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Identification of potential anticancer compounds from Oplopanax horridus
Wang C.-Z.1; Zhang Z.1; Huang W.-H.2; Du G.-J.1; Wen X.-D.1; Calway T.1; Yu C.1; Nass R.1; Zhao J.2; Du W.1; Li S.-P.2; Yuan C.-S.1
Source PublicationPhytomedicine
ISSN09447113 1618095X

Oplopanax horridus is a plant native to North America. Previous reports have demonstrated that this herb has antiproliferative effects on cancer cells but study mostly focused on its extract or fractions. Because there has been limited phytochemical study on this herb, its bioactive compounds are largely unknown. We recently isolated and identified 13 compounds, including six polyynes, three sesquiterpenes, two steroids, and two phenolic acids, of which five are novel compounds. In this study, we systemically evaluated the anticancer effects of compounds isolated from O. horridus. Their antiproliferative effects on a panel of human colorectal and breast cancer cells were determined using the MTS assay. Cell cycle distribution and apoptotic effects were analyzed by flow cytometry. The in vivo antitumor effect was examined using a xenograft tumor model. Among the 13 compounds, strong antiproliferative effects were observed from falcarindiol and a novel compound oplopantriol A. Falcarindiol showed the most potent antiproliferative effects, significantly inducing pro-apoptosis and cell cycle arrest in the S and G2/M phases. The anticancer potential of falcarindiol was further verified in vivo, significantly inhibiting HCT-116 tumor growth in an athymic nude mouse model at 15 mg/kg. We also analyzed the relationship between polyyne structures and their pharmacological activities. We observed that both the terminal hydroxyl group and double bond obviously affected their anticancer potential. Results from this study supplied valuable information for future semi-synthesis of polyyne derivatives to develop novel cancer chemopreventive agents. © 2013 Elsevier GmbH.

KeywordAnticancer Apoptosis Cell Cycle Falcarindiol Oplopanax Horridus Oplopantriol a Phytochemistry Polyynes Structure-activity Relationship
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Indexed BySCI
WOS Research AreaPlant Sciences ; Pharmacology & Pharmacy ; Integrative & Complementary Medicine
WOS SubjectPlant Sciences ; Chemistry, Medicinal ; Integrative & Complementary Medicine ; Pharmacology & Pharmacy
WOS IDWOS:000323299200009
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Cited Times [WOS]:27   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Affiliation1.University of Chicago
2.University of Macau
Recommended Citation
GB/T 7714
Wang C.-Z.,Zhang Z.,Huang W.-H.,et al. Identification of potential anticancer compounds from Oplopanax horridus[J]. Phytomedicine,2013,20(11):999-1006.
APA Wang C.-Z..,Zhang Z..,Huang W.-H..,Du G.-J..,Wen X.-D..,...&Yuan C.-S..(2013).Identification of potential anticancer compounds from Oplopanax horridus.Phytomedicine,20(11),999-1006.
MLA Wang C.-Z.,et al."Identification of potential anticancer compounds from Oplopanax horridus".Phytomedicine 20.11(2013):999-1006.
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