1 research outputs found
Synthesis and Antitumor Activity of Ellagic Acid Peracetate
Ellagic acid (<b>1</b>) was synthesized for the
first time from methyl gallate through α-pentagalloylglucose
(α-PGG), and ellagic acid peracetate (3,4,3′,4′-tetra-<i>O</i>-acetylellagic acid, <b>2</b>) was derived from <b>1</b> by acetylation. Oral administration of <b>2</b> suppressed
melanoma growth significantly in C7BL/6 immunocompetent mice without
having any effect on natural killer (NK) cell activity. Comparison
of the immunoenhancing activities of <b>1</b> and <b>2</b> indicated that the latter compound increased white blood cell quantities
in peripheral blood and immune cells enriched from the bone marrow
and liver of mice. Therefore, both the antitumor efficacy and the
immunity enhancement by <b>2</b> were greater than those by <b>1</b>. In addition, on oral administration, neither <b>1</b> nor <b>2</b> resulted in whole body, liver, or spleen weight
changes of normal, tumor-free mice, indicating that these compounds
are potentially nontoxic to mice. It was shown that ellagic acid peracetate
(<b>2</b>) inhibits B16 melanoma cell growth in vitro and induces
B16 cell apoptosis, corresponding to BCL-2 down-regulation. Collectively,
the present data imply that <b>2</b> can suppress tumor growth
by enhancing mouse immunity and inducing tumor cell apoptosis without
apparent side effects