To develop effective and safe acne vulgaris therapies with a continuing demand for new solutions, we investigated unique efficacy of an antibacterial agent from marine brown alga Eisenia bicyclis in treating acne vulgaris. The methanolic extract of E. bicyclis exhibited potential antibacterial activity against acne-related bacteria. The ethyl acetate fraction showed the strongest antibacterial activity against the bacteria among solvent fractions. Six compounds (1-6), previously isolated from the ethyl acetate fraction of E. bicyclis, were evaluated for antibacterial activity against acne-related bacteria. Among them, compound 2 (fucofuroeckol-A [FF]) exhibited the highest antibacterial activity against acne-related bacteria with a minimum inhibitory concentration (MIC) ranging from 32 to 128 μg mL -1 . Furthermore, FF clearly reversed the high-level erythromycin and lincomycin resistance of Propionibacterium acnes. The MIC values of erythromycin against P. acnes were dramatically reduced from 2,048 to 1.0 μg mL -1 in combination with MIC of FF (64 μg mL -1). The fractional inhibitory concentration indices of erythromycin and lincomycin were measured from 0.500 to 0.751 in combination with 32 or 64 μg mL -1 of FF against all tested P. acnes strains, suggesting that FF-erythromycin and FF-lincomycin combinations exert a weak synergistic effect against P. acnes. The results of this study suggest that the compounds derived from E. bicyclis can be a potential source of natural antibacterial agents and a pharmaceutical component against acnerelated bacteria.Key Words: acne-related bacteria; antimicrobial activity; Eisenia bicyclis; phlorotannins; synergistic effect INTRODUCTIONAcne vulgaris is a common skin disease affecting children and adolescents. The pathogenesis of acne is multifactorial and complex. There are four important factors that cause acne in humans, such as an increase in sebum secretion, keratinization of the follicle, bacteria, and inflammation (Farrar and Ingham 2004). Pro pionibacterium acnes, Staphylococcus epidermidis, S. aureus, and Pseudomonas aeruginosa are often involved in the development of abnormal follicular keratinization and inflammation (Yamaguchi et al. 2009 This is an Open Access article distributed under the terms of the Creative Commons Attribution Non-Commercial License (http://creativecommons.org/licenses/by-nc/3.0/) which permits unrestricted non-commercial use, distribution, and reproduction in any medium, provided the original work is properly cited. 48 MATERIALS AND METHODS Raw materials and extractionIn late September 2010, E. bicyclis was purchased from Ulleung Trading Co. (Ulleung-gun, Korea). A voucher specimen has been deposited in the author's laboratory. Dried E. bicyclis was finely ground and powdered with a food mixer (HMF-1000A; Hanil Electronics, Seoul, Korea). The dried powder was vacuum-packed and kept at -20°C until use. The dried E. bicyclis powder (1.0 kg) was extracted with methanol (MeOH; 10 L × 3) at 70°C for 3 h (3 times) and the solvent was evaporated ...
To find more effective ways of overcoming methicillin-resistant Staphylococcus aureus (MRSA), there has been considerable interest in the use of marine-derived constituents as alternatives to control pathogenic microorganisms. In this study, we investigated whether phlorofucofuroeckol-A (PFF) isolated from the edible brown alga Eisenia bicyclis suppressed production or function of penicillin-binding protein 2a (PBP2a). The antimicrobial mode of action of PFF in MRSA was identified by measuring cell membrane integrity and using the time-kill curve method. We attempted to determine the antimicrobial effects of PFF on the expression level of the resistance determinants mecA and its regulatory genes mecI and mecR1 in MRSA by reverse transcriptase polymerase chain reaction. PFF suppressed mecI, mecR1, and mecA gene expression in a dose-dependent manner. In addition, we revealed PFF mediates the suppressive effect of PBP2a expression in MRSA by Western blot analysis. PFF suppressed production of the PBP2a protein, suggesting that PFF probably acts by controlling the methicillin resistance-associated genes involved in the cell wall and production of PBP2a. These results demonstrate that PFF isolated from E. bicyclis significantly suppressed the expression of the methicillin resistance-associated genes and production of PBP2a, which is considered the primary cause of methicillin resistance.
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