کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1362228 | 981481 | 2007 | 6 صفحه PDF | دانلود رایگان |
The cytotoxicity of four triterpenoids, euscaphic acid (1), tormentic acid (2), 2α-acetyl tormentic acid (3), and 3β-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.
In vitro cytotoxicity of Cecropia lyratiloba triterpenoids, euscaphic acid (1), tormentic acid (2), 2α-acetyl tormentic acid (3), and 3β-acetyl tormentic acid (4) against K562 and K562/VCR leukemia cell lines.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry - Volume 15, Issue 23, 1 December 2007, Pages 7355–7360