scholarly journals Benzimidazole and Aminoalcohol Derivatives Show in Vitro Anthelmintic Activity Against Trichuris Muris and Heligmosomoides Polygyrus

2022 ◽  
Author(s):  
Elora Valderas-García ◽  
Cécile Häberli ◽  
María Álvarez Bardón ◽  
Nerea Escala ◽  
Verónica Castilla Gómez de Agüero ◽  
...  
Keyword(s):  
Adult Stage ◽  
Anthelmintic Activity ◽  
Gastrointestinal Nematodes ◽  
Economic Losses ◽  
Parasitic Infections ◽  
Trichuris Muris ◽  
Heligmosomoides Polygyrus ◽  
Derivatives Of

Abstract Background: Infections by gastrointestinal nematodes cause significant economic losses and disease in both human and animals worldwide. The discovery of novel anthelmintic drugs is a crucial point in maintaining control of these parasitic infections.Methods: For this purpose, the aim of the present study was to evaluate the potential anthelmintic activity of three series of compounds against the gastrointestinal nematodes Trichuris muris and Heligmosomoides polygyrusin vitro. The compounds tested are derivatives of benzimidazole, lipidic aminoalcohols and diamines. A primary screening was performed to select those compounds with an ability to inhibit T. muris L1 motility by more than 90% at a single concentration of 100 µM, and then, their respective IC50s were calculated. Those compounds with IC50 lower than 10 µM were also tested against the adult stage of T. muris and H. polygyrus at a single concentration of 10µM.Results: Of the 41 initial compounds screened, only compounds AO14, BZ6 and BZ12 had IC50s lower than 10 µM on T. muris L1 assay, showing IC50 values of 3.30, 8.89 and 4.17 µM, respectively. However, only two of them displayed activity against the adult stage of the parasites: BZ12 killed 81% of adults of T. muris (IC50 of 8.1 µM) and 53% of H. polygyrus while BZ6 killed 100% of H. polygyrus adults (IC50 of 5.3 µM) but only 17% of T. muris. Conclusions: BZ6 and BZ12 could be considered as potential candidates for further in vivo efficacy testing.

scholarly journals In vitro and in vivo anthelmintic activity of extracts from Artemisia parviflora and A. sieversiana

2017 ◽  
Vol 54 (3) ◽  
pp. 218-224 ◽  
Author(s):  
S. Irum ◽  
H. Ahmed ◽  
B. Mirza ◽  
K. Donskow-Łysoniewska ◽  
A. Muhammad ◽  
...  
Keyword(s):  
Adult Worm ◽  
Plant Extracts ◽  
Small Ruminants ◽  
Anthelmintic Activity ◽  
Gastrointestinal Nematodes ◽  
Economic Losses ◽  
Egg Hatching ◽  
Infective Larvae

SummaryIn the northern areas of Pakistan, the use of Artemisia based therapeutics is a common practice. Plants of genus Artemisia are known to possess anthelmintic and therapeutic effect. Infections caused by gastrointestinal nematodes are major threat to livestock industry across the world resulting in loss of production and indirect economic losses due to high cost of anthelmintic drugs. Present study was carried out to evaluate in vitro and in vivo effect of Artemisia sieversiana and Artemisia parviflora on Haemonchus contortus, a parasitic nematode of small ruminants. Methanolic plant extract was tested against three different developmental stages using an egg hatch assay, infective larvae and adult worm motility assay. Different concentrations were used for the bioassays and post exposure mortality was recorded after 8 hr for adult worms and infective larvae, while egg inhibition percentage was observed after 27 hr. A highly significant ability to inhibit the egg hatching (100 %) was recorded for both plant extracts while, the highest activity for adult worm assay and larvicidal assay was 90 % for A. sieversiana. The highest activity for adult motility and larvicidal assay for A. parviflora was 89 % and 86.6 % respectively. For in vivo trials maximum parentage reduction was 77.0 % for A. sieversiana and 73.6 % for A. parviflora. It is concluded that selected plant extracts were effective in reducing worm burden in animals.

scholarly journals Anthelmintic action of plant cysteine proteinases against the rodent stomach nematode,Protospirura muricola,in vitroandin vivo

Parasitology ◽  
2006 ◽  
Vol 134 (1) ◽  
pp. 103-112 ◽  
Author(s):  
G. STEPEK ◽  
A. E. LOWE ◽  
D. J. BUTTLE ◽  
I. R. DUCE ◽  
J. M. BEHNKE
Keyword(s):  
Detrimental Effect ◽  
Gastrointestinal Nematodes ◽  
Cysteine Proteinases ◽  
Trichuris Muris ◽  
Kiwi Fruit ◽  
Heligmosomoides Polygyrus ◽  
Anthelmintic Efficacy ◽  
Papaya Latex

Cysteine proteinases from the fruit and latex of plants, including papaya, pineapple and fig, were previously shown to have a rapid detrimental effect,in vitro, against the rodent gastrointestinal nematodes,Heligmosomoides polygyrus(which is found in the anterior small intestine) andTrichuris muris(which resides in the caecum). Proteinases in the crude latex of papaya also showed anthelmintic efficacy against both nematodesin vivo. In this paper, we describe thein vitroandin vivoeffects of these plant extracts against the rodent nematode,Protospirura muricola, which is found in the stomach. As in earlier work, all the plant cysteine proteinases examined, with the exception of actinidain from the juice of kiwi fruit, caused rapid loss of motility and digestion of the cuticle, leading to death of the nematodein vitro. In vivo, in contrast to the efficacy againstH. polygyrusandT. muris, papaya latex only showed efficacy againstP. muricolaadult female worms when the stomach acidity had been neutralized prior to administration of papaya latex. Therefore, collectively, our studies have demonstrated that, with the appropriate formulation, plant cysteine proteinases have efficacy against nematodes residing throughout the rodent gastrointestinal tract.

scholarly journals Essential Oils and Their Bioactive Compounds in the Control of Gastrointestinal Nematodes of Small Ruminants

2018 ◽  
Vol 46 (1) ◽  
pp. 14 ◽  
Author(s):  
Weibson Paz Pinheiro André ◽  
Wesley Lyeverton Correia Ribeiro ◽  
Lorena Mayana Beserra de Oliveira ◽  
Iara Tersia Freitas Macedo ◽  
Fernanda Cristina Macedo Rondon ◽  
...  
Keyword(s):  
Natural Products ◽  
Essential Oils ◽  
Bioactive Compounds ◽  
Small Ruminant ◽  
Anthelmintic Activity ◽  
Gastrointestinal Nematodes ◽  
In Vivo Tests ◽  
Anthelmintic Effect

Background: Gastrointestinal nematodes are one of the major health and economic problem of sheep and goats in the world. The control of these nematodes is carried out conventionally with synthetic anthelminths, which favored the selection of gastrointestinal nematode (GIN) populations multiresistant to anthelmintics. The emergence of anthelmintic resistance has stimulated the search for new alternatives to control small ruminant GIN, standing out the use of plants and their bioactives compounds, such as essential oils (EO). The objective of this review was to present the main characteristics and anthelmintic activity of EO, their isolated compounds and drug delivery systems in the control of GIN.Review: Essential oils are a complex blend of bioactive compounds with volatile, lipophilic, usually odoriferous and liquid substances. EO are composed of terpenes, terpenoids, aromatic and aliphatic constituents. EO has various pharmacological activities of interest in preventive veterinary medicine such as antibacterials, antifungals, anticoccicids, insecticides and anthelmintics. In vitro and in vivo tests are used to validate the anthelmintic activity of EO on GIN. In vitro tests are low cost screening tests that allow the evaluation of the anthelmintic activity of a large amount of bioactive compounds on eggs, first (L1) and third stage larvae (L3), and adult nematodes. The antiparasitic effect of EO is related to its main compound or to the interaction of the compounds. These bioactive compounds penetrate the cuticle of the nematodes by transcuticular diffusion, altering the mechanisms of locomotion, besides causing cuticular lesions. Following in vitro evaluation, the acute and sub-chronic toxicity test should be performed to assess the toxicity of the bioactive compounds and to define the dose to be used in in vivo tests. In vivo tests are more reliable because the anthelmintic effectiveness of bioactive compounds is evaluated after the metabolization process. The metabolization process of the bioactive compounds can generate metabolites that exhibit or not anthelmintic effectiveness. The in vivo tests assessing the anthelmintic effectiveness of bioactive compounds in sheep and goats are the fecal egg count reduction test and the controlled test.  OE promoted reduction of egg elimination in faeces which may be related to cuticular and reproductive alterations in GIN, and reduction of parasite burden in in vivo tests. Due to the promising results obtained with OE in the in vivo tests, interest has been aroused in using nanotechnology as an alternative to increase the bioavailability of OE and consequently, potentializing its anthelmintic effect, reducing the dose and  toxicity of the biocompounds. In addition to nanotechnology, the isolation and chemical modification of compounds isolated from OE have been employed to obtain new molecules with anthelmintic action and understand the mechanism of action of EO on the small ruminant GIN.Conclusion: The use of EO and their compound bioactive in the control of resistant populations of GIN is a promising alternative. The adoption of strategies in which natural products can replace synthetic anthelmintics, such as in dry periods and use synthetic anthelmintics in the rainy season when the population in refugia in the pasture is high, thus reducing the dissemination of GIN resistant populations. As perspective, the evaluation of pharmacokinetics and pharmacodynamics of these natural products should be performed so that one defines treatment protocols that optimize the anthelmintic effect.

scholarly journals Evaluation of Eucalyptus citriodora essential oil on goat gastrointestinal nematodes

2011 ◽  
Vol 20 (3) ◽  
pp. 223-227 ◽  
Author(s):  
Iara Tersia Freitas Macedo ◽  
Claudia Maria Leal Bevilaqua ◽  
Lorena Mayana Beserra de Oliveira ◽  
Ana Lourdes Fernandes Camurça-Vasconcelos ◽  
Luiz da Silva Vieira ◽  
...  
Keyword(s):  
Acute Toxicity ◽  
Essential Oil ◽  
Larval Development ◽  
Anthelmintic Activity ◽  
Gastrointestinal Nematodes ◽  
Gastrointestinal Parasites ◽  
Eucalyptus Citriodora ◽  
Egg Hatching

Phytotherapy may be an alternative strategy for controlling gastrointestinal parasites. This study evaluated the anthelmintic efficacy of Eucalyptus citriodora essential oil (EcEO). The in vitro effects of EcEO were determined through testing the inhibition of egg hatching and larval development of Haemonchus contortus. EcEO was subjected to acute toxicity testing on mice, orally and intraperitoneally. The in vivo effects of EcEO were determined by the fecal egg count reduction test (FECRT) in goats infected with gastrointestinal nematodes. The results showed that 5.3 mg.mL-1 EcEO inhibited egg hatching by 98.8% and 10.6 mg.mL-1 EcEO inhibited H. contortus larval development by 99.71%. The lethal doses for 50% of the mice were 4153 and 622.8 mg.kg-1, for acute toxicity orally and intraperitoneally. In the FECRT, the efficacy of EcEO and ivermectin was 66.25 and 79.16% respectively, on goat gastrointestinal nematodes eight days after treatment. EcEO showed in vitro and in vivo anthelmintic activity.

Anthelmintic activity of plants against gastrointestinal nematodes of goats: a review

Parasitology ◽  
2019 ◽  
Vol 146 (10) ◽  
pp. 1233-1246 ◽  
Author(s):  
Francianne Oliveira Santos ◽  
Amanda Ponce Morais Cerqueira ◽  
Alexsandro Branco ◽  
Maria José Moreira Batatinha ◽  
Mariana Borges Botura
Keyword(s):  
Animal Feed ◽  
Chemical Constituents ◽  
Plant Secondary Metabolites ◽  
Herbal Medicines ◽  
Anthelmintic Activity ◽  
Gastrointestinal Nematodes ◽  
Free Living ◽  
Anthelmintic Effect

AbstractThe gastrointestinal nematodes (GIN) stand out as an important cause of disease in small ruminant, especially on goat farm. Widespread resistance to synthetic anthelminthics has stimulated the research for alternative strategies of parasite control, including the use of medicinal plants. The present work summarizes the in vitro and in vivo studies of plants with activity against GIN of goats, focusing on the description of chemical constituents related to this effect. This review retrieved 56 scientific articles from 2008 to 2018 describing more than 100 different plant species. The most frequently investigated family was Fabaceae (30.7%). Most in vitro studies on the activity of plant extracts and fractions were carried out with of free-living stages nematodes. In vivo studies were conducted mainly with the use of plants in animal feed and generally showed lower effectiveness compared to in vitro assays. The main plant secondary metabolites associated with anthelmintic effect are condensed tannins, saponin and flavonoids. However, the studies with compounds isolated from plants and elucidation of their mechanisms of action are scarce. Herbal medicines are thought to be promising sources for the development of effective anthelmintic agents.

scholarly journals Ovicidal activity of succinic acid isolated from sisal waste (Agave sisalana) against gastrointestinal nematodes of goats

2017 ◽  
Vol 47 (8) ◽  
Author(s):  
Nathália Silva de Souza Santos ◽  
Jener David Gonçalves Santos ◽  
Francianne Oliveira Santos ◽  
Taiane Menezes Serra ◽  
Hélimar Gonçalves de Lima ◽  
...  
Keyword(s):  
Succinic Acid ◽  
Anthelmintic Activity ◽  
Vero Cells ◽  
Gastrointestinal Nematodes ◽  
Significant Inhibition ◽  
Egg Hatching ◽  
The Mean ◽  
Agave Sisalana

ABSTRACT: This study was conducted to evaluate the in vitro anthelmintic activity of the succinic acid (SA) isolated from sisal waste against gastrointestinal nematodes of goats, using the egg hatching and larvae motility assays. In addition, potential cytotoxicity of SA on Vero cell cultures was investigated by means of MTT (3-4,5-dimethylthiazol-2-yl, 2,5diphenyltetrazolium bromide) test. The SA induced a significant inhibition of egg hatching (P<0.05) at all concentrations tested (60 to 250µg mL-1), and the concentrations to inhibit 50% (EC50) and 90% (EC90) values (mean ± standard deviation) were 90.3±2.8 and 130.6±3.5µg mL-1, respectively. The SA has not shown larvicidal activity. The SA was less toxic to the Vero cells, with the mean percentage of cell viability equal to 85±6.2% at the concentration of 130µg mL-1. The results suggested that SA has potential anthelmintic effect; although, more research is needed to confirm its activity in vivo.

Anthelmintic efficacy ofAchillea millifoliumagainst gastrointestinal nematodes of sheep:in vitroandin vivostudies

2008 ◽  
Vol 82 (3) ◽  
pp. 227-233 ◽  
Author(s):  
K.A. Tariq ◽  
M.Z. Chishti ◽  
F. Ahmad ◽  
A.S. Shawl
Keyword(s):  
Body Weight ◽  
Anthelmintic Activity ◽  
Gastrointestinal Nematodes ◽  
Water Soluble ◽  
Aqueous Extracts ◽  
Anthelmintic Efficacy ◽  
Ethanolic Extracts ◽  
Motility Inhibition

AbstractAchillea millifoliumLinn., commonly called ‘Pehl-ghasa’, is used by farmers in traditional animal health care as a vermifuge. The objective of this study was to evaluate the anthelmintic efficacy of crude aqueous extracts and crude ethanolic extracts of entireA. millifoliumagainst the gastrointestinal nematodes of sheep. The worm motility inhibition assay was used forin vitrostudies and faecal egg count reduction assay was used forin vivostudies.In vitrostudies revealed significant anthelmintic effects of aqueous extracts and ethanolic extracts on liveHaemonchus contortusworms (P < 0.05) as evident from their paralysis and/or death at 8 h post exposure. Aqueous extracts ofA. millifoliumresulted in a mean worm motility inhibition of 94.44%, while ethanolic extracts resulted in mean worm motility inhibition of 88.88%. The mean mortality index of aqueous extracts was 0.95 while for ethanolic extracts it was 0.9. The lethal concentration 50 was 0.05 mg ml− 1for aqueous extracts and 0.11 mg ml− 1for ethanolic extracts. Thein vivoanthelmintic activity of aqueous and ethanolic extracts ofA. millifoliumdemonstrated a maximum (88.40%) nematode egg count reduction in sheep treated with aqueous extracts at 2 g kg− 1body weight on day 15 after treatment. Ethanolic extracts resulted in a maximum of 76.53% reduction in faecal egg counts on day 15 after treatment with 2 g kg− 1body weight. Thus, the aqueous extracts exhibited greater anthelmintic activity under bothin vitroandin vivoconditions, and could be due to the presence of water-soluble active principle/s inA. millifolium. It is concluded that the entire plant ofA. millifoliumpossesses significant anthelmintic activity and could be a potential alternative for treating cases of helminth infections in ruminants.

scholarly journals In vitro anthelmintic effects of cysteine proteinases from plants against intestinal helminths of rodents

2007 ◽  
Vol 81 (4) ◽  
pp. 353-360 ◽  
Author(s):  
Gillian Stepek ◽  
Ann E. Lowe ◽  
David J. Buttle ◽  
Ian R. Duce ◽  
Jerzy M. Behnke
Keyword(s):  
Rapid Development ◽  
Intestinal Helminths ◽  
Cysteine Proteinases ◽  
Trichuris Muris ◽  
Heligmosomoides Polygyrus ◽  
Development Of Resistance ◽  
Taxonomic Groups ◽  
Gi Helminths

AbstractInfections with gastrointestinal (GI) nematodes are amongst the most prevalent worldwide, especially in tropical climates. Control of these infections is primarily through treatment with anthelmintic drugs, but the rapid development of resistance to all the currently available classes of anthelmintic means that alternative treatments are urgently required. Cysteine proteinases from plants such as papaya, pineapple and fig are known to be substantially effective against three rodent GI nematodes, Heligmosomoides polygyrus, Trichuris muris and Protospirura muricola, both in vitro and in vivo. Here, based on in vitro motility assays and scanning electron microscopy, we extend these earlier reports, demonstrating the potency of this anthelmintic effect of plant cysteine proteinases against two GI helminths from different taxonomic groups – the canine hookworm, Ancylostoma ceylanicum, and the rodent cestode, Rodentolepis microstoma. In the case of hookworms, a mechanism of action targeting the surface layers of the cuticle indistinguishable from that reported earlier appears to be involved, and in the case of cestodes, the surface of the tegumental layers was also the principal location of damage. Hence, plant cysteine proteinases have a broad spectrum of activity against intestinal helminths (both nematodes and cestodes), a quality that reinforces their suitability for development as a much-needed novel treatment against GI helminths of humans and livestock.

In vitro anthelmintic activity of active compounds of the fringed rue Ruta chalepensis against dairy ewe gastrointestinal nematodes

2016 ◽  
Vol 91 (4) ◽  
pp. 447-453 ◽  
Author(s):  
E. Ortu ◽  
G. Sanna ◽  
A. Scala ◽  
G. Pulina ◽  
P. Caboni ◽  
...  
Keyword(s):  
Essential Oil ◽  
Small Ruminant ◽  
Methanol Extract ◽  
Anthelmintic Activity ◽  
Gastrointestinal Nematodes ◽  
Economic Losses ◽  
Ruta Chalepensis ◽  
Alternative Ingredients ◽  
Third Stage

AbstractInfections by gastrointestinal nematodes negatively affect small ruminant health and at the same time cause substantial economic losses worldwide. Because resistance to conventional anthelmintic compounds is growing, target studies evaluating the effectiveness of alternative ingredients of botanical origin on gastrointestinal nematodes are needed. In this study, we evaluated the in vitro anthelmintic activity of Ruta chalepensis L. extracts on the third-stage larvae of sheep gastrointestinal nematodes. A methanol extract showed the highest anthelmintic activity, with an EC50 = 0.10 ± 0.06 mg/ml after 96 h, while the essential oil had an EC50 = 1.45 ± 1.22 mg/ml after 48 h. Moreover, three secondary metabolites of the essential oil, i.e. 2-decanone, 2-nonanone and 2-undecanone, showed EC50 values of 0.07 ± 0.06, 0.25 ± 0.29 and 0.88 ± 0.73 mg/ml at 24 h, respectively. The present study indicated that the R. chalepensis methanol extract, the essential oil and its metabolites 2-decanone, 2-nonanone and 2-undecanone showed promising anthelmintic activity on gastrointestinal nematodes.

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