Pancreatic lipase-inhibiting triterpenoid saponins from fruits of Acanthopanax senticosus

Pancreatic lipase-inhibiting triterpenoid saponins from fruits of Acanthopanax senticosus
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DOI:
10.1248/cpb.55.1087
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发表时间:
2007-07-01
影响因子:
1.7
通讯作者:
Koike, Kazuo
Koike, Kazuo
中科院分区:
医学4区
文献类型:
--
作者:
Li, Fang;Li, Wei;Koike, Kazuo

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从刺五加果实中分离得到16个三萜皂苷类化合物,其中包括一个新化合物刺五加皂苷E(1),经各种光谱分析和化学降解鉴定为3- o - β - d -葡萄糖醛基棘囊酸28- o - β - d -葡萄糖醛基棘五加苷。胰脂肪酶抑制实验表明,粗皂苷部分对胰脂肪酶具有抑制作用,胰脂肪酶是脂质消化的关键酶。在所分离到的化合物中,松果苷F(2)、黄连苷B(3)、异源皂苷3- o - β - d -葡糖苷- 6′- o -甲酯(4)和gypsogenin 3- o - β - d -葡糖苷- pyranoside 6′- o -甲酯(5)对胰脂肪酶具有抑制活性,IC50值分别为0.22、0.25、0.26和0.29 mM,其化学结构中28位的游离羧基是增强胰脂肪酶抑制作用所必需的。
Sixteen triterpenoid saponins were isolated from the fruits of Acanthopanax senticosus, including a new compound, acanthopanaxoside E (1), which was established as 3-O-beta-D-glucuronopyranosyl echinocystic acid 28-O-beta-D-glucopyranoside on the basis of various spectroscopic analyses and chemical degradation. By using a pancreatic lipase-inhibiting assay system, the crude saponin fraction showed inhibitory activity on pancreatic lipase, which is a key enzyme in lipid digestion. Among the isolated compounds, silphioside F (2), copteroside B (3), hederagenin 3-O-beta-D-glucuronopyranoside 6 '-O-methyl ester (4) and gypsogenin 3-O-beta-D-glucuronopyranoside (5) showed inhibitory activity toward pancreatic lipase with IC50 values of 0.22, 0.25, 0.26 and 0.29 mM, respectively, and the free carboxylic acid groups in position 28 within their chemical structures were required for enhancement of pancreatic lipase inhibition.