Lee Yeon Sil, Lee Sanghyun, Lee Hye Seung, Kim Bak-Kwang, Ohuchi Kazuo, Shin Kuk Hyun
Seokwon Life Science Research Institute, World Sea Green Co. Ltd., Paju 413-832, Korea.
Biol Pharm Bull. 2005 May;28(5):916-8. doi: 10.1248/bpb.28.916.
The inhibitory effects of compounds from Salicornia herbacea (Chenopodiaceae) on rat lens aldose reductase (RLAR) and sorbitol accumulation in streptozotocin-induced diabetic rat tissues were investigated. The various fractions from the MeOH extract of S. herbacea were tested for their effects on RLAR in vitro. Among them, the EtOAc fraction was found to exhibit a potent RLAR inhibition (IC(50)=0.75 microg/ml), from which an active principle as a potent AR inhibitor was isolated and its chemical structure was elucidated as isorhamnetin-3-O-beta-D-glucoside (1) by spectral analysis. Compound 1 exhibited a potent RLAR inhibition in vitro, its IC(50) being 1.4 microM. Compound 1, when administered orally at 25 mg/kg in streptozotocin (STZ)-induced diabetic rats, caused not only a significant inhibition of serum glucose concentration but also sorbitol accumulation in the lenses, red blood cells (RBC), and sciatic nerves. These results indicate that compound 1 from S. herbacea is a leading compound for further study as a new drug for the prevention and/or treatment of diabetes and its complications.
研究了盐角草(藜科)化合物对链脲佐菌素诱导的糖尿病大鼠组织中大鼠晶状体醛糖还原酶(RLAR)和山梨醇积累的抑制作用。测试了盐角草甲醇提取物的不同馏分对RLAR的体外作用。其中,乙酸乙酯馏分表现出强效的RLAR抑制作用(IC(50)=0.75微克/毫升),从中分离出一种作为强效AR抑制剂的活性成分,并通过光谱分析阐明其化学结构为异鼠李素-3-O-β-D-葡萄糖苷(1)。化合物1在体外表现出强效的RLAR抑制作用,其IC(50)为1.4微摩尔。化合物1以25毫克/千克的剂量口服给予链脲佐菌素(STZ)诱导的糖尿病大鼠时,不仅显著抑制血清葡萄糖浓度,还抑制晶状体、红细胞(RBC)和坐骨神经中山梨醇的积累。这些结果表明,盐角草中的化合物1是作为预防和/或治疗糖尿病及其并发症的新药进行进一步研究的先导化合物。