The effect of diaminoalkyl-anthraquinone derivatives on the growth of the promastigotes of Leishmania tropica minor, L. t. major, L. donovani and L. aethiopica.
By combining knowledge of polyamine biosynthesis and its inhibition by various analogues with that on the activity of synthetic anthraquinones, a series of six anthraquinone derivatives were synthesized. Their ability to inhibit the growth of leishmanial promastigotes in vitro was used as a preliminary screen to check their potential as new antileishmanial chemotherapeutics. They were tested against four strains, representing four different species; Leishmania tropica major, L. tropica minor, L. aethiopica and L. donovani, associated with four separate disease syndromes. All six derivatives exhibited a fair degree of antileishmanial activity, some being more effective than others. They all inactivated cultures at 100 micrograms/ml and some did so at 10 micrograms/ml and even 1 microgram/ml; but taking different lengths of time to achieve this. Antileishmanial activity associated with anthraquinone derivatives might provide a new approach to the chemotherapy of leishmaniasis.
D000880:Anthraquinones / Q000138:chemical synthesis* / Q000494:pharmacology; D000981:Antiprotozoal Agents / Q000138:chemical synthesis*; D007891:Leishmania / Q000187:drug effects* / Q000254:growth & development; D011073:Polyamines / Q000096:biosynthesis; D013045:Species Specificity
D000880:Anthraquinones; D000981:Antiprotozoal Agents; D011073:Polyamines