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Bioorg Med Chem ; 18(22): 7997-8004, 2010 Nov 15.
Article in English | MEDLINE | ID: mdl-20943402

ABSTRACT

Lipidic α-amino acids (LAAs) have been described as non-natural amino acids with long saturated or unsaturated aliphatic chains. In the continuing prospect to discover anticancer agents from marine sources, we have obtained a mixture of two cytotoxic LAAs (1a and 1b) from the zoanthid Protopalythoa variabilis. The anti-proliferative potential of 14 synthetic LAAs and 1a/1b were evaluated on four tumor cell lines (HCT-8, SF-295, MDA-MB-435, and HL-60). Five of the synthetic LAAs showed high percentage of tumor cell inhibition, while 1a/1b completely inhibited tumor cell growth. Additionally, apoptotic effects of 1a/1b were studied on HL-60 cell line. 1a/1b-treated cells showed apoptosis morphology, loss of mitochondrial potential, and DNA fragmentation.


Subject(s)
Amino Acids, Neutral/pharmacology , Anthozoa/metabolism , Antineoplastic Agents/chemistry , Amino Acids, Neutral/chemistry , Amino Acids, Neutral/isolation & purification , Animals , Antineoplastic Agents/isolation & purification , Antineoplastic Agents/pharmacology , Apoptosis/drug effects , Cell Line, Tumor , Drug Screening Assays, Antitumor , Erythrocytes/drug effects , Hemolysis , Humans , Membrane Potential, Mitochondrial/drug effects , Mice
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