In Vitro Schistosomicidal Activity of the Alkaloid-Rich Fraction from Ruta graveolens L. (Rutaceae) and Its Characterization by UPLC-QTOF-MS

Abstract

Schistosomiasis is a neglected tropical disease that affects million people worldwide, mostly in developing countries. Ruta graveolens (Rutaceae) is a plant used in folk medicine to treat several diseases, including parasitic infections. In this study, we reported the in vitro schistosomicidal activity of the R. graveolens extract (Rg) and its active fraction (Rg-FAE). Also, the characterization of Rg-FAE by UPLC-ESI-QTOF-MS analysis and its in vitro antileishmanial activity against Leishmania braziliensis were also performed. In vitro schistosomicidal assays were assessed against adult worms of S. mansoni, while cell viability against peritoneal macrophages was measured by MTT assay. Rg (100 μg/mL) exhibited noticeable schistosomicidal activity, causing 100% mortality and decreasing motor activity of all adult male and female schistosomes, but with low activity against L. braziliensis. After chromatographic fractionation of Rg, fraction Rg-FAE was obtained, showing high activity against adult schistosomes. UPLC-ESI-QTOF-MS analysis of Rg-FAE revealed the presence of eleven alkaloids and one furanocoumarin. No significant antileishmanial activity was found for Rg, while Rg-FAE exhibited activity against L. braziliensis promastigotes. We demonstrated, for the first time, that the R. graveolens extract (Rg) and its alkaloid-rich fraction (Rg-FAE) are active against adult worms of S. mansoni, with no significant cytotoxicity on macrophages. Our findings open the route to further antiparasitic studies with the active fraction of R. graveolens and its identified compounds, especially alkaloids.

Cardamonin Presents in Vivo Activity against Schistosoma mansoni and Inhibits Potato Apyrase

“…Although PZQ is effective in chronic infection, it has a limited effect on granulomatous lesions and against juvenile Schistosoma [3–5] . Additionally, the concerns over the emerging PZQ‐resistance development [6] have renewed interest in the search for new antischistosomal agents, particularly from natural sources [1,7,8] . Among natural compounds, chalcones have been shown promising antischistosomal activities [1,5,9,10] …”

Assessment of the In Vitro Antischistosomal Activities of the Extracts and Compounds from Solidago Microglossa DC (Asteraceae) and Aristolochia Cymbifera Mart. & Zucc. (Aristolochiaceae)

“…Parasites were kept for 48 h (37°C, 5% CO 2 ), and their viability was assessed via microscopic readout (Leica Microsystems, Wetzlar, Germany) [ 34 ]. Next, samples presenting antischistosomal activity were tested at lower concentrations, as described above, and each experiment was performed at least three times [ 35 ].…”

“…Mammalian Vero cells (African green monkey kidney fibroblast) used in this study were obtained from the American Type Culture Collection (ATCC CCL-81; Manassas, VA) and provided by Instituto Butantan (São Paulo, Brazil). Cytotoxicity of the samples was determined using the MTT assay [ 35 ]. The values of cytotoxic concentration reducing 50% of viable cells (CC 50 ) were obtained using GraFit Version 5 software.…”

Phenolic Characterization Using cLC-DAD Analysis and Evaluation of In Vitro and In Vivo Pharmacological Activities of Ruta tuberculata Forssk

“…Indeed, plants are considered a natural source for desired secondary metabolites such as phenolic compounds, flavonoids, tannins, terpens, essential oils, alkaloids and other bioactive compounds. The presence of these bioactive compounds is responsible for the antioxidant activity of Ruta tuberculata Forssk, which helps in the prevention against several types of diseases including preventing the development of chronic illness related to oxidative stress by inhibiting or reducing free radicals’ production, such as ROS and NOS [ 8 , 9 ]. Furthermore, the anti-inflammatory, anti-ulcer [ 2 , 5 ], neuroprotective and anti-cholinesterase activities of these bio-compounds were widely screened and documented [ 10 ].…”

“…In addition, several studies have reported the antioxidant, anti-inflammatory, anti-ulcer, hepatoprotective and anti-Alzheimer effects of Ruta plants [ 1 , 2 , 3 , 13 ]. In fact, the pharmacological proprieties of Ruta species could be attributed to the presence of diverse chemical classes of secondary biocompounds, including coumarine, alkaloid derivatives [ 8 , 14 ], essential oils [ 11 , 15 ], lignanes [ 16 ], polyphenols and flavonoids [ 3 , 17 , 18 ]. Based on the previous literature, there are no studies reported on phenolic characterization of the aerial parts of R. tuberculata growing in Algeria and their pharmacological activities.…”