Regulatory effects of deoxycholic acid, a component of the anti-inflammatory traditional Chinese medicine Niuhuang, on human leukocyte response to chemoattractants

Biochem Pharmacol. 2002 Feb 1;63(3):533-41. doi: 10.1016/s0006-2952(01)00917-0.


Niuhuang is a commonly used Chinese traditional medicine with immunoregulatory and anti-inflammatory properties. Deoxycholic acid (DCA) is a major active constituent of Niuhuang. The reaction of human leukocytes to chemoattractants is an important part of the host immune response and also plays a crucial role in the development of inflammation. We, therefore, investigated the in vitro effects of DCA on human monocyte and neutrophil responses to classic chemoattractants [fMet-Leu-Phe (fMLP), complement fraction 5a (C5a)], CC chemokine [monocyte chemoattractant protein-1 (MCP-1/CCL2)], and/or CXC chemokines [stromal cell-derived factor-1 (SDF-1alpha/CXCL12), interleukin-8 (IL-8/CXCL8)]. The results showed that DCA significantly inhibited fMLP-induced monocyte and neutrophil chemotaxis and calcium mobilization, and also blocked the binding of [3H]fMLP and anti-formyl peptide receptor (FPR) monoclonal antibodies (mAb) to the cells. The inhibitory effects of DCA on calcium mobilization and anti-FPR-mAb binding to the receptor could be abrogated by washing DCA out of the cell suspension, suggesting that DCA blocked fMLP receptors via a steric hindrance mechanism, not via receptor internalization. DCA had no significant inhibitory effects on MCP-1-, SDF-1alpha-, or C5a-induced monocyte function, or C5a- or IL-8-induced neutrophil function. Taken together, our experimental results suggest that blockade of fMLP receptors may contribute to the anti-inflammatory effects of traditional medicine containing DCA.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Anti-Inflammatory Agents / pharmacology*
  • Antibodies / immunology
  • Calcium / metabolism
  • Cell Movement / drug effects*
  • Cell Respiration / drug effects
  • Chemokines / pharmacology
  • Chemotactic Factors / pharmacology
  • Deoxycholic Acid / pharmacology*
  • Drug Interactions
  • Humans
  • In Vitro Techniques
  • Interleukin-8 / metabolism
  • Leukocytes / drug effects*
  • Leukocytes / physiology
  • Medicine, Chinese Traditional
  • N-Formylmethionine Leucyl-Phenylalanine / metabolism
  • Receptors, Formyl Peptide
  • Receptors, Immunologic / immunology
  • Receptors, Immunologic / metabolism
  • Receptors, Interleukin-8A / immunology
  • Receptors, Interleukin-8A / metabolism
  • Receptors, Interleukin-8B / immunology
  • Receptors, Interleukin-8B / metabolism
  • Receptors, Peptide / immunology
  • Receptors, Peptide / metabolism
  • Tritium


  • Anti-Inflammatory Agents
  • Antibodies
  • Chemokines
  • Chemotactic Factors
  • Interleukin-8
  • Receptors, Formyl Peptide
  • Receptors, Immunologic
  • Receptors, Interleukin-8A
  • Receptors, Interleukin-8B
  • Receptors, Peptide
  • Deoxycholic Acid
  • Tritium
  • N-Formylmethionine Leucyl-Phenylalanine
  • Calcium