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) 以 2 μM 的IC50值抑制大鼠主动脉平滑肌（A10）细胞中血管加压素诱导的花生四烯酸的释放。(S)-Bromoenol lactone 是一种不可逆的、手性的、基于机制的钙非依赖性磷脂酶A2β (iPLA2β) 抑制剂。