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J Asian Nat Prod Res ; 16(6): 623-8, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-24911667

RESUMO

Resibufogenin (RB), a major bioactive bufadienolide, has the potential anticancer activity. In the present work, biotransformation of RB by Actinomucor elegans AS 3.2778 yielded five products, namely 3-oxo-resibufogenin (1), 3-epi-resibufogenin (2), 3-epi-12-oxo-hydroxylresibufogenin (3), 3α-acetoxy-15α-hydroxylbufalin (4), and 3-epi-12α-hydroxylresibufogenin (5), respectively. Among them, metabolites 3 and 4 are previously unreported. The chemical structures of metabolites 1-5 were fully elucidated on the basis of 2D NMR and HR-MS. The highly stereo- and regio-specific isomerization, hydroxylation, and esterification reactions were observed in the biotransformation process of RB by A. elegans. Their cytotoxicities against A549 and H1299 cells were evaluated.


Assuntos
Antineoplásicos/metabolismo , Bufanolídeos/metabolismo , Mucorales/metabolismo , Antineoplásicos/química , Antineoplásicos/farmacologia , Biotransformação , Bufanolídeos/química , Bufanolídeos/farmacologia , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Hidroxilação , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular
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