| RRC ID |
41341
|
| Author |
Fukuda K, Akao S, Ohno Y, Yamashita K, Fujiwara H.
|
| Title |
Inhibition by costunolide of phorbol ester-induced transcriptional activation of inducible nitric oxide synthase gene in a human monocyte cell line THP-1.
|
| Journal |
Cancer Lett
|
| Abstract |
Costunolide, the predominant sesquiterpene lactone in Saussureae radix, has been reported to exhibit potent chemopreventive effects on carcinogenesis. Effects of costunolide on cellular activation induced by a tumor-promoting phorbol ester 12-O-tetradecanoylphorbol-13-acetate (TPA) were investigated using a reporter gene assay which was designed to reflect the promoter activity of the inducible nitric oxide synthase (iNOS) gene in a human monocyte cell line THP-1. iNOS promoter-dependent reporter gene activity was significantly increased by TPA, and the TPA-induced increase of the reporter gene activity was efficiently reduced by costunolide, with an IC50 of approximately 2 microM. The addition of sulfhydryl (SH) compounds effectively abrogated the inhibitory effects of costunolide, suggesting the involvement of its reactivity with SH groups of target proteins and/or thiol-depleting property. The present findings may further explain the cancer-preventive property of costunolide.
|
| Volume |
164(1)
|
| Pages |
7-13
|
| Published |
2001-3-10
|
| DOI |
10.1016/s0304-3835(00)00704-7
|
| PII |
S0304383500007047
|
| PMID |
11166910
|
| MeSH |
Anticarcinogenic Agents / pharmacology
Ascorbic Acid / pharmacology
Cell Line
Cell Survival / drug effects
Dose-Response Relationship, Drug
Enzyme Activation
Gallic Acid / analogs & derivatives
Gallic Acid / pharmacology
Genes, Reporter
Humans
Inhibitory Concentration 50
Luciferases / metabolism
Monocytes / metabolism*
Nitric Oxide Synthase / genetics
Nitric Oxide Synthase / metabolism*
Nitric Oxide Synthase Type II
Phorbol Esters / metabolism*
Promoter Regions, Genetic
Protein Kinase C / metabolism
Sesquiterpenes / pharmacology*
Sulfhydryl Compounds / metabolism
Tetradecanoylphorbol Acetate / metabolism
Transcriptional Activation
Vitamin E / pharmacology
|
| IF |
7.36
|
| Times Cited |
27
|
|
WOS Category
|
ONCOLOGY
|
| Resource |
| Human and Animal Cells |
THP-1(RCB1189) |
