Jeong Seung I, Kim Kang Ju, Choi Min Kyu, Keum Kyung Soo, Lee Seoul, Ahn Seon Ho, Back Seung Hoon, Song Ju Hung, Ju Young Sung, Choi Bong Kyu, Jung Kyu Yong
Department of Pharmacology, Wonkwang University School of Medicine, Jeonbuk, Korea.
Planta Med. 2004 Aug;70(8):736-9. doi: 10.1055/s-2004-827204.
Based on an inhibitory activity-guided fractionation for the high glucose-induced proliferation of glomerular mesangial cells (GMCs), chloroform extracts of the roots of Phytolacca americana were found to contain alpha-spinasterol (C (29)H (48)O), a delta (7)-sterol. This phytosterol proved to be a potent inhibitor (IC (50) = 3.9 x 10 (-12) g/mL, 9.5 pmol/L) of glomerular mesangial cell proliferation caused by high-ambient glucose (5.6 mM vs. 25 mM), and its inhibitory potency was about 1,000 times higher than that of simvastatin, an HMG-CoA reductase inhibitor used as a positive control. alpha-Spinasterol also significantly reduced the increases of serum triglycerides, renal weight and urinary protein excretion in streptozotocin-induced diabetic mice, and these were comparable to the results observed in insulin-treated diabetic mice. Therefore, the results obtained in this study suggest that alpha-spinasterol has a significant therapeutic potential to modulate the development and/or progression of diabetic nephropathy.
基于对高糖诱导的肾小球系膜细胞（GMCs）增殖的抑制活性导向分级分离，发现美洲商陆根的氯仿提取物含有α-菠菜甾醇（C₂₉H₄₈O），一种δ⁷-甾醇。这种植物甾醇被证明是高环境葡萄糖（5.6 mM对25 mM）引起的肾小球系膜细胞增殖的有效抑制剂（IC₅₀ = 3.9×10⁻¹² g/mL，9.5 pmol/L），其抑制效力比用作阳性对照的HMG-CoA还原酶抑制剂辛伐他汀高约1000倍。α-菠菜甾醇还显著降低了链脲佐菌素诱导的糖尿病小鼠的血清甘油三酯、肾脏重量和尿蛋白排泄的增加，这些结果与胰岛素治疗的糖尿病小鼠中观察到的结果相当。因此，本研究获得的结果表明，α-菠菜甾醇在调节糖尿病肾病的发生和/或进展方面具有显著的治疗潜力。
