Lipophile-conjugated sulfated oligosaccharides as novel microbicides against HIV-1

Said, J, Trybala, E, Andersson, E, Johnstone, K, Liu, LG, Wimmer, N, Ferro, V and Bergstrom, T (2010) Lipophile-conjugated sulfated oligosaccharides as novel microbicides against HIV-1. Antiviral Research, 86 3: 286-295. doi:10.1016/j.antiviral.2010.03.011

Author Said, J
Trybala, E
Andersson, E
Johnstone, K
Liu, LG
Wimmer, N
Ferro, V
Bergstrom, T
Title Lipophile-conjugated sulfated oligosaccharides as novel microbicides against HIV-1
Journal name Antiviral Research   Check publisher's open access policy
ISSN 0166-3542
Publication date 2010-06-01
Sub-type Article (original research)
DOI 10.1016/j.antiviral.2010.03.011
Open Access Status
Volume 86
Issue 3
Start page 286
End page 295
Total pages 10
Place of publication Amsterdam, Netherlands
Publisher Elsevier BV
Language eng
Formatted abstract
With the aim of providing compounds suitable for further development as microbicides active against human immunodeficiency virus 1 (HIV-1) a library containing 37 lipophile-conjugated sulfated oligosaccharides was screened for antiviral and virucidal activity against this virus. Four highly active compounds had low drug inhibition concentrations (IC50) for HIV-1 and inactivated viral particles, suggestive of virucidal properties. Two of these compounds comprising a sulfated tetrasaccharide linked to a cholestanol group by a glycosidic bond, showed low toxicity and high selectivity indices. The two compounds were active both against CCR5 and dual-tropic CCR5/CXCR4 clinical HIV-1 isolates. Since herpes simplex virus type 2 (HSV-2) may be a cofactor for HIV-1 infection, the virucidal effect of the compounds was demonstrated against both viruses when mixed and incubated together on permissive cells. Incubation of compounds with serum, and to a lesser degree, cervical secretions, reduced the HIV-1 inactivating capacity, which suggests the need for molecular modification to reduce host protein binding. Considering the virucidal effect and low toxicity, these sulfated oligosaccharides with lipophilic tails may offer new possibilities of microbicide development.
© 2010 Elsevier B.V.
Keyword HIV-1
Virucidal activity
Q-Index Code C1
Q-Index Status Confirmed Code
Institutional Status Non-UQ

Document type: Journal Article
Sub-type: Article (original research)
Collections: Non HERDC
School of Chemistry and Molecular Biosciences
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Created: Tue, 01 Mar 2011, 00:27:10 EST by Jennifer Falknau on behalf of School of Chemistry & Molecular Biosciences