Title: Modified cyclodextrin sulphates (mCDS11) have potent inhibitory activity against HIV and high oral bioavailability
Authors: Otake, T ×
Schols, Dominique
Witvrouw, Myriam
Naesens, Lieve
Nakashima, H
Moriya, T
Kurita, H
Matsumoto, K
Ueba, N
De Clercq, Erik #
Issue Date: 1994
Publisher: Blackwell Scientific Publications
Series Title: Antiviral Chemistry & Chemotherapy vol:5 issue:3 pages:155-161
Abstract: Modified cyclodextrin sulphate (mCDS) in which lipophilic groups were introduced to cyclodextrin sulphate (CDS) was synthesized and proved more inhibitory to the replication of HIV-1 and HIV-2 than CDS or dextran sulphate (DS). The anti-coagulant activity of mCDS was lower than that of DS. Cyclodextrin phosphate (CDP) showed anti-HIV activity similar to that of CDS, and its anti-coagulant activity was even lower than that of mCDS. Flow cytometric analysis suggested that the mechanism of the anti-HIV-1 action of CDS, mCDS, and CDP is based on inhibition of HIV-1 binding to the cells. The peak blood concentration after oral administration of mCDS11(potassium tris[6-benzylthio-6-deoxy]-beta-cyclodextrin hexadecasulphate) to rabbits was about 1000 times higher than the concentration showing anti-HIV activity. The retention time in the blood was also long (blood half-life: 4 h). These results point to the potential usefulness of oral mCDS administration in the prophylaxis and/or therapy of HIV infections.
ISSN: 0956-3202
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
Molecular Virology and Gene Therapy
× corresponding author
# (joint) last author

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