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Cytotoxic Constituents and Mechanism from Peganum harmala
Author(s) -
Wang Chunhua,
Zhang Zhenxue,
Wang Yihai,
He Xiangjiu
Publication year - 2016
Publication title -
chemistry and biodiversity
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.427
H-Index - 70
eISSN - 1612-1880
pISSN - 1612-1872
DOI - 10.1002/cbdv.201500384
Subject(s) - peganum harmala , chemistry , mechanism (biology) , traditional medicine , cytotoxic t cell , biochemistry , in vitro , epistemology , philosophy , medicine
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 α ‐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 IC 50 value of 8.03 ± 0.81 μ 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.