Apoptosis induction in HL-60 cells and inhibition of topoisomerase II by triterpene celastrol
| Autor: | Kouichi Yube, Sin Sugiyama, Masahiro Nagase, Yoshihisa Takaishi, Jinsei Oto, Nobuo Sakato |
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| Rok vydání: | 2003 |
| Předmět: |
Programmed cell death
Time Factors Apoptosis HL-60 Cells DNA Fragmentation Pharmacology Applied Microbiology and Biotechnology Biochemistry Analytical Chemistry chemistry.chemical_compound Inhibitory Concentration 50 Triterpene medicine Humans Topoisomerase II Inhibitors Enzyme Inhibitors Molecular Biology Etoposide chemistry.chemical_classification biology Dose-Response Relationship Drug Molecular Structure Topoisomerase Organic Chemistry General Medicine Flow Cytometry Antineoplastic Agents Phytogenic Triterpenes chemistry Celastrol biology.protein DNA fragmentation Topoisomerase-II Inhibitor Pentacyclic Triterpenes Biotechnology medicine.drug |
| Zdroj: | Bioscience, biotechnology, and biochemistry. 67(9) |
| ISSN: | 0916-8451 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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