Mechanisms in mediating the anti-inflammatory effects of baicalin and baicalein in human leukocytes

作者：Shen YC; Chiou WF; Chou YC; Chen CF^*

来源：European Journal of Pharmacology, 2003, 465(1-2): 171-181.

DOI：10.1016/S0014-2999(03)01378-5

• baicalin
• baicalein
• Ca2+
• NADPH oxidase
• myeloperoxidase
• reactive oxygen intermediate

To evaluate the possible mechanisms responsible for the anti-inflammatory effects of baicalin or baicalein, phorbol-12-myristate-13-acetate (PMA)- or N-formyl-methionyl-leucyl-phenylalanine (fMLP)-activated inflammatory responses of peripheral human leukocytes were studied. Both baicalin and baicalein diminished fMLP- or PMA-induced reactive oxygen intermediates production in neutrophils or monocytes. Neither baicalin nor baicalein prevented the protein kinase C (PKC)-dependent assembly of the NADPH oxidase. Conversely, myeloperoxidase (MPO) activity was inhibited by baicalin or baicalein. fMLP-induced activation of leukocytes, as reflected by increased surface expression of Mac-1 (CD11b/CD18) and Mac-1-dependent neutrophil adhesion, were also inhibited by baicalin or baicalein. Furthermore, baicalein, but not baicalin, impeded fMLP- or AlF4--induced Ca2+ influx. We conclude that impairment of reactive oxygen intermediates production, through scavenging reactive oxygen intermediates by baicalin, or antagonizing ligand-initiated Ca2+ influx by baicalein, accounts for the inhibition of Mac-1-dependent leukocyte adhesion that confers the anti-inflammatory activity of baicalin or baicalein.

• 出版日期2003-3-28