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      Astaxanthin from Haematococcus pluvialis Prevents Oxidative Stress on Human Endothelial Cells without Toxicity

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          Abstract

          Astaxanthin, a powerful antioxidant, is a good candidate for the prevention of intracellular oxidative stress. The aim of the study was to compare the antioxidant activity of astaxanthin present in two natural extracts from Haematococcus pluvialis, a microalgae strain, with that of synthetic astaxanthin. Natural extracts were obtained either by solvent or supercritical extraction methods. UV, HPLC-DAD and (HPLC-(atmospheric pressure chemical ionization (APCI)+)/ion trap-MS) characterizations of both natural extracts showed similar compositions of carotenoids, but different percentages in free astaxanthin and its ester derivatives. The Trolox equivalent antioxidant capacity (TEAC) assay showed that natural extracts containing esters displayed stronger antioxidant activities than free astaxanthin. Their antioxidant capacities to inhibit intracellular oxidative stress were then evaluated on HUVEC cells. The intracellular antioxidant activity in natural extracts was approximately 90-times higher than synthetic astaxanthin (5 µM). No modification, neither in the morphology nor in the viability, of vascular human cells was observed by in vitro biocompatibility study up to 10 µM astaxanthin concentrations. Therefore, these results revealed the therapeutic potential of the natural extracts in vascular human cell protection against oxidative stress without toxicity, which could be exploited in prevention and/or treatment of cardiovascular diseases.

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            ORAC and TEAC assays comparison to measure the antioxidant capacity of food products

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              Astaxanthin: a novel potential treatment for oxidative stress and inflammation in cardiovascular disease.

              Oxidative stress and inflammation are implicated in several different manifestations of cardiovascular disease (CVD). They are generated, in part, from the overproduction of reactive oxygen species (ROS) and reactive nitrogen species (RNS) that activate transcriptional messengers, such as nuclear factor-kappaB, tangibly contributing to endothelial dysfunction, the initiation and progression of atherosclerosis, irreversible damage after ischemic reperfusion, and even arrhythmia, such as atrial fibrillation. Despite this connection between oxidative stress and CVD, there are currently no recognized therapeutic interventions to address this important unmet need. Antioxidants that provide a broad, "upstream" approach via ROS/RNS quenching or free radical chain breaking seem an appropriate therapeutic option based on epidemiologic, dietary, and in vivo animal model data. However, human clinical trials with several different well-known agents, such as vitamin E and beta-carotene, have been disappointing. Does this mean antioxidants as a class are ineffective, or rather that the "right" compound(s) have yet to be found, their mechanisms of action understood, and their appropriate targeting and dosages determined? A large class of potent naturally-occurring antioxidants exploited by nature-the oxygenated carotenoids (xanthophylls)-have demonstrated utility in their natural form but have eluded development as successful targeted therapeutic agents up to the present time. This article characterizes the mechanism by which this novel group of antioxidants function and reviews their preclinical development. Results from multiple species support the antioxidant/anti-inflammatory properties of the prototype compound, astaxanthin, establishing it as an appropriate candidate for development as a therapeutic agent for cardiovascular oxidative stress and inflammation.
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                Author and article information

                Contributors
                Role: Academic Editor
                Journal
                Mar Drugs
                Mar Drugs
                marinedrugs
                Marine Drugs
                MDPI
                1660-3397
                07 May 2015
                May 2015
                : 13
                : 5
                : 2857-2874
                Affiliations
                [1 ]INSERM U1148, Laboratory for Vascular Translational Science; University Paris 13, PRES Sorbonne Paris Cité 99, Av. Jean-Baptiste Clément, 93430 Villetaneuse, France; E-Mails: philregnier@ 123456hotmail.fr (P.R.); violeta.rodriguezruiz@ 123456univ-paris13.fr (V.R.-R.); axelle.fuentes@ 123456gmail.com (A.F.); murielle.maire@ 123456univ-paris13.fr (M.M.); michel.crepin@ 123456inserm.fr (M.C.); didier.letourneur@ 123456inserm.fr (D.L.); virginie.gueguen@ 123456univ-paris13.fr (V.G.)
                [2 ]CORDUNAP IBT, Avenida Playa Brava 3256, 1100000 Iquique, Chile; E-Mail: jorge.bastias@ 123456cordunap.cl
                [3 ]Department of Analytical Chemistry, Institute of Fine Chemistry and Nanochemistry, Campus of Rabanales, University of Córdoba, 14071 Córdoba, Spain; E-Mails: noelia.caballero.c@ 123456gmail.com (N.C.-C.); calic_amb@ 123456hotmail.es (C.C.); qa1sicrm@ 123456uco.es (D.S.); qa1rubrs@ 123456uco.es (S.R.)
                Author notes
                [* ]Author to whom correspondence should be addressed; E-Mail: graciela.pavon@ 123456univ-paris13.fr ; Tel.: +33-(0)-1-49-40-33-39; Fax: +33-(0)-1-49-40-30-83.
                Article
                marinedrugs-13-02857
                10.3390/md13052857
                4446609
                25962124
                a79747bf-c823-47ed-bd1a-447707247f41
                © 2015 by the authors; licensee MDPI, Basel, Switzerland.

                This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license ( http://creativecommons.org/licenses/by/4.0/).

                History
                : 27 January 2015
                : 27 April 2015
                Categories
                Article

                Pharmacology & Pharmaceutical medicine
                astaxanthin,antioxidants,haematococcus pluvialis,oxidative stress,huvec,teac

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