Schistosomiasis stands as one of the most significant parasitic diseases on a global scale, with approximately 250 million infections worldwide. It is imperative to address this pressing issue by developing new antischistosomal drugs. Chalcones have emerged as a promising class of natural compounds, demonstrating noteworthy effects observed in in vitro experiments with Schistosoma mansoni, and demonstrating the ability to inhibit SmNTPDases and apyrase from potatoes.
View Article and Find Full Text PDFWith praziquantel being the sole available drug for schistosomiasis, identifying novel anthelmintic agents is imperative. A chemical investigation of the fruiting body of the bioluminescent mushroom Berk. resulted in the isolation of new conjugated long-chain fatty acids (8,10,12,13)-12,13-dihydroxy-7-oxo-octadeca-8,10-dienoic acid () and (7,8,9,11)-7,8-dihydroxy-13-oxo-octadeca-9,11-dienoic acid () and three previously described compounds, (7,8,9)-7,8-dihydroxyoctadec-9-enoic acid (), (2)-dec-2-ene-1,10-dioic acid (), and a ketolactone marasmeno-1,15-dione ().
View Article and Find Full Text PDFSchistosoma mansoni, an intravascular parasitic worm and the causative agent of schistosomiasis, relies on its tegument (outer layer) for survival and host interaction. This study explored the morphology and mechanical properties of S. mansoni tegument using Atomic Force Microscopy (AFM).
View Article and Find Full Text PDFBackground: Schistosomiasis, caused by the parasitic blood fluke Schistosoma mansoni, is a significant global health concern, particularly in tropical and subtropical regions. The available chemotherapeutic drug is restricted to praziquantel with present problems related to efficacy, toxicity and resistance, justifying the search for new drugs. Different natural products, including γ-lactones, have demonstrated anthelmintic activity.
View Article and Find Full Text PDFSchistosomiasis, a neglected tropical disease impacting over 250 million individuals globally, remains a major public health challenge due to its prevalence and significant impact on affected communities. Praziquantel, the sole available treatment, highlights the urgency of the need for novel anthelmintic agents to achieve the World Health Organization (WHO) goal of schistosomiasis elimination. Previous studies reported the promising antiparasitic activity of different terpenoids against Sambon (Diplostomida: Schistosomatidae).
View Article and Find Full Text PDFBaccharis mattogrosensis is a species from Asteraceae which has been used in Brazilian folk medicine to treatment of several illnesses, including those caused by parasites. In the present work, the MeOH extract of aerial parts of B. mattogrosensis was subjected to chromatographic fractionation to afford three flavonoids: apigenin (1), quercetin (2), and kaempferol (3) as well as a mixture three chlorogenic acids: 3,4-O-dicaffeoylquinic (4), 3,5-O-dicaffeoylquinic (5), and 4,5-O-dicaffeoylquinic (6) acids.
View Article and Find Full Text PDFTo identify potential antischistosomal agents through 3D pharmacophore-based virtual screening of US FDA approved drugs. A comprehensive virtual screening was conducted on a dataset of 10,000 FDA approved drugs, employing praziquantel as a template. Promising candidates were selected and assessed for their impact on viability and using infected mice.
View Article and Find Full Text PDFInfections caused by parasitic helminths pose significant health concerns for both humans and animals. The limited efficacy of existing drugs underscores the urgent need for novel anthelmintic agents. Given the reported potential of antihistamines against various parasites, including worms, this study conducted a screening of clinically available antihistamines against -a nematode with widespread implications for vertebrate hosts, including humans.
View Article and Find Full Text PDFSchistosomiasis is a neglected disease of poverty that affects over 200 million people worldwide and relies on a single drug for therapy. The cathepsin B1 cysteine protease (SmCB1) of has been investigated as a potential target. Here, a structure-based pharmacophore virtual screening (VS) approach was used on a data set of approved drugs to identify potential antischistosomal agents targeting SmCB1.
View Article and Find Full Text PDFSchistosomiasis, a widespread parasitic disease caused by the blood fluke of the genus , affects over 230 million people, primarily in developing countries. Praziquantel, the sole drug currently approved for schistosomiasis treatment, demonstrates effectiveness against patent infections. A recent study highlighted the antiparasitic properties of amiodarone, an anti-arrhythmic drug, exhibiting higher efficacy than praziquantel against prepatent infections.
View Article and Find Full Text PDFSchistosomiasis is a major neglected disease that imposes a substantial worldwide health burden, affecting approximately 250 million people globally. As praziquantel is the only available drug to treat schistosomiasis, there is a critical need to identify new anthelmintic compounds, particularly from natural sources. To enhance the activity of different natural products, one potential avenue involves its combination with silver nanoparticles (AgNP).
View Article and Find Full Text PDFThe chemical classes of semicarbazones, thiosemicarbazones, and hydrazones are present in various compounds, each demonstrating diverse biological activities. Extensive studies have revealed their potential as schistosomicidal agents. Thiosemicarbazones, in particular, have shown inhibitory effects on Schistosoma mansoni's cathepsin B1 enzyme (SmCB1), which plays a crucial role in hemoglobin degradation within the worm's gut and its nutrition processes.
View Article and Find Full Text PDFThe impact of schistosomiasis, which affects over 230 million people, emphasizes the urgency of developing new antischistosomal drugs. Artificial intelligence is vital in accelerating the drug discovery process. We developed classification and regression machine learning models to predict the schistosomicidal activity of compounds not experimentally tested.
View Article and Find Full Text PDFSchistosomiasis, a parasitic disease affecting nearly 250 million individuals globally, poses a significant health challenge. With praziquantel being the sole available treatment and its limited efficacy in early stage infections, the identification of novel bioactive compounds becomes imperative. This study examines the potential of dehydrodieugenol B () and its methyl ether (), derived from the leaves of the Brazilian plant (Lauraceae), in combatting infections through a preclinical approach.
View Article and Find Full Text PDFSchistosomiasis is a parasitic disease that afflicts approximately 250 million people worldwide. There is an urgent demand for new antiparasitic agents because praziquantel, the only drug available for the treatment of schistosomiasis, is not universally effective and may derail current progress toward the WHO goal of eliminating this disease as a public health problem by 2030. Nifuroxazide (NFZ), an oral nitrofuran antibiotic, has recently been explored to be repurposed for parasitic diseases.
View Article and Find Full Text PDFJ Ethnopharmacol
September 2023
Ethnopharmacological Relevance: Roots of Pothomorphe umbellata (L.) Miq. are used in traditional medicine of Africa and South America for the treatment of malaria and helminthiasis.
View Article and Find Full Text PDFTo formulate a carvacryl acetate nanoemulsion (CANE) and test its antischistosomal activity. CANE was prepared and tested on adult worms and both human and animal cell lines. Next, CANE was administered orally to mice infected with either a prepatent infection or a patent infection of .
View Article and Find Full Text PDFCurr Top Med Chem
July 2023
Nitroaromatic compounds have been used for treating parasitic diseases since the 1960s. Pharmacological alternatives to treat them are under observation. However, for the most neglected diseases, such as those caused by worms and less known protozoans, nitro compounds are still among the drugs of choice, despite their well-known collateral effects.
View Article and Find Full Text PDFInfections caused by parasitic helminths rank among the most prevalent infections of humans and animals. Toxocariasis, caused by nematodes of the genus Toxocara, is one of the most widespread and economically important zoonotic parasitic infections that humans share with dogs and cats. Despite the completion of the Toxocara canis draft genome project, which has been an important step towards advancing the understanding of this parasite and the search for drug targets, the treatment of toxocariasis has been dependent on a limited set of drugs, necessitating the search for novel anthelmintic agents, specially against Toxocara larvae in tissues.
View Article and Find Full Text PDFSchistosomiasis, a parasitic disease caused by the blood fluke of the genus Schistosoma, affects over 230 million people, especially in developing countries. Despite the significant economic and public health consequences, only one drug is currently available for treatment of schistosomiasis, praziquantel. Thus, there is an urgent demand for new anthelmintic agents.
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