Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:3.1.1.7 (acetylcholinesterase)
 28,390 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The distribution of cholinesterase activity in the microfilaria of the nocturnally periodic Wuchereria bancrofti has been described. Using histochemical methods, cholinesterase activity has been demonstrated in the amphids (Mundgebilde), phasmids (Schwanzgebilde), nerve-ring, excretory and anal vesicles of the microfilaria. It has been found that the enzyme activity disappeared completely after treatment with the specific cholinesterase inhibitor eserine. Evidence is presented that the greater amount of the cholinesterase activity detected is related to acetylcholinesterase and the functional significance of the enzyme in the enzyme reactive structures is discussed.
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PMID:Cholinesterase activity in the microfilaria of Wuchereria bancrofti Cobbold. 7 89

Metrifonate, in doses of 10 mg/kg for 3 consecutive days, demonstrated partial microfilaricidal activity against Onchocerca volvulus in humans. Higher doses were not investigated because of the toxic reactions obtained and the absence of monitoring of the blood cholinesterase levels. Spaced doses of 10 mg/kg every 2 weeks or once monthly up to 3 doses showed neither micro- nor macrofilaricidal activity against Wuchereria bancrofti.
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PMID:Metrifonate in onchocerciasis and lymphatic filariasis. 67 39

The acetylcholinesterase (AChE) activity was measured in human serum from persons infected with the filarial parasite Wuchereria bancrofti. The asymptomatic microfilaremic serum showed five times increase in AChE-activity as compared with normal serum, whereas only little difference was observed in serum from patients with elephantiasis. Similar results were obtained when the enzyme activity was measured in the immune complexes precipitated with polyethyleneglycol. Further, the effect of the antifilarial drug diethylcarbamazine (DEC), on the AChE activity of infected and normal serum was studied in in vivo and in vitro experiments. In vitro, DEC was found to be effective only with respect to AChE from asymptomatic microfilaremic serum where 75% decrease in enzyme activity was observed at 100 mumol. The oral administration of DEC (5 mg/kg of body weight/day) effected the activity of AChE from microfilaremic serum as shown after 1 hr, 1 and 3 weeks. A regular decrease in enzyme activity of asymptomatic microfilaremic serum was observed. By increasing time periods and after three weeks the level of AChE reaches the normal value. In vitro and in vivo the same concentration of DEC has negligible effect on the normal serum suggesting that in case of asymptomatic microfilaremic serum the increased activity of AChE is different in nature than the host acetylcho-[abstract incomplete in journal]
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PMID:In vitro and in vivo effect of diethylcarbamazine on the activity of acetylcholinesterase from Wuchereria bancrofti infected human serum. 151 32

An antigen with cholinesterase activity was detected in the sera of patients infected with Wuchereria bancrofti. The asymptomatic microfilaremic sera showed 3 to 4 times more cholinesterase activity for acetylthiocholine (ATCh) as compared to sera of symptomatic amicrofilaremic, hookworm infected and endemic normals, whereas the activities for butyrylthiocholine (BTCh) did not significantly differ. The enzyme activities from both sources, namely from sera of microfilaremic cases and from endemic normals, were partially purified and according to substrate specificity for ATCh and BTCh as well as inhibition of the former activity by excess substrate classified as acetylcholinesterase (AChE; EC 3.1.1.7) and pseudocholinesterase (AChE; EC 3.1.1.8), respectively. The Km-value for ATCh of the cholinesterase from the microfilaremic sera was determined to be 0.87 mM. Eserine competitively inhibited the AChE activity; the inhibition constant was found to be 1.3 microM. The BChE from the normal sera had Km-values of 0.15 and 0.20 mM for BTCh and ATCh, respectively, and did not show significant inhibition by eserine. These and other dissimilarities suggest a difference in nature of the cholinesterases in microfilaremic and normal sera and propose that the former enzyme, a true acetylcholinesterase, originates from the parasite. Additional evidence for the origin of the AChE-activity from the parasite was provided by ELISA-studies; anti-Brugia malayi AChE antibodies confirmed antigenecity and cross reactivity of the AChE in infected sera, whereas the antibodies did not show any cross reactivity with the BChE in normal sera.
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PMID:Wuchereria bancrofti: identification of parasitic acetylcholinesterase in microfilariae infected human serum. 836 69

We measured the levels of lysosomal enzymes and acetylcholine in Wuchereria bancrofti-infected asymptomatic microfilaraemic human serum, and found a significant decrease in the activity of beta-glucuronidase and acid phosphatase compared to normal serum. Acetylcholine levels were also decreased during infection. However, after giving diethylcarbamazine (6 mg/kg body wt/day) the level of lysosomal enzymes and acetylcholine increased and reached a normal value after two weeks of therapy. It is proposed that parasites secrete acetylcholinesterase in the circulation which degrades acetylcholine. Since acetylcholine stimulates the release of lysosomal enzymes and phagocytosis, the immune response of the host is suppressed during infection. During diethylcarbamazine (DEC) therapy the parasitic enzyme is inhibited by the drug and the normal level of acetylcholine is resumed, which again stimulates the release of lysosomal enzyme and the process of phagocytosis.
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PMID:Diethylcarbamazine: effect on lysosomal enzymes and acetylcholine in Wuchereria bancrofti infection. 927 Jul 36

Setaria cervi, a bovine filarial parasite, secretes acetylcholinesterase during in vitro cultivation. A significant amount of enzyme activity was detected both in culture media and somatic extracts of different developmental stages of the parasite. The microfilarial stage showed a higher level of AChE activity than adult worms, with females being considerably more active than males. The secretory enzyme from microfilariae preferentially utilized acetylthiocholine iodide as substrate and showed two electrophoretically distinct isoforms in native PAGE. Secretory enzyme was purified from the excretory/secretory products of microfilariae using edrophonium chloride linked to epoxy-activated sepharose. Analysis of purified acetylcholinesterase by SDS-PAGE revealed the existence of two proteins of 75kD and 45kD under nonreducing conditions. These secretory enzymes are antigenic and cross-reactive with Wuchereria bancrofti-infected asymptomatic microfilaraemic human sera when tested by enzyme linked immunosorbent assay and immunoblotting. The secretory AChE(s) from S. cervi microfilariae may be utilized for diagnosis of early filarial infections.
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PMID:Secretory acetylcholinesterase of Setaria cervi microfilariae and its antigenic cross-reactivity with Wuchereria bancrofti. 948 68

Organophosphate/carbamate target resistance has emerged in Culex pipiens L. (Diptera: Culicidae), the vector of Wuchereria bancrofti and West Nile virus (family Flaviviridae, genus Flavivirus) in China. The insensitive acetylcholinesterase was detected in only one of 20 samples collected on a north-to-south transect. According to previous findings, a unique mutation, G119S in the ace-1 gene, explained this high insensitivity. Phylogenetic analysis indicates that the mutation G119S recently detected in China results from an independent mutation event. The G119S mutation thus occurred at least three times independently within the Cx. pipiens complex, once in the temperate (Cx. p. pipiens) and twice in the tropical form (Cx. p. quinquefasciatus). Bioassays performed with a purified G119S strain indicated that this substitution was associated with high levels of resistance to chlorpyrifos, fenitrothion, malathion, and parathion, but low levels of resistance to dichlorvos, trichlorfon, and fenthion. Hence, it is possible that in China, dichlorvos, trichlorfon, and fenthion will still achieve effective control even in the presence of the G119S mutation.
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PMID:Recent emergence of insensitive acetylcholinesterase in Chinese populations of the mosquito Culex pipiens (Diptera: Culicidae). 1701 23