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Human onchocerciasis is caused by the filarial worm. Onchocerca volvulus is a parasite that forms nodules under the skin. The aim of this work was to assess the nematicidal activities of Aloe vera on Onchocerca ochengi and Caenorahbditis elegans and to determine the phytochemical compounds. Nodules were collected from the umbilical region of infected cattle, dissected and male worms were cultured in RPMI-1640. Worms were incubated with different concentrations of A. vera extracts in RPMI-1640 and M9-buffer. Polyphenol, tannin and flavonoid contents of extract were determined by using gallic acid and rutin as standards. The anthelmintic effect of A. vera extract against O. ochengi was concentration dependent with LC50 of 20.71 µg/mL and 11.75 µg/mL after 48 and 72 h respectively. A. vera extract exerted concentration dependent lethal effects (LC50 = 2747 and LC50 = 31,937 µg/mL) against C. elegans (Wild Type). Methanolic-methylene chloride (MeOH–CH2Cl2) of A. vera extract exhibited high DPPH activity with an IC50 value of 15 µg/mL and 9 µg/mL for ascorbic acid. The highest activity in adult worms was observed with the MeOH (100: 0) and AcOEtMeOH fractions with LC50 values of 12.82 and 15.50 µg/mL respectively. EcOEtMeOH (8:2 v/v) was more effective (LC50 = 250 µg/mL) on WT of C. elegans. A. vera contains polyphenols (1015.05 and AcOEtMeOH = 893.60), flavonoids (25.35 and MeOH = 225.76) and tannins (401.37 and Hex = 788.89). A. vera showed in vitro nematicidal activity against O. ochengi and C. elegans. A. vera could be used as an alternative anthelmintic for onchocerciasis treatment. [ABSTRACT FROM AUTHOR]

This study focuses on developing novel antimicrobials to combat drug‐resistant pathogens, addressing compounds failing clinical trials due to inadequate physicochemical properties. Sixteen imidazolidine‐4‐one derivatives were synthesized by extensive evaluation using molecular docking, absorption, distribution, metabolism, excretion (ADME) predictions, and antimicrobial testing. Molecular docking studies conducted with Schrödinger's Glide revealed that compounds S4 and G8 exhibited superior docking scores of −7.839 and −7.776, respectively. The G series outperformed the S series in scores. ADME analysis confirmed all compounds adhered to Lipinski's rule of five. In addition, IR and NMR provided details about the structure of the compounds. Antimicrobial activity was assessed against Escherichia coli, Staphylococcus aureus, and Candida albicans, with compounds G2 and S2 showing exceptional minimum inhibitory concentration (MIC) values of 6.25 μg/mL against E. coli. S2 also demonstrated impressive activity against S. aureus (MIC 3.12 μg/mL), and S4 exhibited potent activity against C. albicans (MIC 0.8 μg/mL) than fluconazole (1.6 μg/mL). Additionally, antihelmintic activity was evaluated, with G1, G3, G8, S2, S4, S7, and S8 showing effective paralysis and death time 20 min and below at 50 mg/mL concentration. These results underscore the potential of new imidazolidine‐4‐one derivatives as suitable sources to develop a drug candidate to treat resistant infections. [ABSTRACT FROM AUTHOR]

Introduction: Baccaurea ramiflora Lour, locally known as Latkan, is a popular fruit in Bangladesh used for its anthelmintic and analgesic activities. This study aimed to compare the anthelmintic and analgesic activities of different solvent fractions of crude extract from B. ramiflora fruit seed and peel. Methods: Cold extraction followed by the Kupchan scheme was employed to obtain various solvent fractions. In vivo anthelmintic activity was assessed using Pheretima posthuman, while analgesic activity was evaluated via writhing and tail immersion tests on Swiss albino mice. Molecular docking studies of four reported phytochemicals from B. ramiflora on analgesic and anti-parasitic protein targets were conducted using the PyRx. Results: Results revealed significant anthelmintic activity in seed petroleum ether, chloroform, ethyl acetate, and acetone solvent fractions in a dose-dependent manner, with acetone extract exhibiting the highest activity. Writhing was significantly reduced in all seed and peel extracts, with the highest inhibition observed at 200 mg/kg dose. Moreover, seed chloroform and peel ethyl acetate extracts displayed the longest pain reaction times in the tail immersion model (6.924 ± 0.264 seconds and 6.562 ± 0.157 seconds, respectively). Molecular docking revealed strong binding interactions of Baccariminose C and D (≥8.2 kcal/mol) with all studied protein targets. Conclusion: This study confirms the anthelmintic and analgesic activities of B. ramiflora fruit peel and seed extracts. These results contribute to the understanding of the medicinal properties of B. ramiflora and its potential applications in pharmaceuticals.

Introduction: Macropanax dispermus is an ethnomedicinal plant, which has been shown to have pharmacological effects against inflammation. Inflammation is also associated with diabetic-related complications. In addition, the indigenous people used this plant to cure numerous digestive system disorders. These ethnomedicinal uses have inspired the current research to focus on determining the biological potential of the crude methanol extract of its leaves (MDML) and stem barks (MDMS) against morbid diseases such as diarrhea, helminthiasis, and diabetes mellitus related to hyperglycemia. This study also identified the functional groups present in MDML which could correlate the presence of different phytochemicals responsible for biological activities. Methods: The hypoglycemic activity and antidiarrheal tests were done on Swiss albino mice through an oral glucose tolerance test (OGTT) and castor-oil-induced diarrhea, respectively. The anthelmintic test was done in vitro on Pheretima posthuma. The functional groups were identified by using Fourier-transform infrared (FTIR) spectroscopy. Results: Here, MDML at 400 mg/kg exhibited a significant (P

One of the most severe parasite infections to ever plague animals, paramphistomosis is particularly devastating in tropical and subtropical areas and causes significant economic losses to the world's food industry and poor animal health. In the present study potency of the crude extract and green synthesized silver nanoparticles from fresh and mature Mammea americana L. leaves was evaluated on trematode Paramphistomum cervi, collected from the infected rumen of the cow (Bos indicus) in 0.9% phosphate-buffered saline (PBS). The crude extract at five dose levels (1 mL, 2 mL, 3 mL 4 mL, and 5 ml), and silver nanoparticles (AgNps) at the five dose levels (10 mg/mL, 30 mg/mL, 50 mg/mL, 70 and 90 mg/mL) were applied. The synthesized AgNPs were characterized using UV–VIS spectrophotometry, X-ray diffraction (XRD), field emission-scanning electron microscopy (FE-SEM), transmission electron microscopy (TEM), and Fourier Transform Infrared Spectroscopy (FTIR) analysis. Characterization studies of AgNPs revealed the synthesis of stable, crystalline AgNPs measuring an average size of 20–50 nm. The efficacy was evaluated based on the spontaneous movement reduction and death of P. cervi. Maximum anthelmintic activity was found at the dose of 5 mL of crude extract and 90 mg/mL of AgNPs of M. americana leaves. The scanning electron micrograph study of treated helminths of crude and AgNps revealed conspicuous distortion on the surface architecture. It also showed shrinkage of the whole body and severe damage on both suckers (anterior and posterior). AgNPs caused more shredded and torn tegumental surfaces with loss of tegumental papillae compared to untreated. Thus, this study confirmed that the M. americana leaves extract and synthesized AgNPs can be a potential alternative herbal drug in traditional folklore medicine against serious helminth infections in our livestock industry. [ABSTRACT FROM AUTHOR]

The present research was conducted to investigate the anthelmintic potential of crude extracts from the stem, leaves, and flowers of two common weeds, Oxalis corymbosa DC. & O. pes-caprae L., of family Oxalidaceae, against gastrointestinal parasitic worm (helminth), Haemonchus contortus in polar & non-polar solvents, i.e. distilled water, ethanol, chloroform, and n-hexane. The time taken for the paralysis and ultimately the death of the worms by the crude extracts of both plants was found reasonably well as compared to that of the standard drug, Albendazole. However, the crude extracts of stem, leaves, and flowers of O. corymbosa in ethanol were found to be more effective than those of O. pes-caprae with paralysis (17.33, 14.20, and 10.13 min, respectively) and death time (18.16, 15.10, and 9.33 min, respectively) while Albendazole recorded paralysis and death time as 59.10 and 60.06 min, respectively. Likewise, the anthelmintic potential of stem, leaves, and flowers extracts of O. corymbosa in n-hexane, chloroform, and distilled water was noticeably higher such as in n-hexane, stem, leaves and flowers extracts of O. corymbosa had paralysis (29.20, 27.33 and 28.0, respectively) and death time (30.20, 30.16 and 30.06, respectively) while the same extracts of O. pes-caprae had paralysis (37.43, 36.40, and 34.06, respectively) and death time (39.10, 36.83, and 35.33, respectively). The results indicated sound anthelmintic potential of the two weeds. [ABSTRACT FROM AUTHOR]

Anthelmintic resistance in livestock animals has been spreading across the world in prevalence and severity. As a result, researchers are exploring alternative strategies to combat this issue, and one promising avenue is the utilization of medicinal plants. This study aims to investigate the anthelmintic efficacy of the crude ethanolic extract (CEE) derived from the leaves of Juglans regia against one of the most detrimental nematode parasites affecting poultry, namely Ascaridia galli (A. galli). For the in vitro studies, adult A. galli worms were collected from the naturally infected chickens and the efficacy of CEE was measured at the concentration of 25, 50, and 100 mg/ml using adult worm motility inhibition (WMI) assay. In addition, levamisole (0.55 mg/ml) was used as the positive control. Likewise, Phosphate buffered saline (PBS) was used as the negative control. For the in vivo studies, CEE of J.regia at the doses of 500, 1000, and 2000 mg/kg were evaluated in chickens experimentally infected with A. galli. The anthelmintic efficacy was monitored using faecal egg count reduction (FECR) and worm count reduction (WCR) assays. In vitro studies revealed significant (P < 0.001) anthelmintic effects of CEE of J.regia on the motility of A. galli worms at different hours post-exposure. At the concentration of 100 mg/ml, CEE resulted in 96.5% inhibition of worm motility at 24 h post-exposure. While the synthetic anthelmintic drug, levamisole caused the highest inhibition of worm motility (100%) at the same time period. The in vivo anthelmintic activity of CEE of J. regia demonstrated a maximum effect on day 14 post-treatment by inducing 67.28% FECR and 65.03% WCR. We observed no significant difference (P > 0.05) in worm counts between the negative control group and the chickens treated with CEE at the dosage of 500 mg/kg. Together, the results of the present study suggest that CEE of J. regia leaves possess anthelmintic properties and could be a potential source of novel anthelmintic compounds for controlling helminth parasites. [ABSTRACT FROM AUTHOR]

The green synthesis of copper nanoparticles refers to the preparation of nanoparticles using eco-friendly and sustainable processes, often involving plant extracts, microorganisms, or other natural sources. As a sustainable approach with many potential applications, plant extracts could be used for the green synthesis of copper nanoparticles. The green synthesis of copper nanoparticles from plants, such as Erioglossum rubiginosum, involves using leaf and seed extracts to reduce copper ions to form nanoparticles. Primarily, copper nanoparticles are confirmed by visual observation of the aluminum vessel’s inner wall exhibiting a glossy, reddish-brown precipitate. Further, the UV–Vis spectrophotometer is employed to detect the presence of CuNPs. The peak is at 631 nm, which is unique to CuNPs. FTIR data show the presence of a capping agent which stabilizes copper nanoparticles. The peaks at 3,265 cm−1 for the hydroxy group (H-bonded OH stretch) indicate alcohols and phenols; 1610 cm−1 for aromatic ring stretch; and 1,075 cm−1 for aliphatic fluoro compounds (C–F stretch). DPPH reducing power assay is used to verify the antioxidant activity. Both plant extracts and the synthesized CuNPs showed considerable antioxidant activity. The seed and leaf extract of Erioglossum rubiginosum used for the green synthesis of copper nanoparticles served as a capping agent due to the presence of antioxidant phytoconstituents. Then, we used Paramphistomum cervi to evaluate the anthelmintic activity of aqueous extracts of leaves and seeds of Erioglossum rubiginosum. After that, we assessed the anthelmintic activity of the green synthesized copper nanoparticles (CuNPs). We observed that the extracts showed a significant and dose-dependent decrease in the paralysis time and death time of parasites whereas better activity was found from the synthesized CuNPs. At last, we claim that comprehensive investigation on plant extracts and CuNPs could be carried out for further study and might pave the way for development of novel therapeutic agents that show efficacy against diverse parasitic infections.

Abstract Objectives Fasciolosis is of significant economic and public health importance worldwide. The lack of a successful vaccine and emerging resistance in flukes to the drug of choice, triclabendazole, has initiated the search for alternative approaches. In recent years, metallic nanoparticles have been extensively investigated for their anthelmintic effects. This study investigates the in vitro anthelmintic activity of copper oxide and zinc oxide nanoparticles against Fasciola hepatica. Methods The in vitro study was based on egg hatchability test (EHA), adult motility inhibition tests, DNA damage, ROS levels, as well as several biomarkers of oxidative stress, including glutathione peroxidase (GSH) and glutathione S-transferase (GST), superoxide dismutase (SOD) and malondialdehyde (MDA). For this purpose, different concentrations of copper oxide nanoparticles (CuO-NPs) and Zinc oxide nanoparticles (ZnO-NPs) (1, 4, 8, 12, and 16 ppm) were used to evaluate the anthelmintic effect on different life stages, including egg and adults of Fasciola hepatica, over 24 h. Results In vitro treatment of F. hepatica worms with both CuO-NPs and ZnO-NPs could significantly increase ROS production and oxidative stress induction (decreased SOD, GST and GSH and increased MDA) compared to control group. Conclusions Based on the results, it seems that CuO-NPs and ZnO-NPs may be effective in the control and treatment of F. hepatica infection. Further research is needed to investigate their potential for in vivo use in the treatment of parasitic infections.

The discovery of antibiotics and pesticides has greatly contributed to the social and economic development of human society but, due to the long-term irrational application, it has led to drug-resistant microorganisms, environmental damage, and other hazards, so the selection of alternative natural, safe, and non-hazardous bioactive substances is an effective solution for this problem. D-limonene is a bioactive compound widely present in various plant essential oils, exhibiting excellent broad-spectrum bioactivity and promising prospects for development and clinical application. This review provides a detailed overview of the biological activities of D-limonene, emphasizing its antimicrobial, anthelmintic, insecticidal, and medicinal potential. While nanoencapsulation technology shows promise in improving the physicochemical properties of D-limonene and enhancing its practical applications, it is also crucial to comprehensively evaluate the potential side effects of D-limonene before use. [ABSTRACT FROM AUTHOR]

Bromelain has been shown to have potential as an anthelmintic for controlling livestock nematodes, such as Haemonchus (H.) contortus. The present study aimed to evaluate the in vitro quality of the laboratory-produced nanoencapsulated bromelain (NEB) and its activity against H. contortus. The acid-base extraction method was employed to extract four different batches of bromelain from the peels of fully ripened pineapples. It was encapsulated in chitosan to form the nano-encapsulated bromelain complex. Standard biochemical methods were employed to determine the bromelain concentration, protein concentration, in vitro anthelmintic activity against various stages of H. contortus (egg, larva, adult), and bacteria contamination for the four NEB batches. The mean concentration of extracted bromelain was 4.3 mg/ml in all four batches. There were no variations in the protein concentrations between the batches of NEB, which ranged from 1,090 mg/ml to 1.205 mg/ml. Although there were no significant differences in different batches, a variation in NEB inhibitory concentration (IC50) was observed according to the different parasitic stages. The highest activity was for adult worms (LC50 =0.2454 ± 0.05 mg/ml), followed by the eggs (IC50 = 0.3 ± 0.07 mg/ml), and the larval stage (IC50 =0.9 ± 0.45 mg/ml). Despite the identification of certain bacterial species in the raw pineapple extract, the final product of all four batches of NEB remained free from any bacterial contamination. The current study indicated that NEB's concentration, protein concentrations, and anthelmintic activity did not vary significantly across the different batches of NEB. Additionally, the encapsulation process ensured that the final product was free of bacterial contamination and thus safe for use in animals. [ABSTRACT FROM AUTHOR]

Objectives: Fasciolosis is of significant economic and public health importance worldwide. The lack of a successful vaccine and emerging resistance in flukes to the drug of choice, triclabendazole, has initiated the search for alternative approaches. In recent years, metallic nanoparticles have been extensively investigated for their anthelmintic effects. This study investigates the in vitro anthelmintic activity of copper oxide and zinc oxide nanoparticles against Fasciola hepatica. Methods: The in vitro study was based on egg hatchability test (EHA), adult motility inhibition tests, DNA damage, ROS levels, as well as several biomarkers of oxidative stress, including glutathione peroxidase (GSH) and glutathione S-transferase (GST), superoxide dismutase (SOD) and malondialdehyde (MDA). For this purpose, different concentrations of copper oxide nanoparticles (CuO-NPs) and Zinc oxide nanoparticles (ZnO-NPs) (1, 4, 8, 12, and 16 ppm) were used to evaluate the anthelmintic effect on different life stages, including egg and adults of Fasciola hepatica, over 24 h. Results: In vitro treatment of F. hepatica worms with both CuO-NPs and ZnO-NPs could significantly increase ROS production and oxidative stress induction (decreased SOD, GST and GSH and increased MDA) compared to control group. Conclusions: Based on the results, it seems that CuO-NPs and ZnO-NPs may be effective in the control and treatment of F. hepatica infection. Further research is needed to investigate their potential for in vivo use in the treatment of parasitic infections. [ABSTRACT FROM AUTHOR]

Objective: Convolvulus arvensis is one of the world's top noxious weeds and is commonly known as field bindweed. The objective of research work was separation and identification of flavonoids and to check the anthelmintic activity of this plant. Methods: The flavonoids were analyzed by High-Performance Liquid Chromatography (HPLC) method from alcoholic, hydroalcoholic and aqueous extract of aerial parts of Convolvulus arvensis. Acetonitrile:water (containing 0.05% Trifluoroacetic Acid (TFA) each) was used as mobile phase and isolation was done by using RP-18 column with UV variable wavelength detector (254 nm). Chromatogram of standards was compared with sample. Anthelmintic activity also was performed on prepared extracts of various concentrations. Results: The presence of flavonoids like rutin, kaemferol, quercetin and quercetrin in crude extract was revealed. Significant anthelmintic activity in ethanolic extract was also reported. [ABSTRACT FROM AUTHOR]

Gastrointestinal parasites which are responsible for soil-transmitted helminthiases cause illness globally. The control of helminthiasis depends on mass distribution of anthelmintics which has been reported for its resistance, toxicity and low efficacy. In this study, anthelmintic potentials of Gongronema latifolium and Picralima nitida which have wide application in traditional medicine were determined in vivo using Heligmosomoides bakeri a naturally occurring gastro-intestinal parasite of rodents that is closely related to highly prevalent human nematode parasites.

The substance fenbendazole is included in the composition of many anthelmintic drugs, in which the “chemical stability” parameter is one of the main characteristics when obtaining permission for the use of drugs in veterinary practice. Fenbendazole is characterized by low solubility in water and therefore the content of the substance is overestimated in its preparations, which increases the cost of the drug as well as the safety risks of pharmacotherapy. The possibilities of mechanochemical modification of fenbendazole were evaluated in order to improve the solubility index. During the mechanical processing treatment of the substance in the presence of polymeric substances, solid dispersions are formed, which have increased solubility and high anthelmintic activity. The inclusion in these dispersions of the third component, which is succinic acid, did not significantly change the solubility of fenbendazole. In all these dispersions, the substance remained unchanged both during the preparation of its solid dispersions and during their storage. When fenbendazole is modified in an organic solvent medium, the substance is partially converted into oxfendazole, which is one of its metabolites. The chemical stability of fenbendazole was confirmed via HPLC/MS and NMR spectroscopy. The anthelmintic activity of these compositions was evaluated and it was found that they have a high nematicidal activity.

Resistance to commonly used anthelmintics stipulate alternative control methods. The use of natural herbal products with anthelmintic properties can address the issue. In this regard, the present study was conducted to determine the in vitro antiparasitic activities of aqueous and methanolic extracts of Aegle marmelos by using different in vitro assays at various concentrations of extracts. The evaluation was done by egg hatch assay (EHA) and larval development assay (LDA) on Strongyle-type eggs and larval stages of Haemonchus contortus isolated from the goat fecal samples respectively. In EHA, 74.34% and 79.71% were the mean inhibition percent against Strongyle type eggs from hatching at the highest concentration of 50 mg/ml tested and the change was 7.2 and 8.24 fold higher than negative PBS control while 77.45% and 85.78% was mean inhibition percentage in terms of Haemonchus contortus L3 larvae development at the highest concentration 1 mg/ml tested and the change was 14.5 and 18.3 fold higher than negative control by aqueous and methanolic extract of A. marmelos, respectively. Both extracts showed dose-dependent inhibition at all the concentrations tested and were similar to positive control-like treatment with 0.125 mg/ml albendazole for EHA and LDA. The study concluded that the aqueous and methanolic extracts of A. marmelos have antiparasitic potential and can be used to control parasitic infection.

The substance fenbendazole is included in the composition of many anthelmintic drugs, in which the "chemical stability" parameter is one of the main characteristics when obtaining permission for the use of drugs in veterinary practice. Fenbendazole is characterized by low solubility in water and therefore the content of the substance is overestimated in its preparations, which increases the cost of the drug as well as the safety risks of pharmacotherapy. The possibilities of mechanochemical modification of fenbendazole were evaluated in order to improve the solubility index. During the mechanical processing treatment of the substance in the presence of polymeric substances, solid dispersions are formed, which have increased solubility and high anthelmintic activity. The inclusion in these dispersions of the third component, which is succinic acid, did not significantly change the solubility of fenbendazole. In all these dispersions, the substance remained unchanged both during the preparation of its solid dispersions and during their storage. When fenbendazole is modified in an organic solvent medium, the substance is partially converted into oxfendazole, which is one of its metabolites. The chemical stability of fenbendazole was confirmed via HPLC/MS and NMR spectroscopy. The anthelmintic activity of these compositions was evaluated and it was found that they have a high nematicidal activity. [ABSTRACT FROM AUTHOR]

Benzimidazole anthelmintic drugs hold promise for repurposing as cancer treatments due to their interference with tubulin polymerization and depolymerization, manifesting anticancer properties. We explored the potential of benzimidazole compounds with a piperazine fragment at C-2 as tubulin-targeting agents. In particular, we assessed their anthelmintic activity against isolated Trichinella spiralis muscle larvae and their effects on glioblastoma (U-87 MG) and breast cancer (MDA-MB-231) cell lines. Compound 7c demonstrated exceptional anthelmintic efficacy, achieving a 92.7% reduction in parasite activity at 100 μg/mL after 48 hours. In vitro cytotoxicity analysis of MDA-MB 231 and U87 MG cell lines showed that derivatives 7b, 7d, and 7c displayed lower IC50 values compared to albendazole (ABZ), the control. These piperazine benzimidazoles effectively reduced cell migration in both cell lines, with compound 7c exhibiting the most significant reduction, making it a promising candidate for further study. The binding mode of the most promising compound 7c, was determined using the induced fit docking–molecular dynamics (IFD–MD) approach. Regular docking and IFD were also employed for comparison. The IFD–MD analysis revealed that 7c binds to tubulin in a unique binding cavity near that of ABZ, but the benzimidazole ring was fitted much deeper into the binding pocket. Finally, the absolute free energy of perturbation technique was applied to evaluate the 7c binding affinity, further confirming the observed binding mode. [ABSTRACT FROM AUTHOR]

This study aims to determinate in vitro anthelmintic activity of the plant extracts from the aerial part of five different Artemisia L. species (A. absinthium L., A. abrotanum L., A. annua L., A. incana (L.) Druce, A. tournefortiana Rchb.) growing in Türkiye. Depending on the ethnobotanical usage, the aqueous plant extracts were prepared by decoction and maceration methods. The anthelmintic activity of the plant extracts on Haemonchus (H.) contortus eggs and larvae was assessed using in vitro test methods. The extracts were prepared in five concentrations (50; 25; 12.5; 6,25; 3.125 and 1.5625 mg/mL) by using PBS for egg hatch and larval motility inhibition assay. In comparison to the negative control group, the extracts had significant anthelmintic effect on H. contortus eggs and larvae (p<0.05). In the egg hatch assay, all plants were found to be fully effective in the concentration range studied. In the analysis of larval motility, the activity was correlated with the quantities of the plant extracts. When the concentration-activity values of the plants were examined for both extraction methods, the highest activity was in A. annua and the lowest activity was observed in A. tournefortiana. Due to the development of resistance to anthelmintic drugs, natural sources such as Artemisia species can be considered as an alternative for the treatment of nematodes. [ABSTRACT FROM AUTHOR]

Background: The purpose of this study was to screen the anthelmintic property of a hydroalcoholic extract of Vitex negundo leaves. It is widely used for the treatment of anti-inflammatory, enzyme inhibitory, oxidative stress, cytotoxic impact in the ayurvedic medicine system as well as it is also used as a folk medicine in joint pain. The other parts of this plant are scientifically proven for its anthelmintic activity. The most important activities like glucose uptake, enzyme inhibitory activity, auxin transportation etc. have already been proven but still there is no scientific data available on anthelmintic activity of Vitex negundo leaves. Methods: The hydroalcoholic extract of Vitex negundo leaves was obtained by maceration process and various phytochemical tests were performed. Limit test, main test and comparative test were performed to investigate the anthelmintic activity. Results: The paralysis and death time of the Tubifex tubifex worms was noted and the minimum concentration of dose responsible for death of all the test worms within 4 hours was calculated. Albendazole suspension was used as standard drug. The data shows statistically significant by using one-way ANNOVA, Dunnett's post-parametric test between test group and standard group data (P<0.01). Conclusion: Therefore, the hydroalcoholic extract of Vitex negundo leaves has the potential to be used as a natural anthelmintic agent. [ABSTRACT FROM AUTHOR]

The discovery of antibiotics and pesticides has greatly contributed to the social and economic development of human society but, due to the long-term irrational application, it has led to drug-resistant microorganisms, environmental damage, and other hazards, so the selection of alternative natural, safe, and non-hazardous bioactive substances is an effective solution for this problem. D-limonene is a bioactive compound widely present in various plant essential oils, exhibiting excellent broad-spectrum bioactivity and promising prospects for development and clinical application. This review provides a detailed overview of the biological activities of D-limonene, emphasizing its antimicrobial, anthelmintic, insecticidal, and medicinal potential. While nanoencapsulation technology shows promise in improving the physicochemical properties of D-limonene and enhancing its practical applications, it is also crucial to comprehensively evaluate the potential side effects of D-limonene before use.

Abstract The aim of this study was to assess the in vitro ovicidal activity of an ethyl acetate extract from Arceuthobium vaginatum (EtOAc-E) and their subfractions (AvR5-AvR14) against Haemonchus contortus using the egg hatching inhibition (EHI) test. The EtOAc-E and subfractions were tested at 0.12-2.00 and at 0.015-2.0 mg/mL, respectively. Distilled water and methanol (2%) were used as negative controls and Thiabendazole (0.10 mg/mL) as a positive control. Treatments with a dependent effect on concentration were subjected to regression analysis to determine the effective concentrations (EC50 and EC90). The major secondary compounds present in the extract and subfractions were identified by high performance liquid chromatography (HPLC). The EtOAc-E and AvR9 exhibited the best ovicidal effect recording 97.5 and 100% of EHI at 0.25 mg/mL, respectively. The EtOAc-E and AvR9 displayed an EC50= 0.12 and 0.08 mg/mL, respectively. The HPLC analysis in the EtOAc-E and bioactive fractions indicated the presence of a polyphenol, glycosylated flavanones, quercetin glucoside, cinnamates, coumarin, cinnamic acid derivative, ferulic acid, coumarate, naringenin, protocatechuic acid and naringin. Results demonstrated that A. vaginatum extract and fraction is able to inhibit the egg hatch process of H. contortus and could be a viable option for the control of small ruminant haemonchosis.

The aim of this research study was to evaluate aqueous and organic extracts of seeds of Samaneasaman (Merr)for their anthelmintic activity using Indian adult earthwormPheretimaposthuma.Different concentrations of aqueous and organic extract ranging from 10 to 100 mg/ml were made and tested on said earthworm. These extracts were tested for bioassays which include time for paralysis and time for death of the worms. Aqueous as well as organic extract of seeds does notexhibited strong anthelmintic activity at concentration of 100 mg/ml. Lower concentrations also did not produced significant anthelmintic activity. The standard reference drug which is used for comparing anthelmintic activity of these extracts was piperazine citrate at concentration of 10 mg/ml.Both aqueous and organic extracts of seeds of Samaneasamanwere evaluated for and showed no potential anthelmintic activity. [ABSTRACT FROM AUTHOR]

The present study aims to find efficient alternatives to synthetic anthelmintics among ethno-veterinary herbs. Ascaridia galli eggs isolated from the worm uterus were exposed in vitro to methanolic extracts (ME) of nine plant species such as Achillea millefolium (AM), Artemisia absinthium (AA), Artemisia vulgaris (AV), Cicerbita alpina (CA), Cichorium intybus (CI), Inula helenium (IH), Origanum vulgare (OV), Tanacetum vulgare (TV), Tanacetum parthenium (TP). Flubendazole (FL), 0.5% formalin with dimethylsulfoxide and Petri dishes without the addition of reagents were used as positive, negative and untreated control respectively. The effects of the different ME at concentrations 0.500, 0.325, 0.200 mg/ml were assessed on the embryonic development (ED) of the eggs in duplicate. Logit analysis was used to calculate EC50 values. A generalized linear mixed model, having plant species and concentration as fixed effect and day as repeated measure, was used to determine differences in ED. Estimated EC50 was the lowest for FL at 0.11 mg/ml. CA and TV followed with 0.27 mg/ml and 0.32 mg/ml. ED for FL was significantly lower (25%) than that of CA (47%). The analysis showed 0.5 mg/ml of the ME of CA and TV significantly affected the ED at 35% and 42% inhibitions respectively. The ED for all ME showed similar pattern i.e., relatively higher efficacy in the first experimental week compared to the rest of the experimental period. The effect from all multicomponent extracts is time and dose dependent. The plants have promising results in inhibiting ED, contributing to the identification of alternative anthelmintic treatments. [ABSTRACT FROM AUTHOR]

Resistance to commonly used anthelmintics stipulate alternative control methods. The use of natural herbal products with anthelmintic properties can address the issue. In this regard, the present study was conducted to determine the in vitro antiparasitic activities of aqueous and methanolic extracts of Aegle marmelos by using different in vitro assays at various concentrations of extracts. The evaluation was done by egg hatch assay (EHA) and larval development assay (LDA) on Strongyle-type eggs and larval stages of Haemonchus contortus isolated from the goat fecal samples respectively. In EHA, 74.34% and 79.71% were the mean inhibition percent against Strongyle type eggs from hatching at the highest concentration of 50 mg/ml tested and the change was 7.2 and 8.24 fold higher than negative PBS control while 77.45% and 85.78% was mean inhibition percentage in terms of Haemonchus contortus L3 larvae development at the highest concentration 1 mg/ml tested and the change was 14.5 and 18.3 fold higher than negative control by aqueous and methanolic extract of A. marmelos, respectively. Both extracts showed dose-dependent inhibition at all the concentrations tested and were similar to positive control-like treatment with 0.125 mg/ml albendazole for EHA and LDA. The study concluded that the aqueous and methanolic extracts of A. marmelos have antiparasitic potential and can be used to control parasitic infection. [ABSTRACT FROM AUTHOR]

Ritter cyclocondensation of 3,4-(R)2-dimethylbenzylcarbinols with thiocyanatoanilines was used to obtain 4-[6,7-(R)2-3,3-dimethyl-3,4-dihydroisoquinolin-1-ylthio]anilines (R = H, MeO). A benzo[f]isoquinoline derivative was obtained similarly. 4-Thiocyanatoaniline, 2-methyl-4-thiocyanatoaniline, 2-thiocyanato-4-aminoethylbenzene, and 4,4′-dithiocyanatodiphenylamine were used as the thiocyanatoanilines. The hydrochlorides of the obtained compounds were used for biological tests. All compounds exhibited an analgesic effect in the hot-plate test that exceeded that of metamizole sodium. Five of the seven compounds exhibited anthelmintic activity. The most active compound caused the death of worms 14.3 times faster than pyrantel. The larvicidal activity of the same compound was 1.63 times greater than that of diazinon for reducing the time of death of larvae. [ABSTRACT FROM AUTHOR]

Background: The helminthiasis parasitic worm present in the gastrointestinal tract of the animal cause infection and physiological damage. This occurs due to poor sanitation, impecunious personal hygiene, low socioeconomic position, and lack of education. Aim: Urochloa distachya (Poaceae) commonly called as signal grass and used as fodder for the animal. The present investigation was undertaken to investigate the phytochemicals and to study the anthelmintic activity. Materials and Methods: The plant material was extracted by using petroleum ether and methanol in Soxhlet apparatus and the obtained extract was subjected to GC-MS analysis for the identification of the bioactive components responsible for anthelmintic activity. The anthelmintic activity was performed against earthworms (Eisenia fetida) at concentrations 12.5, 25, and 50 mg/mL using piperazine citrate as standard. Results: The GC-MS analysis of the petroleum ether extract showed five major and ten minor compounds. The major compounds were identified as Stigmasterol (14.76%); α-Amyrin (12.47%); γ-Sitosterol (10.31%); 17-(1,5-Dimethyl-3-phen ylthiohex-4-enyl) -4,4,10,13,14-pentamethyl 2,3,4,5,6,7,10,11,12-(9.12%) and β-Amyrin (8.83%). The minor compounds were D:C-Friedo-B': A'-neogammacer-9(11)-ene, 3-methoxy-, (3β)-(8.28%); Tritetracontane (7.23%); Campesterol (4.68%); Phytol (4.05%); Cholesterol (3.39%); Hexadecanoic acid, methyl ester (2.20%); 2-Pyrrolidinone, 1-methyl-(1.46%); Oleic acid, 3-(octadecyloxy) propyl ester (1.27%); Squalene (0.84%) and 9,19-Cyclolanostane-3,7-diol (0.68%). The time taken for paralysis and death of Eisenia fetida parasite was noticed by methanolic and petroleum ether extract at a concentration of 50 mg/kg as compared to the standard drug. Conclusion: The anthelmintic activity of the plant was most achieved by methanolic extract which could be attributed to the presence of the Octadecanoic acid. Also, the anthelmintic active of the petroleum ether extract could be attributed to the antimicrobial, antibacterial, antifungal, and antiprotozoal activities of the Hexadecanoic acid, methyl ester; Phytol; Squalene; Cholesterol, and γ-Sitosterol. [ABSTRACT FROM AUTHOR]

Abstract Background Vernonia amygdalina (leaf), Garcinia kola (seed), and Leucaena leucocephala (seed) are three well-known tropical plants used in African ethnomedicine to reduce parasitic worm burdens and are potential sources of alternative solution for controlling parasitic helminths infection in grazing livestock. This study investigated extracts from these plants for anthelmintic activity against adult Haemonchus placei, an haematophagous nematode from cattle abomasa. Powdered plant materials were macerated in acetone and the crude acetone extracts evaluated for anthelmintic activity using H. placei adult worm motility assay. Afterwards, fresh sample of V. amygdalina was macerated successively in chloroform and acetone and the extracts evaluated for anthelmintic activity. The chloroform extract was subjected to phytochemical and FT-IR analyses and fractionated by vacuum liquid chromatography. Anthelmintic data were fitted to a nonlinear regression equation (Log [extract or fraction] vs. lethality; variable slope) to produce best-fit sigmoidal curves and LC50 values computed with associated uncertainty. Results Of the three tropical plants, only V. amygdalina was active against adult H. placei with best-fit LC50 of 6.51 mg/mL (95% CI: 5.32–7.75). Evaluation of the two extracts obtained by successive maceration showed that chloroform extract (LC50, 2.46 mg/mL, 95% CI: 1.87–3.28) was 11 times as potent as acetone extract (LC50, 27.01 mg/mL, 95% CI: 21.32–48.57) (α

Parasitic infections with gastrointestinal nematodes are a serious problem for the health and welfare of domestic animals and negatively affect the economics of animal production. Haemonchus contortus is a haematophagous nematode of small ruminants responsible for significant mortality and morbidity. In addition, the widespread resistance to synthetic anthelmintic drugs emphasizes the urgent need of alternative treatment options against haemonchosis. This work aims to investigate the anthelmintic activity of an hydroethanolic Combretum mucronatum leaf extract (CMLE) against Haemonchus contortus in goats. Goats were artificially infected with 3500 third-stage larvae of H. contortus , and 21 days later, treated with CMLE (1000, 500, 250 mg/kg) for 4 consecutive days. Different parameters such as faecal egg count reduction, weight and haematocrit were monitored during the experimental period. The number of eggs per gram of faeces (EPG) was concentration-depended lower and significantly reduced compared to the untreated control (p < 0.0001). The effect of the highest CMLE dose (4 ×1000 mg/kg body weight) was similar to the effect of albendazole (1 ×5 mg/kg of body weight). The ED 50 and ED 90 values calculated were 189.17 and 392.33 mg/kg body weight respectively. ED 50 and ED 90 values were time-dependent. Moreover, CMLE improved haematocrit and weight of goats in dose-dependent and time-dependent manner. These results showed that CMLE could be used for haemonchosis treatment in small ruminants. [Display omitted] • Calves that received powdered colostrum replacer had more tick fever agents (TFA). • Calves obtained by embryo transfer received more treatments against TFA. • Calves that suffered 4 to 10 TFA relapses had lower weaning weights. • Each TFA relapse in calves reduced 213.5 liters of milk in the 1st lactation. [ABSTRACT FROM AUTHOR]

This study assessed the i n vitro anthelmintic activity of ethyl acetate extract (Cn-EtOAc) and its bioactive fractions (CnR3 and CnR5) obtained from Chamaecrista nictitans aerial parts against two Haemonchus contortus (Hc) isolates, one resistant (strain Hc IVM-R) and another susceptible (strain Hc IVM-S) to ivermectin. Ferulic acid and p -coumaric acid were identified in the bioactive fractions; therefore, their commercial standards were also assessed. A colocalization analysis between the ferulic acid commercial standard and eggs of the Hc IVM-R strain was performed using confocal laser scanning microscopy and the ImageJ program. The ovicidal effects of the Cn-EtOAc extract, bioactive fractions and commercial compounds were tested through the egg hatching inhibition (EHI) assay on H. contortus isolates Hc IVM-R and Hc IVM-S. The Cn-EtOAc caused 88 % and 92 % EHI at 5000 µg/mL on Hc IVM-R and Hc IVM-S, respectively. Fractions CnR3 and CnR5 displayed the highest ovicidal activity against Hc IVM-S, with effective concentrations (EC 90) of 2134 and 601 µg/mL, respectively. Meanwhile, the commercial standards ferulic acid and p -coumaric acid also resulted in higher effectiveness on the same strain, with EC 90 of 57.5 and 51.1 µg/mL. A colocalization analysis of ferulic acid and eggs of Hc IVM-R revealed that this compound is localized to the cuticle surface of the embryo inside the egg parasite. The results demonstrated that both ferulic and p -coumaric acids interrupt the egg-hatching processes of the two Hc isolates. Both phenolic acids isolated from C. nictitans and commercial standards exhibited the best anthelmintic effect on Hc IVM-S. These findings indicate that the phenolic acids were less effective in egg hatch inhibiting on the Hc IVM-R strain compared to the Hc IVM-S strain. [Display omitted] [ABSTRACT FROM AUTHOR]

Benzimidazole anthelmintic drugs hold promise for repurposing as cancer treatments due to their interference with tubulin polymerization and depolymerization, manifesting anticancer properties. We explored the potential of benzimidazole compounds with a piperazine fragment at C-2 as tubulin-targeting agents. In particular, we assessed their anthelmintic activity against isolated Trichinella spiralis muscle larvae and their effects on glioblastoma (U-87 MG) and breast cancer (MDA-MB-231) cell lines. Compound 7c demonstrated exceptional anthelmintic efficacy, achieving a 92.7% reduction in parasite activity at 100 μg/mL after 48 hours. In vitro cytotoxicity analysis of MDA-MB 231 and U87 MG cell lines showed that derivatives 7b, 7d, and 7c displayed lower IC50 values compared to albendazole (ABZ), the control. These piperazine benzimidazoles effectively reduced cell migration in both cell lines, with compound 7c exhibiting the most significant reduction, making it a promising candidate for further study. The binding mode of the most promising compound 7c, was determined using the induced fit docking–molecular dynamics (IFD–MD) approach. Regular docking and IFD were also employed for comparison. The IFD–MD analysis revealed that 7c binds to tubulin in a unique binding cavity near that of ABZ, but the benzimidazole ring was fitted much deeper into the binding pocket. Finally, the absolute free energy of perturbation technique was applied to evaluate the 7c binding affinity, further confirming the observed binding mode.

Haemonchus contortus is a gastrointestinal nematode that negatively affects the meat and milk production of husbandry animals. The purpose of the study was to determine the anthelmintic activity of Chenopodium album plant extract in controlling H. contortus parasites. The antioxidant, cytotoxic, and antibacterial activities of the C. album plants were also investigated. In an anthelmintic activity test, 100% of H. contortus parasite mortality was observed after 3 h exposure at a dose of 150 μg/mL. The antioxidant properties of C. album showed an IC50 value of 90.98 μg/mL, indicating moderate antioxidant activity when compared to the BHT standard. The cytotoxic effect showed LC50 values of 4.52, 3.11, 2.3, 1.52, and 1.167 μg/mL after 12, 18, 24, 30, and 36 h against Artemia salina, respectively. However, the C. album extract did not demonstrate any antibacterial properties against Bacillus subtilis, Staphylococcus aureus, Salmonella typhi, Shigella dysentriae, Shigella boydii, or E. coli at a concentration of 150 μg/mL. A molecular docking study showed that isolariciresinol 4'-O-beta-D-glucoside, (1S,2S,4R)-1,8-epoxy-p-menthan-2-ol glucoside and linalool (CID-74407576, CID-73815050, and CID-6549) had binding energies of −7.8, −7.5, and −7.1 kcal/mol, respectively, with the Nu-class GST protein. Moreover, the ADMET properties of hit compounds also similarly showed ideal behavior to known drug molecules. Hence, C. album could be a promising candidate for developing an effective drug against H. contortus.

Parasitic helminths continue to pose problems in human and veterinary medicine, as well as in agriculture. Semen pharbitidis, the seeds of Pharbitis nil (Linn.) Choisy (Convolvulaceae), is a well-known traditional Chinese medicinal botanical preparation widely used for treating intestinal parasites in China owing to its desirable efficacy. However, the anthelmintic compounds in Semen pharbitidis and their mechanism of action have not been investigated yet. This study aimed to identify the compounds active against helminths from Semen pharbitidis, and to establish the mechanism of action of these active compounds. Bioassay-guided fractionation was used to identify the anthelmintic compounds from Semen pharbitidis. The anthelmintic assay was performed by monitoring Caenorhabditis elegans (C. elegans) motility with a WMicrotracker instrument. Active compounds were identified by high-resolution mass spectrometry. Several (analogues of) fragments of the anthelmintic compounds were purchased and tested to explore the structure–activity relationship, and to find more potent compounds. A panel of C. elegans mutant strains resistant to major currently used anthelmintic drugs was used to explore the mechanism of action of the active compounds. The bioassay-guided isolation from an ethanol extract of Semen pharbitidis led to a group of glycosides, namely pharbitin (IC50: 41.0 ± 9.4 μg/mL). Hit expansion for pharbitin fragments yielded two potent analogues: 2-bromohexadecanoic acid (IC50: 1.6 ± 0.7 μM) and myristoleic acid (IC50: 35.2 ± 7.6 μM). One drug-resistant mutant ZZ37 unc-63 (x37) demonstrated a ~17-fold increased resistance to pharbitin compared with wild-type worms. Collectively, we provide further experimental scientific evidence to support the traditional use of Semen pharbitidis for the treatment of intestinal parasites. The anthelmintic activity of Semen pharbitidis is due to pharbitin, whose target could be UNC-63 in C. elegans. [ABSTRACT FROM AUTHOR]

Tetrazoles and 1,2,3-triazoles are poorly understood regarding their anthelmintic activity. Therefore, an effort was taken to identify novel chemical scaffolds as anthelmintic agents; a series of 1,2,3-triazole–tetrazole conjugates were synthesized. The synthesis of 1,2,3-triazole based tetrazole derivatives has carried out via [2+3]-cycloaddition reaction of triazolyl nitriles with sodium azide. The present design and synthetic strategy offers excellent yields of the products in the presence of [DBU][OAc] under ultrasonic irradiations. The synthesized triazole–tetrazole conjugates were characterized by spectroscopic techniques and screened for their anthelmintic activity. Most of the compounds have shown better anthelmintic activity as compared to standard drug Albendazole. Furthermore, molecular docking study revealed the binding interaction of all these compounds with the active site of β-tubulin receptor which provides an insight into their plausible mechanism of anthelmintic action. [ABSTRACT FROM AUTHOR]

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Ritter reactions of 1-(3,4-diethoxyphenyl)-2-methylpropanol-2 with 2-alkylcyanoacetamides (alkyl = Et, n-Pr, n-Bu, n-Am, i-Am) were used to synthesize 2-(3,3-dimethyl-6,7-diethoxy-3,4-dihydroisoquinolin-1-yl)carboxylic acid amides. Similarly, reactions of 1-(2-naphthyl)-2-methylpropanol-2 with these same nitriles were used to obtain 2-(2,2-dimethyl-1,2-dihydrobenzo[f]isoquinolin-1-yl)carboxylic acid amides. Hydrochlorides of the synthesized compounds were tested for antiarrhythmic activity, which was not observed. With respect to the effect on blood clotting, nine compounds proved to be hemostatics; one compound, an anticoagulant. Three compounds of the benzo[f]isoquinoline series were the most active and increased blood coagulation by 31.7, 29.1, and 28.9%. All 10 compounds showed anthelmintic activity exceeding that of pyrantel. Two amides had anthelmintic activity exceeding that of levamisole and reduced the lifespan of worms by 11.4 and 11.6 min (vs. 20.2 min for levamisole). Nine compounds had larvicidal action exceeding that of imidacloprid. Two of them reduced the larval lifespan to 10.2 and 13.8 min, exceeding the effect of diazinon (17.0 min). [ABSTRACT FROM AUTHOR]

Simple Summary: In the present study, we explored the anthelmintic activity, cytotoxicity, and chemical composition of the main plants used by small ruminant breeders in Benin to treat digestive parasitosis. The results obtained are relevant in the sense that they will allow a rational use of the plants studied in the control of digestive parasites but also to initiate the process of identification of new anthelmintic molecules in the context of the development of resistance against the most currently used anthelmintic molecules. Medicinal plants continue to be used alone or in combination with veterinary drugs to treat animal ailments, especially in developing countries where livestock farmers often lack access to modern veterinary services and drugs. In addition, digestive parasitosis remain a major constraint for small ruminant livestock. The objective of this study was to screen the anthelmintic activity of the main plants used in the treatment of the digestive parasitosis of small ruminants in Benin. A total of 40 extracts were prepared using the successive maceration of 10 plants in four solvents of increasing polarity. The phytochemical screening of the plants was performed, and the anthelmintic activity of the extracts was evaluated on L3 larvae of Haemonchus contortus. The cytotoxicity of the 40 extracts was determined on WI38 noncancerous fibroblast cells using the MTT assay, and the total phenol content (TPC), total flavonoid content (TFC), and condensed tannin content (CTC) were quantified in the most effective extracts using colorimetric methods. The results show that the plants contained tannins, flavonoids, and triterpenoids which may, in part, justify their anthelmintic activities. All plants gave active extracts at the highest concentration tested (1200 µg/mL). Methanol (MeOH) extracts were, in general, more effective than the hexane (HEX), dichloromethane (DCM), and aqueous (H2O) ones in inhibiting larval migration, with the MeOH extracts of Terminalia leiocarpa, Adansonia digitata, and Momordica charantia being the most effective. Nevertheless, the MeOH extract of M. charantia was highly cytotoxic at the concentration of 100 µg/mL. The anthelmintic activity of M. charantia, Vitex doniana, and Caesalpinia bonduc was studied on H. contortus for the first time. These results provide scientific information that can be used for better valorization of the anthelmintic potential of the studied plants and to initiate the process of the identification of new anthelmintic molecules. [ABSTRACT FROM AUTHOR]

Background: Parasitic infections have become a serious threat to the lives of human beings and animals and helminthiasis is the major parasitic infection. A wide range of anthelmintic agents have been used to treat these parasitic infections. Synthetic anthelmintic has various limitations like resistance. So, the major practical way of developing efficacious and cheaper anthelmintics is to consider herbal plants. Materials and Methods: The three plants selected in the study are Citrus medica, Coleus aromaticus and Murraya koenigii, belonging to the family Rutaceae, Lamiaceae and Rutaceae respectively. Traditionally, all these plants are used as vermicides. The main goal of the study was to examine the anthelmintic activity of these three plants using earthworms (Pheretima posthuma). 50% Hydroethanolic extracts of the three plants at different concentrations (20, 50, 80 mg/ml) showed dose-dependent anthelmintic response. Results: At concentrations of 20, 50, 80 mg/ml, all three plant extracts caused paralysis at 16.4, 28.33, 28.17, 11.35, 23.17, 22.4, 9.1, 19.33, 19.21 min. and death at 60.1, 84.56, 40.06, 46.08, 67.06, 37.42, 25.54, 56.56, 29.35 min. respectively. Albendazole was used as a reference standard at three different concentrations 20, 50, 80 mg/ml and caused paralysis at 40.37, 36.12, 24.44 min and death at 50.1, 39, 30.49 min. Conclusion: After analysing results, it was concluded that the three plants possess effective anthelmintic activity when compared with standard drug Albendazole and Citrus medica was found to be much more effective than all. [ABSTRACT FROM AUTHOR]

Pithecellobium dulce (Robx.) Benth is an arboreal legume used in traditional medicine for the treatment of several ailments, including a number of intestinal disorders, and as a natural deworming. The objective of this study was to evaluate the ovicidal activity of a hydroalcoholic extract (HA-E) and its fractions (aqueous, Aq-F and organic, EtOAc-F) from P. dulce leaves, as well as subfractions (C1F1–C17) obtained from EtOAc-F against Haemonchus contortus eggs. The HA-E, Aq-F, and EtOAc-F were assessed at 0.03–5.00 mg/mL and subfractions (C1F1–C17) were assessed at 0.06–1.00 mg/mL. The HA-E and Aq-F showed an ovicidal activity close to 100% at 2.5 mg/mL, and EtOAc-F displayed the highest anthelmintic effect (100% at 0.25 mg/mL). Meanwhile, the sub-fractions with the highest ovicidal effect were C1F6, C1F9, C1F10, C1F11, and CIF13. The main compounds identified in the most active fractions (C1F9, C1F11, and C1F13) were kaempferol (1), quercetin (2), coumaric acid (3), ferulic acid (4), luteolin 7-O-rhamnoside (5), quercetin 3-O-rhamnoside (6), and a caffeoyl derivate (NI). The results indicate that P. dulce leaves exhibit a potent anthelmintic activity and contain bioactive compounds able to inhibit egg hatching in H. contortus. Therefore, this plant could be used for the control of gastrointestinal nematodes in small ruminants. [ABSTRACT FROM AUTHOR]

The purpose of the present study was to assess the ovicidal and larvicidal activity of a hydroalcoholic extract (HAE) and their fractions (aqueous, Aq-F and organic, EtOAc-F) from Guazuma ulmifolia leaves using Haemonchus contortus as a biological model. The egg hatching inhibition (EHI) and larval mortality against infective larvae (L3) tests were used to determine the anthelmintic effect of the treatments. The extract and fractions were tested at different concentrations against eggs and L3. Additionally, distilled water and methanol were used as negative controls and ivermectin as a positive control. The extract and fractions were subjected to HPLC analysis to identify the major compounds. The HAE displayed the highest ovicidal activity (100% EHI at 10 mg/mL). Fractionation of the HA extract allowed increasing the nematicidal effect in the EtOAc-F (100% EHI at 0.62 mg/mL and 85.35% mortality at 25 mg/mL). The phytochemical analysis of the extract and fractions revealed the presence of kaempferol, ethyl ferulate, ethyl coumarate, flavonol, luteolin, ferulic acid, luteolin rhamnoside, apigenin rutinoside, coumaric acid derivative, luteolin glucoside, and quercetin glucoside. These results suggest that G. ulmifolia leaves could be potential candidates for the control of H. contortus or other gastrointestinal parasitic nematodes. [ABSTRACT FROM AUTHOR]

This study focuses on developing novel antimicrobials to combat drug-resistant pathogens, addressing compounds failing clinical trials due to inadequate physicochemical properties. Sixteen imidazolidine-4-one derivatives were synthesized by extensive evaluation using molecular docking, absorption, distribution, metabolism, excretion (ADME) predictions, and antimicrobial testing. Molecular docking studies conducted with Schrödinger's Glide revealed that compounds S4 and G8 exhibited superior docking scores of -7.839 and -7.776, respectively. The G series outperformed the S series in scores. ADME analysis confirmed all compounds adhered to Lipinski's rule of five. In addition, IR and NMR provided details about the structure of the compounds. Antimicrobial activity was assessed against Escherichia coli, Staphylococcus aureus, and Candida albicans, with compounds G2 and S2 showing exceptional minimum inhibitory concentration (MIC) values of 6.25 μg/mL against E. coli. S2 also demonstrated impressive activity against S. aureus (MIC 3.12 μg/mL), and S4 exhibited potent activity against C. albicans (MIC 0.8 μg/mL) than fluconazole (1.6 μg/mL). Additionally, antihelmintic activity was evaluated, with G1, G3, G8, S2, S4, S7, and S8 showing effective paralysis and death time 20 min and below at 50 mg/mL concentration. These results underscore the potential of new imidazolidine-4-one derivatives as suitable sources to develop a drug candidate to treat resistant infections., (© 2024 John Wiley & Sons Ltd.)

Current research work is focused on incorporation of thiosemicarbazide, triazole in one framework and observed for antifungal, antibacterial and anthelmintic activities. Derivatives of 1,2,4-triazole-3-thiol are synthesized with thiosemicarbazide and semicarbazide as a starting material. Thiosemicarbazide are subjected to intermolecular cyclization in alkaline medium followed by acidification to give 1,2,4-triazole-3-thiol. Equimolar mixture of thiosemicarbazide and different consecutive acids are heated, fusion occurred to give different triazoles derivatives. The minimum inhibitory concentrations for synthesized compounds are in the range of 3.12-25 μg/mL. [ABSTRACT FROM AUTHOR]