1. Cinnamaldehyde: An effective component of Cinnamomum cassia inhibiting Helicobacter pylori.
- Author
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Li, Chen-yan, Liao, Li-juan, Yang, Shi-xian, Wang, Lu-yao, Chen, Hao, Luo, Peipei, Huang, Gan-rong, and Huang, Yan-Qiang
- Subjects
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ANTIBIOTICS , *HELICOBACTER pylori , *IN vitro studies , *CHINESE medicine , *COMPUTER-assisted molecular modeling , *MICROBIAL sensitivity tests , *BIOFILMS , *ALDEHYDES , *POLYMERASE chain reaction , *TREATMENT effectiveness , *IN vivo studies , *CINNAMON , *PLANT extracts , *MICE , *HELICOBACTER diseases , *ANIMAL experimentation , *SCANNING electron microscopy , *PHARMACODYNAMICS - Abstract
Cinnamomum cassia Presl (Cinnamomum cassia) is a common traditional Chinese medicine, which can promote the secretion and digestion of gastric juice, improve the function of gastrointestinal tract. Cinnamaldehyde (CA) is a synthetic food flavoring in the Chinese Pharmacopoeia. This study aimed to search for the active ingredient (CA) of inhibiting H. pylori from Cinnamomum cassia , and elucidate mechanism of action, so as to provide the experimental basis for the treatment of H. pylori infection with Cinnamomum cassia. It's in vitro and in vivo pharmacological properties were evaluated based on minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC), and an acute gastric inflammation model in mice infected with H. pylori. Drug safety was evaluated using the CCK8 method and high-dose administration in mice. The advantageous characteristics of CA in inhibiting H. pylori were confirmed using acidic conditions and in combination with the antibiotics. The mechanism underlying the action of CA on H. pylori was explored using scanning electron microscopy (SEM), adhesion experiments, biofilm inhibition tests, ATP and ROS release experiments, and drug affinity responsive target stability (DARTS) screening of target proteins. The protein function and target genes were verified by molecular docking and Real-Time quantitative reverse transcription PCR (qRT-PCR). The results demonstrated that CA was found to be the main active ingredient against H. pylori in Cinnamomum cassia in-vitro tests, with a MIC of 8–16 μg/mL. Moreover, CA effectively inhibited both sensitive and resistant H. pylori strains. The dual therapy of PPI + CA exhibited remarkable in vivo efficacy in the acute gastritis mouse model, superior to the standard triple therapy. DARTS, molecular docking, and qRT-PCR results suggested that the target sites of action were closely associated with GyrA , GyrB , AtpA , and TopA , which made DNA replication and transcription impossible, then leading to inhibition of bacterial adhesion and colonization, suppression of biofilm formation, and inhibition ATP and enhancing ROS. This study demonstrated the suitability of CA as a promising lead drug against H. pylori , The main mechanisms can target GyrA ect, leading to reduce ATP and produce ROS, which induces the apoptosis of bacterial. [Display omitted] • Cinnamaldehyde can inhibit the sensitive and resistant Helicobacter pylori. • Helicobacter pylori is not easy to develop resistance to cinnamaldehyde. • Cinnamaldehyde has a good antibacterial effect under acidic conditions. • Cinnamaldehyde can treat acute gastritis with Helicobacter pylori infecting. • Cinnamaldehyde can target the GyrA , GyrB , AtpA and TopA. [ABSTRACT FROM AUTHOR]
- Published
- 2024
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