|Title:||Synthesis of new series of quinoline derivatives with insecticidal effects on larval vectors of malaria and dengue diseases||Authors:||Murugan, Kadarkarai
Shafi, S. Syed
Portilla-Pulido, Johan S.
Mendez, Stelia C.
Duque, Jonny E.
Aziz, Al Thabiani
|Keywords:||PLASMODIUM-FALCIPARUM;IN-VITRO;SILVER NANOPARTICLES;CHLOROQUINE;HYBRIDS;ANTIMALARIALS;NANOCRYSTALS;IRRADIATION;INHIBITION;ANALOGS||Issue Date:||19-Mar-2022||Publisher:||NATURE PORTFOLIO||Journal Volume:||12||Journal Issue:||1||Source:||SCI REP-UK||Abstract:||
Mosquito borne diseases are on the rise because of their fast spread worldwide and the lack of effective treatments. Here we are focusing on the development of a novel anti-malarial and virucidal agent with biocidal effects also on its vectors. We have synthesized a new quinoline (4,7-dichloroquinoline) derivative which showed significant larvicidal and pupicidal properties against a malarial and a dengue vector and a lethal toxicity ranging from 4.408 mu M/mL (first instar larvae) to 7.958 mu M/mL (pupal populations) for Anopheles stephensi and 5.016 mu M/mL (larva 1) to 10.669 mu M/mL (pupae) for Aedes aegypti. In-vitro antiplasmodial efficacy of 4,7-dichloroquinoline revealed a significant growth inhibition of both sensitive strains of Plasmodium falciparum with IC50 values of 6.7 nM (CQ-s) and 8.5 nM (CQ-r). Chloroquine IC50 values, as control, were 23 nM (CQ-s), and 27.5 nM (CQ-r). In vivo antiplasmodial studies with P. falciparum infected mice showed an effect of 4,7-dichloroquinoline compared to chloroquine. The quinoline compound showed significant activity against the viral pathogen serotype 2 (DENV-2). In vitro conditions and the purified quinoline exhibited insignificant toxicity on the host system up to 100 mu M/mL. Overall, 4,7-dichloroquinoline could provide a good anti-vectorial and anti-malarial agent.
|Appears in Collections:||海洋生物研究所|
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