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@ARTICLE{Taiwo:858910,
author = {Taiwo, Bamigboye J. and Olubiyi, Olujide O. and Wang, Xue
and Fisusi, Funmilola A. and Akinniyi, Ganiyu Akintayo and
Van Heerden, Fanie R. and Strodel, Birgit},
title = {{S}chistosomiasis: {S}nail-vector control, molecular
modelling and dynamic studies of bioactive
{N}-acetylglycoside saponins from {T}etrapleura tetraptera},
journal = {Computational biology and chemistry},
volume = {77},
issn = {1476-9271},
address = {Oxford},
publisher = {Elsevier Science},
reportid = {FZJ-2018-07746},
pages = {363 - 372},
year = {2018},
abstract = {Schistosomiasis, a chronic neglected tropical disease
caused by the Schistosoma spp. parasite, is associated with
disabling patient symptoms. The new focus of the WHO roadmap
on 'transmission control, wherever possible’ offers drug
development opportunities for intermediate-host control to
prevent human-to-snail-to-human parasite transmission.
Reports on the analysis of the impact of ‘chemical-based
mollusciciding’ have concluded that constant application
of molluscicides may contribute significantly towards the
elimination of schistosomiasis in endemic areas. In
South-Western Nigeria, Tetrapleura tetraptera is a tree
whose fruit has been widely used in snail vector control.
The presence of molluscicidal N-acetyl triterpene glycosides
in the fruit has been reported. In this study, a
bioactivity-directed fractionation of the fruit extract was
performed to isolate the most potent molluscicidal saponin
from the fruit. In an attempt to provide mechanistic insight
into the observed activity, in silico screening was
performed, profiling the molluscicidal N-acetyl triterpene
glycosides reported from the fruit against two potential
therapeutic targets in the mollusk used, NADH-ubiquinone
oxidoreductase (NAD1) and retinoid X receptor. The docking
predicted binary complexes of the saponins, which were
subjected to explicit solvent conformational sampling from
which patterns of structural stability were obtained. The
binding energies alone did not account for the potency of
the saponins indicating the influence of other factor like
pharmacokinetic parameters. The study concluded that there
is a preferential suitability of ND1’s MWFE site for the
rational design and development of novel molluscicidal
agents.},
cin = {ICS-6},
ddc = {004},
cid = {I:(DE-Juel1)ICS-6-20110106},
pnm = {551 - Functional Macromolecules and Complexes (POF3-551)},
pid = {G:(DE-HGF)POF3-551},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:30466045},
UT = {WOS:000455858400037},
doi = {10.1016/j.compbiolchem.2018.09.011},
url = {https://juser.fz-juelich.de/record/858910},
}