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Antibacterial active compounds from Hypericum ascyron L. induce bacterial cell death through apoptosis pathway
Xiu-Mei Li1, Xue-Gang Luo1, Chuan-Ling Si2
1Key Lab of Industrial Fermentation Microbiology of the Ministry of Education, Tianjin Key Lab of Industrial Microbiology, College of Biotechnology, Tianjin University of Science and Technology, Tianjin, 300457, PR China.
European Journal of Medicinal Chemistry
|April 29, 2015
Summary
Hypericum ascyron L. compounds exhibit antibacterial properties by inducing apoptosis in bacteria. This study identifies quercetin and a novel compound, Kaempferol 3-O-β-(2″-acetyl)-galactopyranoside, demonstrating their potential as new antibacterial agents.
Area of Science:
- Phytochemistry
- Microbiology
- Pharmacology
Background:
- Hypericum ascyron L. possesses a long history of traditional medicinal use in China.
- Scientific validation of its traditional applications, particularly its antimicrobial effects, is lacking.
- Understanding the mechanisms of action for H. ascyron L. is crucial for modern therapeutic development.
Purpose of the Study:
- To investigate the antimicrobial mechanism of compounds isolated from Hypericum ascyron L.
- To identify the specific compounds responsible for the observed antibacterial activity.
- To provide a scientific basis for the traditional use of H. ascyron L.
Main Methods:
- Bioguided fractionation of H. ascyron L. extract.
- Minimum Inhibitory Concentration (MIC) and Minimum Bactericidal Concentration (MBC) determination using cup plate and MTT assays.
- Apoptosis induction analysis via Annexin V-FITC/PI staining, TUNEL assay, and DNA gel electrophoresis.
- Cell membrane potential disruption assessment.
- Compound identification using Mass Spectrometry and Nuclear Magnetic Resonance.
Main Results:
- Fraction 8 of H. ascyron L. extract demonstrated significant antibacterial activity with MIC and MBC values of 5 mg/mL.
- Compounds from fraction 8 induced apoptosis-like cell death in bacteria.
- Fraction 8 disrupted bacterial cell membrane potential, indicating a membrane-mediated apoptosis pathway.
- Quercetin and Kaempferol 3-O-β-(2″-acetyl)-galactopyranoside were identified as the active compounds.
Conclusions:
- Kaempferol 3-O-β-(2″-acetyl)-galactopyranoside, a novel compound found in Clusiaceae, along with quercetin, exhibits potent antibacterial activity through apoptosis induction.
- The findings support the traditional use of H. ascyron L. and suggest its potential for developing new antibacterial drugs.
- This study provides the first evidence of Kaempferol 3-O-β-(2″-acetyl)-galactopyranoside's antibacterial mechanism via apoptosis.
Keywords:
Antimicrobial activityApoptosisHypericum ascyron L.Preparative high performance liquid chromatographyStructure identificationStructure–activity relationshipMore Related Videos
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