Abstract:
:Dehydrozingerone analogs and related compounds were screened as potential antitumor promoters by using the in vitro short-term 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced Epstein-Barr virus early antigen activation assay. Among the 40 synthesized compounds, the prenylated analogs 16 and 34-36 showed the most significant and promising activity (100% inhibition of activation at 1 x 10(3) mol ratio/TPA, and 82-80%, 37-35%, and 13-11% inhibition at 5 x 10(2), 1 x 10(2), and 1 x 10 mol ratio/TPA, respectively) in this screening. Their activity profiles were comparable to those of the reference standard curcumin. While a prenyl moiety conferred potent chemopreventive activity, an extended prenyl unit such as a farnesyl moiety did not improve activity. Because in vitro inhibitory effects in this assay generally correlate well with in vivo inhibitory effects on tumor promotion, our results strongly suggested that prenylated 16 and 34-36 are likely to be promising antitumor promoters.
journal_name
J Asian Nat Prod Resjournal_title
Journal of Asian natural products researchauthors
Tatsuzaki J,Nakagawa-Goto K,Tokuda H,Lee KHdoi
10.1080/10286021003591617subject
Has Abstractpub_date
2010-03-01 00:00:00pages
227-32issue
3eissn
1028-6020issn
1477-2213pii
920383936journal_volume
12pub_type
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journal_title:Journal of Asian natural products research
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journal_title:Journal of Asian natural products research
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journal_title:Journal of Asian natural products research
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pub_type: 杂志文章
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journal_title:Journal of Asian natural products research
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journal_title:Journal of Asian natural products research
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journal_title:Journal of Asian natural products research
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journal_title:Journal of Asian natural products research
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journal_title:Journal of Asian natural products research
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journal_title:Journal of Asian natural products research
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journal_title:Journal of Asian natural products research
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journal_title:Journal of Asian natural products research
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journal_title:Journal of Asian natural products research
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journal_title:Journal of Asian natural products research
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journal_title:Journal of Asian natural products research
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abstract::The loss of glutamate transporter-1 (GLT-1) is associated with temporal lobe epilepsy (TLE). A recent study reported that Hsp90β interacted with GLT-1 and recruited it to 20S proteasome for degradation. Therefore, inhibiting Hsp90β may be a new strategy for treating epilepsy. So far, no studies have shown whether the ...
journal_title:Journal of Asian natural products research
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journal_title:Journal of Asian natural products research
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journal_title:Journal of Asian natural products research
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