[The ajoene blockade of integrin-dependent processes in an HIV-infected cell system].
Ajoene, (E,Z)-4,5,9-trithiadodeca-1,6,11-triene-9-oxide, isolated from extracts of garlic (Allium sativum) has been previously shown to inhibit platelet aggregation by inactivating allosterically the platelet integrin, GP IIb/IIIa. The structural and functional similarity of integrins led the authors to suggest that ajoene may also inhibit adhesive interactions and fusion of leukocytes. Synthetic stereoisomers of ajoene synthesized by the authors exhibited equal antiaggregatory activities (IC100 approximately 50 microM for platelets; IC100 approximately 10 microM for fMLP-stimulated neutrophils). Racemic ajoene inhibited the fusion of H9 cells with HIV-infected H9:RF cells (IC50 approximately 45 microM; 16 h of incubation) and also exhibited a degree of antiviral activity (IC50 approximately 5 microM as assessed by inhibition of HIV-1/CEM/Lav 1 Bru replication in CEM13 cells; m. o. i. 0.1; 72 h). A considerable increase in the latter became evident when the compound was administered in aliquots of 50 microM per 12 h of incubation (inhibition by 30%; total concentration 0.25 microM; 72 h).(ABSTRACT TRUNCATED AT 250 WORDS)
Tatarintsev
A V
AV
Vrzhets
P V
PV
Ershov
D E
DE
Shchegolev
A A
AA
Turgiev
A S
AS
Karamov
E V
EV
Kornilaeva
G V
GV
Makarova
T V
TV
Fedorov
N A
NA
Varfolomeev
S D
SD
D000998:Antiviral Agents / Q000494:pharmacology*; D002448:Cell Adhesion / Q000187:drug effects; D002459:Cell Fusion; D002460:Cell Line; D002469:Cell Separation; D002478:Cells, Cultured / Q000187:drug effects; D004220:Disulfides / Q000494:pharmacology*; D015726:Giant Cells / Q000187:drug effects; D015658:HIV Infections / Q000097:blood* / Q000382:microbiology; D015497:HIV-1 / Q000187:drug effects / Q000502:physiology; D006801:Humans; D016023:Integrins / Q000037:antagonists & inhibitors*; D009504:Neutrophils / Q000187:drug effects; D010936:Plant Extracts / Q000494:pharmacology*; D010974:Platelet Aggregation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000494:pharmacology*; D013454:Sulfoxides; D014779:Virus Replication / Q000187:drug effects
D000998:Antiviral Agents; D004220:Disulfides; D016023:Integrins; D010936:Plant Extracts; D010975:Platelet Aggregation Inhibitors; D013454:Sulfoxides; C048980:ajoene
Blokada adzhoenom integrinzavisimykh protsessov v sisteme kletok, infitsirovannykh VICh.