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Piplartine induces genotoxicity in eukaryotic but not in prokaryotic model systems.

Abstract
Piplartine {5,6-dihydro-1-[(2E)-1-oxo-3-(3,4,5-trimethoxyphenyl)-2-propen-1-yl]-2(1H)-pyridinone} is an alkamide present in Piper species that exhibits promising anticancer properties. It was previously shown that piplartine is mutagenic in yeast and cultured mammalian cells. This study was performed to increase the knowledge on the mutagenic potential of piplartine using the Salmonella/microsome assay, V79 cell micronucleus and chromosome aberration assays, and mouse bone-marrow micronucleus tests. Piplartine was isolated from the roots of Piper tuberculatum. This extracted compound was unable to induce a mutagenic response in any Salmonella typhimurium strain either in the presence or absence of metabolic activation. Piplartine showed mutagenic effects in V79 cells, as there was an increased frequency of aberrant cells and micronuclei formation. In addition, piplartine administered at 50mg/kg did not induce micronucleus formation in vivo, but a dose of 100mg/kg induced an increase in the levels of micronucleus polychromatic erythrocytes (MNPCEs). Overall, these results provide further support that piplartine induces in vivo and in vitro mutagenicity in eukaryotic models.
AuthorsDaniel P Bezerra, Marne C Vasconcellos, Miriana S Machado, Izabel V Villela, Renato M Rosa, Dinara J Moura, Cláudia Pessoa, Manoel O Moraes, Edilberto R Silveira, Mary Anne S Lima, Nayara C Aquino, João Antonio P Henriques, Jenifer Saffi, Letícia V Costa-Lotufo
JournalMutation research (Mutat Res) 2009 Jun-Jul Vol. 677 Issue 1-2 Pg. 8-13 ISSN: 0027-5107 [Print] Netherlands
PMID19379832 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Antineoplastic Agents, Phytogenic
  • Mutagens
  • Piperidones
  • piplartine
Topics
  • Animals
  • Antineoplastic Agents, Phytogenic (toxicity)
  • Chromosome Aberrations
  • Cricetinae
  • Eukaryotic Cells (drug effects)
  • Female
  • Male
  • Mice
  • Mutagenicity Tests
  • Mutagens
  • Piperidones (toxicity)
  • Prokaryotic Cells (drug effects)
  • Salmonella (genetics)

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