Antibiotics & Antibiotic Resistance

Purpose: The purpose of this work was to evaluate the antidiarrheal, vasorelaxant, sedative, anxiolytic, and antidepressant actions of tilifodiolide (TFD), a natural diterpene obtained from Salvia tiliifolia Vahl (Lamiaceae).

Methods: The antidiarrheal activity of 1-50mg/kg TFD was assessed with the castor oil test, the charcoal meal test, and the castor oil induced-enteropooling. The relaxation effect of TFD (0.9-298µM) was carried out using smooth muscle tissues from rats, and its mechanism of action was evaluated using different inhibitors involved in muscle relaxation. The sedative, anxiolytic, and antidepressant effects of 1-100mg/kg TFD were calculated with the pentobarbital-induced sleeping time assay, the elevated plus maze test, the light-dark test, the cylinder exploratory test, and the forced swimming test.

Key findings: TFD exhibited anti-diarrheal activity (ED50=10.62mg/kg p.o.) and vasorelaxant effects (EC50=48±3.51µM). The coadministration of TFD with L-NAME or ODQ reverted the vasorelaxant action exposed by TFD alone. TFD exerted anxiolytic activity in all tests and decreased the time of immovability in the forced swimming test. 

Conclusions: TFD exerted antidiarrheal activity by decreasing the intestinal fluid accumulation, and vasorelaxant effects, mediated by NO and cGMP, in isolated aortic rings with intact-endothelium. TFD showed anxiolytic and antidepressant effects in mice.