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Isolation, Characterization, and Bioactivity of Cyclotides from the Micronesian Plant Psychotria leptothyrsa
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy.
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy.
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2010 (English)In: Journal of natural products (Print), ISSN 0163-3864, E-ISSN 1520-6025, Vol. 73, no 7, 1207-1213 p.Article in journal (Refereed) Published
Abstract [en]

Cyclotides, the largest known family of head-to-tail cyclic peptides, have approximately 30 amino acid residues with a complex structure containing a circular peptide backbone and a cystine knot. They are found in plants from the Violaceae and Rubiaceae families and are speculated to function in plant protection. In addition to their insecticidal properties, cyclotides display cytotoxic. anti-IIIV, antimicrobial, and inhibition of neurotensin binding activities. Although cyclotides are present in all violaceous species hitherto screened, their distribution and expression in Rubiaceae are not fully understood. In this study, we show that Psychotria leptothyrsa var. longicarpa (Rubiaceae) contains a suite of different cyclotides. The cyclotide fractions were isolated by RP-HPLC, and sequences of six new peptides, named psyles A-F. were determined by MS/MS sequencing. One or these, psyle C. is the first rubiaceous linear variant known. Psyles A, C, and E were analyzed in a fluorometric microculture assay to determine cytotoxicity toward the human lymphoma cell line U937-GTB. The IC50 values of psylcs A. C. and E were 26, 3.50, and 0.76 mu M. respectively. This study expands the number of known rubiaceous cyclotides and shows that the linear cyclotide maintains cytotoxicity.

Place, publisher, year, edition, pages
2010. Vol. 73, no 7, 1207-1213 p.
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Biological Sciences
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URN: urn:nbn:se:uu:diva-135949DOI: 10.1021/np9007365ISI: 000280140500004PubMedID: 20575512OAI: oai:DiVA.org:uu-135949DiVA: diva2:375878
Available from: 2010-12-09 Created: 2010-12-09 Last updated: 2017-12-11Bibliographically approved

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