Department of Pharmacognosy and Molecular Basis of Phytotherapy, Centre for Preclinical Studies, Faculty of Pharmacy with the Laboratory Medicine Division, Medical University of Warsaw, Ul. Banacha 1, 02-097, Warsaw, Poland; MicrobiotaLab, Centre for Preclinical Studies, Medical University of Warsaw, Ul. Banacha 1b, 02-097, Warsaw, Poland.
Department of Pharmacognosy and Molecular Basis of Phytotherapy, Centre for Preclinical Studies, Faculty of Pharmacy with the Laboratory Medicine Division, Medical University of Warsaw, Ul. Banacha 1, 02-097, Warsaw, Poland.
J Ethnopharmacol. 2021 Jun 12;273:113924. doi: 10.1016/j.jep.2021.113924. Epub 2021 Feb 17.
Solidago virgaurea L. (also known as European goldenrod) is a pharmacopoeial plant material popularly used by patients in the form of an infusion. It was traditionally used in Europe and North America for the treatment of urinary tract conditions. It is also reported as a topical agent for skin disorders.
Gut microbiota metabolism plays a crucial role in the bioavailability of natural products contained in plant extracts taken orally. The aim of the current study was to establish the biotransformation of compounds contained in an infusion from goldenrod using human and piglet fecal microbiota in vitro. The permeability of unmetabolized natural products and gut microbiota metabolites was evaluated using a Caco-2 cell model. Preliminary anti-inflammatory assays of raw extract using human neutrophils were also established.
An infusion was prepared from Solidaginis virgaureae herba commercially available on the market. The characterization of the raw extract was performed by UHPLC-DAD-MS method. The infusion was incubated with human or swine fecal samples in anaerobic conditions. Metabolism products were analyzed and identified by UHPLC-DAD-MS technique. The permeability of the natural products contained in the raw infusion and after metabolism was checked by UHPLC method. The influence of raw extracts on proinflammatory functions of human neutrophils after LPS stimulation was established by flow cytometry and ELISA.
The experiments showed that goldenrod infusion contains mainly caffeoylquinic acid derivatives, flavonoids, and some phenylpropanoids. Natural products present in the extract were transformed by human and swine microbiota to smaller molecules mainly phenylpropanoid acid derivatives. The permeability assays showed that most of the parental compound present in the infusion cannot cross the gut epithelial barrier. In contrast, metabolites were able to cross the Caco-2 monolayer. Depending on the structure, different possible mechanisms of transport were observed. The infusion did not significantly influence the proinflammatory functions of human neutrophils.
Following oral administration of goldenrod infusion, phytochemicals are prone to undergoing metabolism by gut microbiota to smaller phenylpropionic acid derivatives that can be bioavailable after crossing the gut epithelial barrier to be further metabolized and distributed. Detected metabolites should be considered as potentially active compounds responsible for the bioactivity of the raw plant material in vivo.
一枝黄花（又名欧洲一枝黄花）是一种药典植物材料，深受患者欢迎，以输液的形式使用。它在欧洲和北美的传统用途是治疗尿路感染。也有报道称其为皮肤疾病的局部制剂。
肠道微生物群代谢在口服植物提取物中天然产物的生物利用度中起着至关重要的作用。本研究的目的是使用人粪和猪粪微生物群在体外建立一枝黄花输液中所含化合物的生物转化。使用 Caco-2 细胞模型评估未代谢的天然产物和肠道微生物群代谢产物的通透性。还建立了使用人嗜中性粒细胞对原始提取物进行初步抗炎测定的方法。
从市售的一枝黄花中制备输液。使用 UHPLC-DAD-MS 方法对原始提取物进行了表征。将输液在厌氧条件下与人或猪粪便样品孵育。通过 UHPLC-DAD-MS 技术分析和鉴定代谢产物。通过 UHPLC 法检查原始输液和代谢后的天然产物的通透性。通过流式细胞术和 ELISA 建立原始提取物对 LPS 刺激后人嗜中性粒细胞的促炎功能的影响。
实验表明，一枝黄花输液主要含有咖啡酰奎宁酸衍生物、类黄酮和一些苯丙素。提取物中存在的天然产物被人及猪的微生物群转化为小分子的主要苯丙素酸衍生物。通透性测定表明，输液中存在的大多数母体化合物不能穿过肠道上皮屏障。相比之下，代谢产物能够穿过 Caco-2 单层。根据结构，观察到不同的可能转运机制。输液对人嗜中性粒细胞的促炎功能没有显著影响。
一枝黄花输液口服后，植物化学物质容易被肠道微生物群代谢为较小的苯丙酸衍生物，这些衍生物可以在穿过肠道上皮屏障后成为生物利用度，然后进一步代谢和分布。检测到的代谢物应被视为潜在的活性化合物，负责体内原始植物材料的生物活性。
