Abstract |
25-Hydroxyprotopanaxadiol (25-OH-PPD) is a natural compound isolated from Panax ginseng, and its anti- tumor activity has been studied in previous publication. In the current study, we investigated the anti- tumor activity of three novel derivatives synthesized from 25-OH-PPD, namely (20R)-12β-O-(l-chloracetyl)-dammarane-3β, 20, 25-triol (xl), (20R)-3β-O-(l-alanyl)-dammarane-12β, 20, 25-triol (1c), and (20R)-3β-O-(Boc-l-arginyl)-dammarane-12β, 20, 25-triol (8b). All three compounds significantly inhibited the growths of human colorectal cancer cells, while having lesser effect on the growth of normal primary muscle cells and spleno-lymphocytes. Further mechanistic study demonstrated that these compounds could induce apoptosis by activating the components of caspase-signaling pathways in HCT116 cells, but not in spleno-lymphocytes. Taken together, the results suggested that 25-OH-PPD derivatives exerted promising anti- tumor activity that is specific to human colorectal cancer cells, and may therefore represent a potential chemotherapeutic strategy for the treatment of colorectal cancer.
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Authors | Xichun Xia, Bowen Jiang, Wei Liu, Peng Wang, Yanhua Mou, Yafei Liu, Yuqing Zhao, Xiuli Bi |
Journal | Steroids
(Steroids)
Vol. 80
Pg. 24-9
(Feb 2014)
ISSN: 1878-5867 [Electronic] United States |
PMID | 24316234
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Copyright | Copyright © 2013 Elsevier Ltd. All rights reserved. |
Chemical References |
- 25-hydroxyprotopanaxadiol
- Antineoplastic Agents, Phytogenic
- Ginsenosides
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Topics |
- Antineoplastic Agents, Phytogenic
(chemistry, isolation & purification, pharmacology)
- Cell Proliferation
(drug effects)
- Cell Survival
(drug effects)
- Colorectal Neoplasms
(drug therapy, pathology)
- Dose-Response Relationship, Drug
- Drug Screening Assays, Antitumor
- Ginsenosides
(chemistry, isolation & purification, pharmacology)
- HCT116 Cells
- HT29 Cells
- Humans
- Molecular Conformation
- Panax
(chemistry)
- Stereoisomerism
- Structure-Activity Relationship
- Tumor Cells, Cultured
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