NO-donating Bergenin derivatives with enhanced anti-inflammatory activity

  • Bioorg Med Chem Lett. 2026 Jun 4:139:130705. doi: 10.1016/j.bmcl.2026.130705.
Enshang Yuan  1 ,  Qi Deng  2 ,  Na Li  1 ,  Li Chen  3
Affiliations
  • 1. State Key Laboratory of Natural Medicines, Department of Natural Medicinal Chemistry, School of Traditional Chinese Pharmacy, China Pharmaceutical University, 639 Longmian Avenue, Nanjing 211198, China.
  • 2. State Key Laboratory of Natural Medicines, Department of Natural Medicinal Chemistry, School of Traditional Chinese Pharmacy, China Pharmaceutical University, 639 Longmian Avenue, Nanjing 211198, China; The First People's Hospital of Jiande, Hangzhou, Zhejiang 311600, China.
  • 3. State Key Laboratory of Natural Medicines, Department of Natural Medicinal Chemistry, School of Traditional Chinese Pharmacy, China Pharmaceutical University, 639 Longmian Avenue, Nanjing 211198, China. Electronic address: [email protected].
PMID: 42248368 DOI: 10.1016/j.bmcl.2026.130705
Abstract

Ten new nitric oxide (NO)-donating Bergenin derivatives were designed, synthesized, and evaluated for their anti-inflammatory activity. Distinguished by its superior safety profile, a single furoxan moiety conjugated hybrid I8 was selected for mechanistic studies. The results revealed that the anti-inflammatory effects of I8 is probably related to the negative feedback inhibition of iNOS expression by promoting NO release, as well as the inhibition of the pro-inflammatory cytokines (TNF-α, IL-6) levels. These findings provide direct evidence supporting the hypothesis that BG-NO hybrids exert enhanced anti-inflammatory effects via NO signaling, identifying I8 as a promising lead compound for further development.

Keywords
Anti-inflammatory; Bergenin; Nitric oxide donor; Structural modification.
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