Pharmacology and Toxicology Research Center, Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100094, China.
Molecules. 2013 Dec 13;18(12):15624-35. doi: 10.3390/molecules181215624.
Sophoricoside, an isoflavone glycoside isolated from Sophora japonica (Leguminosae), has been widely reported as an immunomodulator. In this study, the effects of sophoricoside on lipogenesis and glucose consumption in HepG2 cells and C2C12 myotubes were investigated. Treatment with sophoricoside at concentrations of 1-10 μM inhibited lipid accumulation in HepG2 cells in a dose-dependent manner. At the same concentration range, no effect on cell viability was observed in the MTT assay. Inhibition of lipogenesis was associated with the downregulation of SREBP-1a, SREBP-1c, SREBP-2 and their downstream target genes (FAS, ACC, HMGR) as revealed by realtime quantitative PCR. The lipid-lowering effect was mediated via the phosphorylation of AMPK. Further investigation of the activities of this isoflavone showed that sophoricoside has the capability to increase glucose uptake by C2C12 myotubes. It also effectively inhibited the activities of α-glucosidase and α-amylase in vitro and remarkably lowered postprandial hyperglycaemia in starch-loaded C57BL6/J mice. These results suggest that sophoricoside is an effective regulator of lipogenesis and glucose consumption and may find utility in the treatment of obesity and type 2 diabetes.
槐糖苷，一种从槐属植物（豆科）中分离出来的异黄酮糖苷，已被广泛报道为一种免疫调节剂。在本研究中，研究了槐糖苷对 HepG2 细胞和 C2C12 肌管中的脂肪生成和葡萄糖消耗的影响。槐糖苷在 1-10 μM 的浓度下处理，以剂量依赖性方式抑制 HepG2 细胞中的脂质积累。在相同的浓度范围内，MTT 测定未观察到对细胞活力的影响。实时定量 PCR 显示，脂肪生成的抑制与 SREBP-1a、SREBP-1c、SREBP-2 及其下游靶基因（FAS、ACC、HMGR）的下调有关。降脂作用是通过 AMPK 的磷酸化介导的。对这种异黄酮的活性的进一步研究表明，槐糖苷具有增加 C2C12 肌管中葡萄糖摄取的能力。它还能有效抑制体外α-葡萄糖苷酶和α-淀粉酶的活性，并显著降低淀粉负荷的 C57BL6/J 小鼠的餐后高血糖。这些结果表明，槐糖苷是脂肪生成和葡萄糖消耗的有效调节剂，可用于治疗肥胖症和 2 型糖尿病。
