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Molecules 2011, 16(6), 5159-5167; doi:10.3390/molecules16065159

Inhibitory Activity of Flavonoids against Class I Phosphatidylinositol 3-Kinase Isoforms

1,2,* , 1, 2, 1,*  and 1
1 School of Pharmaceutical Sciences and Research Center of Basic Medical Sciences, Tianjin Medical University, Tianjin 300070, China 2 Division of Molecular Pharmacology, Cancer Chemotherapy Center, Japanese Foundation for Cancer Research, 3-10-6, Ariake, Koto-ku, Tokyo 135-8550, Japan
* Authors to whom correspondence should be addressed.
Received: 3 June 2011 / Revised: 16 June 2011 / Accepted: 17 June 2011 / Published: 21 June 2011
(This article belongs to the Section Natural Products)
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Class I PI3 Kinase (PI3K) phosphorylates phosphatidylinositol 4,5-bisphophate (PIP2) to generate the second messenger phosphatidylinositol 3,4,5-trisphosphate (PIP3) and therefore plays an important role in fundamental cellular responses such as proliferation. There are four isoforms of class I PI3K which are known to have different functions and relate to various diseases such as cancer and inflammation. Flavonoids are abundant in fruits, vegetables and plant-derived beverages such as tea. So far, various pharmacological effects of flavonoids have been reported. We previously reported that the flavonoid baicalein exhibits potent PI3K-inhibitory activity. Recently we examined the inhibitory activity of eighteen flavonoids against PI3Ka by using an in vitro homogenous time resolved fluorescence (HTRF) kinase assay, and deduced their structure-activity relationships by comparing the activities of the analogues. Our result suggests that the number of hydroxyl groups in the A and B rings might promote the activity, while loss of C2-C3 double bond might reduce the activity. Furthermore, the activity against 4 class I PI3K isoforms of some selected flavonoids was investigated, and the results indicate that the flavonoids seem to exhibit more potent activity on PI3Ka and d isoforms compared with that on PI3Kb and g isoforms.
Keywords: phosphatidylinositol 3-kinase; flavonoid; structure-activity relationship phosphatidylinositol 3-kinase; flavonoid; structure-activity relationship
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Kong, D.; Zhang, Y.; Yamori, T.; Duan, H.; Jin, M. Inhibitory Activity of Flavonoids against Class I Phosphatidylinositol 3-Kinase Isoforms. Molecules 2011, 16, 5159-5167.

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