Spasmolytic Activity of Gentiana lutea L. Root Extracts on the Rat Ileum: Underlying Mechanisms of Action

Abstract

The roots of Gentiana lutea L. are utilized in the preparation of various beverages and herbal remedies, serving as a traditional remedy for gastrointestinal ailments. The spasmolytic activity that could substantiate the traditional use of G. lutea root had not been investigated. The main objective goal of the study was to determine the validity of its use as a traditional remedy. The extraction of G. lutea root was performed using a 50% hydroethanolic solvent with three different extraction techniques: ultrasound-assisted extraction (UAE), heat-assisted extraction, and percolation. The spasmolytic activity was tested on isolated rat ileum. The mechanism of action was monitored using the models of spontaneous contractions and acetylcholine-, histamine-, CaCl2-, Bay K8644-, L-NAME-, ODQ-, apamin-, BaCl2-, charybdotoxin-, glibenclamide-, TRAM-34-, and quinine-modified contractions. UAE, having the best bioactivity, was further subjected to a liquid–liquid extraction fractionation. HPLC phytochemical analysis was performed for all tested extracts and fractions. Gentian root extracts were rich in secoiridoids, xanthones, and flavonoids. The UAE has shown better results on spontaneous contractions in comparison to its fractions, leading to the more detailed testing of its spasmolytic mechanism of activity. The extract’s activity is primarily mediated through intermediate conductance Ca2+-activated K+ channels, ATP-sensitive K+ channels, voltage-sensitive K+ channels, and mechanisms that activate Ca2+ channels. Overall, the G. lutea root shows great potential in the treatment of spasmodic gastrointestinal ailments.

Spasmolytic, Antimicrobial, and Antioxidant Activities of Spray-Dried Extracts of Gentiana asclepiadea L. with In Silico Pharmacokinetic Analysis

“…Finally, consistent with our findings, Kitić et al ( 2024) reported that the spasmolytic activity of Gentiana lutea root extract was mediated through multiple pathways, with the primary mechanism involving the direct activation of Ca 2+ and K + channels [34].…”

“…Papaverine (0.01–3 µg/mL), an alkaloid compound of proven spasmolytic activity, was used as a positive control. Guided by the results of this set of experiments (absence of spasmolytic activity of WP), in the following experiments performed to elucidate the mechanisms of spasmolytic activity, only the effects of E and EWP were examined [ 34 ].…”

“…The obtained results of ileum contractility in the presence of the tested sample were compared with the control curve and the effect of the sample was expressed as a percentage of contractility. Atropine, a non-selective blocker of muscarinic receptors, was tested at a concentration of 140 nmol/L as a positive control [ 34 ].…”

“…The spasmolytic effects of samples on the rat ileum, previously treated with KCl, are expressed as a percentage of the control response. Verapamil, as a proven antagonist of calcium channels, was used as a positive control and was tested at concentrations from 0.015 to 1.5 µg/mL [ 34 ].…”

“…The spasmolytic activity was investigated in the isolated rat ileum according to the experimental procedure described by Kitić et al (2024) [34]. Immediately after sacrificing the animals, the abdomen was opened and the ileum was dissected.…”