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Pharmaceuticals, Volume 2, Issue 2 (September 2009), Pages 11-65

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Research

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Open AccessArticle Knowledge and Implementation of the New European Guide in the Management of Arterial Hypertension. The Cigema Survey
Pharmaceuticals 2009, 2(2), 11-32; doi:10.3390/ph2020011
Received: 8 July 2009 / Revised: 21 July 2009 / Accepted: 27 July 2009 / Published: 28 July 2009
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Abstract
Knowledge of guideline implementation pitfalls allows anticipation and solving of problems and may help to promote implementation. The aims of this study were: 1) to find out how much is known among medical professionals about the recommendations for the Management of Arterial [...] Read more.
Knowledge of guideline implementation pitfalls allows anticipation and solving of problems and may help to promote implementation. The aims of this study were: 1) to find out how much is known among medical professionals about the recommendations for the Management of Arterial Hypertension; 2) to study in depth the extent of implementation and 3) to evaluate the manner in which this guide will be applied to daily medical practice. The Delphi method was used for this work. The total estimated sample size was 2,250 physicians. The carefully selected experts answered questionnaires in two or more rounds. The final sample size was 2,475 physicians. Results of the study are detailed in the article. Among the resultsIt is noteworthy that the guide is viewed as needed among all those who have been interviewed and this agreement about its need is generalised and that the improvement in medical practice, together with individual treatment and cardiovascular risk stratification are viewed positively in opinions reached by consensus by the majority of physicians, regardless of whether they are specialists or general practitioners. The main results of this study emphasize the fact that physicians need a guideline for the management of hypertensive patients and that most of physicians agree with them. The new guidelines on arterial hypertension management are widely known among physicians and there appears to be a global agreement regarding the need for the implementation of the new recommendations. Full article
Open AccessArticle Antitumor Activity of Some Prenylated Xanthones
Pharmaceuticals 2009, 2(2), 33-43; doi:10.3390/ph2020033
Received: 1 July 2009 / Revised: 29 July 2009 / Accepted: 10 August 2009 / Published: 11 August 2009
Cited by 13 | PDF Full-text (190 KB) | HTML Full-text | XML Full-text
Abstract
Pyranoxanthones 6-8 were obtained by dehydrogenation of the respective dihydropyranoxanthones 3-5 with DDQ in dry dioxane. Two prenylated xanthones 10,11 were obtained from the reaction of 1-hydroxyxanthone (9) with prenyl bromide in alkaline medium, or by condensation of xanthone 9 with isoprene [...] Read more.
Pyranoxanthones 6-8 were obtained by dehydrogenation of the respective dihydropyranoxanthones 3-5 with DDQ in dry dioxane. Two prenylated xanthones 10,11 were obtained from the reaction of 1-hydroxyxanthone (9) with prenyl bromide in alkaline medium, or by condensation of xanthone 9 with isoprene in the presence of orthophosphoric acid. The structural elucidation of the two new compounds 6,11, as well as an update of data for the already described prenylated derivatives 7,8,10 were accomplished by IR, UV, HRMS and NMR (1H, 13C, HSQC and HMBC) techniques. The effect of the prenylated xanthone derivatives on the in vitro growth of human tumor cell lines MCF-7 (breast adenocarcinoma) and NCI-H460 (non-small cell lung cancer) is also reported. Compounds 10 and 11 have been found to exhibit a moderate growth inhibitory activity against the MCF-7 cell line. Full article
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Open AccessArticle Fusion of a Short HA2-Derived Peptide Sequence to Cell-Penetrating Peptides Improves Cytosolic Uptake, but Enhances Cytotoxic Activity
Pharmaceuticals 2009, 2(2), 49-65; doi:10.3390/ph2020049
Received: 10 August 2009 / Revised: 22 September 2009 / Accepted: 24 September 2009 / Published: 25 September 2009
Cited by 26 | PDF Full-text (513 KB) | HTML Full-text | XML Full-text
Abstract
Cell-penetrating peptides (CPP) have become a widely used tool for efficient cargo delivery into cells. However, one limiting fact is their uptake by endocytosis causing the enclosure of the CPP-cargo construct within endosomes. One often used method to enhance the outflow into [...] Read more.
Cell-penetrating peptides (CPP) have become a widely used tool for efficient cargo delivery into cells. However, one limiting fact is their uptake by endocytosis causing the enclosure of the CPP-cargo construct within endosomes. One often used method to enhance the outflow into the cytosol is the fusion of endosome-disruptive peptide or protein sequences to CPP. But, until now, no studies exist investigating the effects of the fusion peptide to the cellular distribution, structural arrangements and cytotoxic behaviour of the CPP. In this study, we attached a short modified sequence of hemagglutinin subunit HA2 to different CPP and analysed the biologic activity of the new designed peptides. Interestingly, we observed an increased cytosolic distribution but also highly toxic activities in the micromolar range against several cell lines. Structural analysis revealed that attachment of the fusion peptide had profound implications on the whole conformation of the peptide, which might be responsible for membrane interaction and endosome disruption. Full article
(This article belongs to the Special Issue Cell-penetrating Peptides 2012)
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Other

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Open AccessOpinion Antihypertensive Drug and Inner Ear Perfusion: An Otologist’s Point of View
Pharmaceuticals 2009, 2(2), 44-48; doi:10.3390/ph2020044
Received: 23 July 2009 / Revised: 4 September 2009 / Accepted: 11 September 2009 / Published: 11 September 2009
Cited by 1 | PDF Full-text (30 KB) | HTML Full-text | XML Full-text
Abstract
A number of labyrinthine disorders with sensorineural hearing loss, vertigo, and tinnitus are known to occur to young people without vascular risk factors, thus being classified as “idiopathic” in the absence of satisfactory explanations; in the last decade, this phenomenon has found [...] Read more.
A number of labyrinthine disorders with sensorineural hearing loss, vertigo, and tinnitus are known to occur to young people without vascular risk factors, thus being classified as “idiopathic” in the absence of satisfactory explanations; in the last decade, this phenomenon has found a reliable explanation by the adverse effect of a sharp decrease of blood pressure values followed by an abnormal vasomotor regulation. This model may not only be applied to healthy subjects, but even had some confirmation in conditions possibly affecting hemodynamic changes, such as heart failure or treated hypertension. In particular, the results of a recent study on the impact of different antihypertensive therapies, which was analyzed by monitoring the onset or enhancement of tinnitus as a symptom of inner ear sufferance, unequivocally demonstrated an increased prevalence of tinnitus in subjects submitted to more “aggressive” treatments. This seems in agreement with recent observations about the model of fluid homeostasis of the inner ear, and suggests, when possible, to resort to treatments with modulatory effects in order to maintain a steady perfusion to the labyrinth thus protecting its function. Full article
(This article belongs to the Special Issue Antihypertensive Drugs)

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