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Bactericidal and cytotoxic activity of a diarylheptanoid (etlingerin) isolated from a ginger (Etlingera pubescens) endemic to Borneo

Daniel‐Jambun, D., Ong, K.S., Lim, Y.Y., Tan, J.B.L., Yap, S.W., Lee, S.M.
Journal of applied microbiology 2019 v.127 no.1 pp. 59-67
Bacillus subtilis, Etlingera pubescens, Gram-positive bacteria, Staphylococcus aureus, acetates, animal models, anti-infective agents, antimicrobial properties, bacterial infections, cell lines, chemical structure, curcumin, cytotoxicity, ginger, humans, inhibitory concentration 50, membrane permeability, methanol, minimum inhibitory concentration, Borneo
AIMS: The aim of this study was to investigate the antimicrobial activities of Etlingera pubescens, and to isolate and identify the antimicrobial compound. METHODS AND RESULTS: The crude extracts of E. pubescens were obtained through methanol extraction, and evaluated for antimicrobial activities. From this extract, 1,7‐bis(3,4‐dihydroxyphenyl)heptan‐3‐yl acetate (etlingerin) was isolated. When compared to curcumin (a compound with a similar chemical structure), etlingerin showed twofold lower minimum inhibitory concentration values while also being bactericidal. Through time kill assay, etlingerin showed rapid killing effects (as fast as 60 min) against the Gram‐positive bacteria (Staphylococcus aureus ATCC 43300 and Bacillus subtilis ATCC 8188). Further assessment revealed that etlingerin caused leakage of intracellular materials, therefore suggesting alteration in membrane permeability as its antimicrobial mechanism. Cytotoxicity study demonstrated that etlingerin exhibited approximately 5‐ to 12‐fold higher IC₅₀ values against several cell lines, as compared to curcumin. CONCLUSIONS: Etlingerin isolated from E. pubescens showed better antibacterial and cytotoxic activities when compared to curcumin. Etlingerin could be safe for human use, though further cytotoxicity study using animal models is needed. SIGNIFICANCE AND IMPACT OF THE STUDY: Etlingerin has a potential to be used in treating bacterial infections due to its good antimicrobial activity, while having potentially low cytotoxicity.