| Description |
Yadanzigan (YDZG) is an anti-inflammatory agent and a NLRP3 inhibitor. Yadanzigan specifically inhibits NLRP3 activation via inhibiting NF-κB pathway and Reactive Oxygen Species production. Yadanzigan also moderates LPS (HY-D1056)-induced acute lung injury (ALI) in mice[1].
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| Related Catalog |
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| Target |
NLRP3 inflammasome
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| In Vitro |
Yadanzigan (20, 40, 80 μM; 1 h) 促进 RAW264.7 巨噬细胞的 Nrf2 从细胞质转位到细胞核[1]。 Yadanzigan (20 μM; 1 h) 抑制 LPS 诱导 HEK293T 细胞线粒体活性氧 (ROS) 的生成 (1 μg/mL; 6 h)[1]。 Yadanzigan (40 μM; 1 h) 显著阻断 J774A 细胞在LPS和ATP诱导下 NLRP3 炎性小体的形成[1]。 Yadanzigan (2.5-10 μM 或 10-40 μM; 1, 6, 12 h) 增强J774A.1 和 THP-1 细胞中 TRIM31 表达，促进 NLRP3 蛋白降解[1]。 Western Blot Analysis[1] Cell Line: J774A.1, and THP-1 cells Concentration: For J774A.1: 2.5 μM, 5 μM, and 10 μM; For THP-1: 10 μM, 20 μM, and 40 μM Incubation Time: For J774A.1: 6 h, 12 h; For THP-1: 1 hour; 2 h before 1 μg/mL LPS stimulated and another 30 min before 5 mM ATP induced Result: Led to a sharp decrease in NLRP3 expression in J774A.1 cells. Led to a large decrease in NLRP3 protein expression in a dose-dependent manner in THP-1 cells. Immunofluorescence[1] Cell Line: RAW264.7 macrophages, THP-1 cells Concentration: 20, 40, and 80 μM Incubation Time: Pre-treated for 1 h, continue to incubate for 18 h Result: Decreased caspase-1 p20 activation and mature IL-1β and inhibited cleaved caspase-1 release into supernatants.
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| In Vivo |
Yadanzigan (5 mg/kg, 10 mg/kg; 静脉注射; 共 3 次) 预防 LPS 诱导的小鼠急性肺损伤[1]。 Animal Model: Male BABL/C mice (18-22 g)[1] Dosage: 5 mg/kg, 10 mg/kg Administration: Intravenous injection; dose at 2 h prior to and 6 h, 12 h after LPS induction Result: Reduced LPS-induced infiltration of inflammatory cells and cytokine levels, such as TNF-α and IL-6. Inhibited NLRP3 inflammasome activation in lung tissue. Resulted significantly greater survival rate.
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| References |
[1]. Cui Y, et al. Yadanzigan, a quassinoid glucoside, attenuates NLRP3 inflammasome activation to prevent LPS-induced acute lung injury. Authorea Preprints, 2020.
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