Isochamaejasmin

Isochamaejasmin is a biflavonoid with anti-cancer, antiplasmodial and insecticidal activities. Isochamaejasmin displays a potent NF-κB (NF-κB) activation activity. Isochamaejasmin could cause DNA damage and induce apoptosis via the mitochondrial pathway in AW1 cells^[1][2]. Isochamaejasmin also has a moderate antiplasmodial activity (IC₅₀ of 7.3 μM for P. falciparum) and relatively low cytotoxicity (CC₅₀ of 29.0 μM)^[3]. In Vitro:Isochamaejasmin (6.25-100 μM; 24-72 h) shows potential toxicity against AW1 cells via time- and dose-dependent manners. Isochamaejasmin (1000 mg/L, 500 mg/L, 250 mg/L, 125 mg/L, 62.5 mg/L; 24 h, 48 h, 72 h, and 96 h) has potential toxicity against H. zea larvae via time- and dose-dependent manners^[1].
Isochamaejasmin (40-80 μM; 24 h) causes DNA damage and increases the levels of γH2AX and OGG1 in AW1 cells. The cell cycle is arrested at the G2/M phase^[1].
Isochamaejasmin (20-80 μM; 24 h) induces apoptosis of AW1 cells in a dose-dependent manner^[1].
Isochamaejasmin (20-80 μM; 24 h) shows decline in the MMP, upregulation of Bax/Bcl-2 expression resulting in the release of cytochrome c into the cytosol, activation of caspase-3/9, and cleavage of PARP^[1].
Isochamaejasmin shows a dose-dependent rise in the reactive oxygen species (ROS) levels, accumulation of a lipid peroxidation product, and inactivation of antioxidant enzymes in AW1 cells^[1].
Isochamaejasmin induces the expression of a NF-κB-directed reporter gene in transfected HeLa cells with an EC₅₀ of 3.23 μM. The Isochamaejasmin-stimulated NF-κB reporter activity is accompanied by nuclear translocation of NF-κB proteins and is blocked by a dominant-negative construct of IκBα. Isochamaejasmin also induces time-dependent phosphorylation of the mitogen-activated protein kinases ERK1/2 and p38, and PKCδ^[2].