Microalgae extracts: Potential anti-Trypanosoma cruzi agents?

INTRODUCTION: Chagas disease, caused by the protozoan parasiteTrypanosoma cruzi, has no effective treatment available. On the other hand, microalgae are aquatic organisms that constitute an interesting reservoir of biologically active metabolites. Moreover, some species of green and red algae present anti-protozoan activity. Our aim was to study the antiparasitic effects of aqueous, methanolic and ethanolic extracts from different microalgae. METHODS AND RESULTS: Our results show that the methanolic extracts of S. obliquus and T. suecica as well as the ethanolic extracts of C. reinhardtii and T. suecica present trypanocidal activity on the infective extracellular trypomastigotes and intracellular amastigotes. In addition, the ethanolic extract of C. reinhardtii potentiates the activity of the conventional antichagasic drug nifurtimox. In order to identify some potential compounds with trypanocidal activity, we performed a phytochemical screening analyzing the presence of phenolic compounds, pigments and terpenoids. CONCLUSION: The different microalgae extracts, particularly the ethanolic extract ofC. reinhardtii, are promising potential candidates for the development of future natural antichagasic drugs.

Ibandronate metal complexes: solution behavior and antiparasitic activity.

To face the high costs of developing new drugs, researchers in both industry and academy are looking for ways to repurpose old drugs for new uses. In this sense, bisphosphonates that are clinically used for bone diseases have been studied as agents against Trypanosoma cruzi, causative parasite of Chagas disease. In this work, the development of first row transition metal complexes (M = Co2+, Mn2+, Ni2+) with the bisphosphonate ibandronate (iba, H4iba representing the neutral form) is presented. The in-solution behavior of the systems containing iba and the selected 3d metal ions was studied by potentiometry. Mononuclear complexes [M(Hxiba)](2-x)- (x = 0-3) and [M(Hiba)2]4- together with the formation of the neutral polynuclear species [M2iba] and [M3(Hiba)2] were detected for all studied systems. In the solid state, complexes of the formula [M3(Hiba)2(H2O)4]·6H2O were obtained and characterized. All obtained complexes, forming [M(Hiba)]- species under the conditions of the biological studies, were more active against the amastigote form of T. cruzi than the free iba, showing no toxicity in mammalian Vero cells. In addition, the same complexes were selective inhibitors of the parasitic farnesyl diphosphate synthase (FPPS) enzyme showing poor inhibition of the human one. However, the increase of the anti-T. cruzi activity upon coordination could not be explained neither through the inhibition of TcFPPS nor through the inhibition of TcSPPS (T. cruzi solanesyl-diphosphate synthase). The ability of the obtained metal complexes of catalyzing the generation of free radical species in the parasite could explain the observed anti-T. cruzi activity.