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Correction published on 26 March 2015, see Molecules 2015, 20(4), 5438-5439.

Open AccessArticle
Molecules 2014, 19(5), 6142-6162;

Anticancer Activities of Polyynes from the Root Bark of Oplopanax horridus and Their Acetylated Derivatives

State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Avenida da Universidade, Macau, China
Tang Center for Herbal Medicine Research, The Pritzker School of Medicine, University of Chicago, 5841 South Maryland Avenue, MC 4028, Chicago, IL 60637, USA
These authors contributed equally to this work.
These authors contributed equally to this work.
Authors to whom correspondence should be addressed.
Received: 12 April 2014 / Revised: 9 May 2014 / Accepted: 12 May 2014 / Published: 14 May 2014
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Six polyynes OH-1~6, some of which are occur naturally in acetylated form, had been isolated and identified from the root bark of Oplopanax horridus (Devil’s Club), a natural dietary supplement and medicinal plant in North America. During the evaluation of the polyynes’ potential anticancer activities, sixteen more acetylated derivatives OHR-1~16 have synthesized and their anti-proliferation activity on MCF-7, MDA-MB-231, A549, HepG2 and LO2 cells assayed to elucidate their structure-activity relationships. The results showed that OH-1 ((3S, 8S)-falcarindiol) had the most potent anticancer activity, with IC50 values of 15.3, 23.5, 7.7 and 4.7 μM on MCF-7, A549, HepG2 and MDA-MB-231 cells, respectively. For the primary structure-activity relationship, the anticancer activities of polyynes become weaker if their hydroxyl groups are acetylated, the terminal double bonds transformed into single bonds or they contain one more methylene group in the main skeleton chain. View Full-Text
Keywords: polyynes; Oplopanax; anticancer; structure-activity relationship polyynes; Oplopanax; anticancer; structure-activity relationship

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This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Meng, L.-Z.; Huang, W.-H.; Wang, C.-Z.; Yuan, C.-S.; Li, S.-P. Anticancer Activities of Polyynes from the Root Bark of Oplopanax horridus and Their Acetylated Derivatives. Molecules 2014, 19, 6142-6162.

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