RESUMO
This study, was to evaluate the acaricidal effect of the essential oil (EO) and fractions (FR) obtained from Laurus nobilis leaves on Rhipicephalus (Boophilus) microplus. Eight fractions were obtained, however FR1: sabinene (37.83%), ß-pinene (13.50%), 1,8-cineole (12.66%), α-pinene (12.56%) and FR8: α-terpineol (79.19%) were highlighted as to the larvicidal potential when submitted by Larval Packet Test. The EO was tested by the Adult Immersion Test, at concentrations of 200.00; 100.00 and 50.00 µL/mL caused mortality of engorged females, egg mass reduction and hatching inhibition. Two fractions are shown to be efficient in controlling larvae FR8 (LC50 = 0.13 µL/mL, LC99 = 0.51 µL/mL) and FR1 (LC50 = 0.20 µL/mL, LC99 = 0.56 µL/mL). The fractionation of EO was determinant to elucidate which compounds were responsible for the larvicidal potential. This study opens new perspectives to direct new bioassays with the compounds obtained in the fractionation, since they present high potential on cattle tick larvae.
Assuntos
Acaricidas/farmacologia , Ericaceae/química , Larva/efeitos dos fármacos , Óleos de Plantas/isolamento & purificação , Rhipicephalus/efeitos dos fármacos , Animais , Monoterpenos Bicíclicos/análise , Bovinos , Monoterpenos Cicloexânicos/análise , Feminino , Inseticidas/química , Inseticidas/farmacologia , Óleos de Plantas/farmacologiaRESUMO
In the present work, we report the synthesis and in vitro anticancer and antimicrobial activity evaluation of a new series of 1-substituted-ß-carboline derivatives bearing a 4-benzylidene-4H-oxazol-5-one unity at C-3. The compound 2-[1-(4-methoxyphenyl)-9H-ß-carbolin-3-yl]-4-(benzylidene)-4H-oxazol-5-one (11) was the most active derivative, exhibiting a potent cytotoxic activity against glioma (U251), prostate (PC-3) and ovarian (OVCAR-03) cancer cell lines with IC50 values of 0.48, 1.50 and 1.07 µM, respectively. An in silico study of the ADME properties of the novel synthesized ß-carboline derivatives was also performed.