Licochalcone A-loaded solid lipid nanoparticles improve antischistosomal activity in vitro and in vivo

Aim: To isolate licochalcone A (LicoA) from licorice, prepare LicoA-loaded solid lipid nanoparticles (L-SLNs) and evaluate the L-SLNs in vitro and in vivo against Schistosoma mansoni. Materials & methods: LicoA was obtained by chromatographic fractionation and encapsulated in SLNs by a modified high shear homogenization method. Results: L-SLNs showed high encapsulation efficiency, with satisfactory particle size, polydispersity index and Zeta potential. Transmission electron microscopy revealed that L-SLNs were rounded and homogenously distributed. Toxicity studies revealed that SLNs decreased the hemolytic and cytotoxic properties of LicoA. Treatment with L-SLNs showed in vivo efficacy against S. mansoni. Conclusion: L-SLNs are efficient in reducing worm burden and SLNs may be a promising delivery system for LicoA to treat S. mansoni infections.

Antibacterial, Antibiofilm, and Antischistosomal Activity of Montrichardia linifera (Arruda) Schott (Araceae) Leaf Extracts

With a broad ethnopharmacological tradition in Brazil, Montrichardia linifera has been reported as a potent antirheumatic, antimicrobial, and antiprotozoan agent. However, there is a lack of studies on its effect on bacterial biofilm formation and Schistosoma mansoni worms. This study reports the effects of antibacterial, antibiofilm, and antischistosomal properties of leaf extracts of M. linifera. Phytochemical screening and identification of the main compounds of the extracts were performed. All the extracts evaluated showed antibacterial activity at the concentrations tested. We checked for the presence of flavonoids and derivatives of phenolic acids by the presence of spectra with bands characteristic of these classes in the sample analyzed. The antibacterial assays showed that the best MICs corresponded to 125 µg/mL against Enterococcus faecalis ATCC 29212 in all fractions. The ethanolic and methanolic extracts showed the ability to inhibit biofilm of Staphylococcus aureus ATCC 25123. For the antischistosomal activity, only the acetone and ethyl acetate extracts had a significant effect against helminths, with potent activity at a concentration of 50 µg/mL, killing 100% of the worms after 72 h of incubation. The M. linifera leaf extracts showed antibacterial activity, biofilm inhibition capacity, and anthelmintic activity against S. mansoni.

Effects of multiple doses of simvastatin and artesunate monotherapy on SCHISTOSOMA MANSONI adult worms during infection in hyperlidemic mice

A single dose of simvastatin and of artesunate monotherapy cause damage to the reproductive system of schistosomes as well as severe tegumental damage in male worms recovered from mice fed high-fat chow. This study aims to investigate whether treatment with multipledose regimes may offer more antischistosomal activity advantages than single daily dosing in mice fed high-fat chow. For this purpose, nine weeks post-infection, Swiss Webster mice were gavaged with simvastatin (200 mg/kg) or artesunate (300 mg/kg) for five consecutive days and euthanized two weeks post-treatment. Adult worms were analyzed using brightfieldmicroscopy, confocal microscopy and scanning electron microscopy, presenting damages caused by simvastatin and artesunate to the reproductive system of males and females as well as tegument alterations, including peeling, sloughing areas, loss of tubercles, tegumental bubbles and tegument rupture exposing subtegumental tissue. The overall findings in this study revealed the potential antischistosomal activity of simvastatin and artesunate against Schistosoma mansoni adult worms, in addition to showing that multiple doses of either monotherapy caused severe damage to the tegument.KEY WORDS: Schistosoma mansoni; hyperlipidemia; simvastatin; artesunate; microscopy.

The in Vitro Antischistosomal Activity and Genotoxicity of the Active Ingredients of Allium sativum (allicin) and Curcuma longa (curcumin)

Background: In this study, we assessed the in vitro antischistosomal activity of the active ingredients of Allium sativum (allicin) and Curcuma longa (curcumin) on Schistosoma mansoni. Methods: This study was conducted in Faculty of Science, Port said University, Egypt (2018). Adult worms were exposed to a range of concentrations of AL or CU, and worm survival was assessed 24 h post-exposure to calculate the lethal concentration of the compounds. Scanning electron microscopy was used to assess ultrastructural changes in the surface of AL- or CU- treated worms. The genotoxicities of AL and CU on S. mansoni were determined by DNA fragmentation analysis. Results: We determined the concentrations of AL and CU required to kill 50% of S. mansoni (LC50). The LC50 of AL was 8.66 µL/mL, whereas 100% mortality of S. mansoni was achieved by AL at concentrations of 50 µL/mL. The LC50 of CU was 87.25 µL/mL, with the highest mortality of 91.3% seen after 24 h exposure to 100 µg/mL CU. Ultrastructural studies revealed that exposure to either AL or CU led to mild or severe surface damage to S. mansion, respectively. The degree of damage in the worms was sex-dependent. Interestingly, while CU exposure resulted in DNA fragmentation in S. mansoni worms, we observed no genotoxic effects of AL. Conclusion: Both AL and CU exhibit antischistosomal activity; the study provided evidence suggesting that these compounds act through distinct mechanisms. These promising results encourage further investigation into these compounds as potential antischistosomal agents, either alone or as complementary treatments to praziquantel.

In Vitro Antischistosomal Activity of the Argemone mexicana Methanolic Extract and Its Main Component Berberine

Background: Schistosomiasis has been identified as a major public health problem in tropical countries. The present study aimed to investigate the schistosomicidal effects of the methanolic extract of Argemone mexicana L. and its active component, berberine against Schistosoma mansoni on in-vitro experiments. Methods: S. mansoni adults were used. Various concentrations of the methanolic extract (10 - 200 µg/ml) and berberine (2.5 - 50 µM) were tested from 24 to 72 h. The viability of S. mansoni was confirmed with an invertoscope-microscope. Furthermore, cytotoxic (Hemolysis test), and antioxidant (DPPH radical scavenging assay) capacities were determined. Results: The viability tests on S. mansoni showed that A. mexicana at 50 μg/mL is lethal at 48 h and berberine at 10 μM is lethal at 24 h. The hemolytic activity at 1,000 μg/mL was 2.9% for A. mexicana and 90.2% for berberine. The antioxidant capacities shown by A. mexicana and berberine, were EC50 156.3 and 84.1 μg/mL, respectively. Conclusion: The extract of A. mexicana and berberine demonstrated high antischistosomal activities in low concentration and short exposure time on the in-vitro model.

Antischistosomal Activity of Zingiber officinale, Piper nigrum, and Coriandrum sativum Aqueous Plant Extracts on Hamster Infected with Schistosoma mansoni

Schistosomiasis continues to affect the health and quality of life of millions of people around the world. Schistosomiasis has been ranked the second disease after malaria in terms of importance as a targeted tropical disease. Praziquantel (PZQ) is the only drug approved by the World Health Organization (WHO) for the treatment of schistosomiasis. Being the only drug, parasite resistance to this drug has developed. Therefore, the search for new alternatives has been the goal of many researchers. In this study, the effects of aqueous extracts of Zingiber officinale, Piper nigrum, and Coriandrum sativum on Schistosoma mansoni infected golden hamsters (Egyptian strain) were evaluated in vitro and in vivo at different doses of 500, 250, 125, 62.5, and 31.25 μg/ml. In vitro, adult worms of S. mansoni were tested in RPMI-1640 medium for 48 hrs. The results showed that the concentrations 500, 250, and 125 μg/ml of Zingiber officinale and Piper nigrum caused dead of 100% of adult worms within 6 and 12 hrs of incubation, respectively. Although, aqueous extract of Coriandrum sativum at concentrations 500, 250, and 125 μg/ml resulted dead of 100% parasites after 12 to 24 hrs of incubation. In conclusion, Zingiber officinale and Piper nigrum showed efficacy against schistosomiasis in both in vitro and biological experiments of Egyptian schistosome strain, while Coriandrum sativum gave less effective results than the previous ones. Therefore, Zingiber officinale and Piper nigrum may become an innovative treatment for schistosomiasis.