Isolation of a novel substrate-competitive tyrosine kinase inhibitor, desmal, from the plant Desmos chinensis

Hideaki Kakeya, Masaya Imoto, Yuji Tabata, Junko Iwami, Haruhiko Matsumoto, Kazuo Nakamura, Takashi Koyano, Kin ichi Tadano, Kazuo Umezawa

Research output: Contribution to journalArticle

27 Citations (Scopus)

Abstract

In the course of a screening program for tyrosine kinase inhibitors, the chloroform extract of a tropical plant, Desmos chinensis, strongly inhibited the enzyme activity. The active substance was purified by silica gel, gel filtration, and finally crystallized. The structure was elucidated by mass spectrometry and X-ray crystallography to be 8-formyl-2,5,7-trihydroxy-6-methylflavanone, and we named it desmal. Desmal competed with peptide substrate and non-competed with ATP. It inhibited tyrosine kinase in situ in epidermal growth factor (EGF) receptor-overexpressing NIH3T3 (ER 12) cells. It also inhibited EGF-induced inositol phosphate formation and morphological changes.

Original languageEnglish
Pages (from-to)169-172
Number of pages4
JournalFEBS Letters
Volume320
Issue number2
DOIs
Publication statusPublished - 1993 Apr 5

Keywords

  • Desmos chinensis, Desmal
  • Epidermal growth factor
  • Tyrosine kinase

ASJC Scopus subject areas

  • Biophysics
  • Structural Biology
  • Biochemistry
  • Molecular Biology
  • Genetics
  • Cell Biology

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    Kakeya, H., Imoto, M., Tabata, Y., Iwami, J., Matsumoto, H., Nakamura, K., Koyano, T., Tadano, K. I., & Umezawa, K. (1993). Isolation of a novel substrate-competitive tyrosine kinase inhibitor, desmal, from the plant Desmos chinensis. FEBS Letters, 320(2), 169-172. https://doi.org/10.1016/0014-5793(93)80085-9