酚类 C-糖苷的合成及降血糖活性。
Synthesis and antihyperglycemic activity of phenolic C-glycosides.
机构信息
Medicinal and Process Chemistry Division, Central Drug Research Institute, CSIR, Lucknow 226 001, India.
出版信息
Bioorg Med Chem Lett. 2011 Jan 1;21(1):228-33. doi: 10.1016/j.bmcl.2010.11.031. Epub 2010 Nov 11.
Various phenolic C-glycosides were evaluated for their in vitro and in vivo antihyperglycemic activity employing glucose uptake by rat muscle cell lines (L-6) and low dosed-streptozotocin-induced diabetic rats, respectively. Some of phenolic C-glycosides were isolated from Pterocarpus marsupium and Ulmus wallichiana and other were synthesized by unprotected sugar and phloroacetophenone using Sc(OTf)(3) in aqueous ethanol. Eight among tested compounds showed significant lowering of blood glucose level on low dosed-streptozotocin-induced diabetic rats. The compound 24 lowered the blood glucose levels by 34.9% and 33.6% during 0-5h and 0-24h, respectively, at the dose of 25mg/kg body weight which is comparable to standard antidiabetic drug metformin.
采用大鼠肌肉细胞系（L-6）摄取葡萄糖和低剂量链脲佐菌素诱导的糖尿病大鼠模型，评估了各种酚类 C-糖苷的体外和体内抗高血糖活性。一些酚类 C-糖苷从紫檀和榆属植物中分离得到，另一些则通过在水乙醇中使用 Sc(OTf)(3)，由未保护的糖和苯乙酮合成得到。在低剂量链脲佐菌素诱导的糖尿病大鼠中，有 8 种测试化合物表现出显著的降血糖作用。化合物 24 在 25mg/kg 体重剂量下，分别在 0-5h 和 0-24h 期间使血糖水平降低了 34.9%和 33.6%，与标准抗糖尿病药物二甲双胍相当。
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