Department of Pharmacognosy and Molecular Basis of Phytotherapy, Faculty of Pharmacy with the Laboratory Medicine Division, Medical University of Warsaw, Ul. Banacha 1, 02-097 Warsaw, Poland; Microbiota Lab, Centre for Preclinical Studies, Medical University of Warsaw, Ul. Banacha 1b, 02-097 Warsaw, Poland.
Institute of Pharmaceutical Biology and Phytochemistry, University of Münster, Corrensstraße 48, 48149 Münster, Germany.
J Ethnopharmacol. 2021 Jun 28;274:114053. doi: 10.1016/j.jep.2021.114053. Epub 2021 Mar 19.
Phaseaoli pericarpium (bean pods) is a pharmacopeial plant material traditionally used as a diuretic and antidiabetic agents. Diuretic activity of pod extracts was reported first in 1608. Since then Phaseoli pericarpium tea figures in many textbooks as medicinal plant material used by patients.
Despite the traditional use of extracts from Phaseolium vulgaris pericarp, limited information is available on bioactivity, chemical composition, and bioavailability of such preparations. The following study aimed to investigate the phytochemical composition, the in vitro permeability of selected extract's constituents over the Caco-2 permeation system, and potential antivirulence activity against uropathogenic Escherichia coli of a hydroalcoholic Phaseoli pericarpium extract (PPX) in vitro to support its traditional use as a remedy used in urinary tract infections.
The chemical composition of the extract PPX [ethanol:water 7:3 (v/v)] investigated by using UHPLC-DAD-MS and subsequent dereplication. The permeability of compounds present in PPX was evaluated using the Caco-2 monolayer permeation system. The influence of PPX on uropathogenic E. coli (UPEC) strain NU14 proliferation and against the bacterial adhesion to T24 epithelial cells was determined by turbidimetric assay and flow cytometry, respectively. The influence of the extract on the mitochondrial activity of T24 host cells was monitored by MTT assay.
LC-MS investigation and dereplication, indicated PPX extract to be dominated by a variety of flavonoids, with rutin as a major compound, and soyasaponin derivatives. Rutin, selected soyasaponins and fatty acids were shown to permeate the Caco-2 monolayer system, indicating potential bioavailability following oral intake. The extract did not influence the viability of T24 cells after 1.5h incubation at 2 mg/mL and UPEC. PPX significantly reduced the bacterial adhesion of UPEC to human bladder cells in a concentration-dependent manner (0.5-2 mg/mL). Detailed investigations by different incubation protocols indicated that PPX seems to interact with T24 cells, which subsequently leads to reduced recognition and adhesion of UPEC to the host cell membrane.
PPX is characterised by the presence of flavonoids (e.g. rutin) and saponins, from which selected compounds might be bioavailable after oral application, as indicated by the Caco-2 permeation experiments. Rutin and some saponins can be considered as potentially bioavailable after the oral intake. The concentration-dependent inhibition of bacterial adhesion of UPEC to T24 cells justifies the traditional use of Phaseoli pericarpium in the prevention and treatment of urinary tract infections.
菜豆种皮(豆荚)是一种药典植物材料,传统上用作利尿剂和抗糖尿病药物。1608 年首次报道了荚提取物的利尿活性。从那时起,菜豆种皮茶就成为许多教科书中药用植物材料,供患者使用。
尽管传统上使用菜豆属植物种皮的提取物,但关于这些制剂的生物活性、化学成分和生物利用度的信息有限。本研究旨在调查水醇法菜豆种皮提取物(PPX)的植物化学成分、通过 Caco-2 渗透系统选择提取物成分的体外渗透性以及对尿路感染尿路致病性大肠杆菌的潜在抗毒力活性,以支持其作为治疗尿路感染的传统用途。
使用 UHPLC-DAD-MS 并随后进行去重复处理来研究提取物 PPX[乙醇:水 7:3(v/v)]的化学组成。使用 Caco-2 单层渗透系统评估化合物在 PPX 中的渗透性。通过浊度测定法和流式细胞术分别确定 PPX 对尿路致病性大肠杆菌(UPEC)菌株 NU14 增殖和细菌对 T24 上皮细胞粘附的影响。通过 MTT 测定法监测提取物对 T24 宿主细胞线粒体活性的影响。
LC-MS 研究和去重复处理表明,PPX 提取物主要由多种类黄酮组成,芦丁是主要化合物,还有大豆皂甙衍生物。芦丁、选定的大豆皂甙和脂肪酸被证明可穿透 Caco-2 单层系统,表明口服摄入后具有潜在的生物利用度。在 2mg/mL 和 UPEC 下孵育 1.5 小时后,提取物不会影响 T24 细胞的活力。PPX 以浓度依赖的方式显著降低 UPEC 对人膀胱细胞的粘附(0.5-2mg/mL)。通过不同孵育方案的详细研究表明,PPX 似乎与 T24 细胞相互作用,这导致 UPEC 对宿主细胞膜的识别和粘附减少。
PPX 的特点是存在类黄酮(如芦丁)和皂甙,其中一些化合物可能通过 Caco-2 渗透实验在口服后具有生物利用度。芦丁和一些皂甙在口服后可能被认为是有潜在生物利用度的。UPEC 对 T24 细胞粘附的浓度依赖性抑制证明了菜豆种皮在预防和治疗尿路感染中的传统用途。