Human helminthiasis affects approximately one in five people in the world and disproportionally affects the poorest and most deprived communities. Human angiostrongyliasis, caused by nematode , is a neglected emerging disease with escalating importance worldwide. Chemotherapy is the main control method for helminthiasis, but the therapeutic arsenal is limited. This study aimed to evaluate the antiparasitic and molecular properties of the major available anthelmintic drugs against . The first-stage larvae (L1), isolated from feces of an -infected rat, were exposed to a set of 12 anthelmintic drugs . The larvae were monitored, and the concentration- and time-dependent viability alterations were determined. From 12 anthelmintic drugs, six (ivermectin, salamectin, moxidectin, pyrantel pamoate, albendazole and levamisole) were identified to affect the viability of . The macrocyclic lactones (ivermectin, salamectin, moxidectin) and the imidazothiazole levamisole, were the most effective drugs, with IC ranging from 2.2 to 2.9 µM and a rapid onset of action. Albendazole, the most widely used anthelmintic in humans, had a slower onset of action, but an IC of 11.3 µM was achieved within 24 h. Molecular properties studies suggest that a less lipophilic character and low molecular weight could be favorable for the biological activity of the non-macrocyclic molecules. Collectively, our study revealed that macrocyclic lactones, levamisole, pyrantel pamoate, and albendazole are important anthelmintic agents against . The results of this study also suggest that L1 may be a particularly sensitive and useful model for anthelmintic studies.
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http://dx.doi.org/10.3389/fphar.2022.901459 | DOI Listing |
Biomed Chromatogr
February 2025
Guangdong Provincial key Laboratory of Veterinary Pharmaceutics Development and Safety Evaluation, South China Agricultural University, Guangzhou, China.
Praziquantel (PZQ) is the most effective treatment for schistosomiasis, commonly administered as a racemic mixture of the two enantiomers. Despite many reports on the pharmacokinetics of PZQ, the stereoselective pharmacokinetics of PZQ and its major metabolite 4-hydroxypraziquantel (4-OH-PZQ) remain poorly understood in goats. In this study, the chiral LC-MS/MS method was further optimized for separating and quantifying PZQ, trans-4-OH-PZQ, and cis-4-OH-PZQ and their enantiomers and then applied for the molecular pharmacokinetics of three analytes in black goat plasma.
View Article and Find Full Text PDFComb Chem High Throughput Screen
January 2025
KIPS, Shri Shankaracharya Professional University, Bhilai, Chhattisgarh, India.
The discovery of novel counteractive pharmaceuticals, which have recently generated much interest, has played a significant role in the development of drugs derived from herbal medicines or botanical sources. Paederia foetida (P. foetida) is one such example of a role in both traditional and traditional medicine.
View Article and Find Full Text PDFAAPS PharmSciTech
January 2025
School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing, 211198, China.
Albendazole serves as a broad-spectrum anthelmintic medication for treating hydatid cysts and neurocysticercosis. However, its therapeutic effectiveness is limited by poor solubility. Nanocrystals offer a promising technology to address this limitation by enhancing drug solubility.
View Article and Find Full Text PDFInt J Parasitol Drugs Drug Resist
December 2024
Bristol Veterinary School, University of Bristol, Bristol, BS40 5DU, UK.
Cyathostomins are the most abundant equid endoparasites globally. There are approximately fifty cyathostomin species and, whilst they occupy distinct niches within the large intestine, they are generally considered to share similar characteristics in terms of pathogenicity and response to drug treatment. There are three classes of anthelmintic licensed in the UK to treat cyathostomins (benzimidazoles, tetrahydropyrimidines and macrocyclic lactones) and cases of resistance have been documented for all classes.
View Article and Find Full Text PDFJ Biochem Mol Toxicol
January 2025
Chemistry Department, Faculty of Science, Ain Shams University, Cairo, Egypt.
Researchers are actively looking for novel anticancer medications because cancer is one of the leading causes of mortality worldwide. A fascinating area of study in medicinal chemistry is the screening of antioxidants for novel anticancer medicines, as antioxidants have lately been used as therapeutic candidates to combat a variety of ailments in aerobic species. Additionally, pyrazole-based heterocycle synthesis is a productive approach to the drug development process.
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