Inhibition of oncogene product enzyme activity as an approach to cancer chemoprevention. Tyrosine-specific protein kinase inhibition by daphnoretin from Thymelaea hirsuta root

Inhibitors of oncogene product enzyme activity were sought as a prescreen for potential cancer chemopreventive agents. Daphnoretin, a dicoumaryl ether from Thymelaea hirsuta root, inhibited the erb‐b oncogene product, the tyrosine‐specific protein kinase of human epidermal growth factor receptor (IC...

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Bibliographic Details
Published in:Phytotherapy research 1998-06, Vol.12 (4), p.282-284
Main Authors: Abou-Karam, Mohamed, El-Shaer, Nagwa S., Shier, W. Thomas
Format: Article
Language:English
Subjects:
Biological and medical sciences
cultured mammalian cells
cytotoxicity
daphnoretin
General pharmacology
Medical sciences
Pharmacognosy. Homeopathy. Health food
Pharmacology. Drug treatments
Thymelaea hirsuta (L.) Endl
Thymelaeaceae
tyrosine kinase inhibition
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Summary:Inhibitors of oncogene product enzyme activity were sought as a prescreen for potential cancer chemopreventive agents. Daphnoretin, a dicoumaryl ether from Thymelaea hirsuta root, inhibited the erb‐b oncogene product, the tyrosine‐specific protein kinase of human epidermal growth factor receptor (IC50 = 97.5 μM). Daphnoretin was moderately cytotoxic (IC50 = 21–114 μM) only in rapidly proliferating cultured mammalian cells. © 1998 John Wiley & Sons, Ltd.
ISSN:0951-418X
1099-1573
DOI:10.1002/(SICI)1099-1573(199806)12:4<282::AID-PTR225>3.0.CO;2-X