Abstract:
Sweet potatoes are rich in cardioprotective phytochemicals with potential anti-platelet aggregation activity, although this benefit may vary among cultivars/genotypes. The phenolic profile [HPLC-ESI(-)-qTOF-MS2], cheminformatics (ADMET properties, affinity toward platelet proteins) and anti-PA activity of phenolic-rich hydroalcoholic extracts obtained from orange (OSP) and purple (PSP) sweet potato storage roots, was evaluated. The phenolic richness [Hydroxycinnamic acids> flavonoids> benzoic acids] was PSP > OSP. Their main chlorogenic acids could interact with platelet proteins (integrins/adhesins, kinases/metalloenzymes) but their bioavailability could be poor. Just OSP exhibited a dose-dependent anti-platelet aggregation activity [inductor (IC50, mg.ml-1): thrombin receptor activator peptide-6 (0.55) > Adenosine-5\'-diphosphate (1.02) > collagen (1.56)] and reduced P-selectin expression (0.75-1.0 mg.ml-1) but not glycoprotein IIb/IIIa secretion. The explored anti-PA activity of OSP/PSP seems to be inversely related to their phenolic richness. The poor first-pass bioavailability of its chlorogenic acids (documented in silico) may represent a further obstacle for their anti-PA in vivo.
摘要:
红薯富含具有潜在抗血小板聚集活性的心脏保护植物化学物质,尽管这种益处可能因品种/基因型而异。酚醛谱[HPLC-ESI(-)-qTOF-MS2],化学信息学(ADMET特性,对血小板蛋白的亲和力)和从橙色(OSP)和紫色(PSP)甘薯贮藏根中获得的富含酚类的水醇提取物的抗PA活性,进行了评估。酚类丰富度[羟基肉桂酸>类黄酮>苯甲酸]为PSP>OSP。它们的主要绿原酸可以与血小板蛋白(整合素/粘附素,激酶/金属酶),但它们的生物利用度可能很差。仅OSP表现出剂量依赖性抗血小板聚集活性[诱导剂(IC50,mg。ml-1):凝血酶受体激活剂肽-6(0.55)>腺苷-5'-二磷酸(1.02)>胶原蛋白(1.56)]和减少的P-选择素表达(0.75-1.0mg。ml-1),但不分泌糖蛋白IIb/IIIa。OSP/PSP的已探索的抗PA活性似乎与其酚类丰富度成反比。其绿原酸的较差的首过生物利用度(在计算机中记录)可能是其体内抗PA的进一步障碍。