The catechins EGCG and GCG show a variety of pharmacological activities, especially an antibacterial capacity, but their modes of antimicrobial action have not been fully elucidated. 1-Deoxy-d-xylulose 5-phosphate reductoisomerase (DXR), the first key enzyme in the MEP pathway for terpenoid biosynthesis, is a recently validated antimicrobial target. In order to disclose the antibacterial mechanism of EGCG and GCG, the DXR inhibitory activity of them was investigated in this study. The data show that EGCG and GCG both could specifically suppress the activity of DXR, with EGCG exhibiting relatively low effect against DXR (IC about 210 μM) and GCG displaying strong activity (IC 27.5 μM). In addition, studies on inhibition kinetics of the catechins against DXR demonstrate that they are competitive inhibitors of DXR against DXP and uncompetitive inhibitors with respect to NADPH. Meanwhile, the possible interactions between DXR and the catechine, esyth onlols were simulated via docking experiments.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.abb.2017.04.007 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Inhibition mechanisms of α-glucosidase by eight catechins: Kinetic, molecular docking, and surface plasmon resonance analysis.
Int J Biol Macromol
December 2024
College of Food Science and Engineering, Tianjin University of Science & Technology, Tianjin 300457, China; Research Centre of Modern Analytical Technology, Tianjin University of Science & Technology, Tianjin 300457, China; State Key Laboratory of Chinese Medicine Modernization, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China. Electronic address:
α-Glucosidase is considered to be one of the effective targets for the treatment of type 2 diabetes. This study examined the inhibitory mechanisms of eight catechins on α-glucosidase, including both the free forms (C, EC, GC, EGC) and esterified forms (CG, ECG, GCG, EGCG). Enzyme kinetics and molecular docking studies demonstrated that catechins primarily inhibit α-glucosidase by binding through hydrogen bonds and hydrophobic interactions, with esterified catechins exhibiting stronger inhibitory effects.
View Article and Find Full Text PDFStructure-based virtual screening discovers novel PKMYT1 inhibitors.
RSC Med Chem
September 2024
Key Laboratory of Structure-Based Drug Design & Discovery of Ministry of Education, Shenyang Pharmaceutical University Shenyang 110016 China
Article Synopsis
- - PKMYT1 is important in the cell cycle as it phosphorylates CDK1-CyclinB, impacting cell growth and division.
- - Amplifying CCNE1 and blocking PKMYT1 leads to synthetic lethality, suggesting that targeting PKMYT1 could be effective for cancer treatment.
- - Virtual screening identified natural compounds like EGCG and luteolin with strong PKMYT1 inhibition, revealing that their binding relies mainly on stable hydrogen bonds in specific regions of the PKMYT1 protein.
Tea's Characteristic Components Eliminate Acrylamide in the Maillard Model System.
Foods
September 2024
State Key Laboratory of Tea Plant Biology and Utilization, Anhui Agricultural University, Hefei 230036, China.
This study investigated the effects of various characteristic components of tea-theaflavins, catechins, thearubigins, theasinensins, theanine, catechin (C), catechin gallate (CG), epicatechin (EC), epicatechin gallate (ECG), epigallocatechin (EGC), epigallocatechin gallate (EGCG), gallocatechin (GC), and gallocatechin gallate (GCG)-on acrylamide formation. The results revealed that most of tea's characteristic components could significantly eliminate acrylamide, ranked from highest to lowest as follows: GC (55.73%) > EC (46.
View Article and Find Full Text PDFThe Potential Mechanisms of Catechins in Tea for Anti-Hypertension: An Integration of Network Pharmacology, Molecular Docking, and Molecular Dynamics Simulation.
Foods
August 2024
Anxi College of Tea Science, Fujian Agriculture and Forestry University, Fuzhou 350002, China.
Catechins, a class of polyphenolic compounds found in tea, have attracted significant attention due to their numerous health benefits, particularly for the treatment and protection of hypertension. However, the potential targets and mechanisms of action of catechins in combating hypertension remain unclear. This study systematically investigates the anti-hypertensive mechanisms of tea catechins using network pharmacology, molecular docking, and molecular dynamics simulation techniques.
View Article and Find Full Text PDFComprehensive Analysis of the Yield and Leaf Quality of Fresh Tea ( cv. Jin Xuan) under Different Nitrogen Fertilization Levels.
Foods
July 2024
College of Horticulture, South China Agricultural University, Guangzhou 510642, China.
Reasonable application of nitrogen fertilizer can improve the yield and quality of tea. This study used Jin Xuan as the tested variety and applied nitrogen fertilizer at rates of 0 kg/ha (N0), 150 kg/ha (N150), 300 kg/ha (N300), and 450 kg/ha (N450) in the summer and autumn seasons to analyze the effects of nitrogen application on the quality components and gene expression of tea leaves. The results showed that the N150 treatment significantly increased total polyphenols (TP), total catechins (TC), and caffeine contents, with the most significant increase observed in the content of six monomers of catechins (EGCG, ECG, EGC, GCG, GC, and EC) in the summer.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!