Suppression of Cyclooxygenase-2 Gene Transcription by Humulon

  • Kei Yamamoto
  • Jining Wang
  • Shozo Yamamoto
  • Hiroyasu Tobe
Part of the Advances in Experimental Medicine and Biology book series (AEMB, volume 507)


Cyclooxygenase is the key enzyme in the biosynthetic pathway of prostaglandins (PGs) and thromboxane from arachidonic acid. There are two isozymes of cyclooxygenase; constitutive cyclooxygenase-1 and inducible cyclooxygenase-2.1’2MC3T3-E1 cell cloned from newborn mouse calvaria is an osteogenic cell line which differentiates into an osteoblast.34Our extensive studies demonstrated the production of PGE2as a major arachidonate metabolite in this cell linesand the induction of cyclooxygenase by various bioregulators including tumor necrosis factor a (TNFa).5-9Later the induced enzyme in MC3T3-E1 cells was identified as cyclooxygenase-2.8-10Previously humulon ((R)-3,5,6-trihydroxy-4,6-bis(3-methyl-2-butenyl)-2-(3-methyl-1oxobutyl)-2,4-cyclohexadien-1-one) (Fig. IA) isolated from hop (Humulus lupulus L.) extract was found as an inhibitor of bone resorption with an IC50of 5.9 nM.“ We noted this activity of humulon, and were interested in a possible inhibitory or suppressive effect of humulon on cyclooxygenase-2 leading to a decreased production of PGE2which is well known as a bone resorption factor.12


Luciferase Activity Glucocorticoid Receptor Sodium Salicylate Thymidine Kinase Gene Glucocorticoid Response Element 
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© Springer Science+Business Media New York 2002

Authors and Affiliations

  • Kei Yamamoto
    • 1
  • Jining Wang
    • 1
  • Shozo Yamamoto
    • 1
  • Hiroyasu Tobe
    • 2
  1. 1.Department of BiochemistryThe University of Tokushima, School of MedicineTokushimaJapan
  2. 2.Kochi National College of TechnologyKochiJapan

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