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      Bioactive Bromotyrosine-Derived Alkaloids from the Polynesian Sponge Suberea ianthelliformis

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          Abstract

          Herein, we describe the isolation and spectroscopic identification of eight new tetrabrominated tyrosine alkaloids 29 from the Polynesian sponge Suberea ianthelliformis, along with known major compound psammaplysene D ( 1), N, N-dimethyldibromotyramine, 5-hydroxy xanthenuric acid, and xanthenuric acid. Cytotoxicity and acetylcholinesterase inhibition activities were evaluated for some of the isolated metabolites. They exhibited moderate antiproliferative activity against KB cancer cell lines, but psammaplysene D ( 1) displayed substantial cytotoxicity as well as acetylcholinesterase inhibition with IC 50 values of 0.7 μM and 1.3 μM, respectively.

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          Olfactory dysfunction in Alzheimer’s disease

          Alzheimer’s disease (AD) is a common neurodegenerative disorder with the earliest clinical symptom of olfactory dysfunction, which is a potential clinical marker for AD severity and progression. However, many questions remain unanswered. This article reviews relevant research on olfactory dysfunction in AD and evaluates the predictive value of olfactory dysfunction for the epidemiological, pathophysiological, and clinical features of AD, as well as for the conversion of cognitive impairment to AD. We summarize problems of existing studies and provide a useful reference for further studies in AD olfactory dysfunction and for clinical applications of olfactory testing.
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            Alzheimer's disease, enzyme targets and drug discovery struggles: from natural products to drug prototypes.

            Alzheimer's disease (AD) is an incapacitating neurodegenerative disease that slowly destroys brain cells. This disease progressively compromises both memory and cognition, culminating in a state of full dependence and dementia. Currently, AD is the main cause of dementia in the elderly and its prevalence in the developed world is increasing rapidly. Classic drugs, such as acetylcholinesterase inhibitors (AChEIs), fail to decline disease progression and display several side effects that reduce patient's adhesion to pharmacotherapy. The past decade has witnessed an increasing focus on the search for novel AChEIs and new putative enzymatic targets for AD, like β- and γ-secretases, sirtuins, caspase proteins and glycogen synthase kinase-3 (GSK-3). In addition, new mechanistic rationales for drug discovery in AD that include autophagy and synaptogenesis have been discovered. Herein, we describe the state-of-the-art of the development of recent enzymatic inhibitors and enhancers with therapeutic potential on the treatment of AD.
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              Application of Solid Phase Adsorption Toxin Tracking (SPATT) for field detection of the hydrophilic phycotoxins domoic acid and saxitoxin in coastal California

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                Author and article information

                Journal
                Mar Drugs
                Mar Drugs
                marinedrugs
                Marine Drugs
                MDPI
                1660-3397
                27 April 2018
                May 2018
                : 16
                : 5
                : 146
                Affiliations
                [1 ]Institut de Chimie des Substances Naturelles, CNRS UPR 2301, University Paris-Sud, University of Paris-Saclay, 1, Avenue de la Terrasse, 91198 Gif-Sur-Yvette, France; eldemerdash555@ 123456gmail.com (A.E.-D.); Celine.Moriou@ 123456cnrs.fr (C.M.)
                [2 ]Organic Chemistry Division, Chemistry Department, Faculty of Science, Mansoura University, Mansoura 35516, Egypt
                [3 ]LEMAR, IRD, UBO, CNRS, IFREMER, IUEM, 29280 Plouzané, France; Jordan.Toullec@ 123456univ-brest.fr (J.T.); sylvain.petek@ 123456ird.fr (S.P.)
                [4 ]CRIOBE, CNRS, EPHE, UPVD, PSL Research University, 98729 Moorea, French Polynesia; bessonmarcluc@ 123456gmail.com (M.B.); david.lecchini@ 123456ephe.sorbonne.fr (D.L.)
                [5 ]Observatoire Océanologique de Banyuls-sur-Mer, Université Pierre et Marie Curie Paris, 66650 Banyuls-sur-Mer, France
                [6 ]EIO, UPF, ILM, IFREMER, IRD, Faa’a, 98702 Tahiti, French Polynesia; stephanie.soulet@ 123456upf.pf (S.S.); nelly.schmitt@ 123456upf.pf (N.S.)
                Author notes
                [* ]Correspondance: cecile.debitus@ 123456ird.fr (C.D.); Ali.ALMOURABIT@ 123456cnrs.fr (A.A.-M.); Tel.: +336-0448-1378 (C.D.); +336-1585-9203 (A.A.-M.)
                Author information
                https://orcid.org/0000-0001-6459-2955
                https://orcid.org/0000-0003-3381-322X
                https://orcid.org/0000-0001-7920-0467
                Article
                marinedrugs-16-00146
                10.3390/md16050146
                5983277
                29702602
                54a5e0a0-45e2-43a5-8e46-77cc0fe537dc
                © 2018 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 (CC BY) license ( http://creativecommons.org/licenses/by/4.0/).

                History
                : 29 March 2018
                : 24 April 2018
                Categories
                Article

                Pharmacology & Pharmaceutical medicine
                brominated tyrosine alkaloids,suberea ianthelliformis,cytotoxicity,acetylcholinesterase inhibition

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