In vitro nematicidal activity of two ferrocenyl chalcones against larvae of Haemonchus contortus (L₃) and Nacobbus aberrans (J₂)

Abstract

The main goal of this work was to evaluate the in vitro biological activity of two ferrocenyl chalcones (FcC-1 and FcC-2) against Haemonchus contortus (third-stage larvae (L3)) and Nacobbus aberrans (second-stage juveniles (J2)). Both compounds were synthesized and characterized by usual spectroscopic methods and their molecular structures were confirmed by single-crystal X-ray diffractometry. Nematode strains were examined in terms of percentage mortality of H. contortus (L3) by the action of FcC-1, which showed an effectivity of 100% at a concentration of 342 μM in 24 h, with EC50 = 20.33 μM and EC90 = 162.76 μM, whereas FcC-2 had an effectivity of 72% at a concentration of 342 μM in 24 h, with EC50 = 167.39 μM and EC90 = 316.21 μM. The effect of FcC-1 against nematode phytoparasite N. aberrans showed a better percentage of 95% at a concentration of 342 μM, with EC50 = 7.18 μM and EC90 = 79.25 μM, whereas the effect of FcC-2 was 87% at 342 μM, with EC50 = 168 μM and EC90 = 319.56 μM at 36 h. After treatment, the scanning electron micrographs revealed deformities in the dorsal flank and posterior part close to the tail of H. contortus L3. They showed moderate in vitro nematicidal activity against H. contortus L3 and N. aberrans J2.

Three Small Molecule Entities (MPK18, MPK334 and YAK308) with Activity against Haemonchus contortus In Vitro

“…The chalcones are known to exert adverse effects on parasitic helminths, including schistosomes and plant nematodes [ 20 , 21 , 22 ] as well as protists such as Plasmodium [ 23 ], Giardia and Leishmania [ 24 , 25 , 26 ]; however, the exact mode(s) of action in parasites is unknown. The chalcone is proposed to induce pathological changes in musculature in H. contortus xL3s by causing cell dysfunction via the inhibition of tyrosine kinase and/or microtubule formation [ 27 ], although such effects have only been observed in mammalian systems—in vitro (mammalian cells) and in vivo (murine models) [ 28 ]. Some of the unique biological activities of known chalcones are associated with their Michael acceptor features [ 28 , 29 , 30 ].…”