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Journal of Infectious Diseases and Therapy ISSN: 2332-0877 | Volume: 6
Infectious Diseases
4
th
Annual Congress on
Neglected Tropical & Infectious Diseases
5
th
International Conference on
August 29-30, 2018 | Boston, USA
&
Trypanosoma congolense
versus geranylacetone:
In vivo
activity with
in vitro
and in silico antisialidase
studies
Saad Bello Saad, Mohammed Auwal Ibrahim, Isah Danladi Jatau
Ahmadu Bello University, Nigeria
T
he menace of animal trypanosomiasis, especially caused by
Trypanosoma congolense
, still wreaks havoc in the livestock industry
of the African continent which demands concerted efforts aimed at reducing the disease burden. An important strategy targeted
against the disease is the use of chemotherapeutic agents but the presently available approved drugs are no longer effective which
necessitates the search for novel agents. In the present study, geranylacetone was investigated for
in vivo
activity against
T. congolense
infected rats as well as the effects on trypanosome-induced pathological changes and
in vitro
and in silico anti-T. congolense sialidase
activity. At a dose of 100 mg/kg bw, geranylacetone significantly (P<0.05) decreased the number of T. congolense in infected animals
whilst an insignificant (P>0.05) reduction was observed with 50mg/kg bw of the compound. Furthermore, the compound was able to
reverse the
T. congolense
-induced anemia and organ damages as evidenced by the significantly (P<0.05) lower values of packed cell
volumes as well as hepatic and renal functions parameters in the treated group compared with infected untreated animals. Considering
the crucial role of anemia in the pathogenesis of the
T. congolense
infection, the effects of geranylacetone on the
T. congolense
sialidase
was further probed using
in vivo
,
in vitro
and in silico approaches. The
in vitro
studies suggested that the compound inhibited
purified bloodstream
T. congolense
sialidase using an uncompetitive inhibition pattern. The mode of binding and critical interactions
alongside the relevant amino acids were predicted using the molecular docking. We concluded that geranylacetone is also another
molecule with therapeutic potency against
T. congolense
and could be added into the library of compounds with validated
in vivo
activity against trypanosomes for further studies as possible next generation trypanocides.
mauwalibrahim@gmail.comJ Infect Dis Ther 2018, Volume 6
DOI: 10.4172/2332-0877-C3-045