Planta Med 2003; 69(7): 673-675
DOI: 10.1055/s-2003-41110
Letter
© Georg Thieme Verlag Stuttgart · New York

In vitro TGF-β1 Antagonistic Activity of Ursolic and Oleanolic Acids Isolated from Clerodendranthus spicatus

Hiromitsu Yoshimura1 , Koko Sugawara1 , Masako Saito1 , Shiuji Saito1 , Shigeru Murakami1 , Noriyuki Miyata1 , Akira Kawashima1 , Shigeo Morimoto1 , Nannan Gao2 , Xingguo Zhang2 , Junshan Yang2
  • 1Medicinal Research Laboratories, Taisho Pharmaceutical Co., Ltd., Saitama, Japan
  • 2Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, P. R. China
Further Information

Publication History

Received: October 16, 2002

Accepted: March 23, 2003

Publication Date:
04 August 2003 (online)

Abstract

The mechanism of action of the aerial parts of Clerodendranthus spicatus (Thunb.) C.Y. Wu, [syn. Orthosiphon aristatus (Blume) Miq,] a medicinal plant used in China to treat human renal disease, was investigated. The aqueous and methanol crude extracts exhibited dose-dependent inhibitory activity on 125I-TGF-β1 binding to its receptor in Balb/c 3T3 cells. Subsequent bioassay-guided fractionation led to identification of two known triterpenoidal constituents, ursolic and oleanolic acids. Ursolic and oleanolic acids inhibited the binding of 125I-TGF-β1 to its receptor with IC50 values of 6.9 ± 0.8 and 21.0 ± 2.3 μM, respectively. The results suggest that TGF-β1 antagonistic activity is responsible, at least in part, for the therapeutic efficacy of this plant to treat humans with renal disease.

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Dr. H. Yoshimura

Molecular Biology Laboratory

Medicinal Research Laboratories

Taisho Pharmaceutical Co., Ltd

Saitama-Shi

Saitama 330-8530

Japan

Fax: +81-48-652-7254

Email: hi.yoshimura@po.rd.taisho. co.jp

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