HY253, a novel compound isolated from Aralia continentalis, induces apoptosis via cytochrome c-mediated intrinsic pathway in HeLa cells

The chemical structure of HY253, 7,8a-divinyl-2,4a,4b,5,6,7,8,8a,9,9a-decahydro-1H-fluorene-2,4a,4b,9a-tetraol. This study was aimed to elucidate the novel structure of HY253 isolated from the roots of Aralia continentalis and to evaluate its detailed mechanisms on apoptotic induction in HY253-treat...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2009-02, Vol.19 (3), p.797-799
Main Authors: Oh, Ha Lim, Lim, Haeyoung, Park, Younghee, Lim, Yoongho, Koh, Hyun Chul, Cho, Youl-Hee, Lee, Chul-Hoon
Format: Article
Language:English
Subjects:
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - pharmacology
Apoptosis
Apoptotic induction
Aralia
Aralia - metabolism
Aralia continentalis
Biological and medical sciences
Cytochrome c
Cytochromes c - metabolism
Drug Design
Drug Screening Assays, Antitumor
Enzyme Activation
Fluorenes - chemical synthesis
Fluorenes - pharmacology
General pharmacology
HeLa Cells
Humans
In Situ Nick-End Labeling
Magnetic Resonance Spectroscopy
Medical sciences
Mitochondria - metabolism
Models, Chemical
Pharmacognosy. Homeopathy. Health food
Pharmacology. Drug treatments
Plant Extracts - chemical synthesis
Plant Extracts - pharmacology
Proto-Oncogene Proteins c-bcl-2 - metabolism
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Summary:The chemical structure of HY253, 7,8a-divinyl-2,4a,4b,5,6,7,8,8a,9,9a-decahydro-1H-fluorene-2,4a,4b,9a-tetraol. This study was aimed to elucidate the novel structure of HY253 isolated from the roots of Aralia continentalis and to evaluate its detailed mechanisms on apoptotic induction in HY253-treated HeLa cells. The structure of HY253 was elucidated based on the interpretation of the NMR spectra, as 7,8a-divinyl-2,4a,4b,5,6,7,8,8a,9,9a-decahydro-1H-fluorene-2,4a,4b,9a-tetraol. The TUNEL assay using flow cytometer revealed an appreciable apoptotic induction in HeLa cells treated with 100 μM of HY253 for 48 h. This apoptotic induction is associated with cytochrome c release from mitochondria, via up-regulation of pro-apoptotic Bcl-2 proteins, such as Bax and Bak, which, in turn, resulted in the activation of caspase-8, -9 and -3, and the cleavage of poly(ADP-ribose) polymerase (PARP).
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2008.12.009