In vitro stability and in vivo anti-inflammatory efficacy of synthetic jasmonates

Hung The Dang, Yoon Mi Lee, Gyeoung Jin Kang, Eun Sook Yoo, Jongki Hong, Sun Mee Lee, Sang Kook Lee, Yuna Pyee, Hwa Jin Chung, Hyung Ryong Moon, Hyung Sik Kim, Jee H. Jung

Research output: Contribution to journalArticlepeer-review

12 Scopus citations

Abstract

A chlorinated methyl jasmonate analog (J7) was elaborated as an in vitro anti-inflammatory lead. However, its in vitro efficacy profile was not reproduced in a subsequent in vivo evaluation, presumably due to its rapid enzymatic hydrolysis in a biological system. In an attempt to improve the metabolic stability of the lead J7 by replacement of its labile methyl ester with reasonable ester groups, several analogs resistant to enzymatic hydrolysis were synthesized. In vivo evaluation of the stability-improved analogs showed that these compounds displayed higher efficacy than the lead J7, suggesting that these new jasmonate analogs may serve as potential anti-inflammatory leads.

Original languageEnglish (US)
Pages (from-to)4109-4116
Number of pages8
JournalBioorganic and Medicinal Chemistry
Volume20
Issue number13
DOIs
StatePublished - Jul 1 2012

Bibliographical note

Funding Information:
This study was financially supported by a Grant from the National Research Foundation of Korea (No. 20090083538 ) and a Grant from the Marine Biotechnology Program funded by Ministry of Land, Transport, and Maritime Affairs, Korea.

Keywords

  • Anti-inflammatory activity
  • Metabolic stability
  • Methyl jasmonate analogs

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