Pharmaceutical Research and Technology Institute, Kinki University, 3-4-1 Kowakae, Higashi-osaka, Osaka, 577-8502, Japan.
J Nat Med. 2014 Jul;68(3):561-6. doi: 10.1007/s11418-014-0837-9. Epub 2014 Apr 19.
Acylated phenylethanoid glycosides, echinacoside (1) and acteoside (2), principal constituents in stems of Cistanche tubulosa (Orobanchaceae), inhibited the increase in postprandial blood glucose levels in starch-loaded mice at doses of 250-500 mg/kg p.o. These compounds (1 and 2) also significantly improved glucose tolerance in starch-loaded mice after 2 weeks of continuous administration at doses of 125 and/or 250 mg/kg/day p.o. without producing significant changes in body weight or food intake. In addition, several constituents from C. tubulosa, including 1 (IC50 = 3.1 μM), 2 (1.2 μM), isoacteoside (3, 4.6 μM), 2'-acetylacteoside (4, 0.071 μM), tubulosides A (5, 8.8 μM) and B (9, 4.0 μM), syringalide A 3-O-α-L-rhamnopyranoside (10, 1.1 μM), campneoside I (13, 0.53 μM), and kankanoside J1 (14, 9.3 μM), demonstrated potent rat lens aldose reductase inhibitory activity. In particular, the potency of compound 4 was similar to that of epalrestat (0.072 μM), a clinical aldose reductase inhibitor.
酰基苯乙醇苷类化合物，毛蕊花糖苷（1）和麦角甾苷（2），是肉苁蓉（列当科）茎中的主要成分，在 250-500mg/kg 口服剂量下可抑制淀粉负荷小鼠餐后血糖升高。这些化合物（1 和 2）在连续 2 周每天口服 125 和/或 250mg/kg 剂量下，也显著改善了淀粉负荷小鼠的葡萄糖耐量，而体重或食物摄入量没有显著变化。此外，肉苁蓉的几种成分，包括 1（IC50=3.1μM）、2（1.2μM）、异麦角甾苷（3、4.6μM）、2'-乙酰麦角甾苷（4、0.071μM）、tubulosides A（5、8.8μM）和 B（9、4.0μM）、丁香苷 A 3-O-α-L-鼠李吡喃糖苷（10、1.1μM）、坎那诺苷 I（13、0.53μM）和 kankanoside J1（14、9.3μM），对大鼠晶状体醛糖还原酶表现出很强的抑制活性。特别是化合物 4 的效力与临床醛糖还原酶抑制剂依帕司他（0.072μM）相似。
