Molecules 2014, 19(5), 6142-6162; doi:10.3390/molecules19056142
Article

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

1,2,* email, 4email, 3email, 3,* email and 1,2email
Received: 12 April 2014; in revised form: 9 May 2014 / Accepted: 12 May 2014 / Published: 14 May 2014
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.
Abstract: 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.
Keywords: polyynes; Oplopanax; anticancer; structure-activity relationship
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MDPI and ACS Style

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

AMA Style

Huang W-H, Shao L, Wang C-Z, Yuan C-S, Zhou H-H. Anticancer Activities of Polyynes from the Root Bark of Oplopanax horridus and Their Acetylated Derivatives. Molecules. 2014; 19(5):6142-6162.

Chicago/Turabian Style

Huang, Wei-Hua; Shao, Li; Wang, Chong-Zhi; Yuan, Chun-Su; Zhou, Hong-Hao. 2014. "Anticancer Activities of Polyynes from the Root Bark of Oplopanax horridus and Their Acetylated Derivatives." Molecules 19, no. 5: 6142-6162.


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