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30%) was observed; this protein increase was not accompanied by a similar increase in FPTase β-subunit m-RNA levels. The Fc
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doi:10.1016/j.bmc.2005.06.029 
Copyright © 2005 Elsevier Ltd All rights reserved.
Cyclopentenediones, inhibitors of farnesyl protein transferase and anti-tumor compounds, isolated from the fruit of Lindera erythrocarpa Makino
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Hyun-Mi Oha, b, †, Sung-Kyu Choia, †, Ji Min Leea, Su-Kyung Leea, Hak-Yung Kimb, Dong Cho Hana, Hwan-Mook Kima, Kwang-Hee Sona, 
, 
and Byoung-Mog Kwona, c, ,
Received 4 May 2005;
Abstract
Four cyclopentenediones, farnesyl protein transferase inhibitors, and anti-tumor compounds were isolated from the methanolic extract of the fruits of Lindera erythrocarpa Makino (Lauraceae). The structure of the compounds was determined by spectral data including NMR and mass spectrometry, and cyclopentenediones such as methyllinderone (1), methyllucidone (2), lucidone (3), and linderone (4) were identified by comparing their reported spectral data with that of the literature values. Compounds 1–4 inhibited farnesyl protein transferase with IC50 value of 55.3 ± 4.1, 42 ± 1.9, 103 ± 5.1, and 40 ± 3.5 μM, respectively. Isolated compounds also inhibited the growth of various human cancer cell lines in a dose-dependent manner. Especially, Compounds 1 and 2 selectively inhibited the growth of H-ras-transformed rat-2 cell lines in comparison with normal rat-2 cells with a GI50 value of 0.3 and 0.85 μM, respectively. Methyllucidone strongly inhibited the growth of human cancer cells and colon tumor xenografted in nude mice. The anti-tumor effects of the compound were further confirmed with caspase-3 activation and degradation of PARP. The results suggest that methyllucidone can be a potential anti-cancer agent against H-ras-transformed tumor and will also be a good lead molecule for the development of anti-tumor drug.
Graphical abstract
Cyclopenetendiones were isolated from the fruits of Lindera erythrocarpa. Cyclopentendiones strongly inhibited the growth of human tumor and H-ras-transformed rat-2 cells.
Keywords: Cyclopentenediones; Farnesyl protein transferase; Anti-tumor; Lindera erythrocarpa
Article Outline
- 1. Introduction
- 2. Results and discussion
- 2.1. Isolation and FPTase inhibition activity
- 2.2. In vitro anti-tumor activity
- 2.3. Methyllucidone (2) induces apoptosis in human colon cancer cell lines
- 2.4. In vivo anti-tumor activity
- 3. Conclusion
- 4. Experimental
- 4.1. General
- 4.2. Plant material
- 4.3. FPTase activity assay
- 4.4. Extraction and isolation
- 4.4.1. Methyllinederone (1)
- 4.4.2. Methyllucidone (2)
- 4.4.3. Lucidone (3)
- 4.4.4. Linderone (4)
- 4.5. Cell growth inhibition assay
- 4.6. Western blotting
- 4.7. In vivo activities of methyllucidone
- Acknowledgements
- References
