a Department of Biology , University of Pisa , Pisa , Italy.
b Interdepartmental Research Center Nutrafood ''Nutraceuticals and Food for Health'' , University of Pisa , Pisa , Italy.
J Enzyme Inhib Med Chem. 2019 Dec;34(1):350-360. doi: 10.1080/14756366.2018.1553166.
Seven triterpenoid saponins were identified in methanolic extracts of seeds of the Zolfino bean landrace (Phaseolus vulgaris L.) by HPLC fractionation, revealing their ability to inhibit highly purified human recombinant aldose reductase (hAKR1B1). Six of these compounds were associated by MS analysis with the following saponins already reported in different Phaseolus vulgaris varieties: soyasaponin Ba (V), soyasaponin Bb, soyasaponin Bd (sandosaponin A), soyasaponin αg, 3-O-[R-l-rhamnopyranosyl(1 → 2)-α-d-glucopyranosyl(1 → 2)-α-d-glucuronopyranosyl]olean-12-en-22-oxo-3α,-24-diol, and soyasaponin βg. The inhibitory activity of the collected fractions containing the above compounds was tested for hAKR1B1-dependent reduction of both l-idose and 4-hydroxynonenal, revealing that some are able to differentially inhibit the enzyme. The present work also highlights the difficulties in the search for aldose reductase differential inhibitors (ARDIs) in mixtures due to the masking effect on ARDIs exerted by the presence of conventional aldose reductase inhibitors. The possibility of differential inhibition generated by a different inhibitory model of action of molecules on different substrates undergoing transformation is also discussed.
七种三萜皂苷在 Zolfino 豆地方品种（菜豆）的甲醇提取物中通过 HPLC 分级分离得到鉴定，揭示了它们抑制高纯度人重组醛糖还原酶（hAKR1B1）的能力。通过 MS 分析，其中 6 种化合物与已在不同菜豆品种中报道的以下皂苷相关：大豆皂苷 Ba（V）、大豆皂苷 Bb、大豆皂苷 Bd（山豆皂苷 A）、大豆皂苷 αg、3-O-[R-l-鼠李吡喃糖基（1 → 2）-α-d-吡喃葡萄糖基（1 → 2）-α-d-吡喃葡萄糖醛酸基]齐墩-12-烯-22-酮-3α，24-二醇和大豆皂苷 βg。测试了含有上述化合物的收集级分对 hAKR1B1 依赖性还原 l--idose 和 4-羟基壬烯醛的抑制活性，结果表明其中一些能够差异抑制酶。本工作还强调了由于常规醛糖还原酶抑制剂的存在对醛糖还原酶差异抑制剂（ARDIs）的掩蔽作用，在混合物中寻找 ARDIs 的困难。还讨论了分子对不同底物的不同抑制作用模式产生差异抑制的可能性。
