Current drug targets for helminthic diseases

Rana, Ajay Kumar; Misra‐Bhattacharya, Shailja

doi:10.1007/s00436-013-3383-6

Cited by 52 publications

(26 citation statements)

References 114 publications

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“…On the other hand, some studies have suggested that treatment with nematicides as albendazole may constitute an effective therapy [10–13]. However, the worldwide development of resistance to chemical anthelmintic drugs [14] and a current social demand for natural therapeutic products has increased the search for new biocide molecules. Plant products are the basis of traditional medicine and the only health resource available in many communities from developing countries.…”

Section: Introductionmentioning

confidence: 99%

Activity of Tea Tree (Melaleuca alternifolia) Essential Oil against L3 Larvae ofAnisakis simplex

Gómez-Rincón

Langa

Murillo

et al. 2014

BioMed Research International

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Nematicidal activity of Melaleuca alternifolia essential oil, commonly known as tea tree oil (TTO), was assayed in vitro against L3 larvae of Anisakis simplex. The results showed a mortality of 100% for concentrations between 7 and 10 μL/mL after 48 h of incubation, obtaining an LD50 value of 4.53 μL/mL after 24 hours and 4.27 μL/mL after 48 hours. Concentration-dependent inhibition of acetylcholinesterase was observed for tea tree essential oil showing inhibition values of 100% at 100 μL/mL. This fact suggests that TTO may act as an AChE inhibitor. Terpinen-4-ol was discarded as main larvicide compound as it did not show larvicidal or anticholinesterase activity. The data obtained suggest that the essential oil of Melaleuca alternifolia may have a great therapeutic potential for the treatment of human anisakiasis.

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Section: Introductionmentioning

confidence: 99%

Activity of Tea Tree (Melaleuca alternifolia) Essential Oil against L3 Larvae ofAnisakis simplex

Gómez-Rincón

Langa

Murillo

et al. 2014

BioMed Research International

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“…Research study of the helminths is aiming to identify potential and drug gable targets through biochemical, biophysical, genomic, proteomic, in vivo and vitro experiments in animal models 13 . Therefore, in the last few years, they recommended to use of biological substance instead of chemicals in the dominate on parasites because of that these natural products have potency against different pathogens and mostly are safe to use 14,15 .…”

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confidence: 99%

Efficacy of Pomegranate (Punica granatum) Peel Extract Against Hymenolepis nana in infections Mice.

Al-Megrin¹

2016

Biosci., Biotech. Res. Asia

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To investigate the efficacy of pomegranate (Punica granatum) as an alternative and safe treatment against Hymenolipes nana through experimental study on the white laboratory mice. Twenty eight Swiss albino mice naturally infected with Hymenolipes nana. Animals were divided into four groups, one group as control and groups 2-4 were fed daily with dose 0.5 ml, 1.0 ml and 1.5 ml pomegranate peel extract (300 mg/kg) respectively, The egg counts per gram (EPG) one day before treatment and on day 1, 7, 14, and 21 after treatment . All animals were then sacrificed under on day 21. The content of intestines were examined for the presence of worms and counting. Results from current Study revealed that, pomegranate peel extract was lead to reduce the eggs output in fecal pellets of treated infected groups comparing with control group. In addition, the different doses 0.5 ml, 1.0 ml and 1.5 ml of a pomegranate peel extract demonstrated a directly proportional reduction in EPG count (31.5, 38.6 and 43.5) respectively. On the other hand, the number of worms at necropsy was decreased (15.6 ±2.6, 8.4 ±2.1 and 5.7±2.5) in treated infected groups (0.5 ml, 1.0 ml and 1.5 ml) respectively. The findings of this study indicate that Pomegranate peel extract has active role to treat infection of H. nana due to possesses potential anti-cestodal activity.

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“…Successful compounds would be inhibitors of an essential or unique bacterial enzyme which has no mammalian homologue. The number of drug targets for helminthic diseases so far identified is few (63), and the threats are compounding with burgeoning resistance against the existing drugs (64,65). The parasites and microorganisms are becoming increasingly resistant to the available antibiotics, which makes the search for novel antibiotic agents inevitable (66).…”

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confidence: 99%

Molecular Characterization of an rsmD -Like rRNA Methyltransferase from the Wolbachia Endosymbiont of Brugia malayi and Antifilarial Activity of Specific Inhibitors of the Enzyme

Rana

Chandra

Siddiqi

et al. 2013

Antimicrob Agents Chemother

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bThe endosymbiotic organism Wolbachia is an attractive antifilarial drug target. Here we report on the cloning and expression of an rsmD-like rRNA methyltransferase from the Wolbachia endosymbiont of Brugia malayi, its molecular properties, and assays for specific inhibitors. The gene was found to be expressed in all the major life stages of B. malayi. The purified enzyme expressed in Escherichia coli was found to be in monomer form in its native state. The activities of the specific inhibitors (heteroaryl compounds) against the enzyme were tested with B. malayi adult and microfilariae for 7 days in vitro at various concentrations, and NSC-659390 proved to be the most potent compound (50% inhibitory concentration [IC 50 ], 0.32 M), followed by NSC-658343 (IC 50 , 4.13 M) and NSC-657589 (IC 50 , 7.5 M). On intraperitoneal administration at 5 mg/kg of body weight for 7 days to adult jirds into which B. malayi had been transplanted intraperitoneally, all the compounds killed a significant proportion of the implanted worms. A very similar result was observed in infected mastomys when inhibitors were administered. Docking studies of enzyme and inhibitors and an in vitro tryptophan quenching experiment were also performed to understand the binding mode and affinity. The specific inhibitors of the enzyme showed a higher affinity for the catalytic site of the enzyme than the nonspecific inhibitors and were found to be potent enough to kill the worm (both adults and microfilariae) in vitro as well as in vivo in a matter of days at micromolar concentrations. The findings suggest that these compounds be evaluated against other pathogens possessing a methyltransferase with a DPPY motif and warrant the design and synthesis of more such inhibitors.

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Current drug targets for helminthic diseases

Cited by 52 publications

References 114 publications

Activity of Tea Tree (Melaleuca alternifolia) Essential Oil against L3 Larvae ofAnisakis simplex

Activity of Tea Tree (Melaleuca alternifolia) Essential Oil against L3 Larvae ofAnisakis simplex

Efficacy of Pomegranate (Punica granatum) Peel Extract Against Hymenolepis nana in infections Mice.

Molecular Characterization of an rsmD -Like rRNA Methyltransferase from the Wolbachia Endosymbiont of Brugia malayi and Antifilarial Activity of Specific Inhibitors of the Enzyme

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