Effects of C-glycosylation on anti-diabetic, anti-Alzheimer's disease and anti-inflammatory potential of apigenin
Effects of C-glycosylation on anti-diabetic, anti-Alzheimer's disease and anti-inflammatory potential of apigenin
复制标题
DOI：
10.1016/j.fct.2013.11.020
复制
发表时间：
2014-02-01
影响因子：
4.3
通讯作者：
Jung, Hyun Ah
中科院分区：
文献类型：
--
作者：
Choi, Jae Sue;Islam, Md. Nurul;Jung, Hyun Ah
近年来，芹菜素作为一种有益健康的促进剂因其低内在毒性而受到人们的特别关注。牡荆素和异牡荆素是天然存在的芹菜素c -糖基化衍生物，已知具有有效的抗糖尿病、抗阿尔茨海默病（抗ad）和抗炎活性。本研究旨在通过对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）、丁基胆碱酯酶（BChE）、β -位点淀粉样蛋白前体（APP）切割酶1 （BACE1）、β -位点淀粉样蛋白前体（APP）切割酶1 （BACE1）、β -位点淀粉样蛋白前体（APP）切割酶1 （BACE1）的体外检测，探讨芹菜素及其两种c -糖基化衍生物——杨桃素和异杨桃素的抗糖尿病、抗ad和抗炎作用。和一氧化氮（NO）、诱导型一氧化氮合酶（iNOS）和环氧合酶-2 （COX-2）在脂多糖（LPS）诱导的RAW 264.7细胞中的表达。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ad的潜力相对较弱，但芹菜素通过抑制NO的产生、iNOS和COX-2的表达显示出强大的抗炎活性，而牡荆素和异牡荆素则无活性。因此，可以推测，芹菜素不同位置的c -糖基化可能与抗糖尿病、抗ad和抗炎潜能的相对强度密切相关。(C) 2013 Elsevier Ltd.版权所有。
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), beta-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 antiinflammatory potentials. (C) 2013 Elsevier Ltd. All rights reserved.