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Molecules 2010, 15(3), 1958-1966; doi:10.3390/molecules15031958

New Cytotoxic Azaphilones from Monascus purpureus-Fermented Rice (Red Yeast Rice)

1, 1,* , 1, 2,* , 1 and 1
1 Beijing Key Laboratory of Bioactive Substances and Functional Foods, Beijing Union University, Beijing 100083, China 2 Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
* Authors to whom correspondence should be addressed.
Received: 18 January 2010 / Revised: 1 March 2010 / Accepted: 8 March 2010 / Published: 18 March 2010
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Using a cell-based cytotoxicity assay three new cytotoxic azaphilones, including two stereoisomers and designated monapurones A-C (1-3), were isolated from the extract of Monascus purpureus-fermented rice (red yeast rice). Their structures were elucidated by detailed interpretation of spectroscopic and chemical data. The relative configurations were assigned on the basis of analysis of NOE data, and the absolute configurations were determined by direct comparison of their CD spectra with those of known azaphilones and chemical correlations. In the in vitro assays, monapurones A-C (1-3) showed selective cytotoxicity against human cancer cell line A549 with IC50 values of 3.8, 2.8 and 2.4mM respectively, while exhibiting no significant toxicity to normal MRC-5 and WI-38 cells at the same concentration.
Keywords: Monascus purpureus; cytotoxicity; azaphilones; absolute configurations Monascus purpureus; cytotoxicity; azaphilones; absolute configurations
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.


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Li, J.-J.; Shang, X.-Y.; Li, L.-L.; Liu, M.-T.; Zheng, J.-Q.; Jin, Z.-L. New Cytotoxic Azaphilones from Monascus purpureus-Fermented Rice (Red Yeast Rice). Molecules 2010, 15, 1958-1966.

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