Baohuoside I

Baohuoside I, a flavonoid isolated from Epimedium koreanum Nakai, acts as an inhibitor of CXCR4, downregulates CXCR4 expression, induces apoptosis and shows anti-tumor activity ^[1].

Baohuoside I exhibited strong inhibition against the α-glucosidase while icariin and epimedin A, B and C were weak or inactive. All compounds were inactive against pancreatic α-amylase. The IC₅₀ of baohuoside I was 28.9 μmol/L^[2].A549 cells were evidently inhibited by Baohuoside I in a time- and concentration-dependent manner. IC₅₀ was approximately 25.1 μM at 24 h, 11.5μM at 48 h and 9.6μM at 72 h, respectively ^[3].

Baohuoside I prolonged graft survival on rat. A negative control group showed a mean survival time of 6.5±0.5 days. Monotherapy with a subtherapeutic oral dose of Baohuoside I (8.0 mg/kg/day) or FK506 (1.0 mg/kg/day) significantly prolonged cardiac allograft survival up to 9.0±2.0 days or 16.4±6.3 days, compared with negative controls. Results with combination therapy of these two drugs in the same doses (25.0±2.0 days) indicate that an additive prolongation of graft survival was produced when compared with monotherapy with Baohuoside I or FK506^[4].

References:
[1]. Kim B, et al. Baohuoside I suppresses invasion of cervical and breast cancer cells through the downregulation of CXCR4 chemokine receptor expression. Biochemistry. 2014 Dec 9;53(48):7562-9.
[2]. M.A.T. Phan, J. Wang, J.Y. Tang, et al. Evaluation of α-glucosidase inhibition potential of some flavonoids from Epimedium brevicornum L. WT-Food Science and Technology, 53 (2013), pp. 492-498.
[3]. Song J, et al. Reactive oxygen species-mediated mitochondrial pathway is involved in Baohuoside I-induced apoptosis in human non-small cell lung cancer. Chem Biol Interact. 2012 Jul 30;199(1):9-17.
[4].A. Ma, S. Qi, D. Xu, X. Zhang, P. Daloze, H. Chen . Baohuoside-1, a novel immunosuppressive molecule, inhibits lymphocyte activation in vitro and in vivo. Transplantation, 78 (2004), pp. 831-838.

宝活苷 I 是一种从淫羊藿中分离出来的黄酮类化合物，可作为 CXCR4 抑制剂，下调 CXCR4 表达，诱导细胞凋亡并具有抗肿瘤活性^[1]。

宝霍苷 I 对 α-葡萄糖苷酶表现出强烈的抑制作用，而淫羊藿苷和淫羊藿苷 A、B 和 C 则较弱或无活性。所有化合物均对胰腺 α-淀粉酶无活性。保活苷I的IC₅₀为28.9 μmol/L^[2]。保活苷I对A549细胞有明显的抑制作用，并呈时间和浓度依赖性。 IC₅₀ 在 24 小时时约为 25.1 μM，在 48 小时时约为 11.5 μM，在 72 小时时约为 9.6 μM ^[3]。

保活苷 I 延长了大鼠移植物的存活时间。阴性对照组显示平均存活时间为 6.5±0.5 天。与阴性对照相比，口服亚治疗剂量的宝活苷 I (8.0 mg/kg/天) 或 FK506 (1.0 mg/kg/天) 的单一疗法可显着延长心脏同种异体移植物的存活时间，达 9.0±2.0 天或 16.4±6.3 天。这两种药物以相同剂量（25.0±2.0 天）联合治疗的结果表明，与保活苷 I 或 FK506 的单药治疗相比，移植物存活时间得到额外延长^[4]。