PMID- 30388752
OWN - NLM
STAT- PubMed-not-MEDLINE
LR  - 20240512
IS  - 2075-4450 (Print)
IS  - 2075-4450 (Electronic)
IS  - 2075-4450 (Linking)
VI  - 9
IP  - 4
DP  - 2018 Nov 1
TI  - Fatty Acid and Related Potassium Kv2 Channel Blockers: Toxicity and Physiological 
      Actions on Mosquitoes.
LID - 10.3390/insects9040155 [doi]
LID - 155
AB  - Potassium channels constitute a very diverse group involved in neural signaling, 
      neuronal activity, membrane potential maintenance, and action potential 
      generation. Here, we tested the mammalian potassium channel blockers TRAM-34 and 
      5-hydroxydecanoate (5-HDC), as well as certain fatty acids (FA) that might fit in 
      the lumen of the pore and block channel activity by obstructing K(+) ion passage. 
      Kv channel blockers could be leads for a novel pesticide type. Insecticidal 
      activity was assessed by topical application to Anopheles gambiae adult 
      mosquitoes, paralysis in a headless larval assay, at the cellular level with 
      patch-clamp recordings of engineered HEK cells expressing AgKv2.1 channels, as 
      well as central nervous system recordings from larval Drosophila melanogaster. 
      With only one hydroxyl group difference, decanoic acid had a consistently greater 
      effect than 5-HDC in blocking Kv channels, paralyzing larvae, and killing 
      mosquitoes. The 11-dansylamino undecanoic acid (DAUDA) blockage of eukaryotic Kv 
      channels is demonstrated for the first time, but it failed to kill adult 
      mosquitoes. We synthesized alkyl esters from DAUDA and decanoic acid in an effort 
      to improve cuticular penetration, but it had little impact upon adult toxicity. 
      TRAM-34 and rolipram did not show activity on Kv channels nor potent insecticidal 
      effect on adult mosquitoes. Furthermore, co-application of test compounds with 
      permethrin did not increase mortality in adults. In conclusion, the compounds 
      tested had modest insecticidal and synergistic activity.
FAU - Demares, Fabien
AU  - Demares F
AUID- ORCID: 0000-0002-2638-4247
AD  - Neurotoxicology Laboratory, Department of Entomology and Nematology, Emerging 
      Pathogens Institute, University of Florida, Gainesville, FL 32610, USA. 
      fabien.demares@ufl.edu.
FAU - Coquerel, Quentin
AU  - Coquerel Q
AD  - Neurotoxicology Laboratory, Department of Entomology and Nematology, Emerging 
      Pathogens Institute, University of Florida, Gainesville, FL 32610, USA. 
      quentin.coquerel@ufl.edu.
FAU - Richoux, Gary
AU  - Richoux G
AD  - Neurotoxicology Laboratory, Department of Entomology and Nematology, Emerging 
      Pathogens Institute, University of Florida, Gainesville, FL 32610, USA. 
      grichoux@ufl.edu.
FAU - Linthicum, Kenneth
AU  - Linthicum K
AD  - USDA, ARS, Center for Medical, Agricultural and Veterinary Entomology, 
      Gainesville, FL 32608, USA. Kenneth.Linthicum@ars.usda.gov.
FAU - Bloomquist, Jeffrey
AU  - Bloomquist J
AUID- ORCID: 0000-0002-9136-4998
AD  - Neurotoxicology Laboratory, Department of Entomology and Nematology, Emerging 
      Pathogens Institute, University of Florida, Gainesville, FL 32610, USA. 
      jbquist@epi.ufl.edu.
LA  - eng
GR  - 58-0208-0-068 and 58-0208-5-001/Deployed War Fighter and USDA Specific 
      Cooperative Agreements/
PT  - Journal Article
DEP - 20181101
PL  - Switzerland
TA  - Insects
JT  - Insects
JID - 101574235
PMC - PMC6315728
OTO - NOTNLM
OT  - Anopheles gambiae
OT  - fatty acids
OT  - patch-clamp
OT  - potassium channel
OT  - toxicity
COIS- The authors declare no conflict of interest.
EDAT- 2018/11/06 06:00
MHDA- 2018/11/06 06:01
PMCR- 2018/11/01
CRDT- 2018/11/04 06:00
PHST- 2018/09/27 00:00 [received]
PHST- 2018/10/19 00:00 [revised]
PHST- 2018/10/30 00:00 [accepted]
PHST- 2018/11/04 06:00 [entrez]
PHST- 2018/11/06 06:00 [pubmed]
PHST- 2018/11/06 06:01 [medline]
PHST- 2018/11/01 00:00 [pmc-release]
AID - insects9040155 [pii]
AID - insects-09-00155 [pii]
AID - 10.3390/insects9040155 [doi]
PST - epublish
SO  - Insects. 2018 Nov 1;9(4):155. doi: 10.3390/insects9040155.