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Cytotoxic effect of the diterpene lactone dehydrocrotonin from Croton cajucara on human promyelocytic leukemia cells.

Abstract
Diterpenes exhibit potent antineoplastic properties against human and murine carcinoma cell lines. trans-Dehydrocrotonin from Croton cajucara, a Brazilian medicinal plant, is a nor-diterpene with antiulcerogenic activity. In this work, we examined the effect of trans-dehydrocrotonin (t-DCTN) on the vitality of HL60 cells by assessing the MTT reduction, protein content and phosphatase activity of these cells. Protein quantification indicated that t-DCTN reduced the number of cells with an IC50 of 500 microM; mitochondrial function (MTT reduction), was also inhibited (IC50 = 300 microM), when the cells were treated for 24 h. In contrast, when the cells were treated with this lactone in the initial plating and cultured for 96 h, t-DCTN was more toxic for all parameters analyzed: MTT and phosphatase activity (IC50 = 180 microM) and protein content (IC50 = 150 microM). The flavonoid utilized as positive control myricetin and the following IC50 values were obtained after 24 h of treatment: 300 and 192 microM for protein content and MTT reduction, respectively. According to the chemical characteristics of both compounds, the cytotoxic effect of t-DCTN could be explained through two mechanisms: adduct formation with DNA and proteins and/or oxidative stress induction.
AuthorsAna Claudia Galvão Freire, Patrícia da Silva Melo, Hiroshi Aoyama, Marcela Haun, Nelson Durán, Carmen Veríssima Ferreira
JournalPlanta medica (Planta Med) Vol. 69 Issue 1 Pg. 67-9 (Jan 2003) ISSN: 0032-0943 [Print] Germany
PMID12567283 (Publication Type: Letter, Research Support, Non-U.S. Gov't)
Chemical References
  • Antineoplastic Agents, Phytogenic
  • Diterpenes
  • Diterpenes, Clerodane
  • Tetrazolium Salts
  • Thiazoles
  • dehydrocrotonin
  • thiazolyl blue
Topics
  • Antineoplastic Agents, Phytogenic (pharmacology)
  • Croton (chemistry)
  • Diterpenes (pharmacology)
  • Diterpenes, Clerodane
  • Drug Screening Assays, Antitumor
  • HL-60 Cells
  • Humans
  • Plants, Medicinal
  • Tetrazolium Salts
  • Thiazoles

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