Department of Biological and Medical Sciences, Faculty of Pharmacy in Hradec Králové, Charles University, Akademika Heyrovskeho 1203/8, 500 05 Hradec Králové, Czech Republic.
Department of Pharmacology and Toxicology, Faculty of Pharmacy in Hradec Králové, Charles University, Akademika Heyrovskeho 1203/8, 500 05 Hradec Králové, Czech Republic.
Nutrients. 2020 Jan 14;12(1):213. doi: 10.3390/nu12010213.
Quercetin is proven to decrease arterial blood pressure when given orally. Its bioavailability is, however, low and, therefore, its metabolites could rather be responsible for this effect. In particular, the colonic metabolites of quercetin, 3,4-dihydroxyphenylacetic acid (DHPA), 4-methylcatechol (4MC), and 3-(3-hydroxyphenyl)propionic acid (3HPPA), have been previously shown to decrease the blood pressure in spontaneously hypertensive rats (SHR). Interestingly, the mechanisms of action of these three metabolites are different. The aim of this study is hence to investigate if these metabolites can potentiate each other and thus decrease blood pressure in reduced doses. Three double-combinations of previously mentioned metabolites were administered to SHR as infusions to mimic a real biological situation. All combinations significantly decreased the blood pressure in SHR but there were important differences. The effect of DHPA and 4MC was mild and very short. A combination of DHPA with 3HPPA caused more pronounced effects, which were also rather short-lived. The last combination of 3HPPA and 4MC caused a long-lasting effect. In conclusion, certain combinations of quercetin metabolites have a more pronounced antihypertensive effect than single metabolites.
槲皮素经口服给药已被证明可降低动脉血压。然而,其生物利用度较低,因此,其代谢物可能是导致这种作用的原因。特别是,槲皮素的结肠代谢物,3,4-二羟基苯乙酸(DHPA)、4-甲基儿茶酚(4MC)和3-(3-羟基苯基)丙酸(3HPPA),先前已被证明可降低自发性高血压大鼠(SHR)的血压。有趣的是,这三种代谢物的作用机制不同。因此,本研究旨在探讨这些代谢物是否可以相互增强作用,从而以较低剂量降低血压。将上述三种代谢物的双重组合以输注形式施用于 SHR,以模拟真实的生物学情况。所有组合均显著降低了 SHR 的血压,但存在重要差异。DHPA 和 4MC 的作用温和且非常短暂。DHPA 与 3HPPA 的组合引起更明显的效果,但其持续时间也相对较短。3HPPA 和 4MC 的最后组合产生了持久的效果。总之,槲皮素代谢物的某些组合比单一代谢物具有更显著的降压作用。