Novel inhibitors of poly(ADP-ribose) glycohydrolase

Kazuma Aoki, Koji Nishimura, Hideaki Abe, Hideharu Maruta, Hiroshi Sakagami, Tsutomu Hatano, Takuo Okuda, Takashi Yoshida, Yan Jyu Tsai, Fumiaki Uchiumi, Sei ichi Tanuma

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Abstract

The inhibitory effects on poly(ADP-ribose) glycohydrolase purified from human placenta of three classes of chemically defined tannins; gallotannins; ellagitannins and condensed tannins, were examined in vitro. Oligometric ellagitannins were found to be most potent inhibitors of poly(ADP-ribose) glycohydrolase, their potencies increasing with increasing number of monomeric residues (dinner < trimer < tetramer). Monomeric ellagitannins and gallotannins were less inhibitory. Condensed tannins, which consist of an epicatechin gallate oligomer without a glucose core, were not appreciably inhibitory. A structure-activity study showed that higher-order confirmations of the conjugates with glucose of hexahydroxydiphenoyl and valoneoyl groups, which are unique components of ellegitannins, cooperatively potentiated the inhibitory activity.

Original languageEnglish
Pages (from-to)251-256
Number of pages6
JournalBBA - General Subjects
Volume1158
Issue number3
DOIs
Publication statusPublished - Nov 28 1993

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Keywords

  • Ellagitannin
  • Enzyme inhibition
  • Poly(ADP-ribose) glycohydrolase
  • Poly(ADP-ribosyl)ation
  • Structure-activity relationship
  • Tannin

ASJC Scopus subject areas

  • Biophysics
  • Biochemistry
  • Molecular Biology

Cite this

Aoki, K., Nishimura, K., Abe, H., Maruta, H., Sakagami, H., Hatano, T., Okuda, T., Yoshida, T., Tsai, Y. J., Uchiumi, F., & Tanuma, S. I. (1993). Novel inhibitors of poly(ADP-ribose) glycohydrolase. BBA - General Subjects, 1158(3), 251-256. https://doi.org/10.1016/0304-4165(93)90022-Z