相关实验视频

Updated: Jun 9, 2025

Ecotoxicological Methodologies to Evaluate Biomarkers at Different Scales in Neotropical Anurans

Ecotoxicological Methodologies to Evaluate Biomarkers at Different Scales in Neotropical Anurans

Published on: April 28, 2023

评估BAC和DDAC生物制剂对胆酶的抑制:一种结合实验和理论的方法

Lynn Mouawad¹, Jeremy Esque², Isabelle André²

¹Biosensors Analysis Environment Group (BAE-LBBM), Université de Perpignan Via Domitia, 66860 Perpignan, France; Laboratoire de Biodiversité et Biotechnologie Microbienne (LBBM), Sorbonne Université, CNRS, UAR 3579, Observatoire Océanologique, 66650 Banyuls-sur-Mer, France.

Biochimica et biophysica acta. General subjects

|October 21, 2024

概括

像甲 (BAC) 和二甲甲 (DDAC) 这样的四次性化合物 (QAs) 抑制胆酶. 这项研究揭示了BAC非竞争性地抑制Drosophila melanogaster AChE,与其他测试的胆酶不同.

科学领域:

生物化学生物化学
毒理学毒理学毒理学
分子生物学分子生物学

背景情况:

消毒生物制剂,特别是四级化合物 (QAs),如化 (BAC) 和二甲化 (DDAC),在家庭,医疗和农业环境中广泛使用.
众所周知,这些QA可以抑制胆化酶,这些酶对神经功能至关重要.

研究的目的:

研究BAC和DDAC对各种胆酶的抑制作用.
用酶试验和分子对接来阐明抑制的机制.

主要方法:

酶抑制试验使用色度测量方法进行.
分子对接模拟以分析抑制剂-酶相互作用.
选择的胆酶包括来自Drosophila melanogaster (DM-AChE) 的乙胆酶 (AChE),来自马血清的Electrophorus electricus (EE-AChE),来自牛的红细胞 (BE-AChE) 和来自马血清的丁胆酶 (BChE).

主要成果:

无论是BAC还是DDAC都表现出了对EE-AChE,BE-AChE和BCHE的竞争性抑制.
BAC显示对DM-AChE的非竞争性抑制,与其对其他酶的影响不同.
分子对接为观察到的抑制模式的结构基础提供了洞察力,表明BAC与DM-AChE中更广泛的活性部位结合.

结论:

在各种胆酶中,BAC和DDAC表现出不同的抑制模式.
BAC对DM-AChE的非竞争性抑制可能是由于其活性位点的结构差异与其他测试的胆酶相比.
了解这些特定的相互作用对于评估常见生物制剂的毒理学概况至关重要.

关键词:

生物杀虫剂是一种杀虫剂.胆化酶是一种胆化酶.酶动力学酶动力学分子对接是分子对接.

更多相关视频

Measurement of Chitinase Activity in Biological Samples

Measurement of Chitinase Activity in Biological Samples

Published on: August 22, 2019

Evaluation of the Efficacy of Organic Peroxyacids for Eradicating Dairy Biofilms Using an Approach Combining Static and Dynamic Methods

Evaluation of the Efficacy of Organic Peroxyacids for Eradicating Dairy Biofilms Using an Approach Combining Static and Dynamic Methods

Published on: December 9, 2022

相关概念视频

Indirect-Acting Cholinergic Agonists: Mechanism of Action

Indirect-Acting Cholinergic Agonists: Mechanism of Action

Indirect-acting cholinergic agonists work by interacting with an enzyme called acetylcholinesterase (AChE) in the synaptic cleft. They can be reversible or irreversible inhibitors and have different effects on the enzyme.
Reversible inhibitors like edrophonium bind to a specific part of the enzyme called the anionic catalytic site. They form noncovalent bonds, which means they are not strongly attached to the enzyme. This creates a temporary and less stable enzyme–inhibitor complex,...

Direct-Acting Cholinergic Agonists: Pharmacokinetics

Direct-Acting Cholinergic Agonists: Pharmacokinetics

Direct-acting cholinergic agonists, such as synthetic choline esters and naturally occurring alkaloids, exert their effects by enhancing the actions of acetylcholine and stimulating the parasympathetic nervous system. Synthetic choline esters share structural similarities with acetylcholine. For example, they have a positively charged quaternary ammonium or onium group, contributing to their hydrophilic characteristics. As a result, they are poorly absorbed in the body through oral...

Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship

Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship

Indirect-acting cholinergic agonists are agents that interact with the acetylcholinesterase enzyme in the synaptic cleft, preventing the breakdown of acetylcholine into choline and acetate. Consequently, the concentration of acetylcholine in the synaptic cleft increases. These agonists can be classified into reversible and irreversible inhibitors based on their duration of action.
Reversible inhibitors display short to medium durations of action. Short-acting agents include simple alcohols with...

Anticholinesterase Agents: Poisoning and Treatment

Anticholinesterase Agents: Poisoning and Treatment

Anticholinesterases, also known as cholinesterase inhibitors, work by blocking the breakdown of acetylcholine, leading to its accumulation in the synaptic cleft. This accumulation indirectly enhances both muscarinic and nicotinic actions. These agents are classified as reversible or irreversible based on their mechanism of action.
Irreversible agents form a strong bond with the cholinesterase enzyme, making it inactive. The breakdown of the phosphorylated enzyme is...

Cholinesterases: Distribution and Function

Cholinesterases: Distribution and Function

Cholinesterases are a group of serine hydrolase enzymes that play a crucial role in the breakdown of choline esters. The two primary types of cholinesterases are acetylcholinesterases (AChEs) and butyrylcholinesterase (BuChEs), which differ in their distribution, function, and substrate specificity. AChEs, also known as true cholinesterases, specifically hydrolyze acetylcholine, while BuChEs, often referred to as pseudocholinesterases, can hydrolyze various choline esters, including...

Antimicrobial Effectiveness

Antimicrobial Effectiveness

The effectiveness of antimicrobial agents depends on various factors influencing their ability to eliminate microbial populations. Larger microbial populations require more time for complete eradication, emphasizing the importance of population size analysis when evaluating antimicrobial efficacy.Microbial resistance to antimicrobial agents varies significantly. Highly resilient microorganisms include endospores, gram-negative bacteria, and non-enveloped viruses, while prions are exceptionally...