Potentiating activity of luteolin on membrane permeabilizing agent and ATPase inhibitor against methicillin-resistant Staphylococcus aureus

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• 作者：Dae-Ki Joung³ ; Young-Seob Lee² ; Sin-Hee Han² ; Sang-Won Lee² ; Seon-Woo Cha² ; Su-Hyun Mun¹ ; Ryong Kong¹ ; Ok-Hwa Kang³ ; Ho-Jun Song¹ ; Dong-Won Shin⁴ ; Dong-Yeul Kwon¹ ; ³ ; ^{sssimi@wku.ac.kr" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Luteolin ; Methicillin-resistant Staphylococcus aureus ; Membrane permeabilizing agent ; ATPase inhibitor ; Peptidoglycan
• 刊名：Asian Pacific Journal of Tropical Medicine
• 出版年：2016
• 出版时间：January 2016
• 年：2016
• 卷：9
• 期：1
• 页码：19-22
• 全文大小：814 K

文摘

To investigate the mechanism of antibacterial activity of luteolin (LUT) against methicillin-resistant Staphylococcus aureus (MRSA).

Methods

The mechanism of anti-MRSA activity of LUT was analyzed by the viability assay in membrane permeabilizing agent, ATPase inhibitors, and peptidoglycan (PGN) derived from Staphylococcus aureus (S. aureus). Also, transmission electron microscopy was used to monitor survival characteristics and changes in S. aureus morphology.

Results

Compared to the LUT alone, the optical density of suspensions treated with the combination of 125 μg/mL Tris and 250 μg/mL N,N′-dicyclohexylcarbodiimide were reduced to 60% and 46% of the control, respectively. PGN (15.6 μg/mL) gradually impeded the activity of LUT, and PGN (62.5 μg/mL) completely blocked the activity of LUT on S. aureus.

Conclusions

Increased susceptibility to LUT with the Tris-dicyclohexylcarbodiimide combinations is evident in all tested MRSA isolates. The results indicate LUT synergy in increasing cytoplasmic membrane permeability and inhibiting ATPase. S. aureus PGN directly blocks the antibacterial activity of LUT, suggesting the direct binding of LUT with PGN. These findings may be validated for the development of antibacterial agent for low MRSA resistance.