Isolinderalactone

Isolinderalactone is a sesquiterpene that exhibits anti-cancer, anti-inflammatory, and neuroprotective effects. Isolinderalactone inhibits VEGF expression and tyrosine phosphorylation of VEGFR2. Isolinderalactone decreases viability and induces apoptosis in U-87 glioblastoma (GBM) cells and colorectal cancer (CRC) cells. Isolinderalactone induces G2/M phase cell cycle arrest, ROS generation, pJNK/p38 MAPK activation, in colorectal cancer (CRC) cells. Isolinderalactone blocks LPS (HY-D1056)-induced NF-κB activation while activating Nrf2-HMOX1 signaling in RAW264.7 macrophages. Isolinderalactone improves cognitive dysfunction in APP/PS1 mice. Isolinderalactone can be used for the study of Glioblastoma multiforme (GBM), colorectal cancer, Alzheimer’s disease and acute lung injury^{[1][2][3][4][5]}. In Vitro:Isolinderalactone (0.5-2.5 μg/mL, 24-72 h) inhibits U-87 glioblastoma cell growth^[1].
Isolinderalactone (0.5-2.5 μg/mL, 48 h) activates the apoptotic pathway in U-87 GBM cells by decreasing BCL-2, survivin, and XIAP expression, increasing cleaved caspase-3, and inducing DNA breakage, thereby promoting cell apoptosis^[1].
Isolinderalactone (0.5-2 μg/mL, 48 h) suppresses VEGF expression in U-87 GBM cells and inhibits VEGF-induced angiogenesis of human brain microvascular endothelial cells (HBMECs)^[2].
Isolinderalactone (2 μg/mL, 8 days) inhibits angiogenic sprouting in a 3D microfluidic chip^[2].
Isolinderalactone (2.5-5 μg/mL, 48 h) decreases HIF expression and activity in U-87 cells and VEGFR2 activation in HBMECs^[2].
Isolinderalactone (0-9 μM, 24-48 h) suppresses proliferation and colony formation of colorectal cancer cells (HCT116, HCT116-OxR, HT29, and HT29-OxR cells)^[3].
Isolinderalactone (0-9 μM, 48 h) induces apoptosis, G2/M cell cycle arrest, ROS generation, and ER stress in colorectal cancer cells^[3].
Isolinderalactone (0-9 μM, 48 h) induces apoptosis in CRC cells via mitochondrial and caspase-dependent pathways, potentially by modulating JNK/p38 MAPK activation, with ROS playing a critical role in this process^[3].
Isolinderalactone (10 μM, 2-27 h) attenuates Aβ_1-42-induced cell damage and reduces neurotoxicity in PC12 cells^[4].
Isolinderalactone (10 μM, 27 h) reduces neuronal cell damage by inhibiting JNK in PC12 cells^[4].
Isolinderalactone (0.5-10 μM, 19 h) inhibits LPS or TNF-α-induced inflammatory response in RAW264.7 cells, MH-S cells and BMDMs^[5].
Isolinderalactone (1-10 μM, 13 h) suppresses the mRNA expression of proinflammatory enzymes and cytokines in LPS-exposed RAW264.7 macrophages^[5].
Isolinderalactone (1-10 μM, 2-9 h) blocks LPS-induced NF-κB activation while activating Nrf2-HMOX1 signaling in RAW264.7 macrophages^[5].
In Vivo:Isolinderalactone (1-5 mg/kg, i.p., every other day, 12 days) inhibits tumor growth in a human GBM xenograft mouse model^[1].
Isolinderalactone (2.5-5 mg/kg, i.p., every other day, 16 days) reduces tumor growth and vasculature in a human GBM xenograft model ^[2].
Isolinderalactone (5 mg/kg, i.p., daily, 6 days) inhibits VEGF-mediated angiogenesis in an in vivo Matrigel plug assay in mice^[2].
Isolinderalactone (1-10 mg/kg, i.p., daily, 30 days) ameliorates learning and memory deficits in APP/PS1 mice^[4].
Isolinderalactone (2.5-10 mg/kg, i.p., daily, 5 days) alleviates LPS-induced lung inflammatory injury in mice^[5].