Loxoribine

鸟苷衍生物和TLR7激动剂；在1mM浓度下，在细胞报告基因检测中对TLR7而非其他人类TLR具有选择性；诱导增殖、增强对绵羊红细胞的抗体应答并激活小鼠脾细胞培养中针对Yac-1淋巴瘤细胞的自然杀伤细胞活性（EC50分别为10-50、3-20和13-22μM）；在250μM浓度下增加人类MoDC产生的IL-12、IL-23、IL-27和IL-10；与对照MoDC相比，洛索立滨处理的MoDC可诱导共培养的同种异体CD4+T细胞分泌更高水平的IL-17和IFN-γ；以120mg/kg的剂量减少B16小鼠黑色素瘤模型中的肺转移数量，通过共同施用IL-2可增强该效果；在用B16肿瘤疫苗免疫的小鼠中表现出佐剂活性。A guanosine derivative and an agonist of TLR7; selective for TLR7 over other human TLRs in a cell-based reporter assay at 1 mM; induces proliferation, increases the antibody response to sheep red blood cells, and activates natural killer cell activity against Yac-1 lymphoma cells in murine splenocyte cultures (EC50s = 10-50, 3-20, and 13-22 μM, respectively); increases production of IL-12, IL-23, IL-27, and IL-10 by human MoDCs at 250 μM; loxoribine-treated MoDCs induce higher levels of IL-17 and IFN-γ secretion by co-cultured allogeneic CD4+ T cells compared to control MoDCs; reduces the number of pulmonary metastases in the B16 mouse model of melanoma at 120 mg/kg, an effect enhanced by co-administration of IL-2; exhibits adjuvant activity in mice immunized with a B16 tumor vaccine.