Key Laboratory of Medicinal Chemistry and Molecular Diagnosis, Ministry of Education & College of Public Health, Hebei University, Baoding 071002, China.
Key Laboratory of Analytical Science and Technology of Hebei Province, College of Chemistry and Environmental Science, Hebei University, Baoding 071002, China.
Molecules. 2019 Jul 25;24(15):2709. doi: 10.3390/molecules24152709.
Aldose reductase (AR) is a drug target for therapies to treat complications caused by diabetes mellitus, and the development of effective AR inhibitors (ARIs) of natural origin is considered to be an attractive option for reducing these complications. In this research, the rat lens AR (RLAR) inhibitory activity of evening primrose () seeds was investigated for the first time. In our results, the 50% (/) methanol extract of evening primrose seeds exhibits excellent RLAR inhibitory activity (IC value of 7.53 μg/mL). Moreover, after enrichment of its bioactive components, the ARIs are more likely to be present in the ethyl acetate fraction of 50% () methanol extract (EME) of evening primrose seeds, which exhibits superior RLAR inhibitory activity (IC value of 3.08 µg/mL). Finally, gallic acid (), procyanidin B3 (), catechin (), and methyl gallate () were identified as the major ARIs from the EME by affinity-based ultrafiltration-high-performance liquid chromatography and were isolated by high speed countercurrent chromatography, with gallic acid (11.46 µmol/L) and catechin (14.78 µmol/L) being the more potent inhibitors of the four ARIs identified. The results demonstrated that evening primrose seeds may be a potent ingredient of ARIs.
醛糖还原酶 (AR) 是治疗糖尿病并发症的药物靶点，开发天然来源的有效 AR 抑制剂 (ARIs) 被认为是减少这些并发症的一种有吸引力的选择。在这项研究中，首次研究了月见草 () 种子对大鼠晶状体 AR (RLAR) 的抑制活性。结果表明，月见草种子的 50%()甲醇提取物具有出色的 RLAR 抑制活性 (IC 值为 7.53 μg/mL)。此外，在富集其生物活性成分后，ARIs 更可能存在于月见草种子 50%()甲醇提取物 (EME) 的乙酸乙酯部分中，该部分具有优异的 RLAR 抑制活性 (IC 值为 3.08 µg/mL)。最后，通过基于亲和性的超滤-高效液相色谱鉴定出 EME 中的主要 ARIs 为没食子酸 ()、原花青素 B3 ()、儿茶素 () 和甲基没食子酸 ()，并用高速逆流色谱法进行分离，其中没食子酸 (11.46 µmol/L) 和儿茶素 (14.78 µmol/L) 是四种 ARIs 中更有效的抑制剂。研究结果表明，月见草种子可能是 ARIs 的有效成分。
