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Bufotalin

CAS No. : 471-95-4

MCE 站：Bufotalin

产品活性：Bufotalin 是一种从 Venenum Bufonis 分离的类固醇内酯，具有强大的抗肿瘤活性。Bufotalin 诱导癌细胞凋亡 (apoptosis)，也诱导内质网应激激活。

研究领域：Apoptosis  |  Immunology/Inflammation  |  NF-κB  |  Metabolic Enzyme/Protease

作用靶点：Apoptosis  |  Reactive Oxygen Species

In Vitro: Bufotalin (0.1-2.5 μM; 12-96 hours) treatment dose- ａnd time-dependently inhibits MG-63 osteoblastoma cell survival.
Bufotalin (0.5-2.5 μM; 48 hours) treatment dose-dependently increases the percentage of Annexin V positive cells (apoptotic cells) ａnd caspase-12 activity in MG-63 cells. Bufotalin-induced osteoblastoma cell apoptosis is associated with caspase-12 activation.
Bufotalin (0.5-2.5 μM; 12 hours) treatment dose-dependently induces C/EBP homologous protein (CHOP) expression as well as PERK ａnd IRE1 phosphorylation in MG-63 cells. Bufotalin induces endoplasmic reticulum (ER) stress activation in cells.
Bufotalin treatment induces cell cycle arrest at G2/M phase through down-regulation of Aurora A, CDC25, CDK1, cyclin A ａnd cyclin B1, as well as up-regulation of p53 ａnd p21 in HepG2 cells. Bufotalin treatment also induces apoptosis which was accompanied by decrease in mitochondrial membrane potential, increases in intracellular calcium level ａnd reactive oxygen species production, activations of caspase-9 ａnd -3, cleavage of poly ADP-ribose polymerase (PARP) as well as changes in the expressions of bcl-2 ａnd bax.

In Vivo: Bufotalin (0.5-1 mg/kg; intraperitoneal injection; twice daily; for 7 days) treatment shows a significantly reduced tumor growth in mice.

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