Planta Med 2001; 67(2): 132-135
DOI: 10.1055/s-2001-11532
Original Paper
Georg Thieme Verlag Stuttgart · New York

Inhibitory Effect of Baicalein, a Flavonoid in Scutellaria Root, on Eotaxin Production by Human Dermal Fibroblasts

Toshiharu Nakajima1 , Masako Imanishi1 , Kazuhiko Yamamoto2 , Jong-Chol Cyong1 , Koichi Hirai1,*
  • 1 Department of Bioregulatory Function, University of Tokyo Graduate School of Medicine, Tokyo, Japan
  • 2 Department of Allergy and Rheumatology, University of Tokyo Graduate School of Medicine, Tokyo, Japan
Further Information

Publication History

Publication Date:
31 December 2001 (online)

Abstract

Eotaxin is an eosinophil-specific chemokine associated with the recruitment of eosinophils to sites of allergic inflammation. „Saiboku-to” (Formula magnoliae et bupleuri) is a kampo herbal medicine used for the treatment of bronchial asthma in Japan. In this study, we investigated the effects of Scutellaria Root, a major herb in Saiboku-to and its components such as baicalein and baicalin on eotaxin production by IL-4 plus TNF-α-stimulated human fibroblasts. An extract of Scutellaria Root markedly inhibited eotaxin production. Four major flavonoids from Scutellaria Root were found to show inhibitory activity on eotaxin production at a concentration of 10 μg/ml in the order of baicalein > oroxylin A > baicalin > skullcapflavon II. The inhibitory effect of baicalein was expressed in a dose-dependent manner, and almost 50 % inhibition was observed at 1.8 μg/ml. Furthermore, baicalein prevented human eotaxin mRNA expression in IL-4 plus TNF-α-stimulated human fibroblasts. These results help explain the pharmacological efficacy of Scutellaria Root in the treatment of bronchial asthma since it would suppress eotaxin associated recruitment of eosinophils.

References

  • 1 Wardlaw  A J,, Moqbel  R,, Kay  A B.. Eosinophils: biology and role in disease.  Adv. Immunol.. 1995;;  60 151-266
  • 2 Hirai  K,, Miyamasu  M,, Takaishi  T,, Morita  Y.. Regulation of the function of eosinophils and basophils.  Crit. Rev. Immunol.. 1997;;  17 325-52
  • 3 Griffiths-Johnson  D A,, Collins  P D,, Rossi  A G,, Jose  P J,, Williams  T J.. The chemokine, eotaxin, activates guinea-pig eosinophils in vitro and causes their accumulation into the lung in vivo.  Biochem. Bioph. Res. Commun.. 1993;;  197 1167-72
  • 4 Kitaura  M,, Nakajima  T,, Imai  T,, Harada  S,, Combadiere  C,, Tiffany  H L,, Murphy  P M,, Yoshie  O.. Molecular cloning of human eotaxin, an eosinophil-selective CC chemokine, and identification of a specific eosinophil eotaxin receptor, CC chemokine receptor 3.  J. Biol. Chem.. 1996;;  271 7725-30
  • 5 Yamada  H,, Hirai  K,, Miyamasu  M,, Iikura  M,, Misaki  Y,, Shoji  S,, Takaishi  T,, Kasahara  T,, Morita  Y,, Ito  K.. Eotaxin is a potent chemotaxin for human basophils.  Biochem. Biophy. Res. Commun.. 1997;;  231 365-8
  • 6 Mochizuki  M,, Bartels  J,, Mallet  A I,, Christophers  E,, Schroder  J M.. IL-4 induces eotaxin: a possible mechanism of selective eosinophil recruitment in helminth infection and atopy.  J. Immunol.. 1998;;  160 60-8
  • 7 Miyamasu  M,, Nakajima  T,, Misaki  Y,, Izumi  S,, Tsuno  N,, Kasahara  T,, Yamamoto  K,, Morita  Y,, Hirai  K.. Dermal fibroblasts represent a potent major source of human eotaxin: In vitro production and cytokine-mediated regulation.  Cytokine. 1999;;  11 751-8
  • 8 Fukagawa  K,, Nakajima  T,, Tsubota  K,, Shimmura  S,, Saito  H,, Hirai  K.. Presence of eotaxin in tears of patients with atopic keratoconjunctivitis with severe corneal damage.  J. Allergy Clin. Immunol.. 1999;;  103 1220-1
  • 9 Iikura  Y,, Saito  H,, Umesato  Y,, Shichijo  K,, Ebisawa  M,, Nagakura  T.. Bronchial asthma and traditional Japanese herbal medicine: In vitro and in vivo studies.  J. Med. Pharm. Soc. Wakan. Yaku.. 1989;;  6 220-3
  • 10 Koda  A.. Inhibition of hypersensitivity reactions by Saiboku-to (TJ-96), particularly on type IV reaction.  Ann. N. Y. Acad. Sci.. 1993;;  685 543-8
  • 11 Kubo  M,, Kimura  Y,, Odani  T,, Tani  T,, Namba  K.. Studies on Scutellariae radix. Part II: The antibacterial substance.  Planta Medica. 1981;;  43 194-201
  • 12 Kitamura  K,, Honda  M,, Yoshizaki  H,, Yamamoto  S,, Nakane  H,, Fukushima  M,, Ono  K,, Tokunaga  T.. Baicalin, an inhibitor of HIV-1 production in vitro.  Antiviral Res.. 1998;;  37 131-40
  • 13 Nakajima  T,, Yamada  H,, Iikura  M,, Miyamasu  M,, Izumi  S,, Shida  H,, Ohta  K,, Imai  T,, Yoshie  O,, Mochizuki  M,, Schroder  J M,, Morita  Y,, Yamamoto  K,, Hirai  K.. Intracellular localization and release of eotaxin from normal eosinophils.  FEBS Lett.. 1998;;  434 226-30
  • 14 Lilly  C M,, Nakamura  H,, Kesselman  H,, Nagler-Anderson  C,, Asano  K,, Garcia-Zepeda  E A,, Rothenberg  M E,, Drazen  J M,, Luster  A D.. Expression of eotaxin by human lung epithelial cells: induction by cytokines and inhibition by glucocorticoids.  J. Clin. Invest.. 1997;;  99 1767-73
  • 15 The Japanese Pharmacopeia XIII:. Scutellaria Root. 896-7. Ed. Ministry of Health and Welfare 1996
  • 16 Miura  Y H,, Tomita  I,, Watanabe  T,, Hirayama  T,, Fukui  S.. Active oxygens generation by flavonoids.  Biol. Pharm. Bull.. 1998;;  21 93-6
  • 17 Yoshino  M,, Murakami  K.. Interaction of iron with polyphenolic compounds: application to antioxidant characterization.  Anal. Biochem.. 1998;;  257 40-4
  • 18 Gao  D,, Tawa  R,, Masaki  H,, Okano  Y,, Sakurai  H.. Protective effects of baicalein against cell damage by reactive oxygen species.  Chem. Pharm. Bull.. 1998;;  46 1383-7
  • 19 Sekiya  K,, Okuda  H.. Selective inhibition of platelet lipoxygenase by baicalein.  Biochem. Biophys. Res. Commun.. 1982;;  105 1090-5
  • 20 Kakegawa  H,, Matsumoto  H,, Satoh  T.. Inhibitory effects of some natural products on the activation of hyaluronidase.  Chem. Pharm. Bull.. 1992;;  40 1439-42

Dr. Koichi Hirai

Department of Bioregulatory Function

University of Tokyo

Graduate School of Medicine

7-3-1 Hongo, Bunkyo-ku

Tokyo 113-8655

Japan

Email: hiraiko-tky@umin.ac.jp

Phone: (Japan: +81) 3-3818-4754

    >