Yakuchinone B Synthesized Through Structural Modification And Enhance The Pharmacological Activity And Therapeutic Potential

Abstract

Yakuchinone B, a phenolic compound isolated from the seeds of Alpinia oxyphylla, exhibits notable anti-inflammatory and anticancer properties. In an effort to enhance its pharmacological activity and therapeutic potential, a series of novel derivatives of Yakuchinone B were synthesized through structural modification. These derivatives were evaluated for their anti-inflammatory activity using in vitro assays, such as inhibition of nitric oxide (NO) production in lipopolysaccharide (LPS)-stimulated macrophages. The synthesized compounds were characterized using various spectroscopic techniques, including NMR, IR, and MS. Structure-activity relationship (SAR) analysis revealed that specific modifications to the phenolic hydroxyl groups and the conjugated aliphatic chain significantly improved anti-inflammatory efficacy. Among the synthesized derivatives, compound X demonstrated the highest activity, with a marked reduction in pro-inflammatory cytokine production (TNF-α, IL-6) and inhibition of NF-κB signaling.