RRC ID 41987
Author Nagase M, Oto J, Sugiyama S, Yube K, Takaishi Y, Sakato N.
Title Apoptosis induction in HL-60 cells and inhibition of topoisomerase II by triterpene celastrol.
Journal Biosci Biotechnol Biochem
Abstract Celastrol, which is a triterpene purified from Celastraceae plants, has anticancer and anti-inflammatory activities. In this study we investigated to clarify whether celastrol can induce apoptosis in a human leukemia HL-60 model system. Celastrol was found to induce apoptosis, and the rank order of the potency of celastrol and its derivatives to induce internucleosomal DNA fragmentation was found to be celastrol>cela-H>the other derivatives=vehicle control. Many anticancer agents are known to possess the ability to inhibit topoisomerase II, so the inhibitory activities of celastrol and its derivatives on topoisomerase II were also explored. The rank order of the inhibitory activity was found to be celastrol>etoposide>cela-H, indicating that the apoptosis-inducing activities of cela derivatives correspond to their inhibitory activities on topoisomerase II. These data suggested that celastrol may cause its effects such as anticancer activity by the mechanism of apoptosis along with topoisomerase II inhibition.
Volume 67(9)
Pages 1883-7
Published 2003-9-1
DOI 10.1271/bbb.67.1883
PMID 14519971
MeSH Antineoplastic Agents, Phytogenic / pharmacology Apoptosis / drug effects* DNA Fragmentation / drug effects Dose-Response Relationship, Drug Enzyme Inhibitors / chemistry Enzyme Inhibitors / pharmacology* Etoposide / pharmacology Flow Cytometry HL-60 Cells Humans Inhibitory Concentration 50 Molecular Structure Time Factors Topoisomerase II Inhibitors* Triterpenes / chemistry Triterpenes / pharmacology*
IF 1.297
Times Cited 89
WOS Category FOOD SCIENCE & TECHNOLOGY CHEMISTRY, APPLIED BIOTECHNOLOGY & APPLIED MICROBIOLOGY BIOCHEMISTRY & MOLECULAR BIOLOGY
Resource
Human and Animal Cells