Antineoplastons, first described by Burzynski, are naturally occurring
peptides and
amino acid derivatives which control neoplastic growth.
Antineoplaston A10 (3-pehnylacetylamino-2,6-piperidinedion) is the first chemically identified antineoplastons and when it is administered orally it is hydrolysed in pancreatic juice to phenylactylglutamine and phenylacetylisoglutamine in the ration of 4 to 1. These metabolites are water soluble and have antitumor effect, they are further degraded to pehnylacetic
acid. The mixture of
phenylacetylglutamine and phenylacetylisoglutamine in the ratio of 4 to 1 was formulated as
Antineoplaston A10 injectable formulation. The mixture of
phenylacetylglutamine and
phenylacetic acid in the ratio of 1 to 4 was also shown to have antitumor effect in tissue culture study, then formulated as
Antineoplaston AS2-1. The reported
cytostatic inhibitory effect of
A10 on human
hepatocellular carcinoma cells and differentiation inducing effect of AS2-1 on various
tumor cells suggest potential benefit for the treatment of human
hepatocellular carcinoma since this
tumor recurs frequently despite initial successful treatment. We report here the effects of
Antineoplaston A10 and AS2-1 on cell proliferation, cell morphology, cell cycle, and
DNA in human
hepatocellular carcinoma cell lines. Both agents inhibited cell proliferation and increased the number of cells in G0 and G1 phases and
Antineoplaston AS2-1 induced apoptosis, we also describe our clinical experience of a hepatocellula
carcinoma (HCC) patient whose
tumor, after incomplete trancathere arterial embolization (TAE) for a 7cm 7cm HCC, has been stable for more than 15 months during which time he has been taking
Antineoplaston AS2-1 continuously without any serious adverse effects.