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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; LC 100 : 50; IC 50 : 8.84 µM) and female adult worms (LC 100 : 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.

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