Usnic acid potassium salt from Cladonia substellata (Lichen): Synthesis, cytotoxicity and in vitro anthelmintic activity and ultrastructural analysis against adult worms of Schistosoma mansoni

Abstract

We report for the first time the in vitro effect of Potassium Salt, derived from Usnic Acid (PS-UA), isolated from the lichen Cladonia substellata Vanio, on couples of Schistosoma mansoni. As schistosomicide parameters, we evaluated mortality, motility, cell viability of the worms and tegument changes by scanning electron microscopy (SEM). Exposure to a concentration of 100 μM caused 75% mortality after 3 h. After 6 h, changes in motility in concentrations of 50 and 25 μM are evidenced. After 12 h and 24h, the concentrations of 50 and 100 μM caused 6.25% and 87.5% and 50% and 100% mortality, respectively. PS-UA reduced the cell viability of the worms by 27.36% and 52.82% at concentrations 50 and 100 μM, respectively. Through SEM we observed progressive dose-and time-dependent, alterations such as swelling, blisters, dorsoventral contraction, erosion until disintegration of the tubercles in the tegument of male and female. PS-UA did not alter the viability of human peripheral blood mononuclear cells and showed high selectivity indices (IC₅₀ > 200 μM). Our results indicate that PS-UA represents a possible candidate for a new anthelmintic drug in the control of schistosomiasis.

Keywords: Anthelmintic activity; Neglected diseases; Schistosoma mansoni; Schistosomiasis; Ultrastructural tegument analysis; Usnic acid potassium salt.