Sappanone A

Sappanone A is an orally active homoisoflavone found in sappan L. Sappanone A is a PDE4 and NF-κB inhibitor with anti-inflammatory and antioxidant effect. Sappanone A induces HO-1 expression through activation of Nrf2 pathway. Sappanone A also inhibits RANKL-induced osteoclastogenesis. Sappanone A has great potential in the research of inflammation-related and cardiovascular ^{[1][2][3][4][5]}. In Vitro:Sappanone A (5-30 μM, pretreatment for 1 h, then 24 h) inhibits LPS-induced NO, IL-6 and PGE 2 production in RAW264.7 cells in a concentration-dependent manner (IC₅₀ 6.8, 11.2 and 12.6 μM, respectively) without cytotoxicity^[1].
Sappanone A (5-30 μM, 24 h) exerts anti-inflammatory effects in RAW264.7 cells by inducing HO-1 expression and inhibits LPS-induced NF-κB activation through activation of Nrf2^[2].
Sappanone A (10-40 μM) remarkably inhibits PDE4 enzyme activity and reduces TNF-α production induced by LPS in RAW264.7 macrophages^[2].
Sappanone A (0.007-1.0 mM, 40 min) has excellent ability to reduce Fe³⁺ and complex Fe²⁺, shows excellent antioxidant activity^[2].
Sappanone A (3-30 μM, 7 days) inhibits RANKL-induced osteoclastogenesis in mouse bone marrow-derived macrophage (BMM)^[3].
Sappanone A (0-30 μM, 7 days) inhibits RANKL-induced NFATc1 activation and AKT phosphorylation in BMMs^[3].
Sappanone A (10-30 μM, pretreatment for 1 hour, then treatment for 24 hours) blocks the NF-κB pathway and inhibits the inflammatory response in the HG-induced mesangial cell model^[5].
In Vivo:Sappanone A (20, 50 mg/kg, i.p., one dose) protects mice from death in the LPS-induced mortality in C57BL/6 mice model^[1].
Sappanone A (50, 100 mg/kg, i.p., twice a day for seven consecutive days) significantly reduces LPS-induced mice acute lung injury (ALI) without obvious toxic side effects^[2].
Sappanone A (50 mg/kg, i.p., injects every other day for a total of eight days) inhibits osteoclast formation in vivo in the LPS-induced mouse bone loss model^[3].
Sappanone A (20 mg/kg, i.p., one dose) can reduce myocardial necrosis and apoptosis and promote the recovery of cardiac function in the myocardial ischemia reperfusion injury (MIRI) rat model^[4].
Sappanone A (10-30 mg/kg, i.g., once a day for twelve weeks) reduces renal injury during hyperglycemia in a dose-dependent manner in a Streptozotocin (HY-13753)-induced diabetic mouse model^[5].