Protein Information

Name Acetylcholinesterase
Synonyms ACHE; ACHE protein; AChE; ARACHE; AcChoEase; Acetylcholine acetylhydrolase; Acetylcholinesterase; Acetylcholinesterase isoform E4 E6 variant…

Compound Information

Name profenofos
CAS

Reference List

PubMed Abstract RScore(About this table)
12698238 Venkateswara Rao J, Shilpanjali D, Kavitha P, Madhavendra SS: Toxic effects of profenofos on tissue acetylcholinesterase and gill morphology in a euryhaline fish, Oreochromis mossambicus. Arch Toxicol. 2003 Apr;77(4):227-32. Epub 2003 Jan 18.

Acute and sub-acute studies of profenofos [ O-(4-bromo-2-chlorophenyl)- O-ethyl- S-propyl phosphorothioate] on fish, Oreochromis (Tilapia) mossambicus, were carried out to assess the toxicity in relation to behaviour, morphology, and interactions with the targeted enzyme acetylcholinesterase (AChE, EC 3.1.1.7).
72(0,2,3,7) Details
20169407 Mdegela RH, Mosha RD, Sandvik M, Skaare JU: Assessment of acetylcholinesterase activity in Clarias gariepinus as a biomarker of organophosphate and carbamate exposure. Ecotoxicology. 2010 Feb 19.

Concentrations of pesticides that inhibited 50% (IC (50)) of AChE activities in brain homogenates following in vitro exposures were 0.003, 0.03, 0.15, 190, 0.2, 0.003 and 0.002 muM for carbaryl, chlorfenvinphos, diazinon, dimethoate, fenitrothion, pirimiphosmethyl and profenofos, respectively.
40(0,1,1,10) Details
11093242 Harold JA, Ottea JA: Characterization of esterases associated with profenofos resistance in the tobacco budworm, Heliothis virescens (F.). Arch Insect Biochem Physiol. 2000 Oct;45(2):47-59.

Finally, reduction in the activity or the sensitivity of acetylcholinesterase to inhibition by chlorpyrifos oxon was observed in laboratory-selected and field-collected larvae that expressed resistance to profenofos.
31(0,1,1,1) Details
3983973 Levi PE, Hodgson E: Oxidation of pesticides by purified cytochrome P-450 isozymes from mouse liver. Toxicol Lett. 1985 Feb-Mar;24(2-3):221-8.

The pesticides parathion, fonofos, DEF, Mocap and profenofos were oxidized by the reconstituted monooxygenase system to form acetylcholinesterase (AChE) inhibitors.
31(0,1,1,1) Details
12173245 Baer KN, Olivier K, Pope CN: Influence of temperature and dissolved oxygen on the acute toxicity of profenofos to fathead minnows (Pimephales promelas). Drug Chem Toxicol. 2002 Aug;25(3):231-45.

Mortality, sublethal effects (erratic and hyperactive swimming), and AChE activity in the head and torso were measured at 2, 4, and 12-h following exposure to profenofos.
8(0,0,1,3) Details
19242633 Ismail M, Ali R, Ali T, Waheed U, Khan QM: Evaluation of the acute toxicity of profenofos and its effects on the behavioral pattern of fingerling common carp (Cyprinus carpio L., 1758). Bull Environ Contam Toxicol. 2009 May;82(5):569-73. Epub 2009 Feb 26.

Profenofos, an organophosphate insecticide is acetylcholinesterase inhibitor that has the potential to contaminate the ground water.
31(0,1,1,1) Details
19883634 Eyer P, Worek F, Thiermann H, Eddleston M: Paradox findings may challenge orthodox reasoning in acute organophosphate poisoning. Chem Biol Interact. 2009 Oct 31.

Similarly, poisoning by profenofos, an O,S-dialkyl phosphate, leads to a rapidly aged enzyme.
It is generally accepted that inhibition of acetylcholinesterase (AChE) is the most important acute toxic action of organophosphorus compounds, leading to accumulation of acetylcholine followed by a dysfunction of cholinergic signaling.
5(0,0,0,5) Details
10025366 Gomes J, Dawodu AH, Lloyd O, Revitt DM, Anilal SV: Hepatic injury and disturbed amino acid metabolism in mice following prolonged exposure to organophosphorus pesticides. Hum Exp Toxicol. 1999 Jan;18(1):33-7.

Chronic occupational exposure to organophosphorus and carbamate-type pesticides significantly inhibits acetylcholinesterase activity and causes morbidity.
Laboratory mice were exposed to a formulated mixture of the six organophosphorus pesticides (Dimethoate, Chlorpyrifos, Profenofos, Pirimiphos methyl, Triazophos and Dimethoate) most commonly used in agriculture in this region of the Middle East.
4(0,0,0,4) Details
18313141 Chakra Reddy N, Venkateswara Rao J: Biological response of earthworm, Eisenia foetida (Savigny) to an organophosphorous pesticide, profenofos. Ecotoxicol Environ Saf. 2008 Oct;71(2):574-82. Epub 2008 Mar 4.

Neurotoxic potentiality of PFF was assessed by measuring acetylcholinesterase (AChE).
3(0,0,0,3) Details
12020023 Byrne FJ, Toscano NC: Evaluation of peracid activated organophosphates in studies of insecticide resistance conferred by insensitive acetylcholinesterases. J Econ Entomol. 2002 Apr;95(2):425-9.

Although profenofos was active against electric eel AChE, incubation of the OP with MCPBA did not enhance its anti-AChE properties toward the eel or insect AChEs.
3(0,0,0,3) Details
16289700 Abdel-Halim KY, Salama AK, El-Khateeb EN, Bakry NM: Organophosphorus pollutants (OPP) in aquatic environment at Damietta Governorate, Egypt: implications for monitoring and biomarker responses. Chemosphere. 2006 Jun;63(9):1491-8. Epub 2005 Nov 14.

The obtained results are in parallel to that found in case of cholinesterase activity where the activity of both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) was declined at these seasonal period.
Chlorpyrifos, chlorpyrifos-methyl, malathion, diazinon, pirimiphos-methyl and profenofos were detected in most samples.
3(0,0,0,3) Details
10214458 Lakew K, Mekonnen Y: The health status of northern Omo State Farm workers exposed to chlorpyrifos and profenofos. Ethiop Med J. 1998 Jul;36(3):175-84.

Plasma ChE (PChE) and erythrocyte ChE (AChE) activities were determined electrometrically before and after pesticide exposure.
2(0,0,0,2) Details
15893542 Quistad GB, Fisher KJ, Owen SC, Klintenberg R, Casida JE: Platelet-activating factor acetylhydrolase: selective inhibition by potent n-alkyl methylphosphonofluoridates. Toxicol Appl Pharmacol. 2005 Jun 1;205(2):149-56. Epub 2004 Nov 11.

Several key OP pesticides and their oxon metabolites were very poor inhibitors of mouse brain and human plasma PAF-AH in vitro but moderately active for mouse brain and blood PAF-AH in vivo (e.g., tribufos defoliant and profenofos insecticide, presumably following oxidative bioactivation).
OP compounds were then designed for maximum in vitro potency and selectivity for mouse brain PAF-AH vs. acetylcholinesterase (AChE).
2(0,0,0,2) Details
19737786 Eddleston M, Worek F, Eyer P, Thiermann H, Von Meyer L, Jeganathan K, Sheriff MH, Dawson AH, Buckley NA: Poisoning with the S-Alkyl organophosphorus insecticides profenofos and prothiofos. QJM. 2009 Nov;102(11):785-92. Epub 2009 Sep 8.

This chemical structure affects their responsiveness to oxime-induced acetylcholinesterase (AChE) reactivation after poisoning.
1(0,0,0,1) Details
19908228 Carletto J, Martin T, Vanlerberghe-Masutti F, Brevault T: Insecticide resistance traits differ among and within host races in Aphis gossypii. Pest Manag Sci. 2010 Mar;66(3):301-7.

Conversely, all clones were resistant to dimethoate (organophosphate) (RF = 4.1-38.1) and carried mutation S431F in the acetylcholinesterase gene.
Auber, PsP4 and Burk also carried mutation A302S in this gene, which possibly conferred moderate resistance (RF = 3.7-6.8) to profenofos and monocrotophos (organophosphates).
1(0,0,0,1) Details
17549541 Venkateswara Rao J, Kavitha P, Jakka NM, Sridhar V, Usman PK: Toxicity of organophosphates on morphology and locomotor behavior in brine shrimp, Artemia salina. Arch Environ Contam Toxicol. 2007 Aug;53(2):227-32. Epub 2007 Jun 1.

The acute toxicity and hatching success of four organophosphorus insecticides--acephate (ACEP), chlorpyrifos (CPP), monocrotophos (MCP), and profenofos (PF)--was studied in a short-term bioassay using brine shrimp, Artemia salina.
The in vivo effect of these insecticides on acetylcholinesterase (Enzyme commission number (EC 3.1.1.7) activity was also determined in LC (50)-exposed nauplii after 24 hours.
1(0,0,0,1) Details
15888665 Quistad GB, Klintenberg R, Casida JE: Blood acylpeptide hydrolase activity is a sensitive marker for exposure to some organophosphate toxicants. Toxicol Sci. 2005 Aug;86(2):291-9. Epub 2005 May 11.

The inhibitory potency of OP pesticides in vivo in mice varies from APH selective (dichlorvos, naled, and trichlorfon), to APH and BChE selective (profenofos and tribufos), to ChE selective or nonselective (many commercial insecticides).
Sarin administered ip at a lethal dose to guinea pigs inhibits blood acetylcholinesterase and BChE completely but erythrocyte APH only partially.
1(0,0,0,1) Details
11350214 Quistad GB, Sparks SE, Casida JE: Fatty acid amide hydrolase inhibition by neurotoxic organophosphorus pesticides. Toxicol Appl Pharmacol. 2001 May 15;173(1):48-55.

These BDPOs and EOPF inhibit mouse brain FAAH in vitro with > or =200-fold higher potency than for AChE.
Five OP pesticides inhibit 50% of the brain FAAH activity (ED50) at <30 mg/kg 4 h after ip administration to mice; while inhibition by chlorpyrifos, diazinon, and methamidophos occurs near acutely toxic levels, profenofos and tribufos are effective at asymptomatic doses.
1(0,0,0,1) Details
19079407 Paudyal BP: Organophosphorus poisoning. JNMA J Nepal Med Assoc. 2008 Oct-Dec;47(172):251-8.

Metacid (Methyl parathion) and Nuvan (Dichlorovos) are commonly ingested OP pesticides; Dimethoate, Profenofos, and Chlorpyrifos are other less frequently ingested compounds in Nepal.
The toxicity of these OP pesticides is due to the irreversible inhibition of acetylcholinesterase (AChE) enzyme leading to accumulation of acetylcholine and subsequent over-activation of cholinergic receptors in various parts of the body.
1(0,0,0,1) Details
6710513 Glickman AH, Wing KD, Casida JE: Profenofos insecticide bioactivation in relation to antidote action and the stereospecificity of acetylcholinesterase inhibition, reactivation, and aging. Toxicol Appl Pharmacol. 1984 Mar 30;73(1):16-22.

Poisoning signs in chicks administered the organophosphorus insecticide profenofos correlated with in vivo inhibition of brain acetylcholinesterase (AChE) activity.
274(3,4,4,4) Details
17705656 Nillos MG, Rodriguez-Fuentes G, Gan J, Schlenk D: Enantioselective acetylcholinesterase inhibition of the organophosphorous insecticides profenofos, fonofos, and crotoxyphos. Environ Toxicol Chem. 2007 Sep;26(9):1949-54.
247(3,3,3,7) Details
6849116 Wing KD, Glickman AH, Casida JE: Oxidative bioactivation of S-alkyl phosphorothiolate pesticides: stereospecificity of profenofos insecticide activation. Science. 1983 Jan 7;219(4580):63-5.

This activation is stereospecific for the chiral isomers of O-(4-bromo-2-chlorophenyl) O-ethyl S-propyl phosphorothiolate (profenofos insecticide); the more toxic (-) isomer becomes a 34-fold better inhibitor of acetylcholinesterase in vitro, whereas the less toxic (+) isomer is deactivated by a factor of 2.
163(2,2,2,3) Details
20021020 Das GP, Jamil K, Rahman MF: Effect of four organophosphorus compounds on human blood acetylcholinesterase: in vitro studies. Toxicol Mech Methods. 2006;16(8):455-9.

The aim of the study was to determine the IC50 concentration of the pesticides monocrotophos, chlorpyrifos, profenofos, and acephate as inhibitors of AChE.
90(1,1,2,5) Details
11401263 Kumar A, Chapman JC: Profenofos residues in wild fish from cotton-growing areas of New South Wales, Australia. J Environ Qual. 2001 May-Jun;30(3):740-50.

Acetylcholinesterase inhibition was a useful indicator of profenofos exposure within a season, particularly if linked with residue measurements.
88(1,1,2,3) Details
16777704 Venkateswara Rao J, Begum G, Jakka NM, Srikanth K, Nageswara Rao R: Sublethal effects of profenofos on locomotor behavior and gill architecture of the mosquito fish, Gambusia affinis. Drug Chem Toxicol. 2006;29(3):255-67.

Subacute studies of profenofos on mosquito fish, Gambusia affinis, were carried out for 20 days to assess the locomotor behavior and structural integrity of gill in relation to bioaccumulation and targeted enzyme acetylcholinesterase (AChE; EC 3.1.1.7).
82(1,1,1,2) Details
7288097 El-Sebae AH, Enan EE, Soliman SA, El-Fiki S, Khamees E: Biochemical effects of some organophosphorus insecticide on new targets in white rats. J Environ Sci Health B. 1981;16(4):475-91.

The three S-n-propyl phosphates and phosphothioates: RH 218, profenofos and prothiophos were compared with fenitrothion in their potential as inhibitors of rat liver and brain AChE.
81(1,1,1,1) Details