In Vitro Screening of Bioactive Compounds in some Gluten-Free Plants.

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.

Comparable clinical safety and efficacy of biodegradable versus durable polymer paclitaxel eluting stents despite shorter dual antiplatelet therapy: insights from a multicenter, propensity score-matched registry.

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.

[Evaluating the applicability of medical examinations constituting "the protocol of obtaining a blood sample" in measuring the degree of intoxication].

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.

Prediction of left ventricular remodeling in patients with STEMI treated with primary PCI: use of quantitative myocardial contrast echocardiography.

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.

Long-term follow-up of the randomised controlled trial to evaluate the safety and efficacy of the zotarolimus-eluting driver coronary stent in de novo native coronary artery lesions: five year outcomes in the ENDEAVOR II study.

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.

Final 5-year results of the TAXUS II trial: a randomized study to assess the effectiveness of slow- and moderate-release polymer-based paclitaxel-eluting stents for de novo coronary artery lesions.

Background: The TAXUS II trial was designed to evaluate the safety and efficacy of the commercialized slow-release (SR) and an investigation-only moderate-release (MR) polymer-based TAXUS paclitaxel-eluting stent compared with a bare-metal stent for the treatment of de novo coronary lesions.

Methods And Results: This prospective, randomized, double-blind, controlled trial enrolled 536 patients in 2 consecutive cohorts to compare TAXUS SR (n=131) and TAXUS MR (n=135) with an identical but uncoated bare-metal stent control (n=270). The present analysis reports final 5-year clinical outcomes of TAXUS II.

The discovery and optimisation of pyrido[2,3-d]pyrimidine-2,4-diamines as potent and selective inhibitors of mTOR kinase.

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.

Influence of different antiplatelet treatment regimens for primary percutaneous coronary intervention on all-cause mortality.

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.

Influence of mussels (Mytilus galloprovincialis) from polluted and non-polluted areas on some atherosclerosis indices in rats fed cholesterol.

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.

Screening of the antioxidant and nutritional properties, phenolic contents and proteins of five durian cultivars.

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.

4-[3-(4-cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one: a novel bioavailable inhibitor of poly(ADP-ribose) polymerase-1.

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.

Influence of extrusion on the bioactive compounds and the antioxidant capacity of the bean/corn mixtures.

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.

Novel alkoxybenzamide inhibitors of poly(ADP-ribose) polymerase.

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.

Comparison of the main bioactive compounds and antioxidant activities in garlic and white and red onions after treatment protocols.

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).

Durian (Durio zibethinus Murr.) cultivars as nutritional supplementation to rat's diets.

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.

The nutritional and metabolic indices in rats fed cholesterol-containing diets supplemented with durian at different stages of ripening.

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.

Two-year serial coronary angiographic and intravascular ultrasound analysis of in-stent angiographic late lumen loss and ultrasonic neointimal volume from the TAXUS II trial.

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.

In vitro studies of polyphenols, antioxidants and other dietary indices in kiwifruit (Actinidia deliciosa).

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.

Dose-dependent influence of commercial garlic (Allium sativum) on rats fed cholesterol-containing diet.

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.

Peristent remodeling and neointimal suppression 2 years after polymer-based, paclitaxel-eluting stent implantation: insights from serial intravascular ultrasound analysis in the TAXUS II study.

Background: The purpose of this study was to evaluate long-term vascular responses as long as 2 years after implantation of polymer-based, paclitaxel-eluting stents in contrast to uncoated stents.

Methods And Results: TAXUS II is a randomized, double-blind trial comparing slow-release (SR) and moderate-release (MR) TAXUS stents with bare-metal control stents (BMSs). One hundred sixty-one event-free patients (SR, 43; MR, 41; and BMS, 77) underwent serial intravascular ultrasound (IVUS) analysis after the procedure and at 6 months and 2 years.

Phthalazinones 2: Optimisation and synthesis of novel potent inhibitors of poly(ADP-ribose)polymerase.

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.

Raw and boiled garlic enhances plasma antioxidant activity and improves plasma lipid metabolism in cholesterol-fed rats.

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.

Red Star Ruby (Sunrise) and blond qualities of Jaffa grapefruits and their influence on plasma lipid levels and plasma antioxidant activity in rats fed with cholesterol-containing and cholesterol-free diets.

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).