| 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
Pentacyclic Triterpenes
Time Factors
Topoisomerase II Inhibitors*
Triterpenes / chemistry
Triterpenes / pharmacology*
|
| IF |
1.516
|
| Times Cited |
89
|
|
WOS Category
|
FOOD SCIENCE & TECHNOLOGY
CHEMISTRY, APPLIED
BIOTECHNOLOGY & APPLIED MICROBIOLOGY
BIOCHEMISTRY & MOLECULAR BIOLOGY
|
| Resource |
| Human and Animal Cells |
HL60(RCB0041) |
