Natural Products & Food Research and Analysis (NatuRA), University of Antwerp, Universiteitsplein 1, 2610, Antwerp, Belgium.
Natural Products & Food Research and Analysis (NatuRA), University of Antwerp, Universiteitsplein 1, 2610, Antwerp, Belgium.
J Ethnopharmacol. 2022 Mar 1;285:114860. doi: 10.1016/j.jep.2021.114860. Epub 2021 Nov 22.
Herniaria hirsuta is traditionally used in Moroccan folk medicine for treatment of urinary stones and as a diuretic. It is rich in saponins, which are known to be deglycosylated in the colon, whereafter aglycones such as medicagenic acid are absorbed and further metabolized in the liver.
A sample of hepatic metabolites of medicagenic acid, with medicagenic acid glucuronide as the most abundant one, was evaluated for in vitro activity against urinary stones. A crystallization assay and a crystal-cell interaction assay were used to evaluate in vitro activity of hepatic metabolites of medicagenic acid on CaCO (calciumoxalate) crystals, present in the majority of urinary stones.
In the crystallization assay the effects on nucleation of Ca and CO and aggregation of the CaCO crystals are studied. In the crystal-cell interaction assay crystal retention is investigated by determining the amount of Ca bound to injured monolayers of MDCK I cells.
Results of the crystallization assay showed a tentative effect on crystal aggregation. The crystal-cell interaction assay showed a significant inhibition of crystal binding, which may reduce crystal retention in the urinary tract.
As both formation of crystals by inhibiting aggregation and retention of crystals is affected, the beneficial effect of H. hirsuta against urinary stones may at least in part be attributed to medicagenic acid metabolites, indicating that saponins containing medicagenic acid may act as prodrugs.
Herniaria hirsuta 在摩洛哥民间医学中传统上用于治疗尿路结石和利尿。它富含皂苷,已知在结肠中发生去糖基化,此后糖苷配基如羽扇豆酸被吸收并在肝脏中进一步代谢。
评估羽扇豆酸苷元作为最丰富的一种肝代谢产物对尿路结石的体外活性。结晶试验和晶体-细胞相互作用试验用于评估羽扇豆酸肝代谢产物对存在于大多数尿路结石中的 CaCO(草酸钙)晶体的体外活性。
在结晶试验中,研究了对 Ca 和 CO 的成核以及 CaCO 晶体聚集的影响。在晶体-细胞相互作用试验中,通过确定结合到受损的 MDCK I 细胞单层上的 Ca 量来研究晶体保留。
结晶试验结果表明对晶体聚集有暂定影响。晶体-细胞相互作用试验显示出对晶体结合的显著抑制作用,这可能减少晶体在泌尿道中的保留。
由于形成晶体的抑制聚集和晶体保留都受到影响,H. hirsuta 对尿路结石的有益作用至少部分归因于羽扇豆酸代谢物,表明含有羽扇豆酸的皂苷可能作为前药发挥作用。