1. Academic Validation
  2. Natural triterpenoids from Cecropia lyratiloba are cytotoxic to both sensitive and multidrug resistant leukemia cell lines

Natural triterpenoids from Cecropia lyratiloba are cytotoxic to both sensitive and multidrug resistant leukemia cell lines

  • Bioorg Med Chem. 2007 Dec 1;15(23):7355-60. doi: 10.1016/j.bmc.2007.07.020.
Gleice da Graça Rocha 1 Marisol Simões Kelly Araujo Lúcio Rodrigo Rodrigues Oliveira Maria Auxiliadora Coelho Kaplan Cerli Rocha Gattass
Affiliations

Affiliation

  • 1 Lab. de Imunologia Celular, Instituto de Biofísica Carlos Chagas Filho, CCS B1 G, Universidade Federal do Rio de Janeiro, 21949-900 Rio de Janeiro, RJ, Brazil.
Abstract

The cytotoxicity of four triterpenoids, euscaphic acid (1), tormentic acid (2), 2alpha-acetyl tormentic acid (3), and 3beta-acetyl tormentic acid (4), isolated from the roots of Cecropia lyratiloba (Moraceae) by countercurrent chromatography, was evaluated in vitro in sensitive and multidrug resistant leukemia cell lines. A structure/activity relationship analysis of the compounds was performed. Acetylation of compound 2 at C2 increased its activity by a factor of 2 while acetylation at C3 had a smaller effect. Compound 1 induces death by activation of Caspase-3, dependent apoptotic pathway. Furthermore, the four triterpenoids were also active toward a multidrug resistant (MDR) leukemia cell line, overexpressing glycoprotein-P (P-gp). These results reveal the potential of the Terpenoids as source for the development of new anti-neoplastic and anti-MDR drugs.

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