近年来,由于其固有毒性低,芹菜素作为有益的和健康促进的试剂获得了特别的兴趣。Vitexin和isovitexin,天然存在的芹菜素的C-糖基化衍生物,已知具有有效的抗糖尿病药,抗阿尔茨海默病(抗AD),和抗炎活性。本研究旨在研究抗糖尿病,反AD,芹菜素及其两种C-糖基化衍生物的抗炎潜力,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),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-位点淀粉样蛋白前体(APP)裂解酶1(BACE1),和一氧化氮(NO),脂多糖(LPS)诱导的RAW264.7细胞中的诱导型一氧化氮合酶(iNOS)和环氧合酶-2(COX-2)。其中,发现异硫酸酯素是最有效的RLAR抑制剂,赫拉,年龄,AChE,和BChE,而牡蛎素显示出最有效的PTP1B抑制活性。尽管抗糖尿病和抗AD潜力相对较弱,芹菜素通过抑制NO的产生以及iNOS和COX-2的表达而表现出强大的抗炎活性,而牡蛎素和异牡蛎素无活性。因此,可以推测芹菜素在不同位置的C-糖基化可能与抗糖尿病的相对强度密切相关,反AD,和抗炎潜力。
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.