Antifertility Activity of an Oxidized Polyphenolic Acid from Lithospermum ruderale.

Abstract

Summary A polyphenolic acid, not previously described, was isolated from the roots of L. ruderale and named “lithospermic acid” (LA). LA showed no biological activity in the rat or the chicken. However, when oxidized enzymically a substance was obtained which inactivated exogenous and endogenous gonadotropins in the female rat and prevented ovulation in the laying hen. In one experiment a cold water extract of the roots was partitioned into 5 fractions which were administered orally to immature female rats. Only the original extract and one fraction (11), composed of oxidized LA showed any significant inactivation of exogenous gonadotropin. In another experiment cold water extract, II, as well as enzymically oxidized lithospermic acid showed antiovulatory properties when injected into the laying hen. These experiments indicate that oxidized LA present in the roots is responsible for some of the antigonadotropic effect noted with cold water extracts of L. ruderale.