Structure-activity relationships of ganoderma acids from Ganoderma lucidum as aldose reductase inhibitors

Sri Fatmawati, Kuniyoshi Shimizu, Ryuichiro Kondo

研究成果: Contribution to journalArticle査読

27 被引用数 (Scopus)

抄録

A series of lanostane-type triterpenoids, known as ganoderma acids were isolated from the fruiting body of Ganoderma lucidum. Some of these compounds were identified as active inhibitors of the in vitro human recombinant aldose reductase. To clarify the structural requirement for inhibition, some structure-activity relationships were determined. Our structure-activity studies of ganoderma acids revealed that the OH substituent at C-11 is an important feature and the carboxylic group in the side chain is essential for the recognition of aldose reductase inhibitory activity. Moreover, double bond moiety at C-20 and C-22 in the side chain contributes to improving aldose reductase inhibitory activity. In the case of ganoderic acid C2, all of OH substituent at C-3, C-7 and C-15 is important for potent aldose reductase inhibition. These results provide an approach to understanding the structural requirements of ganoderma acids from G. lucidum for aldose reductase inhibitor. This understanding is necessary to design a new-type of aldose reductase inhibitor.

本文言語英語
ページ(範囲)7295-7297
ページ数3
ジャーナルBioorganic and Medicinal Chemistry Letters
21
24
DOI
出版ステータス出版済み - 12 15 2011

All Science Journal Classification (ASJC) codes

  • 生化学
  • 分子医療
  • 分子生物学
  • 薬科学
  • 創薬
  • 臨床生化学
  • 有機化学

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