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Title of Journal: Int J Pept Res Ther

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Abbravation: International Journal of Peptide Research and Therapeutics

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Springer Netherlands

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DOI

10.1016/0006-8993(92)90710-q

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ISSN

1573-3904

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Comparative αNaphthoflavone and βNaphthoflavone

Authors: Xin Meng Zhigang Wang Lianrong Yang Shujun Xu Yuan Tian Hui Sun
Publish Date: 2016/10/14
Volume: 23, Issue: 3, Pages: 291-295
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Abstract

17βEstradiol E2 is hydrolyzed to 2hydroxyE2 and 4hydroxyE2 4OHE2 via cytochrome P450 CYP 1B1 In estrogen target tissues including the mammary gland ovaries and uterus CYP1B1 is highly expressed and 4OHE2 is predominantly formed in cancerous tissues In the present study we investigated the inhibitory activity of αnaphthoflavone and βnaphthoflavone against CYP1B1 using estrogen E2 as substrate in vitro to reveal structure–activity relationship between structure of flavonoids and inhibition The results showed that αnaphthoflavone and βnaphthoflavone possessed inhibitory activity against CYP1B1mediated E2 and the inhibition of αnaphthoflavone was stronger than βnaphthoflavone By kinetic analyses αnaphthoflavone displayed uncompetitive inhibition while βnaphthoflavone displayed mixed inhibition Taken together the data suggested that the benzo at A ring of flavonoids play a prominent role in CYP1B1 inhibition especially 78benzo is better than 56benzo This study may help to reveal the relationship between the structure of flavonoids and the inhibition CYP1B1 for discovering new drugs in cancer therapy and prevention

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  2. Identification of Bilirubin Binding Site in Type I Collagen
  3. An Efficient Approach for the Total Synthesis of Cyclotides by Microwave Assisted Fmoc-SPPS
  4. Development of Grb2 SH2 Domain Signaling Antagonists: A Potential New Class of Antiproliferative Agents
  5. Simple Branched Arginine-Based Structures can Enhance the Cellular Uptake of Peptide Cargos
  6. The Influences of a Targeting Peptide on the Ovarian Cancer Cell Motility
  7. Rational Improvement of Peptide Affinity to Human Pregnancy-Related Serine Protease HtrA3 PDZ Domain by Introducing a Halogen Bond to the Domain–Peptide Complex Interface
  8. The Protective Effect of a Metallic Selenopeptide with Superoxide Dismutase and Glutathione Peroxidase Activities Against Alcohol Induced Injury in Hepatic L02 Cells
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