2. Academic Validation
  3. Design and synthesis of sorbicillinoid-derived bibenzyl and brominated analogues as anti-inflammatory agents

Design and synthesis of sorbicillinoid-derived bibenzyl and brominated analogues as anti-inflammatory agents

  • Bioorg Med Chem Lett. 2026 Mar 30:137:130645. doi: 10.1016/j.bmcl.2026.130645.
Bei Zhang 1,  Zhipeng Xu 2,  Meng Zhang 1,  Guanyuan Ma 1,  Yiqun Chang 1,  Danmei Tian 3,  Jinshan Tang 4
Affiliations

Affiliations

  • 1 Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy/State Key Laboratory of Bioactive Molecules and Druggability Assessment/International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development of Ministry of Education (MOE) of China, Jinan University, Guangzhou 510632, China.
  • 2 Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy/State Key Laboratory of Bioactive Molecules and Druggability Assessment/International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development of Ministry of Education (MOE) of China, Jinan University, Guangzhou 510632, China; Department of Pharmacy, Central Hospital of Guangdong Provincial Nongken, Zhanjiang 524000, China.
  • 3 Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy/State Key Laboratory of Bioactive Molecules and Druggability Assessment/International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development of Ministry of Education (MOE) of China, Jinan University, Guangzhou 510632, China. Electronic address: danmeitianjnu@163.com.
  • 4 Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy/State Key Laboratory of Bioactive Molecules and Druggability Assessment/International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development of Ministry of Education (MOE) of China, Jinan University, Guangzhou 510632, China. Electronic address: gztangjinshan@126.com.
PMID: 41921825 DOI: 10.1016/j.bmcl.2026.130645
Abstract

Sorbicillinoids, a class of Fungal metabolites, have shown promising anti-inflammatory activity. Considering the importance of the biphenyl pharmacophore in anti-inflammatory agents and the favorable role of halogenation in optimizing drug-like properties, we designed and synthesized a series of novel sorbicillinoid derivatives. This study reports the first preparation of 12 sorbicillinoid-based bibenzyl analogues and two brominated sorbicillinoid analogues. Their anti-inflammatory effects were assessed in lipopolysaccharide (LPS)-stimulated RAW264.7 macrophages by measuring nitric oxide (NO) production and the expression of key inflammation-related proteins. Most analogues inhibited NO release and downregulated the expression of these proteins to varying degrees. Notably, the bibenzyl analogue 1i exhibited dose-dependent suppression of NO production, with potency comparable to the lead compound JNUTS013 (12a). Furthermore, 1i exerted superior activity in suppressing the expression of iNOS, COX-2, and NLRP3, and showed a strong binding affinity with NLRP3 (-6.76 kcal/mol). These findings highlight 1i as a promising anti-inflammatory lead compound and its underlying mechanism may involve the interaction with NLRP3.

Keywords

Anti-inflammatory effects; Bibenzyl analogues; Brominated analogues; NLRP3; NO production; Sorbicillinoid.

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