scholarly journals Overcoming insecticide resistance through computational inhibitor design

2017 ◽  
Author(s):  
Galen J. Correy ◽  
Daniel Zaidman ◽  
Alon Harmelin ◽  
Silvia Carvalho ◽  
Peter D. Mabbitt ◽  
...  
Keyword(s):  
High Selectivity ◽  
Computational Design ◽  
Agricultural Pests ◽  
Potato Aphid ◽  
Global Food Security ◽  
Evolution Of Resistance ◽  
The Common ◽  
Hydrolysis Of ◽  
Peach Potato Aphid ◽  
Global Food

AbstractInsecticides allow control of agricultural pests and disease vectors and are vital for global food security and health. The evolution of resistance to insecticides, such as organophosphates (OPs), is a serious and growing concern. OP resistance often involves sequestration or hydrolysis of OPs by carboxylesterases. Inhibiting carboxylesterases could therefore restore the effectiveness of OPs for which resistance has evolved. Here, we use covalent computational design to produce nano/pico-molar boronic acid inhibitors of the carboxylesterase αE7 from the agricultural pest Lucilia cuprina, as well as a common Gly137Asp αE7 mutant that confers OP resistance. These inhibitors, with high selectivity against human acetylcholinesterase, and low to no toxicity in human cells and mice, act synergistically with the OPs diazinon and malathion to reduce the amount of OP required to kill L. cuprina by up to 16-fold, and abolish resistance. The compounds exhibit broad utility in significantly potentiating another OP, chlorpyrifos against the common pest, the peach-potato aphid (Myzus persicae). These compounds represent a solution to OP resistance as well as to environmental concerns regarding overuse of OPs, allowing significant reduction of use without compromising efficacy.

scholarly journals Overcoming insecticide resistance through computational inhibitor design

2019 ◽  
Vol 116 (42) ◽  
pp. 21012-21021 ◽  
Author(s):  
Galen J. Correy ◽  
Daniel Zaidman ◽  
Alon Harmelin ◽  
Silvia Carvalho ◽  
Peter D. Mabbitt ◽  
...  
Keyword(s):  
Boronic Acid ◽  
High Selectivity ◽  
Agricultural Pests ◽  
Potato Aphid ◽  
Global Food Security ◽  
Evolution Of Resistance ◽  
The Common ◽  
Hydrolysis Of ◽  
Peach Potato Aphid ◽  
Global Food

Insecticides allow control of agricultural pests and disease vectors and are vital for global food security and health. The evolution of resistance to insecticides, such as organophosphates (OPs), is a serious and growing concern. OP resistance often involves sequestration or hydrolysis of OPs by carboxylesterases. Inhibiting carboxylesterases could, therefore, restore the effectiveness of OPs for which resistance has evolved. Here, we use covalent virtual screening to produce nano-/picomolar boronic acid inhibitors of the carboxylesterase αE7 from the agricultural pest Lucilia cuprina as well as a common Gly137Asp αE7 mutant that confers OP resistance. These inhibitors, with high selectivity against human acetylcholinesterase and low to no toxicity in human cells and in mice, act synergistically with the OPs diazinon and malathion to reduce the amount of OP required to kill L. cuprina by up to 16-fold and abolish resistance. The compounds exhibit broad utility in significantly potentiating another OP, chlorpyrifos, against the common pest, the peach–potato aphid (Myzus persicae). These compounds represent a solution to OP resistance as well as to environmental concerns regarding overuse of OPs, allowing significant reduction of use without compromising efficacy.

scholarly journals The properties of a carboxylesterase from the peach-potato aphid, Myzus persicae (Sulz.), and its role in conferring insecticide resistance

1977 ◽  
Vol 167 (3) ◽  
pp. 675-683 ◽  
Author(s):  
Alan L. Devonshire
Keyword(s):  
Insecticide Resistance ◽  
Myzus Persicae ◽  
Order Rate Constant ◽  
Preliminary Evidence ◽  
Exchange Chromatography ◽  
Potato Aphid ◽  
First Order ◽  
Different Strains ◽  
Hydrolysis Of ◽  
Peach Potato Aphid

Carboxylesterases from different strains of Myzus persicae were examined to try to understand their contribution to insecticide resistance. Preliminary evidence that they are involved comes from the good correlation between the degree of resistance and the carboxylesterase and paraoxon-degrading activity in aphid homogenates. Furthermore the carboxylesterase associated with resistance could not be separated from the insecticide-degrading enzyme by electrophoresis or ion-exchange chromatography. Homogenates of resistant aphids hydrolysed paraoxon 60 times faster than did those of susceptible aphids, yet the purified enzymes from both sources had identical catalytic-centre activities towards this substrate and also towards naphth-1-yl acetate, the latter being hydrolysed by both 2×106 times faster than paraoxon. These observations provide evidence that the enzyme from both sources is identical, and that one enzyme hydrolyses both substrates. This was confirmed by relating the rate of paraoxon hydrolysis to the rate at which paraoxon-inhibited carboxylesterase re-activated. Both had the same first-order rate constant (0.01min−1), showing clearly that the hydrolysis of both substrates is brought about by the same enzyme. Its Km for naphth-1-yl acetate was 0.131mm, and for paraoxon 75pm. The latter very small value could not be measured directly, but was calculated from substrate-competition studies coupled with measurements of re-activation of the diethyl phosphorylated enzyme. Since the purified enzymes from resistant and susceptible aphids had the same catalytic-centre activity, the 60-fold difference between strains must be caused by different amounts of the same enzyme resulting from mutations of the regulator gene(s) rather than of the structural gene.

scholarly journals Role of Global Food Security in the Common Agrarian Policy of the European Union

2014 ◽  
pp. 130-138
Author(s):  
I. N. Shcherbak
Keyword(s):  
European Union ◽  
Food Security ◽  
Agricultural Policy ◽  
Common Agricultural Policy ◽  
Agricultural Sector ◽  
The European Union ◽  
Global Food Security ◽  
The Common ◽  
Global Food

The author devoted his research to the role of the global food security in the priorities of the Common Agricultural Policy of the European Union (CAP). The research sheds light on the parameters of the Common Agricultural Policy and the basic steps on the path of its reform. The research demonstrates that the priorities of the EC are mainly concentrated on achieving food security for the member-states of the EC, its population and the interests of the agricultural sector. The modern challenges to the Global Food Security (global food crises of 2007-2009, acute food shortages and hunger in crises regions of Africa and chronic malnutrition) are placed high on the agenda of the CAP. In this situation, the EU is trying in the interests of stabilization of the world agricultural market to solve simultaneously the tasks of providing assistance for development and mitigation of the threats to the Global Food security. The deepening rift between the strategy of the CAP oriented towards promotion of agricultural export and real contribution of the EC to the Global Food Security and assistance for development is becoming more and more the most «vulnerable» place of the CAP.

scholarly journals Genetic covariation between effectiveness and cost of defence in aphids

2008 ◽  
Vol 4 (6) ◽  
pp. 674-676 ◽  
Author(s):  
Christoph Vorburger ◽  
Alexandre Gouskov ◽  
Simone von Burg
Keyword(s):  
Genetic Variation ◽  
Ecological Immunology ◽  
Short Term ◽  
Potato Aphid ◽  
Trade Off ◽  
Evolution Of Resistance ◽  
Benefits And Costs ◽  
Peach Potato Aphid ◽  
Aphid Clones

Ecological immunology distinguishes between the long-term evolutionary costs of possessing defences against parasites and the short-term costs of using them. Evolutionary biologists have typically focused on the former in the search for constraints on the evolution of resistance. Here, we show in the peach-potato aphid, Myzus persicae , that short-term costs may be of equal evolutionary importance. Survivors of more resistant aphid clones suffered a higher reduction of fecundity upon parasitoid attack than survivors of more susceptible clones. This genetically based trade-off between benefits and costs of defence may limit the evolution of increased resistance and explain the maintenance of genetic variation for resistance under environmental variation in parasitism risk.

GLOBAL FOOD SECURITY AMID THE GLOBAL CRISIS

2020 ◽  
Vol 1 (10) ◽  
pp. 134-141
Author(s):  
P. M. TARANOV ◽  
◽  
A. S. PANASYUK ◽  
Keyword(s):  
Food Security ◽  
Short Term ◽  
Global Food Security ◽  
Food Problem ◽  
Supply Problem ◽  
Coronavirus Infection ◽  
Food Security Indicators ◽  
Security Indicators ◽  
Global Food

The authors assess the prospects for solving the global food problem based on an analysis of the dynamics of food security indicators at the global and regional levels. The global food problem at work refers to the growing population of a planet affected by hunger and other forms of malnutrition. The food security situation has worsened for five years - in 2015–2019, and the COVID-19 pandemic has further exacerbated the food supply problem. The prevalence of moderate to severe food insecurity has affected more than 25% of the world's population. In lowincome countries, malnutrition affects more than 58% of the population. Food security is threatened by the consequences of the spread of coronavirus infection in the short term. In the medium and long term, climate change and the crisis in the governance of the world economy are the greatest threats. Modern international economic institutions are unable to withstand the prospect of declining global food security.

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