Anti-filarial activity of novel formulations of albendazole against experimental brugian filariasis

Gaur, Ritu; Dixit, Saurabh; Sahoo, Malaya K.; Khanna, Madhu; Singh, Satyendra; Murthy, P. K.

doi:10.1017/s0031182006001612

Cited by 27 publications

(15 citation statements)

References 31 publications

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“…Tissues were teased gently and the parasites recovered were then examined under microscope for status of the motility, cell adherence on their surface, dead or calcified worms [23], [24]. Number of worms recovered from the treated and untreated animals was recorded.…”

Section: Methodsmentioning

confidence: 99%

“…All the surviving females were teased individually in a drop of saline to examine condition of intrauterine mf stages of the parasite [23], [24]. Number of sterile female worms recovered from the treated animals was compared with that of control animals and percent sterilization of female worms was determined in treated or control groups over total live female worms recovered from the respective groups.…”

Section: Methodsmentioning

confidence: 99%

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In Vitro, In Silico and In Vivo Studies of Ursolic Acid as an Anti-Filarial Agent

et al. 2014

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As part of our drug discovery program for anti-filarial agents from Indian medicinal plants, leaves of Eucalyptus tereticornis were chemically investigated, which resulted in the isolation and characterization of an anti-filarial agent, ursolic acid (UA) as a major constituent. Antifilarial activity of UA against the human lymphatic filarial parasite Brugia malayi using in vitro and in vivo assays, and in silico docking search on glutathione-s-transferase (GST) parasitic enzyme were carried out. The UA was lethal to microfilariae (mf; LC100: 50; IC50: 8.84 µM) and female adult worms (LC100: 100; IC50: 35.36 µM) as observed by motility assay; it exerted 86% inhibition in MTT reduction potential of the adult parasites. The selectivity index (SI) of UA for the parasites was found safe. This was supported by the molecular docking studies, which showed adequate docking (LibDock) scores for UA (−8.6) with respect to the standard antifilarial drugs, ivermectin (IVM −8.4) and diethylcarbamazine (DEC-C −4.6) on glutathione-s-transferase enzyme. Further, in silico pharmacokinetic and drug-likeness studies showed that UA possesses drug-like properties. Furthermore, UA was evaluated in vivo in B. malayi-M. coucha model (natural infection), which showed 54% macrofilaricidal activity, 56% female worm sterility and almost unchanged microfilaraemia maintained throughout observation period with no adverse effect on the host. Thus, in conclusion in vitro, in silico and in vivo results indicate that UA is a promising, inexpensive, widely available natural lead, which can be designed and developed into a macrofilaricidal drug. To the best of our knowledge this is the first ever report on the anti-filarial potential of UA from E. tereticornis, which is in full agreement with the Thomson Reuter's ‘Metadrug’ tool screening predictions.

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Section: Methodsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

In Vitro, In Silico and In Vivo Studies of Ursolic Acid as an Anti-Filarial Agent

et al. 2014

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“…Different trials were made to use the known drug at its maximum capacity in absence of new drugs. In a study from India, it has been shown that a formulation of albendazole has better anti-filarial efficacy than albendazole itself 17 .…”

Section: Treatment: Medicationmentioning

confidence: 99%

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2015

IJPSR

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Lymphatic Filariasis (LF) is a major public health problem not only in India but also other developed countries. Filariasis is the disease which is caused by a group of filarial worms. It is transmitted by mosquitoes -Culex quinquefasciatus globally the most important vector. They cause high morbidity and mortality among humans. The proper management is needed for preventing the morbidity and mortality by laboratory diagnostic methods. Irreversible "elephantiasis" is the major clinical manifestation for LF. Diethylcarbamazine (DEC) is the drug of choice for treating lymphatic filariasis. Sequential gradient pump therapy and complete decongestive therapy (CDT) are some additional treatment for better therapeutic value.

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“…[22] Briefly, 8-10 weeks old male jirds were transplanted intraperitoneally (i.p.) with adult worms isolated from the PC of jirds harboring 4-5 months old B. malayi infection.…”

Section: In Vivo Efficacymentioning

confidence: 99%

Antifilarial activity of gum from Moringa oleifera Lam. on human lymphatic filaria Brugia malayi

Kushwaha¹,

Kc²,

Verma³

et al. 2011

Chron Young Sci

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Aim: Currently available antifilarial drugs diethylcarbamazine, ivermectin and albendazole and their combinations, are not able to control lymphatic filariasis. Therefore, a better antifilarial agent is urgently required for proper management of the disease. Materials and Methods: In this study, we evaluated the antifilarial activity of gum extract of plant Moringa oleifera Lam. against the human lymphatic filarial parasite Brugia malayi using adult worms and microfilariae (mf) in two in vitro assays (motility and inhition in MTT reduction) for viability and two animal models, primary (Meriones unguiculatus implanted with B. malayi adult worms in the peritoneal cavity) and secondary (subcutaneous B. malayi infective larvae induced Mastomys coucha, the model closer to the natural human filarial infection) screens. Results: The gum extract inhibited 100% motility (irreversible loss of motility) of mf and inhibited more than 56% MTT reduction potential of the adult female worms. The extract was safe in cytotoxicity test using Vero cell line, therefore followed in vivo in primary and secondary screens. In primary screen, the extract (5×500 mg/kg) caused 69% macrofilaricidal and 83% sterilization of female worms and 44% macrofilaricidal activity in secondary screen (5 × 1000 mg/kg) by oral route. Conclusion: Thus, it is concluded that the gum of the plant is macrofilaricidal in both in vitro and in vivo and may provide valuable leads for design and development of new antifilarial agents. This is the first ever report on the antifilarial efficacy of M. oleifera.

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Anti-filarial activity of novel formulations of albendazole against experimental brugian filariasis

Cited by 27 publications

References 31 publications

In Vitro, In Silico and In Vivo Studies of Ursolic Acid as an Anti-Filarial Agent

In Vitro, In Silico and In Vivo Studies of Ursolic Acid as an Anti-Filarial Agent

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Antifilarial activity of gum from Moringa oleifera Lam. on human lymphatic filaria Brugia malayi

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