Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 11, Issue 4, Pages 479-484Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.9b00596
Keywords
Resolvin E2; anti-inflammatory; benzene congener; proresolving lipid mediator; stable equivalent; skipped diene
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Funding
- Japan Society for the Promotion of Science [25860087, 17K08360, 15H02495, 19H0101409]
- Takeda Science Foundation
- Platform Project for Supporting Drug Discovery and Life Science Research (BINDS) from AMED [JP18am0101093]
- Grants-in-Aid for Scientific Research [17K08360, 25860087, 15H02495] Funding Source: KAKEN
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Resolvins (Rvs) are highly potent anti-inflammatory lipid mediators that are chemically and biologically unstable because of their polyunsaturated structures. To address this issue, we designed benzene congeners of RvE2, i.e., o-, m-, and p-BZ-RvE2s, as stable equivalents of RvE2 by replacing the unstable skipped diene moiety with a benzene ring on the basis of computational conformation studies and synthesized these congeners via a short common route through two Stille couplings. o-BZ-RvE2 exhibited more potent anti-inflammatory activity and much higher metabolic stability than RvE2. Thus, o-BZ-RvE2 was identified as a stable equivalent of RvE2, which is useful as a lead for anti-inflammatory drugs with a new mechanism of action as well as a biotool for investigating RvE2-mediated inflammation resolving pathways.
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