| Bioactivity | Praelolide is a potent Nrf2 activator. Praelolide suppresses osteoclastogenesis and reactive oxygen species (ROS) production. Praelolide disrupts Keap1-Nrf2 protein-protein interactions by noncovalent binding to Keap1. Praelolide has the potential for the research of osteoclastogenic bone disease[1]. |
| Invitro | Praelolide (compound 21) (10 µM) 在骨髓单核细胞/巨噬细胞 (BMM 中显示出抗破骨细胞生成活性，抑制率为 100%)[1]。Praelolide (1, 1.25, 5, 10 µM; 1-5 days) 抑制 RANKL 诱导的破骨细胞形成，且无细胞毒性，抑制 BMMs 中破骨细胞的骨吸收和肌动蛋白环形成[1]。Praelolide (5, 10 µM) 抑制 BMMs 中 RANKL 诱导的 NFATc1、组织蛋白酶 K、MMP-9 和 TRAP 的 mRNA 水平[1]。Praelolide (5, 10 µM; 6 h) 增加 Nrf2、HO-1 和 NQO1 蛋白表达，增强 Nrf2 蛋白的稳定性[1]。Praelolide (10 µM; 0-60 min) 抑制 RANKL 诱导的 NF-κB 和 MAPK 信号通路，并抑制前破骨细胞中 RANKL 诱导的 ERK、p38 MAPK、IKBα 和 p65 NF-kB 磷酸化[1] 。Praelolide (0, 20, 50, 100 µM; 24 h) 再RAW264.7 细胞中通过结合 Keap1 蛋白来干扰 Keap1 和 Nrf2 之间的相互作用[1]。 Cell Viability Assay[1] Cell Line: |
| In Vivo | Praelolide (2, 5, 10 µM; co-treated for 6 days) 可挽救泼尼松诱导的斑马鱼的骨质流失[1]。 Animal Model: |
| Name | Praelolide |
| Formula | C28H35ClO12 |
| Molar Mass | 599.02 |
| 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]. Qi X, et al. Briarane-type diterpenoids, the inhibitors of osteoclast formation by interrupting Keap1-Nrf2 interaction and activating Nrf2 pathway. Eur J Med Chem. 2022 Nov 24;246:114948. |