Influence of Tilia tomentosa Moench Extract on Mouse Small Intestine Neuromuscular Contractility

Abstract

Functional gastrointestinal disorders (FGIDs) are characterized by abdominal pain, bloating and bowel disturbances. FGID therapy is primarily symptomatic, including treatment with herbal remedies. Flower extract of Tilia tomentosa Moench (TtM) is occasionally used as an anti-spasmodic in popular medicine. Since its effect on intestinal response is unknown, we evaluated the influence of TtM extract on small intestine contractility. Ileal preparations from C57BL/6J mice were mounted in organ baths to assess changes in muscle tension, following addition of TtM extract (0.5–36 μg/mL) or a vehicle (ethanol). Changes in contractile response to receptor- and non-receptor-mediated stimuli were assessed in ileal preparations pretreated with 12 μg/mL TtM. Alterations in the enteric nervous system neuroglial network were analyzed by confocal immunofluorescence. Increasing addition of TtM induced a marked relaxation in ileal specimens compared to the vehicle. Pretreatment with TtM affected cholinergic and tachykininergic neuromuscular contractions as well as K+-induced smooth muscle depolarization. Following incubation with TtM, a significant reduction in non-adrenergic non-cholinergic-mediated relaxation sensitive to Nω-Nitro-L-arginine methyl ester hydrochloride (pan-nitric oxide synthase inhibitor) was found. In vitro incubation of intestinal specimens with TtM did not affect the myenteric plexus neuroglial network. Our findings show that TtM-induced intestinal relaxation is mediated by nitric oxide pathways, providing a pharmacological basis for the use of TtM in FGIDs.

Spray-drying Microencapsulation of an Extract from Tilia tomentosa Moench Flowers: Physicochemical Characterization and in Vitro Intestinal Activity

“…This result agrees with previously published data about the thermal degradation of flavonoids [21,22]. Kinetic parameters of Q and K are presented in Table 2 and confirm that flavonols could be better protected acetylcholine, which interacts primarily with cholinergic receptors, expressed mainly on smooth muscle cells [8].…”

“…Based on these results, the quantitative data were reported as equivalents of these two flavonols. The contents of quercetin and kaempferol were 399 µg/mL ± 2.1 and 252 µg/mL ± 1.7 , respectively as recently found by Cerantola et al [8]. These values are in good accordance with the TFC of the extract, confirming that the protocol of Pekal et al [17] here adopted is suitable for quantifying the flavonols present in TtME.…”

“…It is well known that the main molecules associated with the biological activity of Tilia flower extract, and in particular with its effects on the nervous system, are mainly kaempferol and quercetin glycosides [7,15,16]. For this reason, the extract was analyzed by RP HPLC-DAD focusing the detection to flavonols as recently described [8]. Briefly, the analysis of the hydrolyzed extract allowed us to identify quercetin and kaempferol as the dominant aglycones (Fig.…”

“…Recently, we described the biological activity in vitro of a commercial TtM flower extract, providing a molecular basis for the use of TtM for the treatment of functional gastrointestinal disorders [8]. In the present study, we aimed at evaluating the effects of spray-drying encapsulation of the same extract using different starch-derived wall materials, i.e., two maltodextrins with different DE, i.e., MD12 and MD19, and octenyl succinic anhydride (OSA) modified starch (OSA-S), comparing their impact on the stability of TtM flower flavonols, and finally confirming the pharmacological properties of the microencapsulated powders (TtMP) on intestinal neuromuscular activity.…”

“…Tilia flowers are also used as diaphoretic, diuretic, and antispasmodic agents [ 4 ]. In recent years, numerous studies confirmed the anti-inflammatory [ 3 ], hepatoprotective [ 5 ], antinociceptive [ 6 ], anxiolytic [ 7 ], and antispasmodic properties of Tilia extracts [ 8 ]. These properties are frequently associated with the presence of specific flavonols, i.e ., phenolic compounds belonging to the broader group of flavonoids acknowledged for their numerous biological properties [ 9 ].…”