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Article

Conjugation of Penicillin-G with Silver(I) Ions Expands Its Antimicrobial Activity against Gram Negative Bacteria

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Inorganic Chemistry laboratory, Department of Chemistry, University of Ioannina, 45110 Ioannina, Greece
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Medical Physics Laboratory, Medical School, University of Ioannina, 45110 Ioannina, Greece
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Laboratory of Analytical Chemistry, Department of Chemistry, University of Ioannina, 45110 Ioannina, Greece
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Department of Physics, University of Ioannina, 45110 Ioannina, Greece
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Physical Chemistry Laboratory, Department of Chemistry, University of Ioannina, 45110 Ioannina, Greece
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Institute of Materials Science and Computing, University Research Center of Ioannina (URCI), 45110 Ioannina, Greece
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Authors to whom correspondence should be addressed.
Received: 25 December 2019 / Revised: 9 January 2020 / Accepted: 10 January 2020 / Published: 13 January 2020
(This article belongs to the Section Novel Antimicrobial Agents)
Conjugation of penicillin G (PenH) with silver(I) ions forms a new CoMeD (conjugate of metal with a drug) with formula [Ag(pen)(CH3OH)]2 (PenAg). PenAg was characterized by a plethora of physical and spectroscopic techniques, which include in the solid state m.p.; elemental analysis; X-ray fluorescence (XRF) spectroscopy; scanning electron microscopy (SEM); energy-dispersive X-ray spectroscopy (EDX); FT-IR; and in solution: attenuated total reflection spectroscopy (FT-IR-ATR), UV–Vis, 1H NMR, and atomic absorption (AA). The structure of PenAg was determined by NMR spectroscopy. Silver(I) ions coordinate to the carboxylic group of PenH, while secondary intra-molecular interactions are developed through (i) the nitrogen atom of the amide group in MeOD-d4 or (ii) the sulfur atom in the thietane ring in deuterated dimethyl sulfoxide DMSO-d6. The antibacterial activities of PenAg and the sodium salt of penicillin (PenNa) (the formulation which is clinically used) against Gram positive (Staphylococcus epidermidis (S. epidermidis) and Staphylococcus aureus (S. aureus)) and Gram negative (Pseudomonas aeruginosa (P. aeuroginosa PAO1)) bacteria were evaluated by the means of minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC), and inhibition zone (IZ). PenAg inhibits the growth of the Gram negative bacterial strain P. aeuroginosa with a MIC value of 23.00 ± 2.29 μM, in contrast to PenNa, which shows no such activity (>2 mM). The corresponding antimicrobial activities of PenAg against the Gram positive bacteria S. epidermidis and S. aureus are even better than those of PenNa. Moreover, PenAg exhibits no in vivo toxicity against Artemia salina at concentration up to 300 μΜ. The wide therapeutic window and the low toxicity, make PenAg a possible candidate for the development of a new antibiotic. View Full-Text
Keywords: biological inorganic chemistry; Diffusion-Ordered NMR Spectroscopy (DOSY-NMR); modified antibiotic; penicillin; antimicrobial activity; toxicity biological inorganic chemistry; Diffusion-Ordered NMR Spectroscopy (DOSY-NMR); modified antibiotic; penicillin; antimicrobial activity; toxicity
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MDPI and ACS Style

Ketikidis, I.; Banti, C.N.; Kourkoumelis, N.; Tsiafoulis, C.G.; Papachristodoulou, C.; Kalampounias, A.G.; Hadjikakou, S.K. Conjugation of Penicillin-G with Silver(I) Ions Expands Its Antimicrobial Activity against Gram Negative Bacteria. Antibiotics 2020, 9, 25. https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics9010025

AMA Style

Ketikidis I, Banti CN, Kourkoumelis N, Tsiafoulis CG, Papachristodoulou C, Kalampounias AG, Hadjikakou SK. Conjugation of Penicillin-G with Silver(I) Ions Expands Its Antimicrobial Activity against Gram Negative Bacteria. Antibiotics. 2020; 9(1):25. https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics9010025

Chicago/Turabian Style

Ketikidis, Ioannis, Christina N. Banti, Nikolaos Kourkoumelis, Constantinos G. Tsiafoulis, Christina Papachristodoulou, Angelos G. Kalampounias, and Sotiris K. Hadjikakou 2020. "Conjugation of Penicillin-G with Silver(I) Ions Expands Its Antimicrobial Activity against Gram Negative Bacteria" Antibiotics 9, no. 1: 25. https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics9010025

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