Acylated phenylethanoid glycosides, echinacoside and acteoside from Cistanche tubulosa, improve glucose tolerance in mice

Acylated phenylethanoid glycosides, echinacoside and acteoside from Cistanche tubulosa, improve glucose tolerance in mice
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DOI:
10.1007/s11418-014-0837-9
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发表时间:
2014-07-01
影响因子:
3.3
通讯作者:
Muraoka, Osamu
Muraoka, Osamu
中科院分区:
医学3区
文献类型:
--
作者:
Morikawa, Toshio;Ninomiya, Kiyofumi;Muraoka, Osamu

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乙酰化苯乙醇苷,紫锥花苷(1)和毛蕊花苷(2),肉苁蓉茎中的主要成分这些化合物(1和2)在连续给予125和/或250 mg/kg/天的剂量2周后,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明显变化。此外,小管藤中1 (IC50 = 3.1 μ M)、2 (IC50 = 1.2 μ M)、异毛蕊糖苷(3,4.6 μ M)、2′-乙酰毛蕊糖苷(4,0.071 μ M)、小管糖苷A (5,8.8 μ M)和B (9,4.0 μ M)、丁香苷A 3- o - α -l-鼠李糖苷(10,1.1 μ M)、杉木糖苷I (13,0.53 μ M)和坎卡诺糖苷J(1) (14,9.3 μ M)对大鼠晶态醛糖还原酶有较强的抑制作用。特别是化合物4的效价与临床醛糖还原酶抑制剂依帕司他(0.072 μ M)相似。
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 mu M), 2 (1.2 mu M), isoacteoside (3, 4.6 mu M), 2'-acetylacteoside (4, 0.071 mu M), tubulosides A (5, 8.8 mu M) and B (9, 4.0 mu M), syringalide A 3-O-alpha-l-rhamnopyranoside (10, 1.1 mu M), campneoside I (13, 0.53 mu M), and kankanoside J(1) (14, 9.3 mu M), demonstrated potent rat lens aldose reductase inhibitory activity. In particular, the potency of compound 4 was similar to that of epalrestat (0.072 mu M), a clinical aldose reductase inhibitor.