Apoptosis induction by 4β-acetoxyscirpendiol from Paecilomyces tenuipes in human leukaemia cell lines

H. C. Han, U. Lindequist, J. W. Hyun, Y. H. Kim, H. S. An, D. H. Lee, Ha Won Kim

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Abstract

The carpophores of Paecilomyces tenuipes are known in the Orient for their strong antitumor activity. In continuation of our study on acetoxyscirpendiol (ASD, 4β-acetoxyscirpene-3α,15-diol) as a cytotoxic component from this fungus, we report particularly on the mode of action of ASD in inducing apoptosis in human MOLT-4, THP-1 and Jurkat T cell leukaemia in vitro. The antiproliferative effects of ASD seem attributable to its induction of apoptosis in the cells, as it blocked the cell cycle, induced hypodiploidity and bound annexin V and also cleaved poly-(ADP-ribose) polymerase (PARP) in these cell lines. The 50% inhibitory concentrations (IC50) of ASD on MOLT-4, THP-1 and Jurkat T cells were found to be 60, 85 and 60 ng/ml, respectively. ASD arrested the cell cycle at the G1/S transition and showed hypodiploidity due to the accumulation of sub-G0 population. Annexin V binding was increased in the presence of ASD in the MOLT-4 cell line in a time-dependent manner. ASD and three of its derivatives also induced cleavage of PARP in both MOLT-4 and Jurkat T cell lines. From these data, it is suggested that ASD exerts its cytotoxic activity by inducing apoptosis in leukaemia cell lines in vitro.

Original languageEnglish (US)
Pages (from-to)42-49
Number of pages8
JournalPharmazie
Volume59
Issue number1
Publication statusPublished - Jan 1 2004
Externally publishedYes

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ASJC Scopus subject areas

  • Pharmaceutical Science

Cite this

Han, H. C., Lindequist, U., Hyun, J. W., Kim, Y. H., An, H. S., Lee, D. H., & Kim, H. W. (2004). Apoptosis induction by 4β-acetoxyscirpendiol from Paecilomyces tenuipes in human leukaemia cell lines. Pharmazie, 59(1), 42-49.