Piplartine induces genotoxicity in eukaryotic but not in prokaryotic model systems.
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.
Bezerra
Daniel P
DP
Campus Arapiraca, Universidade Federal de Alagoas, Arapiraca, Alagoas, Brazil.
Vasconcellos
Marne C
MC
Machado
Miriana S
MS
Villela
Izabel V
IV
Rosa
Renato M
RM
Moura
Dinara J
DJ
Pessoa
Cláudia
C
Moraes
Manoel O
MO
Silveira
Edilberto R
ER
Lima
Mary Anne S
MA
Aquino
Nayara C
NC
Henriques
João Antonio P
JA
Saffi
Jenifer
J
Costa-Lotufo
Letícia V
LV
D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000633:toxicity*; D002869:Chromosome Aberrations; D006224:Cricetinae; D005057:Eukaryotic Cells / Q000187:drug effects*; D005260:Female; D008297:Male; D051379:Mice; D009152:Mutagenicity Tests; D009153:Mutagens; D010881:Piperidones / Q000633:toxicity*; D011387:Prokaryotic Cells / Q000187:drug effects*; D012475:Salmonella / Q000235:genetics
D000972:Antineoplastic Agents, Phytogenic; D009153:Mutagens; D010881:Piperidones; C498077:piperlongumine