Activity of perillyl alcohol, perillyl aldehyde and perillic acid against leishmania (2005)
- Authors:
- Autor USP: ULIANA, SILVIA RENI BORTOLIN - ICB
- Unidade: ICB
- Assunto: PARASITOLOGIA
- Language: Inglês
- Abstract: The chemotherapy of leishmaniasis is far from satisfactory and represents a considerable constraint for the disease control. The first choice pentavalent antimonials as well as the second choice drugs amphotericin B and pentamidine are highly toxic and resistance to the antimonial compounds is spreading. Perillyl alcohol (POH), perillyl aldehyde (PCO) and perillic acid (PCOOH) are derived from limonene, a monoterpene synthesized by plants through the isoprenoid biosynthesis pathway. Limoneno is oxidized by limonene monooxygenase to POH and by alcohol dehydrogenase and aldehyde dehydrogenase to PCO and PCOOH. Limonene and its metabolic derivatives have been evaluated in the therapy against cancer in various preclinical models, due to their action as inhibitors of the posttranslational isoprenylation of small G proteins and induction of apoptosis. We have investigated the activity of POH, PCO and PCOOH against promastigotes of L. major and the citotoxicity of these drugs against J774A1 macrophages and human fibroblasts (HFF). Cell viability was evaluated by cleavage of MTT. The sensitivity of L. major promastigotes to these compounds was not uniform. IC50s for POH were calculated as 730 and 310 mM, respectively after 24 h and 48 h of incubation. However, POH was toxic to macrophages with a CC50 of 260 mM. L. major promastigotes were killed by PCO with an IC50 of 37mM after 24h but PCO was also toxic to macrophages with a CC50 of 50 mM. Human fibroblasts were lesssensitive to PCO with a CC50 of 330 mM. The IC50 of PCOOH against L. major promastigotes after 24 h was 630mM while the CC50 for J774 macrophages was 1660 mM. In conclusion, the metabolites of limonene have antileishmanial activity but their citotoxicity for cells as macrophages represent a possible limitation. The activity of PCO deserves more investigation, given the greater tolerance of fibroblasts against this drug
- Imprenta:
- Publisher: Comissão de Cultura e Extensão Universitária do ICB/USP
- Publisher place: São Paulo
- Date published: 2005
- Source:
- Título: Resumos
- Conference titles: Congresso do Instituto de Ciências Biomédicas
-
ABNT
NIÑO DE GUZMÁN, J. A. e ULIANA, Silvia Reni Bortolin. Activity of perillyl alcohol, perillyl aldehyde and perillic acid against leishmania. 2005, Anais.. São Paulo: Comissão de Cultura e Extensão Universitária do ICB/USP, 2005. . Acesso em: 14 mar. 2026. -
APA
Niño de Guzmán, J. A., & Uliana, S. R. B. (2005). Activity of perillyl alcohol, perillyl aldehyde and perillic acid against leishmania. In Resumos. São Paulo: Comissão de Cultura e Extensão Universitária do ICB/USP. -
NLM
Niño de Guzmán JA, Uliana SRB. Activity of perillyl alcohol, perillyl aldehyde and perillic acid against leishmania. Resumos. 2005 ;[citado 2026 mar. 14 ] -
Vancouver
Niño de Guzmán JA, Uliana SRB. Activity of perillyl alcohol, perillyl aldehyde and perillic acid against leishmania. Resumos. 2005 ;[citado 2026 mar. 14 ] - Tamoxifen is effective against Leishmania and induces a rapid alkalinization of parasitophorous vacuoles harbouring Leishmania (Leishmania) amazonensis amastigotes
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