(±)-Aiphanol is a newly discovered stilbenolignan analog. (±)-Aiphanol exhibits significant anti-inflammatory activity, acting through inhibition of COX-1 and COX-2. The inhibitory effect on COX-1 (IC 50 = 1.9 μM) is particularly strong, while the effect on COX-2 (IC 50 = 9.9 μM) is relatively weak.(±)-Aiphanol effectively inhibits VEGFR2 ( IC 50 =0.92 µM). (±)-Aiphanol blocks angiogenesis and promotes apoptosis through inhibition of VEGFR2 and COX2 activity. (±)-Aiphanol is orally active.