anthelmintic activity
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Author(s):  
Faustin Parfait Koutouan ◽  
Yapo Magloire Yapi ◽  
Souleymane Kande ◽  
Eboua Narcisse Wandan

Background: Internal parasitosis is the most important parasitism in small ruminants in tropical region. Synthetic anthelmintics are usually used for their control. Due to the emergence of resistance in worm population, the use of alternative methods such as plants bioactive molecules are developed. This study aimed at assessing anthelmintic activity of nine varieties of Cajanus cajan, a taniferous plant cultivated in West Africa. Methods: Leaves of the nine varieties of Cajanus cajan were dried, ground and hydroacetonic extracts were obtained by cold maceration at a concentration of 60 mg/ml. Live adult of Haemonchus contortus were obtained from sheep’s stomach and exposed, in triplicate, to the following solutions: hydroacetonic extracts (60 mg/ml), hydroacetonic extracts (60 mg/ml) associated with polyvinylpyrrolidone (PVP) (50 mg/ml), Levamisole (20 mg/ml) and phosphate buffered saline (PBS) solution. Worm death time was recorded for each treatment. Result: Worms exposed to Levamisole recorded the shortest death time about 9.73±1.77 min. The potent of the extracts induced worm death time of 64.83±4.73 min while the least efficient induced a death time of 156.50±23.20 min. Worms in the PBS solution were still alive after 24 hours of exposure. These results indicated that the four varieties of C. cajan used in this study have promising wormicidal. Besides that, the effect of tannins were not the only compound responsible for the anthelmintic activity.


2022 ◽  
Author(s):  
Elora Valderas-García ◽  
Cécile Häberli ◽  
María Álvarez Bardón ◽  
Nerea Escala ◽  
Verónica Castilla Gómez de Agüero ◽  
...  

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.


Author(s):  
Shiny Joy ◽  
P. Eswara Prasad ◽  
K. Padmaja ◽  
K. Adilaxamamma ◽  
V. Chengalva Rayulu ◽  
...  

Background: A study was conducted to evaluate the antioxidant and immunological profile of methanolic extract of Adhatoda vasica leaves (AVE) in naturally infected sheep with gastrointestinal nematodes and compared with commonly used anthelmintic albendazole in sheep. Methods: Fifty four sheep found positive for gastrointestinal nematodes were divided into 3 equal groups, GI (infected-untreated: control), GII (infected- AVE treated) and GIII (infected- albendazole treated). Blood samples were drawn on 5th and 14th day after treatment for analysis of oxidative stress markers such as TBARS, TAC, SOD and catalase and immunological parameters such as total immunoglobulin, IgG and IL-10. Result: Helminthiasis in sheep cause a considerable oxidative stress. The anthelmintic activity of Adhatoda vasica surpassed the conventional synthetic drug albendazole in sheep in terms of oxidative and immunological changes in blood.


2022 ◽  
Vol 23 (2) ◽  
pp. 771
Author(s):  
José Manuel Ezquerra-Aznárez ◽  
Giulia Degiacomi ◽  
Henrich Gašparovič ◽  
Giovanni Stelitano ◽  
Josè Camilla Sammartino ◽  
...  

Avermectins are macrocyclic lactones with anthelmintic activity. Recently, they were found to be effective against Mycobacterium tuberculosis, which accounts for one third of the worldwide deaths from antimicrobial resistance. However, their anti-mycobacterial mode of action remains to be elucidated. The activity of selamectin was determined against a panel of M. tuberculosis mutants. Two strains carrying mutations in DprE1, the decaprenylphosphoryl-β-D-ribose oxidase involved in the synthesis of mycobacterial arabinogalactan, were more susceptible to selamectin. Biochemical assays against the Mycobacterium smegmatis DprE1 protein confirmed this finding, and docking studies predicted a binding site in a loop that included Leu275. Sequence alignment revealed variants in this position among mycobacterial species, with the size and hydrophobicity of the residue correlating with their MIC values; M. smegmatis DprE1 variants carrying these point mutations validated the docking predictions. However, the correlation was not confirmed when M. smegmatis mutant strains were constructed and MIC phenotypic assays performed. Likewise, metabolic labeling of selamectin-treated M. smegmatis and M. tuberculosis cells with 14C-labeled acetate did not reveal the expected lipid profile associated with DprE1 inhibition. Together, our results confirm the in vitro interactions of selamectin and DprE1 but suggest that selamectin could be a multi-target anti-mycobacterial compound.


2022 ◽  
Vol 2022 ◽  
pp. 1-7
Author(s):  
Thierry Roland Kang ◽  
Jerome Nyhalah Dinga ◽  
Ayuk Elizabeth Orock ◽  
Elvis Monya ◽  
Moses Njutain Ngemenya

Onchocerciasis is a parasitic infection affecting a relatively small population globally but has very devastating pathological outcomes. Ivermectin and recently moxidectin are the only drugs approved for clinical management of the disease, both of which have several limitations. In particular, they are efficacious against microfilariae (microfilaricidal) with no activity against adult worms (nonmacrofilaricidal). Promising anthelmintic activity has been reported in some lichens. This study investigated three lichens, Usnea articulata, Parmotrema tinctorum, and Heterodermia obscurata, found on Mount Cameroon, for potential macrofilaricidal activity. Organic extracts were screened for anti-Onchocerca activity against Onchocerca ochengi isolated from cattle skin using worm motility and MTT formazan assays. Toxicity of highly active extracts was investigated on monkey kidney epithelial (LLCMK2) cells and in BALB/c mice (2000 mg/kg body weight) including effects on liver enzymes. The methanol extract of P. tinctorum (Pammet) was the most active against adult male worms ( I C 50 = 8.1  μg/mL) with the highest selectivity index ( SI = 21.3 ). U. articulata was the most active against the adult female ( I C 50 = 36.3  μg/mL) but had a low SI value (3.4). No mortality and no adverse effects were recorded in the acute toxicity test. These two most active extracts had no significant effect on liver enzymes, alanine aminotransferase, and aspartate ( P values < 0.05), but a high AST : ALT ratio (2.59) for Pammet indicates likely reversible adverse hepatic toxicity. The high macrofilaricidal activity and selectivity of P. tinctorum suggest it is a potential source of new macrofilaricides which should be further investigated to identify its bioactive constituents.


2022 ◽  
Author(s):  
Raveesha Peeriga ◽  
Keerthi Priyanka Adarapu ◽  
Kavya Sri Sanivar ◽  
Jyothsna Kanumuri ◽  
Rikith Swamy Akunuri ◽  
...  

Abstract Background:Worm infections in developing countries were reported high. Phytoconstituents have been a vital role for the treatment of many ailments. The current study was aimed assess for anthelmintic activity of different root extracts of Dechaschistia crotonifolia Wight & Arn. belongs to the family Ebanaceae against Pheretima posthuma. Further Insilico study was carried out for phytocompounds present in Dechaschistia. Results: The chloroform, ethylacetate and ethanol extract of Dechaschistia crotonifolia Wight & Arn. were considered for the study of anthelmintic property on earthworms at concentrations 20 mg/ml, 40 mg/ml and 60 mg/ml. During this study, the parameters paralysis time (Pt) and Death Time (Dt) of adult Indian earthworms was observed. As a standard and control Albendazole 10 mg/ml and 2% Tween 80 in distilled water were taken respectively. The study resulted that ethanolic extract was significant when compared with the Albendazole 10 mg/ml. Docking studies revealed the all phytocompounds in Dechaschistia shown binding affinity, however comparatively scopoletin and stigmasterol had shown a good binding affinitiy about -7.7 Kcal/mol and -7.6 Kcal/mol compared to standard drug Albendazole which was shown about -8.7 Kcal/mol. Conclusion: The study revealed that the ethanol extract of Dechaschistia crotonifolia Wight & Arn. at a concentration of 60mg/ml exhibited a stronger anthelmintic property compared to Albendazole 10mg/ml. A dose dependent anthelmintic activity is exerted by all the extracts in an ascending manner Chloroform<Ethyl acetate<Ethanol. These observations were made evidenced by docking studies of phytocompounds in Dechaschistia as the phytocompounds were shown excellent docking score when compared with standard Albendazole.


2022 ◽  
Vol 46 (1) ◽  
Author(s):  
Haladu Ali Gagman ◽  
Hamdan Ahmad ◽  
Nik Ahmad Irwan Izzaudin Nik Him ◽  
Silas Wintuma Avicor

Abstract Background Although Guiera senegalensis is used as a dewormer in ethnoveterinary health care in Nigeria, its anthelmintic potential has not been validated. Hence, this work investigated the in vitro anthelmintic potential of G. senegalensis extracts on two Caenorhabditis elegans strains: Bristol N2 (wild type/ivermectin susceptible) and DA1316 (ivermectin resistant). Results Aqueous and methanol extracts of G. senegalensis were tested against the motility of the L4 larvae at two exposure periods of 24 and 48 h and found to be active against the C. elegans strains. Motility of C. elegans DA1316 was reduced to 18.6% and 8.3% by aqueous and methanol extracts, respectively, at 2.0 mg/ml after 48 h, whereas that of C. elegans DA1316 treated with ivermectin (0.02 µg/ml) remained above 95%. The motility of C. elegans Bristol N2 was reduced to 16.6% and 7.2% by aqueous and methanol extracts, respectively, at 2.0 mg/ml after 48 h and ≤ 2.7% by ivermectin (0.02 µg/ml). Activity of the plant extracts was concentration and time dependent. Conclusions This work confirms the anthelmintic activity of G. senegalensis and its effectiveness against ivermectin-resistant nematodes, thus validating its ethnoveterinary use as an animal dewormer in Nigeria and pharmacological potential as a source of anthelmintic compounds against ivermectin-resistant nematodes. There is, however, the need for in vivo studies to confirm the in vitro efficacy of the extracts.


2021 ◽  
Vol 18 ◽  
Author(s):  
Abdallah Aissa ◽  
Sujogya Kumar Panda ◽  
Haibo hu ◽  
Abdelkrim Kameli ◽  
Walter Luyten

Background: Plants are an abundant natural source of potential chemical compounds; they have been widely used in various industries, such as pharmaceuticals, cosmetics and food. This work aims to study two Saharan medicinal plants by evaluating the activity of plant extract against bacterial and fungal plant pathogens as well as against the model nematode Caenorhabditis (C.) elegans. Methods: The antimicrobial activity of plant extracts against plants pathogen is assessed in a 96-well plate assay by calculating the percentage of inhibition of bacteria. The antifungal activity against plant pathogenic fungi was evaluated by the agar diffusion method, inhibition was calculated by measuring the diameter of the inhibition zone. Anthelmintic activity was evaluated by calculating the average movement of C. elegans worms. Preliminary Phytochemical Screening is realized with HPTLC. Results: Hexane and ethyl acetate extract of Pergularia tomentosa showed broad-spectrum antimicrobial activity; this plant has the potential to act as a broad-spectrum antibacterial biopesticide. Hexane extract of Forsskaolea tenacissima exhibited good activity against one fungus. The extracts of Pergularia tomentosa showed good activity against Caenorhabditis elegans, the extracts of Forsskaolea tenacissima exhibited a low activity. Preliminary phytochemical screening with HPTLC shows that both plants are rich in steroids and flavonoids. Conclusion: Our study shows that the studied plants may possess a broad-spectrum antibacterial effect with a narrow-spectrum antifungal properties which can offer a more sustainable crop protection with a much safer environmental and human health impact. Plant extracts that inhibited C. elegans could provide a starting point for the development of new anthelmintic drugs.


Biomolecules ◽  
2021 ◽  
Vol 11 (12) ◽  
pp. 1893
Author(s):  
Mthandazo Dube ◽  
Mohamad Saoud ◽  
Robert Rennert ◽  
Ghislain Wabo Fotso ◽  
Kerstin Andrae-Marobela ◽  
...  

Ozoroa insignis Del. is an ethnobotanical plant widely used in traditional medicine for various ailments, including schistosomiasis, tapeworm, and hookworm infections. From the so far not investigated fruits of Ozoroa insignis, the anthelmintic principles could be isolated through bioassay-guided isolation using Caenorhabditis elegans and identified by NMR spectroscopic analysis and mass spectrometric studies. Isolated 6-[8(Z)-pentadecenyl] anacardic (1), 6-[10(Z)-heptadecenyl] anacardic acid (2), and 3-[7(Z)-pentadecenyl] phenol (3) were evaluated against the 5 parasitic organisms Schistosoma mansoni (adult and newly transformed schistosomula), Strongyloides ratti, Heligmosomoides polygyrus, Necator americanus, and Ancylostoma ceylanicum, which mainly infect humans and other mammals. Compounds 1–3 showed good activity against Schistosoma mansoni, with compound 1 showing the best activity against newly transformed schistosomula with 50% activity at 1µM. The isolated compounds were also evaluated for their cytotoxic properties against PC-3 (human prostate adenocarcinoma) and HT-29 (human colorectal adenocarcinoma) cell lines, whereby compounds 2 and 3 showed antiproliferative activity in both cancer cell lines, while compound 1 exhibited antiproliferative activity only on PC-3 cells. With an IC50 value of 43.2 µM, compound 3 was found to be the most active of the 3 investigated compounds.


Parasitology ◽  
2021 ◽  
pp. 1-37
Author(s):  
C.M. Albani ◽  
J. Borgo ◽  
J. Fabbri ◽  
P. Pensel ◽  
L. Fasciani ◽  
...  

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