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dc.creatorCheng, Ken Chih-Chien
dc.creatorCao, Shugeng
dc.creatorRaveh, Avi
dc.creatorMacArthur, Ryan
dc.creatorDranchak, Patricia
dc.creatorChlipala, George
dc.creatorOkoneski, Matthew T.
dc.creatorGuha, Rajarshi
dc.creatorEastman, Richard T.
dc.creatorYuan, Jing
dc.creatorSchultz, Pamela J.
dc.creatorSu, Xin-zhuan
dc.creatorTamayo Castillo, Giselle
dc.creatorMatainaho, Teatulohi
dc.creatorClardy, Jon
dc.creatorSherman, David H.
dc.creatorInglese, James
dc.date.accessioned2018-03-06T20:45:48Z
dc.date.available2018-03-06T20:45:48Z
dc.date.issued2015
dc.identifier.citationhttps://pubs.acs.org/doi/10.1021/acs.jnatprod.5b00489es_ES
dc.identifier.issn0163-3864
dc.identifier.issn1520-6025
dc.identifier.urihttp://hdl.handle.net/10669/74238
dc.description.abstractMethods to identify the bioactive diversity within natural product extracts (NPEs) continue to evolve. NPEs constitute complex mixtures of chemical substances varying in structure, composition, and abundance. NPEs can therefore be challenging to evaluate efficiently with high-throughput screening approaches designed to test pure substances. Here we facilitate the rapid identification and prioritization of antimalarial NPEs using a pharmacologically driven, quantitative high-throughput-screening (qHTS) paradigm. In qHTS each NPE is tested across a concentration range from which sigmoidal response, efficacy, and apparent EC50s can be used to rank order NPEs for subsequent organism reculture, extraction, and fractionation. Using an NPE library derived from diverse marine microorganisms we observed potent antimalarial activity from two Streptomyces sp. extracts identified from thousands tested using qHTS. Seven compounds were isolated from two phylogenetically related Streptomyces species: Streptomyces ballenaensis collected from Costa Rica and Streptomyces bangulaensis collected from Papua New Guinea. Among them we identified actinoramides A and B, belonging to the unusually elaborated nonproteinogenic amino-acid-containing tetrapeptide series of natural products. In addition, we characterized a series of new compounds, including an artifact, 25-epi-actinoramide A, and actinoramides D, E, and F, which are closely related biosynthetic congeners of the previously reported metabolites.es_ES
dc.description.sponsorshipNational Institutes of Health/[U01 TW007404]/NIH/Estados Unidoses_ES
dc.description.sponsorshipInstituto Nacional de Biodiversidad/[R-CM-INBio-82-2009-OT]/INBio/Costa Ricaes_ES
dc.language.isoen_USes_ES
dc.sourceJournal of Natural Products, Vol.78, Núm. 10, 2015es_ES
dc.subjectNatural productses_ES
dc.subjectMarine Extractses_ES
dc.subjectPotent Antimalariales_ES
dc.titleActinoramide A Identified as a Potent Antimalarial from Titration-Based Screening of Marine Natural Product Extractses_ES
dc.typeinfo:eu-repo/semantics/articlees_ES
dc.typeArtículo científicoes_ES
dc.identifier.doi10.1021/acs.jnatprod.5b00489
dc.description.procedenceUCR::Vicerrectoría de Investigación::Unidades de Investigación::Ciencias Básicas::Centro de Investigaciones en Productos Naturales (CIPRONA)es_ES
dc.identifier.pmid26465675
dc.identifier.pmidPMC4633019


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