Impacts of baicalein analogs with modification of the 6th position of A ring on the activity toward NF-kappaB-, AP-1-, or CREB-mediated transcription.

Bioorganic & Medicinal Chemistry Letters
Sheng-Teng HuangYung-Chi Cheng

Abstract

The water extract of Scutellariae baicalensis Georgi (S. baicalensis) has potential anti-tumor and anti-inflammatory activities. A major flavonoid isolated from S. baicalensis, baicalein, was also found to have anti-tumor and anti-inflammatory activities. These biological activities could be due to their antioxidant action and/or effect on different signal transduction pathways. We investigated the effects of several baicalein analogs with a substitution of hydrogen of the hydroxyl group at the 6th position of A ring on three signal pathway mediated transcription (NF-kappaB, AP-1, and CREB) associated with inflammation and cancer growth. We found that the analogs with O-alkyl group of the different carbon chain length or O-benzyl activated NF-kappaB transcription without TNFalpha stimulation. Some of the analogs increased TNFalpha stimulated NF-kappaB transcription by two- to threefold. None of the analogs studied has major effect on AP-1 signal transduction with or without TPA stimulation. All of the analogs increased CREB transcription with forskolin stimulation up to twofold. However, they did not have a potent effect (less or about twofold activation) on intrinsic CREB signal transduction. The modification of baicalein at t...Continue Reading

References

Oct 16, 2004·Journal of Medicinal Chemistry·Yashang LeeYung-chi Cheng
Feb 22, 2005·The Journal of Pharmacy and Pharmacology·Wen-Hsin HuangTz-Chong Chou
Oct 13, 2006·Bioscience, Biotechnology, and Biochemistry·Wen-Hsin HuangChing-Huey Yang
May 29, 2007·Bioorganic & Medicinal Chemistry Letters·Wenli GaoYung-Chi Cheng
Dec 14, 2007·Bioorganic & Medicinal Chemistry Letters·Wenli GaoYung-Chi Cheng
May 27, 2008·The Journal of Steroid Biochemistry and Molecular Biology·Olivier HennebertRobert Morfin

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Aug 7, 2021·Saudi Journal of Biological Sciences·Dong WangSeyyed Shamsadin Athari

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