Planta Med 2016; 82(01/02): 171-179
DOI: 10.1055/s-0035-1557900
Analytical Studies
Original Papers
Georg Thieme Verlag KG Stuttgart · New York

Bioassay Guided Fractionation Identified Hederagenin as a Major Cytotoxic Agent from Cyclocarya paliurus Leaves

Ying Gao*
1   Tennessee Center for Botanical Medicine Research and the Department of Biology, Middle Tennessee State University, Murfreesboro, TN, USA
,
Chunnian He*
2   Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences, Hai Dian District, Beijing, P. R. China
,
Wu Bi
2   Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences, Hai Dian District, Beijing, P. R. China
,
Guofan Wu
3   College of Life Science, Northwest Normal University, Lanzhou, Gansu Province, P. R. China
,
Elliot Altman
1   Tennessee Center for Botanical Medicine Research and the Department of Biology, Middle Tennessee State University, Murfreesboro, TN, USA
› Author Affiliations
Further Information

Publication History

received 05 May 2015
revised 13 July 2015

accepted 27 July 2015

Publication Date:
21 September 2015 (online)

Abstract

An ethanol extract prepared from the leaves of Cyclocarya paliurus, also known as sweet tea, which is one of the most popular teas utilized in traditional Chinese medicine, exhibited significant cytotoxicity against human lung and breast cancer cells. Using a bioassay-guided fractionation, we purified a pentacyclic triterpenoid, hederagenin, which exhibited superior and selective cytotoxicity against human breast and lung cancer cells. Evaluation of the structure-activity relationship between hederagenin and seven other pentacyclic triterpenoids revealed that the C3 hydroxyl group, the C17 carboxyl group and the Δ 12,13 double bond could be important active groups for the bioactivity of pentacyclic triterpenoids, whereas introduction of a hydroxyl group at C2 or C23 might reduce their bioactivity. We also investigated the cytotoxic activity of hedeargenin and demonstrated that it induces apoptosis, increases the cell membrane permeability, reduces the mitochondria potential, and suppresses NF-κB activation.

* These authors contributed equally to this work.


Supporting Information

 
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