The Novo Nordisk Foundation Center for Biosustainability, Technical University of Denmark, Building 220, Søltofts Plads, 2800 Kongens Lyngby, Denmark.
School of Food Science & Nutrition, University of Leeds, Leeds LS2 9JT, UK.
Int J Mol Sci. 2024 Aug 21;25(16):9082. doi: 10.3390/ijms25169082.
Kynurenic acid (KYNA) is an antioxidant degradation product of tryptophan that has been shown to have a variety of cytoprotective, neuroprotective and neuronal signalling properties. However, mammalian transporters and receptors display micromolar binding constants; these are consistent with its typically micromolar tissue concentrations but far above its serum/plasma concentration (normally tens of nanomolar), suggesting large gaps in our knowledge of its transport and mechanisms of action, in that the main influx transporters characterized to date are equilibrative, not concentrative. In addition, it is a substrate of a known anion efflux pump (ABCC4), whose in vivo activity is largely unknown. Exogeneous addition of L-tryptophan or L-kynurenine leads to the production of KYNA but also to that of many other co-metabolites (including some such as 3-hydroxy-L-kynurenine and quinolinic acid that may be toxic). With the exception of chestnut honey, KYNA exists at relatively low levels in natural foodstuffs. However, its bioavailability is reasonable, and as the terminal element of an irreversible reaction of most tryptophan degradation pathways, it might be added exogenously without disturbing upstream metabolism significantly. Many examples, which we review, show that it has valuable bioactivity. Given the above, we review its potential utility as a nutraceutical, finding it significantly worthy of further study and development.
犬尿酸(KYNA)是色氨酸的抗氧化降解产物,已显示出具有多种细胞保护、神经保护和神经元信号特性。然而,哺乳动物转运体和受体的结合常数为微摩尔;这些与通常为微摩尔的组织浓度一致,但远高于其血清/血浆浓度(通常为数十纳摩尔),这表明我们对其转运和作用机制的了解存在很大差距,因为迄今为止所描述的主要内流转运体是平衡的,而不是浓缩的。此外,它是一种已知阴离子外排泵(ABCC4)的底物,其体内活性尚不清楚。外源性添加 L-色氨酸或 L-犬尿氨酸会导致 KYNA 的产生,但也会导致许多其他共代谢物的产生(包括一些可能有毒的物质,如 3-羟基-L-犬尿氨酸和喹啉酸)。除了栗子蜜外,KYNA 在天然食品中的含量相对较低。然而,其生物利用度是合理的,并且作为大多数色氨酸降解途径的不可逆反应的末端元素,它可以被外源添加而不会显著干扰上游代谢。我们回顾的许多例子表明它具有有价值的生物活性。鉴于上述情况,我们回顾了它作为营养保健品的潜在用途,发现它非常值得进一步研究和开发。