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具有保肝活性的酰化苯乙醇苷低聚糖从沙漠植物肉苁蓉中分离得到。

Acylated phenylethanoid oligoglycosides with hepatoprotective activity from the desert plant Cistanche tubulosa.

机构信息

Pharmaceutical Research and Technology Institute, Kinki University, 3-4-1 Kowakae, Higashi-osaka, Osaka 577-8502, Japan.

出版信息

Bioorg Med Chem. 2010 Mar 1;18(5):1882-90. doi: 10.1016/j.bmc.2010.01.047. Epub 2010 Jan 25.

DOI:10.1016/j.bmc.2010.01.047
PMID:20159656
Abstract

The methanolic extract from fresh stems of Cistanche tubulosa (Orobanchaceae) was found to show hepatoprotective effects against D-galactosamine (D-GalN)/lipopolysaccharide (LPS)-induced liver injury in mice. From the extract, three new phenylethanoid oligoglycosides, kankanosides H(1) (1), H(2) (2), and I (3), were isolated together with 16 phenylethanoid glycosides (4-19) and two acylated oligosugars (20, 21). The structures of 1-3 were determined on the basis of spectroscopic properties as well as of chemical evidence. Among the isolates, echinacoside (4, IC(50)=10.2 microM), acteoside (5, 4.6 microM), isoacteoside (6, 5.3 microM), 2'-acetylacteoside (8, 4.8 microM), and tubuloside A (10, 8.6 microM) inhibited D-GalN-induced death of hepatocytes. These five isolates, 4 (31.1 microM), 5 (17.8 microM), 6 (22.7 microM), 8 (25.7 microM), and 10 (23.2 microM), and cistantubuloside B(1) (11, 21.4 microM) also reduced TNF-alpha-induced cytotoxicity in L929 cells. Moreover, principal constituents (4-6) exhibited in vivo hepatoprotective effects at doses of 25-100mg/kg, po.

摘要

从肉苁蓉(列当科)新鲜茎的甲醇提取物中发现其对 D-半乳糖胺(D-GalN)/脂多糖(LPS)诱导的小鼠肝损伤具有保护作用。从提取物中分离得到三种新的苯乙醇苷寡糖苷,分别为坎卡诺苷 H(1)(1)、H(2)(2)和 I(3),此外还分离得到 16 种苯乙醇苷(4-19)和两种酰化寡糖(20、21)。根据光谱性质和化学证据确定了 1-3 的结构。在分离得到的化合物中,毛蕊花糖苷(4,IC50=10.2 μM)、麦角甾苷(5,4.6 μM)、异麦角甾苷(6,5.3 μM)、2'-乙酰麦角甾苷(8,4.8 μM)和肉苁蓉苷 A(10,8.6 μM)抑制 D-GalN 诱导的肝细胞死亡。这 5 种分离得到的化合物,4(31.1 μM)、5(17.8 μM)、6(22.7 μM)、8(25.7 μM)和 10(23.2 μM)以及仙茅苷 B(1)(11,21.4 μM)也降低了 L929 细胞中 TNF-α诱导的细胞毒性。此外,主要成分(4-6)在 25-100mg/kg 剂量下具有体内保肝作用,po。

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