Cysticidal activity of extracts and isolated compounds from Teloxys graveolens: In vitro and in vivo studies

Palomares-Alonso, Francisca; Rojas-Tomé, Irma Susana; Rocha, Victorino Juárez; Hernández, Guadalupe; González-Maciel, Angélica; Ramos-Morales, Andrea; Santiago-Reyes, Rosalba; González-Hernández, Iliana; Jung‐Cook, Helgi

doi:10.1016/j.exppara.2015.06.001

Cited by 8 publications

(5 citation statements)

References 23 publications

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“…More recently, a study by Dhakal et al (2015) also conclusively proved that tannins from three different plants (Pinus sp., Corylus avellana and Trifolium repens) bring out significant in vitro anthelmintic effects on Hymenolepis diminuta. Likewise, Palomares-Alonso et al (2015) also reported that the in vitro and in vivo cysticidal activity of Teloxys graveolens against Taenia crassiceps cysts is due to its flavonoid active principle, pinocembrin. Therefore, it is assumed that either of the reported phytoconstituents of C. joufra may be responsible for its observed anthelmintic activity in the present study.…”

Section: Discussionmentioning

confidence: 92%

Therapecutic efficacy of the leaf extract of Croton joufra Roxb. against experimental cestodiasis in rats

Gogoi

Yadav

2016

J Parasit Dis

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The leaves of have been used as a traditional medicine in Assam (Northeast India) to treat the intestinal helminthic infections. The aim of this study was to establish the in vitro and in vivo anthelmintic efficacy of the leaf extract of this plant on, a zoonotic tapeworm. The plant extract was also screened for its chemical constituents. The in vitro anthelmintic efficacy of the plant was evaluated by physical motility test on adult cestodes, following their exposure to 10, 20, 30 mg/ml concentrations of the crude leaf extract, while the in vivo effect was determined based on the eggs per gram (EPG) counts and worm recovery rates, using an experimentally induced model of infections in Wistar rats. The in vitro study results showed a dose-dependent effect on the parasite and the highest concentration of the extract (30 mg/ml) caused mortality of the worms in 1.53 ± 0.12 h as compared to 3.46 ± 0.10 h shown by 1 mg/ml concentration of the reference drug, praziquantel (PZQ). The in vivo results showed that a single 800 mg/kg dose of the extract, given for 3 days, was highly efficacious against adult parasites as it reduced the EPG count and worm burdens of rats by 94.74 and 75 %, respectively. The extract also showed almost similar degree of effects against the larval stage of the parasite. As ascertained by the qualitative screening tests, the leaf extract of contains terpenoids, tannins, alkaloids, flavonoids, glycosides and reducing sugar. The overall findings of this study suggest that leaf extract possesses significant anthelmintic efficacy and support its traditional anthelmintic claims.

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Section: Discussionmentioning

confidence: 92%

Therapecutic efficacy of the leaf extract of Croton joufra Roxb. against experimental cestodiasis in rats

Gogoi

Yadav

2016

J Parasit Dis

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“…14) These considerations have proved to be key structural features required for the binding of other tubulin polymerization inhibitors to this binding site. 30) Figure 2A shows the rDock score profile of the predicted binding modes and its RMSD when compared with the lowest binding free energy conformation. Contrary to what is observed in the NZ and ABZ-SO binding modes, the best rDock scores with the lowest RMSD values were obtained with the 1,5-tautomer due to the presence of the bulky substituent (Fig.…”

Section: Resultsmentioning

confidence: 99%

Evaluation of New Benzimidazole Derivatives as Cysticidal Agents: <i>In Vitro</i>, <i>in Vivo</i> and Docking Studies

González-Hernández

Palomares-Alonso

Becerril-Vega

et al. 2019

CHEMICAL & PHARMACEUTICAL BULLETIN

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Based on our previous research on cysticidal drugs, we report the synthesis and evaluation of three new benzimidazole derivatives. In these compounds, the amido group was used as a bioisosteric replacement of the ester group. The molecular docking on β-tubulin revealed that the derivatives interacted through hydrogen bonding with N165, E198 and V236. All compounds showed in vitro activity against Taenia crassiceps cysts. Among them, benzimidazole 3 was found to be the most potent of the series (EC 50 0.86 µM). This compound also exhibited the highest probability of binding and the lowest binding free energy score and was therefore selected for in vivo evaluation. Results indicated that the efficacy of compound 3 was comparable to that of the reference drug, albendazole (50.39 vs. 47.16% parasite reduction). Animals treated with compound 3 seemed to tolerate this benzimidazole well, with no changes in behavior, or food and water consumption. These findings are consistent with the in silico prediction results, which indicated low toxicity risks. The pharmacokinetic study showed that the half-life and mean residence time (6.06 and 11.9 h, respectively) were long after oral administration. Together, these results indicate that this new benzimidazole derivative represents a promising structure with cysticidal activity.

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“…The criteria to assess parasite mortality were loss of vesicular fluid, paralysis of the membrane and collapse of parasites. 42 On day 12, the mortality of parasites was established using the Trypan Blue exclusion test (Louis, K.S., Siegel, A.C., 2011). To evaluate the effect of each treatment in vitro , a sample of living cysts was extracted on day 12 and observed under the microscope.…”

Section: Methodsmentioning

confidence: 99%

β-cyclodextrin dendritic derivatives as permeation mediators to enhance the in vitro albendazole cysticidal activity by the improvement of the diffusion component

et al. 2022

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Cysticidal activity of extracts and isolated compounds from Teloxys graveolens: In vitro and in vivo studies

Cited by 8 publications

References 23 publications

Therapecutic efficacy of the leaf extract of Croton joufra Roxb. against experimental cestodiasis in rats

Therapecutic efficacy of the leaf extract of Croton joufra Roxb. against experimental cestodiasis in rats

Evaluation of New Benzimidazole Derivatives as Cysticidal Agents: <i>In Vitro</i>, <i>in Vivo</i> and Docking Studies

β-cyclodextrin dendritic derivatives as permeation mediators to enhance the in vitro albendazole cysticidal activity by the improvement of the diffusion component

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