Cytotoxic and antibacterial activities of the analogues of pogostone

Abstract

Six new (A5-A6, A8-A11) and six known (A1-A4, A7, PO) α-pyrone compounds were synthesized with dehydroacetate and aldehydes in tetrahydrofuran at room temperature. And their structures were determined by 1H-NMR, 13C-NMR and mass spectroscopy. In the bioscreening experiments, ten compounds (A1-A5, PO, A7-A10) exhibited antibacterial activities against Staphylococcus aureus ATCC 25923 with minimum inhibitory concentration (MIC) values of 4–512mg/L, and nine compounds (A1-A5, PO, A7–A8, A10) exhibited antibacterial activities against Methicillin-resistant S. aureus (MRSA) ATCC 43300 with MIC values of 4–256mg/L. Moreover, compound A10 showed the highest antibacterial activity against S. aureus ATCC 25923 and MRSA with MIC values of 4mg/L, while the MIC values of Amoxicillin were 8mg/L and >256mg/L, respectively. Two compounds (A8 and PO) exhibited antibacterial activities against Escherichia coli ATCC 25922 with MIC values of 32–512mg/L. However, only one compound (A8) exhibited significant antibacterial activity against Pseudomonas aeruginosa CVCC 3360 with MIC value of 256mg/L. Moreover, A10 exhibited significant inhibition of proliferation in the four cell lines MCF-10, A549, A2780 and MFC, and showed stronger inhibitive activity of these four selected cell lines than cisplatin in the cytotoxic assay. Thus, this study suggests that pogostone analogues, especially A10, represented a kind of promising antibacterial and antineoplastic agents.