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Anti-tumor activity of three novel derivatives of ginsenoside on colorectal cancer cells.

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.
AuthorsXichun Xia, Bowen Jiang, Wei Liu, Peng Wang, Yanhua Mou, Yafei Liu, Yuqing Zhao, Xiuli Bi
JournalSteroids (Steroids) Vol. 80 Pg. 24-9 (Feb 2014) ISSN: 1878-5867 [Electronic] United States
PMID24316234 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
CopyrightCopyright © 2013 Elsevier Ltd. All rights reserved.
Chemical References
  • 25-hydroxyprotopanaxadiol
  • Antineoplastic Agents, Phytogenic
  • Ginsenosides
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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