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W Regelson

Publications and source records attributed to W Regelson.

At least 73 records · Page 4Linked to original sources

Antitumor activity of tetraacetylglucosamine mustard.

1,3,4,6-Tetra-O-acetyl-2-(di-2-chloroethyl)amino-2-deoxy-D-glucopyranose is active against L1210 leukemia, giving over 100% increased life-span at optimal dose. Against P388 leukemia, it gives 200% increased life-span with long-term survivors. The compound is most active when given i.p., but shows some activity when given s.c. than p.o., and is more potent (therapeutic and toxic effect) than mechlorethamine on both a molar and a mg basis. Of importance, the schedule dependency for the administration of 1,3,4,6-tetra-O-acetyl-2-(di-2-chloroethyl)amino-2-deoxy-D-glucopyranose in L1210 leukemia differs from most alkylating agents in that it is best given by multiple daily injections rather than as a single large injection on Day 1. This characteristic can be attributed to the amino-glucose moiety.

Acetylglucosamine↗

Antiviral activity and side effects of polyriboinosinic-cytidylic acid complexes as affected by molecular size.

The decrease of the molecular size of poly(I.C) to less than 10(6) decreases its ability to induce interferon, protect mice against virus, or enhance the immune response. Immune adjuvant activity appeared more sensitive to molecular weight than the other protective activities. The composition of the complex-the molecular size of the individual homopolymers when one was large and the other small-did not affect antiviral activity; the activity of a complex made from large poly(I) and small poly(C) was similar to one made from small poly(I) and large poly(C). Molecular size of the complex did not profoundly alter the side effects of poly(I.C). At 2 mg/kg, none of the complexes markedly altered phagocytic function. Only the largest complex sensitized the mouse to endotoxin. However, all of the complexes studied profoundly inhibited drug metabolism by the liver microsomal enzymes between 24 and 72 hr after their inoculation. Decreasing the molecular weight did not alter this inhibition.

Adjuvants, Immunologic↗

Pyran and polyribonucleotides: differences in biological activities.

Maleic anhydride-divinyl ether copolymer (pyran) and the polyribonucleotides are both large polyanions with potent antiviral activity. However, they are biologically quite different. Interferon levels of 100 units or more/ml were associated with antiviral activity of polyribonucleotides. Interferon induction by pyran compounds was not primarily involved in antiviral resistance because preparations that did not induce interferon possessed antiviral activity equal to that of interferoninducing preparations. Both polyriboinosinic-cytidylic acid [poly (rI.rC)] and pyran increased the immune response to sheep erythrocytes in the Jerne hemolytic plaque-forming cell (PFC) assay, but their modes of immunoadjuvant action differed. On peak day, poly (rI.rC)-treated mice demonstrated 5.1 x 10(4) PFC/spleen (557 PFC/10(6) nucleated cells) and pyran-treated mice exhibited 4.5 x 10(4) PFC/spleen (299 PFC/10(6) nucleated cells), as compared with 2.7 x 10(4) PFC/spleen (261 PFC/10(6) nucleated cells) in controls. The compounds also differed in phagocytic alteration; polyribonucleotides did not affect phagocytosis whereas pyran produced a biphasic response. Both polyanions exhibited toxic inhibition of liver microsomal enzyme metabolism of type I and type II drugs. However, whereas pyran sensitized mice 50-fold to the lethal effects of endotoxin, the polyribonucleotides did not significantly sensitize mice to endotoxin.

Adjuvants, Immunologic↗