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

Research output: Contribution to journalArticle

47 Citations (Scopus)

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
JournalBiochimica et Biophysica Acta - General Subjects
Volume1158
Issue number3
DOIs
Publication statusPublished - Nov 28 1993

Keywords

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

ASJC Scopus subject areas

  • Biochemistry
  • Biophysics
  • Molecular Biology

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