Bioactivity | (±)-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 (IC50 = 1.9 μM) is particularly strong, while the effect on COX-2 (IC50= 9.9 μM) is relatively weak[1].(±)-Aiphanol effectively inhibits VEGFR2 (IC50=0.92 µM). (±)-Aiphanol blocks angiogenesis and promotes apoptosis through inhibition of VEGFR2 and COX2 activity. (±)-Aiphanol is orally active[2]. |
Invitro | (±)-Aiphanol (7.5-30 μM; 6 h) 剂量依赖性的抑制 HUVECs 细胞的 VEGF 诱导的新血管形成。显著降低 HUVECs 细胞的 PGE2 和 VEGF 水平,这一效果在 COX2 沉默后消失。在抑制 HUVECs 细胞的 VEGF 诱导的管状结构形成方面比 Celecoxib (HY-14398) 效果更强[2]。(±)-Aiphanol (7.5-30 μM; 6h) 显著抑制 CAM 的微血管生长,效果与 Bevacizumab (HY-P9906) 相当[2]。(±)-Aiphanol 抑制 VEGFR3/FLT4,VEGFR2/KDR 和 VEGFR1/FLT1 的活性,同时对 PI3K-AKT 和 MAPK 通路中的某些激酶有中等或弱的抑制作用[2]。(±)-Aiphanol (30 μM; 24 h) HUVECs 的增殖受到抑制,并诱导了细胞凋亡[2]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> (±)-Aiphanol 相关抗体: Apoptosis Analysis[2] Cell Line: |
In Vivo | (±)-Aiphanol (30 mg/kg; p.o.; 单剂量) 显著抑制 MC38 同系小鼠模型中的肿瘤生长,肿瘤重量显著减少[2]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
CAS | 578020-29-8 |
Formula | C25H24O8 |
Molar Mass | 452.45 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Kuboki A, et al. Total Synthesis of (.+-.)-Aiphanol, a Novel Cyclooxygenase-inhibitory Stilbenolignan[J]. Chemistry letters, 2003, 32(5): 420-421. [2]. Chen S, et al. Aiphanol, a native compound, suppresses angiogenesis via dual-targeting VEGFR2 and COX2. Signal Transduct Target Ther. 2021 Dec 3;6(1):413. |