| Autor: |
Gaur M; Radiation & Photochemistry Division, Bhabha Atomic Research Centre, Mumbai 400085, India.; Homi Bhabha National Institute, Anushaktinagar, Mumbai 400094, India., Marathe AS; Radiation & Photochemistry Division, Bhabha Atomic Research Centre, Mumbai 400085, India., Kakatkar AS; Food Technology Division, Bhabha Atomic Research Centre, Mumbai 400085, India., Barooah N; Radiation & Photochemistry Division, Bhabha Atomic Research Centre, Mumbai 400085, India.; Homi Bhabha National Institute, Anushaktinagar, Mumbai 400094, India., Chatterjee S; Homi Bhabha National Institute, Anushaktinagar, Mumbai 400094, India.; Food Technology Division, Bhabha Atomic Research Centre, Mumbai 400085, India., Bhasikuttan AC; Radiation & Photochemistry Division, Bhabha Atomic Research Centre, Mumbai 400085, India.; Homi Bhabha National Institute, Anushaktinagar, Mumbai 400094, India., Mohanty J; Radiation & Photochemistry Division, Bhabha Atomic Research Centre, Mumbai 400085, India.; Homi Bhabha National Institute, Anushaktinagar, Mumbai 400094, India. |
| Abstrakt: |
Bacterial infection is one of the major concerns of the growing society, and over the years, different permutations and combinations of various drugs and adjuvants have been attempted, which led to considerable improvements in the efficacy of the antibacterial drugs. In this regard, macrocyclic receptors such as cyclodextrin, cucurbiturils, calixarene, etc., have played a major role by modulating the drug properties that supplement the antibacterial efficacy. In this study, we have developed cucurbit[7]uril (CB7)-functionalized Au nanoparticles (CB7AuNPs) to modulate the activity of an antibiotic, levofloxacin (LOFL). From the spectroscopic and thermodynamic changes in the LOFL, it has been established that two of the prototropic forms, LOFLH and LOFLH 2 + , form strong 1:1 host/guest complexes with CB7/CB7AuNP. Both these interactions led to significant upward shifts in the p K a values as well as photostability of LOFL, thereby enhancing the availability of the active form for the antibacterial activity, at the physiological pH. Further, the LOFL uptake has also been established on CB7AuNP, which retained the CB7-LOFL activity at very low concentration of the CB7 host, functionalized on AuNP. Detailed antibacterial studies of LOFL, both as complexed with CB7 and CB7AuNP, were carried out using four food-borne pathogens ( Escherichia coli , S. Typhimurium , Bacillus cereus, and Staphylococcus aureus ), which revealed a creditable enhancement in the antibacterial property, irrespective of the bacterium strain. These results are quite promising at this stage for the development of drugs customized for multidrug-resistant bacteria. |
