| Bioactivity | Anti-inflammatory agent 35 (compound 5a27) is an orally active curcumin analogue with anti-inflammatory activity. Anti-inflammatory agent 35 blocks mitogen-activated protein kinase (MAPK) signaling and p65 nuclear translocation of NF-kB. Anti-inflammatory agent 35 also inhibits yellow neutrophil infiltration and pro-inflammatory cytokine production. Anti-inflammatory agent 35 significantly attenuates lipopolysaccharide (LPS)-induced acute lung injury (ALI) in vivo[1]. |
| Invitro | Anti-inflammatory agent 35 (化合物 5a27) (10 μM;30 分钟) 抑制 LPS (0.5 μg/mL;24 小时) 对促炎细胞因子 (IL-6、TNF-α) 产生的诱导作用,对小鼠原代巨噬细胞没有细胞毒性。Anti-inflammatory agent 35 抑制 IL-6、TNF-α 的产生,IC50 分别为 2.23 μM 和 2.40 μM[1]。Anti-inflammatory agent 35 (10 μM;30 分钟) 显着抑制 RAW 264.7 小鼠巨噬细胞中 LPS 诱导的激活。并且它显着抑制 p-p38 和 p-ERK,降低 IκB 水平,表明对 MAPK 和 NF-κB 信号的抑制[1]。 Western Blot Analysis[1] Cell Line: |
| In Vivo | Anti-inflammatory agent 35 (化合物 5a27) (50 mg/kg;口服;单剂量,监测 0-25 分钟) 比姜黄素 (HY-N0005) 具有更好的生物利用度[1]。Anti-inflammatory agent 35 (10 mg/kg;腹腔注射;每天 1 次,共 1 周) 通过抑制小鼠模型中的炎症改善 LPS 诱导的 ALI[1]。在大鼠中的药代动力学参数[1]Route |
| Name | Anti-inflammatory agent 35 |
| CAS | 2293951-00-3 |
| Formula | C27H29NO8 |
| Molar Mass | 495.52 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| Reference | [1]. Qian J, et al. Design and synthesis novel di-carbonyl analogs of curcumin (DACs) act as potent anti-inflammatory agents against LPS-induced acute lung injury (ALI). Eur J Med Chem. 2019 Apr 1;167:414-425. |