Uncovering the anti-inflammatory and anti-angiogenesis activities of sinensetin orally administered to arthritic mice: synthesis, in vivo and in vitro evaluation.

Sinensetin, a prominent flavone from Orthosiphon stamineus is a promising constituent for anti-rheumatoid arthritis. This study evaluated the oral anti-inflammatory and anti-angiogenic efficacy of sinensetin. In carrageenan-induced arthritic mice, oral sinensetin (25-100 mg/kg) significantly reduced paw edema with dose-correlated plasma kinetics, confirming functional oral bioavailability despite a delayed onset compared to intraperitoneal administration. Ex vivo rat aortic ring and in vitro human endothelial assays revealed that sinensetin robustly suppressed microvessel outgrowth and cell migration via VEGF downregulation. These findings demonstrate that sinensetin is an orally bioavailable agent capable of suppressing inflammation and angiogenesis.