1994
DOI: 10.1177/095632029400500303
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Modified Cyclodextrin Sulphates(mCDS11) have Potent Inhibitory Activity against HIV and High Oral Bioavailability

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 o… Show more

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Cited by 19 publications
(18 citation statements)
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“…Its half-life was 4 h (Otake et al, 1994). Similar findings were also obtained following oral administration of mCDS11 to rats (Moriya et el., 1991).…”
Section: Pharmacokinetic Profilesupporting
confidence: 75%
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“…Its half-life was 4 h (Otake et al, 1994). Similar findings were also obtained following oral administration of mCDS11 to rats (Moriya et el., 1991).…”
Section: Pharmacokinetic Profilesupporting
confidence: 75%
“…Similar findings were also obtained following oral administration of mCDS11 to rats (Moriya et el., 1991). Toxicity was not observed after oral administration of mCDS11 to mice at a dose of 3 g kg-1 (Moriya et al, 1991) and at doses of 0.5 and 2 g kg-1 day ' for 5 days (Otake et al, 1994). Recently, Moriya et al (1993) reported an advanced investigation of modified CDS.…”
Section: Pharmacokinetic Profilementioning
confidence: 99%
See 1 more Smart Citation
“…Among them, mCDS71, in which the C-2 position was modified with a lipophilic benzyloxy group, exhibited 32-to 125-fold higher anti-HIV activity compared with the original unmodified form (Moriya et al, 1993). After oral administration of mCDS71 in rats, the peripheral blood possessed anti-HIV activity (Moriya et al, 1993) and anti-HIV activity of mCDS11, the prototype of mCDS71, had a half-life of 4 h in rabbits (Otake et al, 1994). This drug had antiviral activity against clinical HIV-1 isolates as well as laboratory strains, and inhibited the formation of multi-nucleated cells (cytopathic effect).…”
mentioning
confidence: 99%
“…We have reported that a series of modified cyclodextrin sulphates, rigid circular forms made of seven glucose residues, introduced sulphate residues and modified by various functional groups, have anti-HIV activities (Moriya et al, 1991(Moriya et al, , 1993Otake et al, 1994). Among them, mCDS71, in which the C-2 position was modified with a lipophilic benzyloxy group, exhibited 32-to 125-fold higher anti-HIV activity compared with the original unmodified form (Moriya et al, 1993).…”
mentioning
confidence: 99%