title: Bioassay Guided Fractionation Identified Hederagenin as a Major Cytotoxic Agent from Cyclocarya paliurus Leaves.
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.
authors.affiliation: Tennessee Center for Botanical Medicine Research and the Department of Biology, Middle Tennessee State University, Murfreesboro, TN, USA.
authors.forename: Ying
authors.initials: Y
authors.lastname: Gao
authors.affiliation: Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences, Hai Dian District, Beijing, P. R. China.
authors.forename: Chunnian
authors.initials: C
authors.lastname: He
authors.affiliation: Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences, Hai Dian District, Beijing, P. R. China.
authors.forename: Wu
authors.initials: W
authors.lastname: Bi
authors.affiliation: College of Life Science, Northwest Normal University, Lanzhou, Gansu Province, P. R. China.
authors.forename: Guofan
authors.initials: G
authors.lastname: Wu
authors.affiliation: Tennessee Center for Botanical Medicine Research and the Department of Biology, Middle Tennessee State University, Murfreesboro, TN, USA.
authors.forename: Elliot
authors.initials: E
authors.lastname: Altman
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D045744:Cell Line, Tumor; D005591:Chemical Fractionation; D004354:Drug Screening Assays, Antitumor; D004365:Drugs, Chinese Herbal / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D006801:Humans; D029525:Juglandaceae / Q000737:chemistry*; D015394:Molecular Structure; D009828:Oleanolic Acid / Q000031:analogs & derivatives* / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D018515:Plant Leaves / Q000737:chemistry; D013329:Structure-Activity Relationship
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D004365:Drugs, Chinese Herbal; D009828:Oleanolic Acid; C025763:hederagenin