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.
journal_name
Cancer Lettjournal_title
Cancer lettersauthors
Fukuda K,Akao S,Ohno Y,Yamashita K,Fujiwara Hdoi
10.1016/s0304-3835(00)00704-7keywords:
subject
Has Abstractpub_date
2001-03-10 00:00:00pages
7-13issue
1eissn
0304-3835issn
1872-7980pii
S0304383500007047journal_volume
164pub_type
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