Flavonoids as inhibitors of human CD38

Bioorg Med Chem Lett. 2011 Jul 1;21(13):3939-42. doi: 10.1016/j.bmcl.2011.05.022. Epub 2011 May 14.


CD38 is a multifunctional enzyme which is ubiquitously distributed in mammalian tissues. It is involved in the conversion of NAD(P)(+) into cyclic ADP-ribose, NAADP(+) and ADP-ribose and the role of these metabolites in multiple Ca(2+) signaling pathways makes CD38 a novel potential pharmacological target. The dire paucity of CD38 inhibitors, however, renders the search for new molecular tools highly desirable. We report that human CD38 is inhibited at low micromolar concentrations by flavonoids such as luteolinidin, kuromanin and luteolin (IC(50) <10 μM). Docking studies provide some clues on the mode of interaction of these molecules with the active site of CD38.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • ADP-ribosyl Cyclase 1 / antagonists & inhibitors*
  • Anthocyanins / chemistry
  • Anthocyanins / pharmacology
  • Catalytic Domain
  • Enzyme Activation / drug effects
  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / pharmacology
  • Flavonoids / chemistry
  • Flavonoids / pharmacology*
  • Humans
  • Inhibitory Concentration 50
  • Models, Molecular
  • Molecular Structure


  • Anthocyanins
  • Enzyme Inhibitors
  • Flavonoids
  • ADP-ribosyl Cyclase 1
  • luteolinidin