bromoenol lactone

Bromoenol lactone ((6E)-Bromoenol lactone) 是一种具有的钙依赖性磷脂酶 A2 (iPLA2β) 和丝氨酸蛋白酶抑制剂，可减弱尼古丁诱导的乳腺癌细胞增殖和迁移，抑制电压门控 Ca2+ 和瞬时受体电位经典通道，可抑制角叉菜胶诱导的大鼠后爪前列腺素生成和痛觉过敏。

The phospholipases are an extensive family of lipid hydrolases that function in cell signaling, digestion, membrane remodeling, and as venom components. The calcium-independent phospholipases (iPLA2) are a PLA2 subfamily closely associated with the release of arachidonic acid in response to physiologic stimuli. (R)-Bromoenol lactone ((R)-BEL) is an irreversible, chiral, mechanism-based inhibitor of calcium-independent phospholipase γ (iPLA2γ). Unlike (S)-BEL, (R)-BEL does not inhibit iPLA2β except at high doses of 20-30 μM. (R)-BEL inhibits human recombinant iPLA2γ with an IC50 of approximately 0.6 μM.

(S)-Bromoenol lactone ((S)-BEL) 是一种基于机制的不可逆钙独立磷脂酶 A2 (iPLA2) 抑制剂。与它的对映体 (R)-BEL 相比，(S)-BEL 表现出对 iPLA2γ (Group VIB) 的相对选择性，其抑制 iPLA2γ 的效力通常比抑制 iPLA2β (Group VIA) 高约 10-100 倍。该化合物与 (R)-BEL 配对使用，是区分 iPLA2β 与 iPLA2γ 在细胞信号传导、花生四烯酸释放及平滑肌收缩等过程中特定功能的关键工具。