In vitro evaluation of (anti)mutagenic activity of an aporphine alkaloid and its synthetic intermediates

Abstract

The use of plants as a source of substances with therapeutic action by man dates back centuries and still remains promising currently. Among the various classes of natural products, aporphine alkaloids are widely distributed in plants of the families Annonaceae and Lauraceae among others, showing various pharmacological activities such as dopaminergic, antiproliferative and anti-Leishmania activities in addition to an inhibitory action on cholinesterase, which makes these alkaloids interesting candidates for the treatment of Alzheimer's disease. Several species of Guatteria genus (family Annonaceae) show various oxoaporphine alkaloids with different biological activities and recently the synthesis for aporphine alkaloid, 7-oxo-7H-dibenzo-quinoline-4,5-dimethyl dicarboxylate was described. This alkaloid, together with its three synthetic precursors, showed promising antimicrobial and antiproliferative activities. This project aims to enhance knowledge on efficiency (antimutagenic) and safety of use (mutagenic) of these four compounds through the micronucleus induction assay in CHO-K1 cells (immortalized hamster ovarian cells) and the antioxidant evaluation, through DPPH and Folin-Ciocalteau assays. Key words: cancer, mutagenic activity, micronucleus, antioxidant activity. (AU)