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dc.contributor.authorZhang, Xue-Qing
dc.contributor.authorSpadafora, Carmenza
dc.contributor.authorPineda, Laura M.
dc.contributor.authorNg, Michelle G.
dc.contributor.authorSun, Ji-Hong
dc.contributor.authorWang, Wei
dc.contributor.authorWang, Chang-Yun
dc.contributor.authorGu, Yu-Cheng
dc.contributor.authorShao, Chang-Lun
dc.date.accessioned2020-06-17T18:39:48Z
dc.date.available2020-06-17T18:39:48Z
dc.date.issued2017-09-18
dc.identifier.otherhttps://www.nature.com/articles/s41598-017-12336-0
dc.identifier.urihttp://repositorio-indicasat.org.pa/handle/123456789/89
dc.descriptionTen antifouling 14-membered resorcylic acid lactones 1–10 were isolated previously with low or trace natural abundance from the zoanthid-derived Cochliobolus lunatus fungus. Further optimization of fermentation conditions led to the isolation of two major natural compounds 7 and 8 with multi-gram quantities. By one or two steps, we semisynthesized the six trace natural compounds 1–6 and a series of derivatives 11–27 of compounds 7 and 8 with high yields (65–95%). Compounds 11–13 showed strong antiplasmodial activity against Plasmodium falciparum with IC50 values of 1.84, 8.36, and 6.95 μM, respectively. Very importantly, 11 and 12 were non-toxic with very safety and high therapeutic indices (CC50/IC50 > 180), and thus representing potential promising leads for antiplasmodial drug discovery. Furthermore, 11 was the only compound showed obvious antileishmanial activity against Leishmania donovani with an IC50 value of 9.22 μM. Compounds 11 and 12 showed the values of IC50 at 11.9 and 17.2 μM against neglected Chagas’ disease causing Trypanosoma cruzi, respectively.en_US
dc.description.abstractTen antifouling 14-membered resorcylic acid lactones 1–10 were isolated previously with low or trace natural abundance from the zoanthid-derived Cochliobolus lunatus fungus. Further optimization of fermentation conditions led to the isolation of two major natural compounds 7 and 8 with multi-gram quantities. By one or two steps, we semisynthesized the six trace natural compounds 1–6 and a series of derivatives 11–27 of compounds 7 and 8 with high yields (65–95%). Compounds 11–13 showed strong antiplasmodial activity against Plasmodium falciparum with IC50 values of 1.84, 8.36, and 6.95 μM, respectively. Very importantly, 11 and 12 were non-toxic with very safety and high therapeutic indices (CC50/IC50 > 180), and thus representing potential promising leads for antiplasmodial drug discovery. Furthermore, 11 was the only compound showed obvious antileishmanial activity against Leishmania donovani with an IC50 value of 9.22 μM. Compounds 11 and 12 showed the values of IC50 at 11.9 and 17.2 μM against neglected Chagas’ disease causing Trypanosoma cruzi, respectively.en_US
dc.language.isoengen_US
dc.rightshttps://creativecommons.org/licenses/by-nc-sa/4.0/
dc.rightsinfo:eu-repo/semantics/openAccess
dc.subjectDiscoveryen_US
dc.subjectSemisynthesisen_US
dc.subjectAntiparasitic and Cytotoxicen_US
dc.subjectEvaluation of 14-Membereden_US
dc.subjectResorcylic Acid Lactonesen_US
dc.subjectTheir Derivativesen_US
dc.titleDiscovery, Semisynthesis, Antiparasitic and Cytotoxic Evaluation of 14-Membered Resorcylic Acid Lactones and Their Derivativesen_US
dc.typeinfo:eu-repo/semantics/articleen_US
dc.typeinfo:eu-repo/semantics/publishedVersion


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