scholarly journals In Vivo and In Vitro Pharmacodynamics of Anthelmintic Medication Used in Sheep

Author(s):  
Mihai CERNEA ◽  
Roxana FILIP ◽  
Raul CĂTANĂ ◽  
Laura CĂTANĂ

Our research aimed to evaluate the efficacy of anthelmintic treatments in sheep, as well as the resistance occurrence risk for the most commonly used substances. Anthelmintic medication efficacy was evaluated on 30 animals from a private farm, located in Sânmihaiu Almaşului, Sălaj County. In vivo studies were performed by using Fecal Egg Count Reduction Test (FECRT) and testing an albendazole-based (ABZ) product. In vitro, we used Egg Hatch Assay (EHA) and Larval Development Assay (LDA) for albendazole (ABZ), mebendazole (MBZ), fenbendazole (FBZ), thiabendazole (TBZ) and ivermectin (IVM) (only for LDA). FECRT showed that intestinal nematodes developed resistance phenomena against the ABZ-based product, with an extensivity of 80% at seven days post therapy, an egg reduction percentage of 41.89% at seven days post-therapy and 43.9% at 14 days post-therapy. The in vitro EHA highlighted a superior efficacy of TBZ (egg hatch percentage at reference concentration being 51.21) compared to ABZ (71.89%), MBZ (84.46%) and FBZ (79.22%), with a minimum risk of anthelmintic resistance. The LDA test revealed the superior efficacy of FBZ (MIC 0.59 mcg/ml) and IVM (MIC 0.078 mcg/ml), with a minimal risk of inducing parasitic resistance. All in vivo and in vitro tests revealed a limited ABZ efficacy, recommending avoiding the therapy with this substance.

Author(s):  
Laura CĂTANĂ ◽  
Raul CĂTANĂ ◽  
Roxana CORA ◽  
Ştefan RĂILEANU ◽  
Mihai CERNEA

The study was conducted using faecal samples from 62 dogs. We tested the ovicidal and larvicidal effects of albendazole (ABZ), mebendazole (MBZ), fenbendazole (FBZ) and flubendazole (FLU) by Egg hatch assay (EHA) and larval development assay (LDA). For pyrantel (PYR) and selamectin (SEL) we tested the larvicidal effects by LDA. In all in vitro tests, benzimidazoles efficacy was low, with a high risk of inducing resistance phenomena. In EHA more than 50% of the hookworm eggs hatched, revealing a low efficacy of all tested benzimidazoles. The regression line was positive for all benzimidazoles, FBZ having the smallest value of the Y parameter (62.62), and lower risk of resistance. When testing the larvicidal effects, a superior efficacy of benzimidazoles was observed. The lowest MIC was for MBZ (0.8672μg/ml). ABZ had a very poor effect (8.46750 μg/ml). The Y parameter showed a lower risk of inducing resistance for MBZ (Y= -64.14) and FBZ (Y= -27.89). Pyrantel and Selamectin were very effective, presenting also a very low risk of inducing resistance phenomena. For PYR and SEL, MIC was 0.2131 μg/ml and 2.7921 μg/ml, respectively. The Y parameter was -448.37 for PYR and -62.74 for SEL, with minimal risk of inducing the adaptive phenomena.


1997 ◽  
Vol 83 (3) ◽  
pp. 1033-1033 ◽  
Author(s):  
Thomas H. Shaffer ◽  
Raymond Foust ◽  
Marla R. Wolfson ◽  
Thomas F. Miller

Shaffer, Thomas H., Raymond Foust IIII, Marla R. Wolfson, and Thomas F. Miller, Jr. Analysis of perfluorochemical elimination from the respiratory system. J. Appl. Physiol. 83(3): 1033–1040, 1997.—We describe a simple apparatus for analysis of perfluorochemicals (PFC) in expired gas and thus a means for determining PFC vapor and liquid elimination from the respiratory system. The apparatus and data analysis are based on thermal conduction and mass transfer principles of gases. In vitro studies were conducted with the PFC vapor analyzer to determine calibration curves for output voltage as a function of individual respiratory gases, respiratory gases saturated with PFC vapor, and volume percent standards for percent PFC saturation (%PFC-Sat) in air. Voltage-concentration data for %PFC-Sat of the vapor from the in vitro tests were accurate to within 2.0% from 0 to 100% PFC-Sat, linear ( r = 0.99, P < 0.001), and highly reproducible. Calculated volume loss of PFC liquid over time correlated well with actual loss by weight ( r = 0.99, P < 0.001). In vivo studies with neonatal lambs demonstrated that PFC volume loss and evaporation rates decreased nonlinearly as a function of time. These relationships were modulated by changes in PFC physical properties, minute ventilation, and postural repositioning. The results of this study demonstrate the sensitivity and accuracy of an on-line method for PFC analysis of expired gas and describe how it may be useful in liquid-assisted ventilation procedures for determining PFC volume loss, evaporation rate, and optimum dosing and ventilation strategy.


2020 ◽  
Vol 26 ◽  
pp. 107602962096082
Author(s):  
Dalia Qneibi ◽  
Eduardo Ramacciotti ◽  
Ariane Scarlatelli Macedo ◽  
Roberto Augusto Caffaro ◽  
Leandro Barile Agati ◽  
...  

Low molecular weight heparins (LMWH) represent depolymerized heparin prepared by various methods that exhibit differential, biochemical and pharmacological profiles. Enoxaparin is prepared by benzylation followed by alkaline depolymerization of porcine heparin. Upon the expiration of its patent, several biosimilar versions of enoxaparin have become available. Heparinox (Sodic enoxaparine; Cristália Produtos Químicos Farmacêuticos LTDA, Sao Paulo, Brazil) is a new biosimilar form of enoxaparin. We assessed the molecular weight and the biochemical profile of Heparinox and compared its properties to the original branded enoxaparin (Lovenox; Sanofi, Paris, France). Clotting profiles compared included activated clotting time, activated partial thromboplastin time (aPTT), and thrombin time (TT). Anti-protease assays included anti-factor Xa and anti-factor IIa activities. Thrombin generation was measured using a calibrated automated thrombogram and thrombokinetic profile included peak thrombin, lag time and area under the curve. USP potency was determined using commercially available assay kits. Molecular weight profiling was determined using high performance liquid chromatography. We determined that Heparinox and Lovenox were comparable in their molecular weight profile. Th anticoagulant profile of the branded and biosimilar version were also similar in the clot based aPTT and TT. Similarly, the anti-Xa and anti-IIa activities were comparable in the products. No differences were noted in the thrombin generation inhibitory profile of the branded and biosimilar versions of enoxaparin. Our studies suggest that Heparinox is bioequivalent to the original branded enoxaparin based upon in vitro tests however will require further in vivo studies in animal models and humans to determine their clinical bioequivalence.


2020 ◽  
Vol 13 ◽  
Author(s):  
A. Sureda ◽  
M. Monserrat-Mesquida ◽  
S. Pinya ◽  
P. Ferriol ◽  
S. Tejada

Background:: Hypertension is a high prevalent chronic disease worldwide and a major cardiovascular risk factor. Oleanolic acid (3β-hydroxy-olea-12-en-28-oic acid) is a wide distributed bioactive pentacyclic triterpenoid with diverse biological activities such as anti-inflammatory, hepaprotective anti-diabetic or anti-hypertensive. Objective:: The aim of this study was to review and highlight the available data about antihypertensive activity of oleanolic acid and the described mechanisms of action. Method:: Extensive searches were made in the available literature on oleanolic acid and the data investigating its antihypertensive effects were analysed. Results:: Most of research has been performed on animal models of hypertension, ex vivo studies with aortic ring and some in vitro tests with cell cultures, whereas clinical trials are still lacking. Treatment of hypertensive animals with oleanolic acid significantly ameliorated the rise in the systolic blood pressure. In addition, the hypotensive effects of oleanolic acid are also related to a potent diuretic-natriuretic activity and nephroprotection. In vitro studies have characterized the participation of various signalling pathways that modulate the release of vasodilation mediators. Conclusion:: In vitro and in vivo studies suggest that oleanolic acid effectively reduce blood pressure and could be an interesting co-adjuvant to conventional treatment of hypertension.


Pathogens ◽  
2020 ◽  
Vol 9 (12) ◽  
pp. 1063
Author(s):  
Fabio Castagna ◽  
Domenico Britti ◽  
Manuela Oliverio ◽  
Antonio Bosco ◽  
Sonia Bonacci ◽  
...  

The worldwide increased difficulty to counteract gastrointestinal nematode (GIN) infection in sheep, due to progressing anthelmintic resistance, has led to the evaluation of other alternative helminth control options, mainly from plants. The anthelmintic efficacy of an aqueous Punica granatum macerate was evaluated in sheep naturally infected by GIN in southern Italy. The macerate was chemically characterized by chromatographic analysis coupled with high-resolution mass spectrometry (LC/HRMS) and an aliquot was concentrated to obtain a dry extract. A part was characterized, the remaining washed with methanol to obtain an insoluble residue and methanol phase. In the methanol fraction, the quantitatively predominant gallic acid was purified to obtain the pure molecule. The three fractions thus obtained were used for in vitro studies (i.e., egg hatch test) to verify anthelmintic efficacy. For this purpose, fecal samples were collected from sheep naturally infected by GINs. Fractions were diluted in H2O/DMSO 0.5% at 1.00, 0.5, 0.25, 0.125, 0.05, and 0.005 mg/mL concentrations. Thiabendazole (0.25 and 0.5 mg/mL) and deionized water were used as positive and negative controls, respectively. Egg hatch test results indicated that all fractions caused a significant (p < 0.05) egg hatch inhibition within 48 h of exposure highlighting a high (>82%) efficacy in vitro at all tested doses. Maximal egg hatching inhibition effect was exhibited by the methanol fraction (99.3% and 89.3% at 1 and 0.005 mg/mL concentrations), followed by the insoluble residue and gallic acid (94.7% and 85.3% and 94.0% and 82.7% at 1 and 0.005 mg/mL, respectively). The current study validated the anthelmintic potential of traditional P. granatum macerate against GIN infection in sheep, thus highlighting the role of gallic acid as principal component and justifying a need to undertake further in vivo studies on these ethno-veterinary remedies.


2015 ◽  
Vol 36 (6) ◽  
pp. 3751
Author(s):  
Natalie Neuwirt ◽  
Lilian Gregory ◽  
Eidi Yoshihara ◽  
Silvana Lima Gorniak

Helminthes are listed as one of the main problems facing the development of goat and sheep production. Haemonchus contortus is the specie that causes greatest negative impact in ranching. Resistance to anti-parasitic drugs and demand for residue-free animal-derived food products has elevated the importance of herbal treatments. The aim of this study was to develop an extract of Musa spp. and assess by in vitro testing, the anthelmintic effect on eggs and larvae in the gastrointestinal nematodes in sheep. Stool samples from sheep naturally infected were used to obtain eggs and larvae and was then followed by a test of hatchability and a larval migration inhibition test. In vitro tests on the inhibition of larval hatchability at concentrations of 160 and 180 mg mL-1 of larval extracts and inhibition of migration at concentrations of 800 and 1000 mg mL-1 were observed. The results indicate that the use of banana leaf has an anthelmintic effect and that in vivo studies on the applicability of this technology to the field should be made to further understanding and bring more information to what has already been revealed in this study.


Nanomedicine ◽  
2021 ◽  
Author(s):  
Reza Hosseinpour-Moghadam ◽  
Shahram Rabbani ◽  
Arash Mahboubi ◽  
Sayyed Abbas Tabatabai ◽  
Azadeh Haeri

Aim: To develop quercetin-loaded poly(caprolactone) (PCL)/soybean phosphatidylcholine (PC) films coated with silver (Ag) to prevent the formation of postoperative adhesions (POA). Materials & methods: Films were prepared using the solvent casting method, coated with Ag, and underwent  in vitro tests. In vivo studies were conducted employing an animal model of sidewall defect and cecum abrasion. Results: Films showed sustained release behavior of quercetin and Ag. Coating films with Ag improved their antimicrobial activity. In vivo studies confirmed superior antiadhesion properties of films compared with the control groups evaluated by gross observation, histochemical staining and immunohistochemistry analyses. Conclusion: Ag-Q-PCL-PC films are a potential candidate to prevent POA by acting as a sustained release delivery system and physical barrier.


2014 ◽  
Vol 2014 ◽  
pp. 1-7 ◽  
Author(s):  
Silvio César Gomes de Lima ◽  
Maria Jania Teixeira ◽  
José Evaldo Gonçalves Lopes Júnior ◽  
Selene Maia de Morais ◽  
Alba Fabiola Torres ◽  
...  

The aim of the present work was to evaluate antileishmanial activity ofAstronium fraxinifoliumandPlectranthus amboinicus. For the in vitro tests, essential oil ofP. amboinicus(OEPA) and ethanolic extracts fromA. fraxinifolium(EEAF) were incubated with 106  promastigotes ofL. (Viannia) braziliensis. The OEPA was able to reduce the parasite growth after 48 h; nonetheless, all the EEAFs could totally abolish the parasite growth. For the in vivo studies, BALB/c mice were infected subcutaneously (s.c.) with 107  L. braziliensispromastigotes. Treatment was done by administering OEPA intralesionally (i.l.) for 14 days. No difference was found in lesion thickness when those animals were compared with the untreated animals. Further, golden hamsters were infected s.c. with 106  L. braziliensispromastigotes. The first protocol of treatment consisted of ethanolic leaf extract fromA. fraxinifolium(ELEAF) administered i.l. for 4 days and a booster dose at the 7th day. The animals showed a significant reduction of lesion thickness in the 6th week, but it was not comparable to the animals treated with Glucantime. The second protocol consisted of 15 daily intralesional injections. The profiles of lesion thickness were similar to the standard treatment. In conclusion, in vivo studies showed a high efficacy when the infected animals were intralesionally treated with leaf ethanolic extract fromA. fraxinifolium.


2018 ◽  
Vol 19 (1) ◽  
pp. 45-45
Author(s):  
Dolores Fernández-Ortuño ◽  
Alejandra Vielba-Fernández ◽  
Alejandro Pérez-García ◽  
Juan A. Torés ◽  
Antonio de Vicente

Botrytis cinerea Pers. is an important fungal pathogen responsible for gray mold, one of the most economically important diseases of strawberry (Fragaria × ananassa) worldwide. The primary disease management strategy involves the application of different classes of fungicides, including the sterol biosynthesis inhibitor class III fungicide fenpyrazamine. In 2014 and 2015, strawberries affected with gray mold symptoms were collected from eight locations in Huelva, where fenhexamid had been used extensively. Twenty-five B. cinerea single-spore isolates were examined to determine EC50 values and to determine a discriminatory dose to monitor fenpyrazamine resistance in the field in future studies. The in vitro tests divided the isolates into two groups: 15 sensitive (EC50 from 0.02 to 1.3 μg/ml) and 10 resistant (EC50 from 50.1 to 172.6 μg/ml), which showed cross-resistance with fenhexamid. Performance of fenpyrazamine in in vivo studies was also carried out. Only the fenpyrazamine-resistant isolates developed gray mold on the fungicide-treated fruit. This is the first report of fenpyrazamine resistance in B. cinerea from strawberry fields in Spain and cross-resistance with fenhexamid.


2017 ◽  
Vol 26 (3) ◽  
pp. 323-330 ◽  
Author(s):  
Weibson Paz Pinheiro André ◽  
Géssica Soares Cavalcante ◽  
Wesley Lyeverton Correia Ribeiro ◽  
Jessica Maria Leite dos Santos ◽  
Iara Tersia Freitas Macedo ◽  
...  

Abstract Thymol is a monoterpene and acetylation form of this compound can reduce the toxicity and enhance its biological effects. The objective of this study was to evaluate the effect of thymol and thymol acetate (TA) on egg, larva and adult Haemonchus contortus and the cuticular changes, acute toxicity in mice and the efficacy on sheep gastrointestinal nematodes. In vitro tests results were analyzed by analysis of variance (ANOVA) and followed by comparison with Tukey test or Bonferroni. The efficacy of in vivo test was calculated by the BootStreet program. In the egg hatch test (EHT), thymol (0.5 mg/mL) and TA (4 mg/mL) inhibited larval hatching by 98% and 67.1%, respectively. Thymol and TA (8 mg/mL) inhibited 100% of larval development. Thymol and TA (800 µg/mL) reduced the motility of adult worms, by 100% and 83.4%, respectively. Thymol caused cuticular changes in adult worm teguments. In the acute toxicity test, the LD50 of thymol and TA were 1,350.9 mg/kg and 4,144.4 mg/kg, respectively. Thymol and TA reduced sheep egg count per gram of faeces (epg) by 59.8% and 76.2%, respectively. In in vitro tests thymol presented better anthelmintic activity than TA. However TA was less toxic and in in vivo test efficacy was similar.


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