Department of Food Science and Nutrition, Pukyong National University, Busan 608-737, Republic of Korea.
Department of Food Science and Nutrition, Pukyong National University, Busan 608-737, Republic of Korea.
Food Chem Toxicol. 2014 Feb;64:27-33. doi: 10.1016/j.fct.2013.11.020. Epub 2013 Nov 27.
Apigenin has gained particular interests in recent years as a beneficial and health promoting agent because of its low intrinsic toxicity. Vitexin and isovitexin, naturally occurring C-glycosylated derivatives of apigenin, have been known to possess potent anti-diabetic, anti-Alzheimer's disease (anti-AD), and anti-inflammatory activities. The present study was designed to investigate the anti-diabetic, anti-AD, and anti-inflammatory potential of apigenin and its two C-glycosylated derivatives, vitexin and isovitexin by in vitro assays including rat lens aldose reductase (RLAR), human recombinant aldose reductase (HRAR), advanced glycation endproducts (AGEs), protein tyrosine phosphatase 1B (PTP1B), acetylcholinesterase (AChE), butyrylcholinesterase (BChE), β-site amyloid precursor (APP) cleaving enzyme 1 (BACE1), and nitric oxide (NO), inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) in lipopolysaccharide (LPS)-induced RAW 264.7 cells. Among them, isovitexin was found as the most potent inhibitor against RLAR, HRAR, AGE, AChE, and BChE while vitexin showed the most potent PTP1B inhibitory activity. Despite the relatively weak anti-diabetic and anti-AD potentials, apigenin showed powerful antiinflammatory activity by inhibiting NO production and iNOS and COX-2 expression while vitexin and isovitexin were inactive. Therefore, it could be speculated that C-glycosylation of apigenin at different positions might be closely linked to relative intensity of anti-diabetic, anti-AD, and anti-inflammatory potentials.
芹菜素由于其低内在毒性，近年来作为有益和促进健康的物质而受到特别关注。牡荆素和异牡荆素是芹菜素的天然 C-糖苷化衍生物，已知具有很强的抗糖尿病、抗阿尔茨海默病（抗 AD）和抗炎活性。本研究旨在通过体外测定包括大鼠晶状体醛糖还原酶（RLAR）、人重组醛糖还原酶（HRAR）、晚期糖基化终产物（AGEs）、蛋白酪氨酸磷酸酶 1B（PTP1B）、乙酰胆碱酯酶（AChE）、丁酰胆碱酯酶（BChE）、β-淀粉样前体蛋白（APP）裂解酶 1（BACE1）和一氧化氮（NO）、诱导型一氧化氮合酶（iNOS）和环氧化酶-2（COX-2）在脂多糖（LPS）诱导的 RAW 264.7 细胞中，研究芹菜素及其两种 C-糖苷化衍生物牡荆素和异牡荆素的抗糖尿病、抗 AD 和抗炎潜力。其中，异牡荆素对 RLAR、HRAR、AGE、AChE 和 BChE 的抑制作用最强，而牡荆素对 PTP1B 的抑制作用最强。尽管抗糖尿病和抗 AD 潜力相对较弱，但芹菜素通过抑制 NO 产生和 iNOS 和 COX-2 表达表现出强大的抗炎活性，而牡荆素和异牡荆素则没有活性。因此，可以推测，芹菜素在不同位置的 C-糖苷化可能与抗糖尿病、抗 AD 和抗炎潜力的相对强度密切相关。
