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Investigation of the antimicrobial and anticancer activity of aminonaphthoquinones

2018; Wiley; Volume: 80; Issue: 1 Linguagem: Inglês

10.1002/ddr.21477

1098-2299

Kevin W. Wellington, Natasha I. Kolesnikova, Nomgqibelo B. P. Nyoka, Lyndy J. McGaw,

Synthesis and biological activity

Abstract In this study, we report on the inhibitory activity of synthesized aminonaphthoquinones against two bacterial and one fungal species to determine their antimicrobial properties. A minimum inhibitory concentration (MIC) of 7.8 μg/mL was obtained against the fungus, Candida albicans , which was better than that of Amphotericin B (MIC = 31.25 μg/mL). Escherichia coli (Gram ‐), was inhibited at a MIC of 23.4 μg/mL and Staphylococcus aureus (Gram +) at a MIC of 31.3 μg/mL. The aminonaphthoquinones were also screened against HCT116 colon, PC3 prostate and HepG2 liver cancer cell lines to evaluate their cytostatic effects. They had potent activity (GI 50 = 5.87–9.90 μM) which was about three‐6‐fold better than that of parthenolide (GI 50 = 25.97 μM) against the prostate cancer cell line. These compounds were generally more selective for cancer cells than for normal human lung fetal fibroblasts (WI‐38).