Inhibition of HIV and virus replication by polysulphated polyxylan: HOE/BAY 946, a new antiviral compound.
Xylanpoly-(hydrogen sulphate) disodium salt with a molecular weight of about 6000 daltons (HOE/BAY 946) completely inhibited syncytium formation induced by the infection of T lymphocytes with HIV as well as viral replication at concentrations above 25 micrograms/ml. This dose was found to be inhibitory for several strains of HIV-1 and HIV-2. Low molecular weight fractions of the compound were less active against HIV, and high molecular derivatives were as active as HOE/BAY 946. A direct influence of the drug on the infectivity of the virus could not be demonstrated. The drug inhibited the reverse transcriptase of HIV. Treatment of permanently HIV-infected U937 cells resulted in a drastic reduction of virus particles released into the supernatant and points to an additional mode of action. A therapeutic effect of HOE/BAY 946 against retroviruses in vivo could be demonstrated in Friend leukaemia virus-infected mice. A clinical pilot study with the compound was started recently in Germany with AIDS patients who did not tolerate or refused to take zidovudine and with asymptomatic virus carriers.
Biesert
L
L
Chemotherapeutisches Forschungsinstitut Georg-Speyer-Haus, Frankfurt, Federal Republic of Germany.
Suhartono
H
H
Winkler
I
I
Meichsner
C
C
Helsberg
M
M
Hewlett
G
G
Klimetzek
V
V
Mölling
K
K
Schlumberger
H D
HD
Schrinner
E
E
D000818:Animals; D000998:Antiviral Agents / Q000494:pharmacology; D001853:Bone Marrow / Q000187:drug effects; D001854:Bone Marrow Cells; D002470:Cell Survival / Q000187:drug effects; D005260:Female; D006678:HIV / Q000187:drug effects* / Q000201:enzymology / Q000502:physiology; D015497:HIV-1 / Q000187:drug effects / Q000502:physiology; D015498:HIV-2 / Q000187:drug effects / Q000502:physiology; D006801:Humans; D066298:In Vitro Techniques; D007375:Interleukin-1 / Q000096:biosynthesis; D008214:Lymphocytes / Q000166:cytology / Q000187:drug effects; D008264:Macrophages / Q000187:drug effects / Q000378:metabolism; D051379:Mice; D010100:Oxygen / Q000378:metabolism; D010426:Pentosan Sulfuric Polyester; D011134:Polysaccharides / Q000494:pharmacology*; D018894:Reverse Transcriptase Inhibitors; D014779:Virus Replication / Q000187:drug effects*
D000998:Antiviral Agents; D007375:Interleukin-1; D011134:Polysaccharides; D018894:Reverse Transcriptase Inhibitors; D010426:Pentosan Sulfuric Polyester; D010100:Oxygen