Emamectin Benzoate (MK-244)
目录号 : GC32172EmamectinBenzoate(MK-244)通过与GABA受体结合,而激活氯离子通道和谷氨酸门控氯离子通道,从而干扰节肢动物神经信号。
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Emamectin Benzoate (MK-244) works as a chloride channel activator by binding gamma aminobutyric acid (GABA) receptor and glutamate-gated chloride channels disrupting nerve signals within arthropods.
Emamectin Benzoate stimulates the release of GABA from the synapses between nerve cells and while additionally increasing GABA's affinity for its receptor on the post-junction membrane of muscle cells in insects and arthropods.
[1]. Cheng X, et al. Effect of Emamectin Benzoate on Root-Knot Nematodes and Tomato Yield. PLoS One. 2015 Oct 28;10(10):e0141235.
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Induction of developmental toxicity and cardiotoxicity in zebrafish embryos by Emamectin Benzoate through oxidative stress
Sci Total Environ 2022 Jun 15;825:154040.PMID:35196543DOI:10.1016/j.scitotenv.2022.154040.
Emamectin Benzoate (EMB) is a widely used pesticide in agriculture, but its potential risks to the environment and health have not been fully evaluated. In this study, we evaluated the toxicity of Emamectin Benzoate using zebrafish model, and found that it affected early embryonic development, such as malformations and delayed hatching. Mechanistically, Emamectin Benzoate increased oxidative stress by excessive production of reactive oxygen species (ROS) and abnormal activities of the antioxidant enzymes. Moreover, Emamectin Benzoate exposure caused abnormalities in zebrafish heart morphology and function, such as long SV-BA distance and slow heart rate. Alterations were induced in the transcription of heart development-related genes (nkx2.5, tbx5, gata4 and myl7). In summary, our data showed that Emamectin Benzoate induces developmental toxicity and cardiotoxicity in zebrafish. Our research provides new evidence on the Emamectin Benzoate's toxicity and potential risk in human health.
Dissipation of Emamectin Benzoate Residues in Rice and Rice-Growing Environments
Molecules 2020 Jan 23;25(3):483.PMID:31979297DOI:10.3390/molecules25030483.
The experiment developed the ultra-high-performance liquid chromatography-tandem mass spectrometry (UPLC/MS/MS) method for testing Emamectin Benzoate, and studied the metabolism of Emamectin Benzoate in rice plants and rice-growing environments via application of this testing method. The dissipation curve of Emamectin Benzoate standard substance was good at 0.5-200 渭g L-1, and its correlation coefficient was greater than 0.99. In the concentration range of 0.1-50 渭g kg-1, the average recovery rate of plants, soil, and field water was 82 %-102 %, and relative standard deviation (RSD) was between 0.3 % and 15.9 %. Half-lives in rice plants and soil were 0.8-2.8 days and 1.9-3.8 days, respectively, and Emamectin Benzoate was not detected in rice or rice hull. The experiment showed that Emamectin Benzoate is harmless to human health at the concentration recommended by the manufacturer.
Sublethal effects and reproductive hormesis of Emamectin Benzoate on Plutella xylostella
Front Physiol 2022 Oct 19;13:1025959.PMID:36338483DOI:10.3389/fphys.2022.1025959.
The diamondback moth (DBM), Plutella xylostella L., is an important pest of cruciferous vegetables, and population control mainly depends on chemical pesticides. Emamectin Benzoate is a highly effective insecticide used for controlling DBM. However, it is unknown how the sublethal effects of low concentration residues of Emamectin Benzoate on DBM. So the population development sublethal effects of Emamectin Benzoate, at LC5, LC10, and LC20 with concentrations of 0.014 mg/L, 0.024 mg/L and 0.047 mg/L, respectively, on adult DBM and their progeny were investigated in this study. The pupal weight, pupal period, female fecundity, and vitellin content of the F0 DBM generation increased significantly compared to the control. And the single female oviposition number of DBM was increased by 20.21% with LC20 treatment. The pupation rate, adult longevity and ovariole length of the treatment groups decreased significantly. The fecundity of DBM in the treatment groups increased, and this increased the population by a presumptive 13.84%. Treatment also led to the shortening of ovarioles and the reduction of egg hatching, and increased pupal weight in the F1 generation. We concluded that the effects of sublethal/low concentration Emamectin Benzoate on the different life stages of DBM were variable, and the reproductive hormesis on DBM adults were attractive findings.
Metabolization of Emamectin Benzoate into desmethyl Emamectin Benzoate in spiked marine sediments
Chemosphere 2023 Feb;313:137635.PMID:36565759DOI:10.1016/j.chemosphere.2022.137635.
Emamectin Benzoate (EMB) (4鈥砫eoxy- 4鈥?epi-methylaminoavermectin) is a pesticide developed to control pests on various crops, and in forestry. It is also used in salmon aquaculture to control sea lice infestations as an in-feed therapeutant. Little is known about EMB metabolites and potential associated toxicities in marine sediments. In this study, we used natural marine sediments (sand and mud) fortified at an EMB concentration of 60 ppb (wet weight). Results show an almost immediate transformation of EMB to Desmethyl EMB (DES) with no increased rates of metabolization when stored sediment samples were incubated for up to 16 h. The transformation ratio of EMB to DES represented between 0.16 and 0.39% of EMB; values are lower than what has been observed in fish tissue. Data suggest that DES is generated through both abiotic (tested after autoclaving marine sediments) and biological processes. Further work on freshly sampled marine sediments with EMB deposits, different organic regimes, and a detailed assessment of active bacterial communities are necessary to better evaluate the EMB to DES rate of transformation around aquaculture sites.
Avermectin use in aquaculture
Curr Pharm Biotechnol 2012 May;13(6):1095-102.PMID:22039799DOI:10.2174/138920112800399158.
The main indication for use of avermectins in aquaculture-produced fish is infestations with ectoparasitic copepods. The compounds ivermectin and Emamectin Benzoate are predominantly used as in-feed formulations on salmonid fish against copepods in the family Caligidae: Lepeophtheirus salmonis, Caligus elongatus and C. rogercresseyi. These agents are well-documented as very effective on all developmental stages of the parasites. The duration of effect can be up to 10 weeks. The safety margin for ivermectin is narrow, but better for Emamectin Benzoate. Environmental impact from these chemicals on bottom-dwelling and sediment-dwelling organisms occurs, but these are restricted to the immediate area around the production site. Avermectins are incompletely absorbed from the intestine of the fish and slowly excreted. They penetrate the blood-brain barrier of the fish, ivermectin more than Emamectin Benzoate. Resistance has developed against these agents in L. salmonis in almost all major salmon producing areas. The situation must be viewed as serious and can render these agents completely ineffective for salmon lice control.