Abstract
BackgroundPolyprenol is an important lipid with many bioactive effects. The study on differences in bioactive effects of polyprenol derivatives having different isoprene units are seldom reported and it is helpful to find out which type of polyprenol derivatives are effective for treating A549/HepG2 cells and E. coli /S. aureus.MethodsAll tested polyprenol derivatives were measured with inhibition halos by Oxford cup assays. MIC values were assessed by the broth dilution method. Time-killing curve studies were conducted in duplicate on separate days. Cytotoxicity study was measured by the MTT assay and genotoxic study was evaluated by comet assay.ResultsWith regard to antibacterial activity, the sensitivities to the quaternary polyprenyl ammonium salt derivatives GAS and MAS were 31.3 μg/mL and 15.6–31.3 μg/mL, respectively. GAS and MAS exhibited cytotoxic activity toward HepG2 cells (IC50 of 10.1–11.6 μg/mL), which was stronger than that exhibited toward A549 cells (IC50 of 13.8–13.9 μg/mL). The bactericidal activity of MAS was stronger than that of GAS at the same concentration at least 48 h. The DNA damage in A549 and HepG2 cells exposed to all 10, 20 and 40 μg/mL MAS was statistically significant in comparison to the control. Our results indicate a dose-dependent increment in DNA damage in A549 and HepG2 cells exposed to 10, 20 and 40 μg/mL MAS for both the percentage of DNA in the tail and tail moment.ConclusionThe quaternary ammonium salt derivatives GAS and MAS exhibited higher antibacterial (E. coli and S. aureus) and cytotoxic activity (A549 and HepG2 cells) than the other derivatives evaluated in this study. The DNA damage in HepG2 cells suggests that MAS induced A549 and HepG2 cells death via apoptotic pathway. Our results provide new evidence supporting the medical use of polyprenol derivatives against bacterial and tumor diseases.
Highlights
Polyprenol is an important lipid with many bioactive effects
Good antibacterial activity against both gram-negative and grampositive bacteria (MIC 6.25–25.0 mg/mL and MBC 12.50–25.0 mg/mL) has been demonstrated in vitro by polyprenols isolated from the leaves of Kirganelia reticulate [9], and we previously reported minimum inhibitory concentration (MIC) values of 31.3 μg/mL and MBC and MFC values of 125 μg/mL for GBP [1]
Antibacterial activity The antibacterial activities of GPH, MPH, GAM, MAM, GAS, MAS, GTF, MTF, GCH and MCH against E. coli and S. aureus were assessed at 500 μg/mL, and their potency was quantitatively assessed based on inhibition halos (Table 1) and MIC values (Table 2)
Summary
Polyprenol is an important lipid with many bioactive effects. The study on differences in bioactive effects of polyprenol derivatives having different isoprene units are seldom reported and it is helpful to find out which type of polyprenol derivatives are effective for treating A549/HepG2 cells and E. coli /S. aureus. Ginkgo biloba (Ginkgoopsida, Ginkgoales, Ginkgoaceae, Ginkgo bilobaL.) leaf polyprenol (GBP) and Morus alba (Dicotyledoneae, Rosales, Moraceae, Morus L.) leaf polyprenol (MBP) are long-chain polyisoprenoid alcohols. These molecules are typically composed of a number of unsaturated isoprene units; they are a type of betulaprenol with an E, E-farnesyl residue at the ω-end of the. Our recent study of five GBP derivatives—polyprenyl acetate (GPA), n-amyl polypentylene (GAP), polyprenyl-3-isoamyl benzyl ether (GPB), polyprenyl dichlorophosphite (GPD) and polyprenyl phosphate disodium salt (GPP) - synthesized from GBPs (C70–C120) suggested a decrease in the antibacterial/antifungal activities and synergistic effect of alkyl-substituted GBP derivatives; an increase was observed with a phosphate-substituted GBP derivative [10]. As phosphorylated polyprenols generally possess higher activity than free polyprenols, studying polyprenyl and dolichyl phosphate analogs modified at the anionic group is of substantial interest, with regard to comparisons of their biological activities [11]
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