The bioactivity of dietary anthocyanins is likely to be mediated by their degradation products
The bioactivity of dietary anthocyanins is likely to be mediated by their degradation products
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DOI：
10.1002/mnfr.200800461
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发表时间：
2009-05-01
影响因子：
5.2
通讯作者：
Cassidy, Aedin
中科院分区：
文献类型：
--
作者：
Kay, Colin D.;Kroon, Paul A.;Cassidy, Aedin
迄今为止，花青素的体外机械生物活性仅使用苷元和糖苷缀合物进行探索，尽管缺乏证据证明它们是生物可用的形式。我们进行了肠上皮细胞（Caco-2细胞）培养实验，结果表明，花青素在无细胞培养基（DMEM）中孵育4小时后，57％的初始花青素-3-葡萄糖苷（C3G）和96％的花青素被降解。降解水平与培养细胞孵育的降解水平没有统计学差异，表明降解是自发的。降解产物被鉴定为原儿茶酸 (PCA) 和间苯三醛 (PGA)，并在其他两种缓冲液基质（磷酸盐和 Hank 缓冲液）中得到证实。在培养的细胞培养基中，降解产物 PCA 和 PGA 被代谢为葡萄糖醛酸和硫酸盐结合物，如酶水解（硫酸酯酶和葡萄糖醛酸酶处理）和 MS 所示（PCA 和 PGA m/z = 155；硫酸盐 = 235；葡萄糖醛酸 = 331）。这些数据表明，很大一部分花青素的肠道代谢物可能是其降解产物的结合物。因此，未来确定花青素生物活性的努力应包括对酚酸和醛降解产物及其各自代谢物的研究。
To date the in vitro mechanistic bioactivity of anthocyanins has been exclusively explored using aglycones and glycoside conjugates, despite a lack of evidence establishing these as the biologically available forms. We conducted intestinal epithelial cell (Caco-2 cells) culture experiments, which indicated that after a 4 h incubation of anthocyanins in cell-free culture media (DMEM), 57% of the initial cyanidin-3-glucoside (C3G) and 96% of cyanidin had degraded. The level of degradation was not statistically different from that of cultured cell incubations, suggesting that degradation was spontaneous. Degradation products were identified as protocatechuic acid (PCA) and phloroglucinaldehyde (PGA), and were confirmed in two other buffer matrices (phosphate and Hank's buffers). In cultured cell media the degradation products PCA and PGA were metabolised to glucuronide and sulphate conjugates, as indicated by both enzyme hydrolysis (sulphatase and glucuronidase treatments) and MS (PCA and PGA m/z = 155; sulphate = 235; glucuronide = 331). These data suggest a significant proportion of intestinal metabolites of anthocyanins are likely to be conjugates of their degradation products. Future efforts to establish the biological activities of anthocyanins should therefore include the investigation of phenolic acid and aldehyde products of degradation, along with their respective metabolites.