Jung Hyun Ah, Park Jin Ju, Min Byung Sun, Jung Hee Jin, Islam Md Nurul, Choi Jae Sue
Department of Food Science and Human Nutrition, Chonbuk National University, Jeonju 561-756, Republic of Korea.
Department of Food and Life Science, Pukyong National University, Busan 608-737, Republic of Korea.
Asian Pac J Trop Med. 2015 Jan;8(1):1-5. doi: 10.1016/S1995-7645(14)60178-4.
To evaluate inhibitory potential of seven Korean thistles against the advanced glycation endproducts (AGE) formation as well as to identify responsible compounds from the most active species.
We used an in vitro AGE inhibition assay to evaluate the anti-diabetic complication potential of the methanol extracts of the selected Korean thistles.
Among the seven Korean thistles, the leaves of Cirsium maackii (C. maackii) exhibited the most significant inhibitory activity against AGE formation. By means of bioassay-directed fractionation, a lignan, chlorogenic acid and 14 flavonoids were isolated from the active ethyl acetate soluble fraction of a methanol extract from C. maackii leaves. Luteolin and its 5-O-glucoside have been previously isolated; however, a lignan and 13 known compounds were isolated for the first time from C. maackii leaves in this study. Most of the isolated compounds exhibited inhibitory activities against potential AGE formation. Among them, cernuoside was shown to be the most potent AGE inhibitor with an IC50 value of 21.21 μ mol/L. Most importantly, two major flavonoids, luteolin and its 5-O-glucoside, also significantly inhibited AGE formation, with IC50 values of 36.33 and 37.47 μ mol/L, respectively. Structure activity relationship revealed that the presence of free 3' and 4' dihydroxyl group in flavonoids skeleton played an important role in AGE inhibition.
These results indicate that C. maackii and C. maackii-derived flavonoids might be explored further to develop therapeutic agents for the prevention of diabetic complications due to their significant inhibitory activity against AGE formation.
评估七种韩国蓟对晚期糖基化终产物（AGE）形成的抑制潜力，并从活性最强的物种中鉴定出起作用的化合物。
我们采用体外AGE抑制试验来评估所选韩国蓟甲醇提取物的抗糖尿病并发症潜力。
在七种韩国蓟中，东北蓟（Cirsium maackii）的叶子对AGE形成表现出最显著的抑制活性。通过生物活性导向分离，从东北蓟叶子甲醇提取物的活性乙酸乙酯可溶部分中分离出一种木脂素、绿原酸和14种黄酮类化合物。木犀草素及其5 - O - 葡萄糖苷此前已被分离出来；然而，在本研究中，一种木脂素和13种已知化合物首次从东北蓟叶子中分离得到。大多数分离出的化合物对潜在的AGE形成表现出抑制活性。其中，紫菀苷被证明是最有效的AGE抑制剂，IC50值为21.21 μmol/L。最重要的是，两种主要的黄酮类化合物，木犀草素及其5 - O - 葡萄糖苷，也显著抑制AGE形成，IC50值分别为36.33和37.47 μmol/L。构效关系表明，黄酮类骨架中游离的3'和4'二羟基的存在在AGE抑制中起重要作用。
这些结果表明，由于东北蓟及其衍生的黄酮类化合物对AGE形成具有显著的抑制活性，可能需要进一步探索以开发预防糖尿病并发症的治疗药物。
