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Article

Flavonoid-Coated Gold Nanoparticles as Efficient Antibiotics against Gram-Negative Bacteria—Evidence from In Silico-Supported In Vitro Studies

1
Department of Medical Laboratory Technology, Faculty of Applied Medical Sciences, King Abdulaziz University, Jeddah 21589, Saudi Arabia
2
Molecular Diagnostic Lab, King Abdulaziz University Hospital, King Abdulaziz University, Jeddah 21589, Saudi Arabia
3
Special Infectious Agent Unit, King Fahd Medical Research Centre, King Abdulaziz University, Jeddah 21589, Saudi Arabia
4
Department of Pharmacognosy, College of Pharmacy, King Saud University, Riyadh 11495, Saudi Arabia
5
National Research Centre, Microbial Chemistry Department, 33 El-Buhouth Street, Dokki, Giza P.O. Box 12622, Egypt
6
Department of Pharmacy Practice, College of Pharmacy, AlMaarefa University, Riyadh 13713, Saudi Arabia
7
Department of Pharmacognosy, Faculty of Pharmacy, Nahda University, Beni-Suef 62513, Egypt
8
Department of Pharmacognosy, Faculty of Pharmacy, Beni-Suef University, Beni-Suef 62513, Egypt
9
School of Computing, Engineering & Physical Sciences, University of the West of Scotland, Paisley PA1 2BE, UK
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Aberdeen Royal Infirmary, Foresterhill Health Campus, Foresterhill Road, Aberdeen AB25 2NZ, UK
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Department of Microbiology, Faculty of Pharmacy, The British University in Egypt (BUE), Cairo 11837, Egypt
*
Authors to whom correspondence should be addressed.
These authors equally contributed to this work.
Academic Editors: Anthony William Coleman and Helena Felgueiras
Received: 2 July 2021 / Revised: 7 August 2021 / Accepted: 9 August 2021 / Published: 12 August 2021
Flavonoids are a class of bioactive plant-derived natural products that exhibit a broad range of biological activities, including antibacterial ones. Their inhibitory activity toward Gram-positive bacterial was found to be superior to that against Gram-negative ones. In the present study, a number of flavonoid-coated gold nanoparticles (GNPs) were designed to enhance the antibacterial effects of chrysin, kaempferol, and quercetin against a number of Gram-negative bacteria. The prepared GNPs were able to conjugate to these three flavonoids with conjugation efficiency ranging from 41% to 80%. Additionally, they were able to exert an enhanced antibacterial activity in comparison with the free flavonoids and the unconjugated GNPs. Quercetin-coated GNPs were the most active nano-conjugates and were able to penetrate the cell wall of E. coli. A number of in silico experiments were carried out to explain the conjugation efficiency and the antibacterial mechanisms of these flavonoids as follows: (i) these flavonoids can efficiently bind to the glutathione linker on the surface of GNPs via H-bonding; (ii) these flavonoids, particularly quercetin, were able to increase the bacterial membrane rigidity, and hence decrease its functionality; (iii) these flavonoids can inhibit E. coli’s DNA gyrase (Gyr-B) with IC50 values ranging from 0.9 to 3.9 µM. In conclusion, these bioactive flavonoid-based GNPs are considered to be very promising antibiotic candidates for further development and evaluation. View Full-Text
Keywords: gold nanoparticles; flavonoids; Gram-negative bacteria; DNA gyrase; in silico gold nanoparticles; flavonoids; Gram-negative bacteria; DNA gyrase; in silico
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MDPI and ACS Style

Alhadrami, H.A.; Orfali, R.; Hamed, A.A.; Ghoneim, M.M.; Hassan, H.M.; Hassane, A.S.I.; Rateb, M.E.; Sayed, A.M.; Gamaleldin, N.M. Flavonoid-Coated Gold Nanoparticles as Efficient Antibiotics against Gram-Negative Bacteria—Evidence from In Silico-Supported In Vitro Studies. Antibiotics 2021, 10, 968. https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics10080968

AMA Style

Alhadrami HA, Orfali R, Hamed AA, Ghoneim MM, Hassan HM, Hassane ASI, Rateb ME, Sayed AM, Gamaleldin NM. Flavonoid-Coated Gold Nanoparticles as Efficient Antibiotics against Gram-Negative Bacteria—Evidence from In Silico-Supported In Vitro Studies. Antibiotics. 2021; 10(8):968. https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics10080968

Chicago/Turabian Style

Alhadrami, Hani A., Raha Orfali, Ahmed A. Hamed, Mohammed M. Ghoneim, Hossam M. Hassan, Ahmed S.I. Hassane, Mostafa E. Rateb, Ahmed M. Sayed, and Noha M. Gamaleldin 2021. "Flavonoid-Coated Gold Nanoparticles as Efficient Antibiotics against Gram-Negative Bacteria—Evidence from In Silico-Supported In Vitro Studies" Antibiotics 10, no. 8: 968. https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics10080968

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