Journal
CHEMISTRY & BIODIVERSITY
Volume 13, Issue 7, Pages 961-968Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cbdv.201500384
Keywords
Peganum harmala; Triterpenoids; Cytotoxic activity; Non-small cell lung cancer; 3 alpha-Acetoxy-27-hydroxyolean-12-en-28-oic acid methyl ester
Funding
- National Natural Science Foundation of China [U1203103]
- Natural Science Foundation of Guangdong Province [2014A030313588]
- Key Project of Xinjiang Production & Construction Corps Key Laboratory of Protection and Utilization of Biological Resources in Tarim Basin [BRZD1205]
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Peganum harmala L. is a traditional Chinese and Uygur medicine used to treat cancer. Bioactivity-guided fractionation was applied to determine the cytotoxic constituents from P. harmala. A novel triterpenoid and a phenolic glycoside were isolated and identified, as well as seven known compounds. The novel metabolites were elucidated to be 3 alpha-acetoxy-27-hydroxyolean-12-en-28-oic acid methyl ester (1, OA) and N-acetyl-9-syringinoside (9). Some compounds exhibited potent cytotoxicity against human tumor cells. Among them, OA showed the highest cytotoxicity against human lung cancer cells A549 with an IC50 value of 8.03 +/- 0.81 mu M. OA had a potent anti-NSCLC cell activity by interfering with the epidermal growth factor receptor (EGFR) activation and its downstream signaling, and could exert an antiproliferative effect by inactivation of EGFR-driven antiapoptotic pathway followed by the release of mitochondrial cytochrome c, which might prove to be a promising leading compound for the development of an anti-lung cancer drug.
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