to positive changes in most of the studied kiwifruit compounds and to an increase in the fruit antioxidant potential. It shortens the ripening time and improves fruit quality by decreasing its flesh firmness and acidity. Some minor changes in the protein profile did not affect the fruit taste and quality.

Unlabelled: In the present study the effect of garlic, in a form more similar to how most people eat garlic, on lipid and antioxidant metabolism in rats was investigated. The antioxidant activity was determined by the efficacy to scavenge 2, 2'-azino-bis (3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) derived radicals in garlic samples. The highest results were estimated in aqueous fraction in comparison with other extracts divided on the basis of polarity. Wistar male rats were randomly divided into 10 diet groups, each with seven animals. The groups were named: Control, RG (raw garlic), BG (boiled garlic for 20 min), AERG (aqueous extract of raw garlic), AEBG (aqueous extract of boiled garlic), Ch (Cholesterol), Ch/RG, Ch/BG, Ch/AERG and Ch/AEBG. All experimental diets were supplemented with 25 mg of lyophilized garlic/kg body weight obtained from raw, boiled and their aqueous extracts over a period of 30 days. Serum lipid (total cholesterol, LDL-cholesterol and triglycerides) concentrations were higher in all groups fed cholesterol (Ch); however, the increase was significant only in Ch group, without garlic supplementation. In groups of rats fed diets with cholesterol, garlic samples significantly hindered the rise of TC and LDL-C (P < 0.05). A significant increase (P < 0.05) in the plasma antioxidant activity was registered in experimental groups of rats fed cholesterol-free diets supplemented with garlic; oppositely, a significant decrease was only in group of rats given food containing cholesterol without garlic. The protein spectra has shown that during short boiling some proteins change their functional properties such as solubility and mobility, resulting in a number of protein bands in SDS-electrophoresis., Conclusions: Raw and boiled garlic improved plasma lipid metabolism and plasma antioxidant activity in an experiment on rats. Thus, dietary hypolipidemic garlic was effective in reducing the oxidant stress, which was indicated by an increase of antioxidant activity and a decrease of lipids in the rats' blood. It was found that garlic boiled for 20 min has the same bioactivity as raw garlic in its antioxidant and protein spectra. Therefore it should be added at this time to foods. The selenium and copper content of raw garlic is not altered by boiling. The protein electrophoretic pattern of raw garlic is altered by boiling.

Bioactive compounds of peels and peeled red Star Ruby (Sunrise) and blond qualities of Jaffa grapefruits were analyzed and their antioxidant potential was assessed. The dietary fibers were determined according to Prosky et al., the total polyphenol content by Folin-Ciocalteu method and measured at 765 nm, minerals and trace elements by atomic absorption spectrometer, phenolic and ascorbic acids by HPLC and the antioxidant potential by two different antioxidant assays (DPPH and beta-carotene linoleate model system). It was found that the contents of most studied bioactive compounds in both qualities are comparable. Only the contents of total polyphenols and flavonoids were higher in red grapefruits, but not significant. The antioxidant potentials of red peeled grapefruits and their peels were significantly higher than of blond peeled grapefruits and their peels (P<0.05 in both cases). Diets supplemented with peeled red and blond qualities of Jaffa grapefruits and their peels have increased the plasma antioxidant capacity and improved plasma lipid levels, especially in rats fed with cholesterol added diet. In conclusion, both qualities of Jaffa grapefruits contain high quantities of bioactive compounds, but the antioxidant potential of red grapefruits is significantly higher. Diets supplemented with both qualities of Jaffa grapefruits improve the plasma lipid levels and increase the plasma antioxidant activity, especially in rats fed with cholesterol added diets. Jaffa grapefruits, especially their red Star Ruby quality, could be a valuable supplementation for diseases-preventing diets.

Screening of the Maybridge compound collection identified 4-arylphthalazinones as micromolar inhibitors of PARP-1 catalytic activity. Subsequent optimisation of both inhibitory activity and metabolic stability led to a novel series of meta-substituted 4-benzyl-2H-phthalazin-1-ones with low nanomolar, cellular activity as PARP-1 inhibitors and promising metabolic stability in vitro.

Garlic (Allium sativum L.) is an essential part of Polish, Ukrainian, and Israeli cuisine. The aim of this investigation was to compare the changes in bioactive compounds, proteins, and antioxidant potentials in fresh Polish, Ukrainian, and Israeli garlic samples after subjection to cooking temperature. Dietary fiber and essential trace elements were comparable. The antioxidant potentials were determined by four scavenging methods using beta-carotene, 1,1-diphenyl-2-picrylhydrazyl (DPPH), nitric oxide (NO), and 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS(*)(+)) radical cation with K(2)S(2)O(8) or MnO(2) assays. Polyphenols, tocopherols, proteins, and antioxidant potentials were higher in Polish garlic, but not significantly (P > 0.05). The SDS- and native-PAGE electrophoretic patterns of all three fresh garlic samples were without significant differences. Most of the proteins were in the molecular mass range of 24-97 kDa, and the more intensive major bands were concentrated at 50 and 12 kDa. The 50 kDa protein nearly disappears and the intensity of the 12 kDa lectin bands slightly decreases during cooking. It was observed that the bioactive compounds, antioxidant potential, and proteins in garlic decrease significantly after 20 min of cooking at 100 degrees C (P < 0.05). In conclusion, (a) the bioactive compounds, electrophoretic patterns, and antioxidant potential of fresh Polish, Ukrainian, and Israeli garlic samples are comparable; (b) garlic samples subjected to 100 degrees C during 20 min preserve their bioactive compounds, antioxidant potential, and protein profile and are comparable with fresh garlic; and (c) fresh garlic should be added to dishes cooked at 100 degrees C in the last 20 min of the cooking process.

Background: The clinical impact of late incomplete stent apposition (ISA) for drug-eluting stents is unknown. We sought to prospectively investigate the incidence and extent of ISA after the procedure and at 6-month follow-up of paclitaxel-eluting stents in comparison with bare metal stents (BMS) and survey the clinical significance of ISA over a period of 12 months., Methods and Results: TAXUS II was a randomized, double-blind study with 536 patients in 2 consecutive cohorts comparing slow-release (SR; 131 patients) and moderate-release (MR; 135 patients) paclitaxel-eluting stents with BMS (270 patients). This intravascular ultrasound (IVUS) substudy included patients who underwent serial IVUS examination after the procedure and at 6 months (BMS, 240 patients; SR, 113; MR, 116). The qualitative and quantitative analyses of ISA were performed by an independent, blinded core laboratory. More than half of the instances of ISA observed after the procedure resolved at 6 months in all groups. No difference in the incidence of late-acquired ISA was observed among the 3 groups (BMS, 5.4%; SR, 8.0%; MR, 9.5%; P=0.306), with a similar ISA volume (BMS, 11.4 mm3; SR, 21.7 mm3; MR, 8.5 mm3; P=0.18). Late-acquired ISA was the result of an increase of vessel area without change in plaque behind the stent. Predictive factors of late-acquired ISA were lesion length, unstable angina, and absence of diabetes. No stent thrombosis occurred in the patients diagnosed with ISA over a period of 12 months., Conclusions: The incidence and extent of late-acquired ISA are comparable in paclitaxel-eluting stents and BMS. ISA is a pure IVUS finding without clinical repercussions.

Background: The dynamic development of interventional cardiology resulted in an increasing proportion of patients treated with various forms of coronary angioplasty instead of surgery. On the other hand, it has been well established that the results of coronary artery by-pass surgery of the left anterior descending (LAD) coronary artery with the use of the internal mammary artery are excellent., Aim: To compare the results of primary direct stenting (PDS) and endoscopic atraumatic coronary artery bypass (EACAB) surgery in patients with an isolated proximal LAD type A or B1 lesion., Methods: This prospective and randomised study included 100 patients with an isolated critical (> or =70%) LAD stenosis who underwent PDS (n=50) or EACAB (n=50)., Results: After a six-month follow-up period, 32 (64%) PDS patients and 47 (94%) EACAB patients were angina-free. The rate of major cardiac adverse events (MACE) was significantly higher in the PDS group than in surgically treated patients (p<0.05). After one year of follow-up, 40 (80%) PDS-treated patients and all 50 EACAB patients had no recurrences of angina. After two-year follow-period, the survival rate without MACE was significantly higher in the EACAB group than in the PDS-treated patients (94% vs 76%, p<0.05)., Conclusions: Minimally invasive cardiac surgery is an alternative method to direct stenting in the treatment of patients with proximal LAD stenosis.

Background: A mild and asymptomatic increase in the troponin level following elective percutaneous coronary interventions (PCI) has been widely reported, however, the prognostic role of this finding has not yet been well established.Aim. To assess prognostic value of troponin I level increase following elective PCI., Methods: The study group consisted of 90 consecutive patients who underwent elective PCI in our institution. Troponin I level (normal values <0.1 ug/L) was assessed at baseline and 12 as well as 24 hours after the procedure. In addition, CK-MB level was measured 12 and 24 hours following PCI. Left ventricular (LV) systolic performance was assessed echocardiographically at baseline and after 12 months. The incidence of major adverse coronary events (MACE) during one-year follow-up was also evaluated., Results: An increase in troponin I level >0.1 ug/L was observed in 66 (73%) patients; of whom, 8 patients had a marked (>1.0 ug/L) increase of troponin I, with a concomitant significant elevation of the CK-MB level. Patients with a positive troponin test developed systolic LV abnormalities more often than patients with a normal troponin I level following PCI (p<0.001). There were 10 MACE in the troponin-positive group and 2 in the troponin-negative patients (NS). Seven MACE occurred in patients with marked increase in troponin I level (>1.0 ug/L) which was significantly more often than in the troponin-negative patients (p<0.001)., Conclusions: A mild increase in troponin I level following elective PCI was frequent and did not predict poor outcome, however, was associated with the development of LV systolic impairment. A marked (>1.0 ug/L) increase in troponin I level identified patients at risk of MACE. An increase in troponin I level was similar following various types of PCI.

The study of chemical composition and dough rheology changes in sieve-classified two fractions (up to 60 and 60-240 microm particles) of wheat flour was the subject of this study. The straight grade flours were obtained by the milling of three Polish varieties of spring wheat, differing in particle size index (PSI) values. The flours were separated with the use of an SZ-1 laboratory sifter. The yield of fine fraction was in the range 50.0-55.7%. The obtained fractions were assayed for the content and composition of free lipids, gluten proteins, damaged starch, ash, water absorption and amylograph viscosity. Dough rheology (extrusion in OTMS cell, alveograph and farinograph tests) and baking trials were also performed. The content of free lipids, including the non-polar and phospholipids was lower and the content of glycolipids was higher in fine flours. Those fractions were more rich in linoleic acid but the lower content of oleic and linolenic acids resulted in a higher oxidizability index of free lipids. Fine flours contained less ash and significantly more damaged starch. At the same time, they were characterized by a higher content of wet gluten, water absorption, amylograph viscosity and better dough parameters. This was reflected in the bread volume, which was higher by 6.3-10.7%. The influence of the changes in composition and the content of free lipids upon the rheology of the dough after the 90 days flour storage has not been defined unambiguously and requires further research.

Background and Method: Although direct coronary stenting does not improve angiographic outcome, it makes sense by reducing procedure times, radiation exposure and costs. Other potential advantages of direct stenting may be a reduction of myocardial ischemia time, which could be clinically relevant in high-risk patients. With the introduction of drug-eluting stents, however, concern arose that direct stenting would possibly damage the polymer coating and change or diminish the efficacy of the programmed drug release. Also, concerns about safety by preventing optimal apposition of single stent struts developed. It is the purpose of this paper to retrospectively analyze the data from the TAXUS-II Trial (536 patients) regarding patients with and without direct stenting. While predilatation was recommended per protocol, direct stenting was not forbidden: thus, direct stenting was performed in 49 patients (TAXUS n = 23, control n = 26)., Results: In the TAXUS groups, there was no significant difference regarding major adverse cardiac events (MACE; 7.5% vs. 4.3%), angiographic restenosis in the analysis segment (4.8% vs. 4.3%), late loss (0.28 +/- 0.36 vs. 0.33 +/- 0.30 mm) or intravascular ultrasound-(IVUS-)measured volume obstruction (7.95 +/- 9.84% vs. 5.61 +/- 7.91%) at six months between the predilated and directly stented patients. The same was true for the patients receiving the control stent. Compared with the directly stented control group, the statistically significant positive effects of TAXUS direct stenting were maintained, regarding angiographic restenosis in the analysis segment (4.3% vs. 30.8%), late loss (0.33 +/- 0.30 vs. 0.80 +/- 0.62 mm) or IVUS-measured volume obstruction (5.61 +/- 7.91% vs. 22.50 +/- 21.62%) at six months. MACE was reduced from 19.2% to 4.3%; due to the small number of patients this trend did not reach statistical significance. After predilatation, all parameters were significantly improved by the TAXUS stent., Conclusion: Comparison of patients receiving TAXUS stents with or without predilatation revealed no differences in clinical, angiographic or IVUS parameters at six months. This suggests that direct stenting with the polymer-based paclitaxel-eluting TAXUS stent is feasible, safe and equally effective. Randomized trials comparing stenting after predilatation versus direct stenting with drug-eluting stents are warranted.