UM
Rhodamine B-conjugated encrypted vipericidin nonapeptide is a potent toxin to zebrafish and associated with in vitro cytotoxicity
Wang L.2; Chan J.Y.W.2; Rego J.V.1; Chong C.-M.2; Ai N.2; Falcao C.B.1; Radis-Baptista G.1; Lee S.M.Y.2
2015
Source PublicationBiochimica et Biophysica Acta - General Subjects
ISSN18728006 03044165
Volume1850Issue:6Pages:1253-1260
AbstractAbstract Background Animal venoms contain a diverse array of proteins and enzymes that are toxic toward various physiological systems. However, there are also some practical medicinal uses for these toxins including use as anti-bacterial and anti-tumor agents. Methods In this study, we identified a nine-residue cryptic oligopeptide, KRFKKFFKK (EVP50) that is repeatedly encoded in tandem within vipericidin sequences. Results EVP50 displayed in vivo potent lethal toxicity to zebrafish larvae (LD = 6 μM) when the peptide's N-terminus was chemically conjugated to rhodamine B (RhoB). In vitro, RhoB-conjugated EVP50 (RhoB-EVP50) exhibited a concentration-dependent cytotoxic effect toward MCF-7 and MDA-MB-231 breast cancer cells. In MCF-7 cells, the RhoB-EVP50 nonapeptide accumulated inside the cells within minutes. In the cytoplasm, the RhoB-EVP50 induced extracellular calcium influx and intracellular calcium release. Membrane budding was also observed after incubation with micromolar concentrations of the fluorescent EVP50 conjugate. Conclusions The conjugate's interference with calcium homeostasis, its intracellular accumulation and its induced membrane dysfunction (budding and vacuolization) seem to act in concert to disrupt the cell circuitry. Contrastively, unconjugated EVP50 peptide did not display neither toxic nor cytotoxic activities in our in vivo and in vitro models. General significance The synergic mechanism of toxicity was restricted to the structurally modified encrypted vipericidin nonapeptide.
KeywordCell-penetrating peptide Cytotoxin Encrypted peptides Rhodamine B-conjugated peptide Vipericidins Zebra-fish model
DOI10.1016/j.bbagen.2015.02.013
URLView the original
Language英語
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Cited Times [WOS]:12   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionUniversity of Macau
Affiliation1.Universidade Federal do Ceara
2.University of Macau
First Author AffilicationUniversity of Macau
Recommended Citation
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Wang L.,Chan J.Y.W.,Rego J.V.,et al. Rhodamine B-conjugated encrypted vipericidin nonapeptide is a potent toxin to zebrafish and associated with in vitro cytotoxicity[J]. Biochimica et Biophysica Acta - General Subjects,2015,1850(6):1253-1260.
APA Wang L..,Chan J.Y.W..,Rego J.V..,Chong C.-M..,Ai N..,...&Lee S.M.Y..(2015).Rhodamine B-conjugated encrypted vipericidin nonapeptide is a potent toxin to zebrafish and associated with in vitro cytotoxicity.Biochimica et Biophysica Acta - General Subjects,1850(6),1253-1260.
MLA Wang L.,et al."Rhodamine B-conjugated encrypted vipericidin nonapeptide is a potent toxin to zebrafish and associated with in vitro cytotoxicity".Biochimica et Biophysica Acta - General Subjects 1850.6(2015):1253-1260.
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