Bryostatin 1

一种具有多种生物活性的海洋大环内酯；可与PKCα、PKCβ1、PKCγ、PKCδ、PKCε、PKCη和PKCθ结合（Kis=0.8-3.0nM）；以浓度依赖性方式诱导癌细胞中的PKC活化或抑制；在50nM时，可降低LPS刺激的小鼠BMDC中的IL-2产生并增加IL-10产生；降低分离的人单核细胞衍生巨噬细胞中的CD4和CCR5细胞表面水平并降低HIV-1感染性；在30µg/kg时，可降低小鼠EAE模型中的脊髓和脑T细胞浸润和疾病严重程度；在2.5mg/kg时，可降低大鼠TBI模型中爆炸引起的BBB通透性增加A marine macrolide with diverse biological activities; binds to PKCα, PKCβ1, PKCγ, PKCδ, PKCε, PKCη, and PKCθ (Kis = 0.8-3.0 nM); induces PKC activation or inhibition in cancer cells in a concentration-dependent manner; reduces the production of IL-2 and increases the production of IL-10 in LPS-stimulated mouse BMDCs at 50 nM; decreases cell surface levels of CD4 and CCR5 and reduces HIV-1 infectivity in isolated human monocyte-derived macrophages; reduces spinal cord and brain T cell infiltration and disease severity in a mouse model of EAE at 30 µg/kg; decreases blast-induced increases in BBB permeability in a rat model of TBI at 2.5 mg/kg.