ABSTRACT
As the world undergone unpreceded time of tragedy with the corona virus, many researchers have raised to showcase their scientific contributions in terms of novel configured anti-viral drugs until now. Herein, we designed pyrimidine based nucleotides and assessed for the binding capability with SARS-CoV-2 viral replication targets of nsp12 RNA-dependent RNA polymerase and Mpro main protease. Molecular docking studies showed all the designed compounds to possess good binding affinity, with a few compounds which outperforms the control drug remdesivir GS-5743 and its active form GS-441524. Further molecular dynamics simulation studies confirmed their stability and preservation of the non-covalent interactions. Based on the present findings Ligand2-BzV_0Tyr, ligand3-BzV_0Ura, and ligand5-EeV_0Tyr showed good binding affinity with Mpro, whereas, ligand1-BzV_0Cys and Ligand2-BzV_0Tyr showed good binding affinity with RdRp, thus could act as potential lead compounds against SARS-CoV-2, which needs further validation studies. In particular, Ligand2-BzV_0Tyr could be more beneficial candidate with the dual target specificity for Mpro and RdRp.
Subject(s)
COVID-19 , SARS-CoV-2 , Humans , SARS-CoV-2/metabolism , Molecular Docking Simulation , COVID-19 Drug Treatment , Antiviral Agents/chemistry , RNA-Dependent RNA Polymerase/genetics , Molecular Dynamics Simulation , Pyrimidines/pharmacologyABSTRACT
OBJECTIVE@#To determine the larvicidal and pupicidal activites of Solanum trilobatum (S. trilobatum) leaf extracts against Aedes aegypti (Ae. aegypti), Culex quinquefasciatus (Cx. quinquefasciatus) and Anopheles stephensi (An. stephensi).@*METHODS@#The larvicidal and pupucidal was determined at five different concentrations of 50, 100, 150, 200 and 250 ppm. Percentage of larval mortality was assessed after 48 h.@*RESULTS@#Methanol extracts of S. trilobatum was found to be more susceptible against the larvae of Ae. aegypti, Cx. quinquefasciatus and An. stephensi at 250 ppm with a LC50 value of 125.43, 127.77 and 116.64 ppm respectively. Leaf methanol extracts of S. trilobatum also exhibited pupicidal and adult emergence properties.@*CONCLUSIONS@#These results suggested that the leaf extracts of S. trilobatum showed potential to be used as an ideal ecofriendly approach for the control of the Ae. Aegypti, Cx. quinquefasciatus and An. stephensi.
Subject(s)
Animals , Female , Humans , Male , Anopheles , Consumer Behavior , Culex , Disease Reservoirs , Drug Resistance , Ghana , Epidemiology , Health Knowledge, Attitudes, Practice , Insect Repellents , Pharmacology , Insecticide-Treated Bednets , Insecticides , Pharmacology , Larva , Malaria , Epidemiology , Ovum , Plant Extracts , Chemistry , Plant Leaves , Chemistry , Plant Preparations , Pharmacology , Solanaceae , Chemistry , Urban PopulationABSTRACT
Objective:To evaluate the antifeedant, insecticidal and growth inhibition activities of Solanum pseudocapsicum (S. pseudocapsicum) seed extracts against Spodoptera litura (S. litura) and Helicoverpa armigera (H. armigera). Methods:Hexane, diethyl ether, dichloromethane and ethyl acetate seed extracts were prepared and tested for antifeedant, insecticidal and growth inhibitory activities against fourth instar larvae of S. litura and H. armigera. Results:Ethyl acetate extract showed promising antifeedant and insecticidal activities against S. litura and H. armigera. Percentage of deformed larvae, pupae and adults were maximum in treatment of ethyl acetate extract. Percentage of successful adult emergence was deteriorated by seeds on extract treated larvae. Conclusions: Ethyl acetate extracts of S. pseudocapsicum, showed higher efficiency of antifeedant, insecticidal and growth inhibition activities. Hence, it can be used to controll agricultural insect pests, S. litura and H. armigera.
ABSTRACT
<p><b>OBJECTIVE</b>To evaluate the antifeedant, insecticidal and growth inhibition activities of Solanum pseudocapsicum (S. pseudocapsicum) seed extracts against Spodoptera litura (S. litura) and Helicoverpa armigera (H. armigera).</p><p><b>METHODS</b>Hexane, diethyl ether, dichloromethane and ethyl acetate seed extracts were prepared and tested for antifeedant, insecticidal and growth inhibitory activities against fourth instar larvae of S. litura and H. armigera.</p><p><b>RESULTS</b>Ethyl acetate extract showed promising antifeedant and insecticidal activities against S. litura and H. armigera. Percentage of deformed larvae, pupae and adults were maximum in treatment of ethyl acetate extract. Percentage of successful adult emergence was deteriorated by seeds on extract treated larvae.</p><p><b>CONCLUSIONS</b>Ethyl acetate extracts of S. pseudocapsicum, showed higher efficiency of antifeedant, insecticidal and growth inhibition activities. Hence, it can be used to controll agricultural insect pests, S. litura and H. armigera.</p>
Subject(s)
Animals , Humans , Insecticides , Pharmacology , Larva , Lethal Dose 50 , Moths , Pest Control , Plant Extracts , Pharmacology , Solanaceae , Chemistry , SpodopteraABSTRACT
The Ethiopian fruit fly, Dacus ciliatus, is an oligophagous pest of cucurbit crops, particularly melons, cucumbers, and marrows (summer squash). The present study aimed to identify host attractants for D. ciliatus and was guided by a behavioral bioassay and an electrophysiological assay. We tested volatile compounds from the fruits of a host plant, ripe and unripe Galia melon, Cucumis melo var. reticulates. Both sexes were attracted to melon volatiles. Those of ripe melon were preferred. Gas chromatography-electroantennographic detection analysis of the behaviorally active ripe melon volatiles consistently showed that 14 compounds elicited similar antennal responses from both sexes. Twelve compounds were identified by gas chromatography-mass spectrometry (GC-MS) using GC-MS libraries, retention indices (RI), and authentic standards. The electrophysiological activities of the compounds that were present at sufficient levels for identification, benzyl acetate, hexanyl acetate, (Z)-3-hexenyl acetate, (Z)-3-octenyl acetate, octanyl acetate, (Z)-3-decenyl acetate, and (E)-beta-farnesene, were evaluated at six different dosage levels by using electroantennography (EAG). Benzyl and hexanyl acetates elicited dose responses only in males, while other tested compounds elicited dose responses in both sexes. The strongest responses were observed for doses between 100 ng and 10 microg. The dose response, in terms of attractiveness to synthetic compounds within the active range (as determined by EAG), also was evaluated in the behavioral bioassay. Synthetic acetates were attractive to both sexes when tested individually. Significant attraction was observed when individual compounds were applied in the bioassay arena at doses of 0.5-1 microg/dispenser. Blends of compounds in equal proportions also were attractive to the insects. The most attractive blend was a mixture of four or five identified acetates. The addition of an equal proportion of (E)-beta-farnesene to this mixture had a deterrent effect.
