Enhanced efficacy of 7-hydroxy-3-methoxycadalene via glycosylation in in vivo xenograft study.

7-Hydroxy-3-methoxycadalene, isolated from Zelkova serrata Makino, was confirmed as a biologically active natural compound. In this study, the efficacy of cadalene as an anticancer agent was tested. In order to address the poor physicochemical properties of cadalene, we designed and synthesized glycosylated cadalene derivatives for improved solubility and efficient drug delivery as a potential prodrug. In vitro cell viability assays confirmed that glycosylated cadalenes were less toxic and more soluble than cadalene. In an in vivo xenograft study in mice, the oral administration of glycosylated cadalenes caused a significant reduction in tumor size.
AuthorsHyang Yeon Lee, Jung-Taek Kwon, Minseob Koh, Myung-Haing Cho, Seung Bum Park
JournalBioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 17 Issue 22 Pg. 6335-9 (Nov 15 2007) ISSN: 0960-894X [Print] England
PMID17889531 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • 7-hydroxy-3-methoxy-cadalene
  • Antineoplastic Agents
  • Naphthalenes
  • Plant Extracts
  • Sesquiterpenes
  • Administration, Oral
  • Animals
  • Antineoplastic Agents (therapeutic use)
  • Cell Line, Tumor
  • Cell Survival (drug effects)
  • Drug Delivery Systems
  • Glycosylation
  • Humans
  • Mice
  • Molecular Structure
  • Naphthalenes (pharmacology)
  • Neoplasms (drug therapy)
  • Phytotherapy
  • Plant Extracts (chemistry)
  • Sesquiterpenes
  • Solubility
  • Tumor Burden (drug effects)
  • Ulmaceae (chemistry)
  • Xenograft Model Antitumor Assays

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