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.
Lee
Hyang Yeon
HY
Department of Chemistry, Seoul National University, Seoul, Republic of Korea.
Kwon
Jung-Taek
JT
Koh
Minseob
M
Cho
Myung-Haing
MH
Park
Seung Bum
SB
D000284:Administration, Oral; D000818:Animals; D000970:Antineoplastic Agents / Q000627:therapeutic use*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D016503:Drug Delivery Systems; D006031:Glycosylation; D006801:Humans; D051379:Mice; D015394:Molecular Structure; D009281:Naphthalenes / Q000494:pharmacology*; D009369:Neoplasms / Q000188:drug therapy*; D008517:Phytotherapy; D010936:Plant Extracts / Q000737:chemistry*; D000081223:Polycyclic Sesquiterpenes; D012717:Sesquiterpenes; D012995:Solubility; D047368:Tumor Burden / Q000187:drug effects; D034401:Ulmaceae / Q000737:chemistry*; D023041:Xenograft Model Antitumor Assays
C492720:7-hydroxy-3-methoxy-cadalene; D000970:Antineoplastic Agents; D009281:Naphthalenes; D010936:Plant Extracts; D000081223:Polycyclic Sesquiterpenes; D012717:Sesquiterpenes