Planta Med 2001; 67(4): 331-334
DOI: 10.1055/s-2001-14328
Original Paper
Pharmacology
© Georg Thieme Verlag Stuttgart · New York

Effects of Baicalein Isolated from Scutellaria baicalensis Radix on Adhesion Molecule Expression Induced by Thrombin and Thrombin Receptor Agonist Peptide in Cultured Human Umbilical Vein Endothelial Cells

Yoshiyuki Kimura1,*, Nobutoshi Matsushita2 , Kumi Yokoi-Hayashi2 , Hiromichi Okuda1
  • 1 2nd Department of Medical Biochemistry, School of Medicine, Ehime University, Ehime, Japan
  • 2 Pharmacology Laboratory, New Drug Research Department, High Quality-Life Research Laboratories, Bio-Medical Division, Sumitomo Metal Industries, Kyoto, Japan
Further Information

Publication History

May 5, 2000

October 10, 2000

Publication Date:
31 December 2001 (online)

Abstract

We examined the effects of various flavonoids isolated from the roots of Scutellaria baicalensis Georgi on adhesion molecule expression induced by thrombin and thrombin receptor agonist peptide (SFLLRNPNDKYEPF, TRAP) in cultured human umbilical vein endothelial cells. Thrombin and thrombin receptor agonist peptide induced endothelial leukocyte adhesion molecule-1 (ELAM-1) expression. Intercellular adhesion molecule-1 (ICAM-1) expression was also induced by thrombin, but not by TRAP. Baicalein isolated from Scutellariae Radix inhibited ELAM-1 expression induced by thrombin and thrombin receptor agonist peptide dose-dependently, with 50 % inhibitory concentrations (IC50) of 5.53 ± 1.68 μM and 2.44 ± 1.08 μM, respectively. Furthermore, baicalein inhibited thrombin-induced ICAM-1 expression with an IC50 of 9.67 ± 1.28 μM. In addition, baicalein inhibited the expressions of ELAM-1 and ICAM-1 stimulated by protein kinase C (PKC) activator phorbol myristate acetate (PMA).

References

  • 1 Weissmann G. The role of lysosomes in inflammation and disease.  Annu. Rev. Med.. 1967;  18 97-112
  • 2 Brunner T, Heusser C H, Dahinden C A. Human peripheral blood basophils primed by interleukin 3 (IL-3) produce IL-4 in response to immunoglobulin E receptor stimulation.  J. Exp. Med.. 1993;  177 605-11
  • 3 Samuelsson B. Leukotrienes: Mediators of immediate hypersensitivity reactions and inflammation.  Science. 1983;  220 568-75
  • 4 Wegner C D, Gundel R H, Reilly P, Haynes N, Letts L G, Rothlein R. Intercellular adhesion molecule-1 (ICAM-1) in the pathogenesis of asthma.  Science. 1990;  247 456-9
  • 5 Cybulsky M I, Gimbrone Jr M A. Endothelial expression of a mononuclear leukocyte adhesion molecule during atherogenesis.  Science. 1991;  251 788-91
  • 6 Kavanaugh A, Norris S, Rothlein R, Nichols L A, Lipsky P F. Pharmacokinetic analysis of rheoumatoid arthritis patients treated with an anti-CD54 (intercellular adhesion molecule-1 ICAM-1) monoclonal antibody.  Arthritis Rheum. Suppl.. 1992;  35 s106
  • 7 Furie B, Furie B C. The molecular basis of blood coagulation.  Cell. 1988;  53 505-18
  • 8 Kimura Y, Okuda H, Arichi S. Effects of various ginseng saponins on 5-hydroxytryptamine release and aggregation in human platelets.  Pharm. Pharmacol.. 1988;  40 838-43
  • 9 Tahamont M V, Malik A B. Granulocytes mediate the increase in pulmonary vascular permeability after thrombin embolism.  J. Appl. Physiol. Respir. Environ. Exercise. Physiol.. 1983;  54 1489-95
  • 10 Vu T KH, Wheaton V I, Hung D T, Charo I, Coughlin S R. Molecular cloning of a functional thrombin receptor reveals a novel proteolytic mechanism of receptor activation.  Cell. 1991;  64 1057-68
  • 11 Kubo M, Matsuda H, Tani T, Arichi S, Kimura Y, Okuda H. Studies on Scutellariae radix XII. Anti-thrombic actions of various flavonoids from Scutellariae Radix.  Chem. Pharm. Bull.. 1985;  33 2411-5
  • 12 Kimura Y, Okuda H, Arichi S. Effects of baicalein on leukotriene C4 biosynthesis in human lymphocytes.  Phytotherapy Res.. 1987;  1 48-9
  • 13 Kimura Y, Okuda H, Arichi S. Effects of baicalein on leukotriene biosynthesis and degranulation in human polymorphonuclear leukocytes.  Biochim. Biophys. Acta. 1987;  922 278-86
  • 14 Kaplanski G, Fabrigoule M, Boulay V, Dinarello C A, Bongrand P, Kaplanski S, Farnarier C. Thrombin induced endothelial type II activation in vitro. IL-1 and TNF-α independent IL-8 secretion and E-selectin expression.  J. Immunol.. 1997;  158 5435-41
  • 15 Rahman A, Anwar K N, True A L, Malik A B. Thrombin-induced p65 homodimer binding to downstream NF-κB site of the promoter mediates endothelial ICAM-1 expression and neutrophil adhesion.  J. Immunol.. 1999;  162 5466-76
  • 16 Kimura Y, Yokoi K, Matsushita N, Okuda H. Effects of flavonoids isolated from Scutellariae Radix on the production of tissue-type plasminogen activator and plasminogen activator inhibitor-1 induced by thrombin and thrombin receptor agonist peptide in cultured human umbilical vein endothelial cells.  J. Pharm. Pharmacol.. 1997;  49 816-22
  • 17 Kimura Y, Okuda H, Yokoi (Hayashi) K, Matsushita N. Effects of baicalein isolated from roots of Scutellaria baicalensis Georgi on interleukin 1β- and tumor necrosis factor α-induced tissue-type plasminogen activator and plasminogen activator inhibitor-1 production in cultured human umbilical vein endothelial cells.  Phytotherapy Res.. 1997;  11 363-7
  • 18 Rosoff P M, Savage N, Dinarello C A. Interleukin-1 stimulates diacylglycerol production in T lymphocytes by a novel mechanism.  Cell. 1988;  54 73-81
  • 19 Ogita Z, Takada A, Kimura Y. Anti-trypsin actions of various flavonoids isolated from Scutellariae Radix.  J. Trad. Med.. 1995;  12 264-7
  • 20 Kimura Y, Matsushita N, Okuda H. Effects of baicalein isolated from Scutellaria baicalensis on interleukin 1β- and tumor necrosis factor α-induced adhesion molecule expression in cultured human umbilical vein endothelial cells.  J. Ethnopharmacol.. 1997;  57 63-7

Dr. Yoshiyuki Kimura

Second Department of Meical Biochemistry

School of Medicine

Ehime University

Shigenobu-cho

Onsen-gun

Ehime 791-0295

Japan

Email: yokim@m.ehime-u.ac.jp

Fax: +81-89-960-5256

Phone: Tel.: +81-89-960-5254