Skip to main content
Open Access Publications from the University of California

Baicalein is a potent in vitro inhibitor against both reticulocyte 15-human and platelet 12-human lipoxygenases

  • Author(s): Deschamps, J D
  • Kenyon, V A
  • Holman, Ted R
  • et al.

Lipoxygenases (LO) have been implicated in asthma, immune disorders, and various cancers and as a consequence, there is great interest in isolating selective LO isozyme inhibitors. Currently, there is much use of baicalein as a selective human platelet 12-LO (12-hLO) inhibitor, however, our current steady-state inhibition data indicate that baicalein is not selective against 12-hLO versus human reticulocyte 15-LO-1 (15-hLO-1) (15/12 = 1.3), in vitro. However, in the presence of detergents baicalein is slightly more selective (15/12 = 7) as seen by the steady-state inhibition kinetics, which may imply greater selectivity in a cell-based assay but has yet to be proven. The mechanism of baicalein inhibition of 15-hLO-1 is reductive, which molecular modeling suggests is through direct binding of the catecholic moiety of baicalein to the iron. A structurally related flavonoid, apigenin, is not reductive, however, molecular modeling suggests a hydrogen bond with Thr591 may account for its inhibitor potency.

Many UC-authored scholarly publications are freely available on this site because of the UC Academic Senate's Open Access Policy. Let us know how this access is important for you.

Main Content
Current View