Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
23
pubmed:dateCreated
2007-10-15
pubmed:abstractText
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.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Dec
pubmed:issn
0968-0896
pubmed:author
pubmed:issnType
Print
pubmed:day
1
pubmed:volume
15
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
7355-60
pubmed:meshHeading
pubmed-meshheading:17889544-Antineoplastic Agents, pubmed-meshheading:17889544-Apoptosis, pubmed-meshheading:17889544-Cecropia Plant, pubmed-meshheading:17889544-Cell Line, Tumor, pubmed-meshheading:17889544-Cell Survival, pubmed-meshheading:17889544-Dose-Response Relationship, Drug, pubmed-meshheading:17889544-Drug Resistance, Multiple, pubmed-meshheading:17889544-Drug Resistance, Neoplasm, pubmed-meshheading:17889544-Drug Screening Assays, Antitumor, pubmed-meshheading:17889544-Humans, pubmed-meshheading:17889544-K562 Cells, pubmed-meshheading:17889544-Leukemia, pubmed-meshheading:17889544-Molecular Conformation, pubmed-meshheading:17889544-Plant Roots, pubmed-meshheading:17889544-Sensitivity and Specificity, pubmed-meshheading:17889544-Stereoisomerism, pubmed-meshheading:17889544-Structure-Activity Relationship, pubmed-meshheading:17889544-Triterpenes
pubmed:year
2007
pubmed:articleTitle
Natural triterpenoids from Cecropia lyratiloba are cytotoxic to both sensitive and multidrug resistant leukemia cell lines.
pubmed:affiliation
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.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't