Chair and Department of Biochemistry and Biotechnology, Medical University of Lublin, Chodzki 1 Street, 20-093 Lublin, Poland.
Department of Chemistry, University of Warsaw, Pasteura 1 Street, 02-093 Warsaw, Poland.
Molecules. 2022 Jul 7;27(14):4366. doi: 10.3390/molecules27144366.
This study aimed to develop, characterize, and evaluate antibacterial and cytotoxic properties of novel fullerene derivative composed of C fullerenol and standard aminoglycoside antibiotic-gentamicin (C fullerenol-gentamicin conjugate). The successful introduction of gentamicin to fullerenol was confirmed by X-ray photoelectron spectroscopy which together with thermogravimetric and spectroscopic analysis revealing the formula of the composition as C(OH)(GLYMO)(Gentamicin). The dynamic light scattering (DLS) revealed that conjugate possessed ability to form agglomerates in water (size around 115 nm), while Zeta potential measurements demonstrated that such agglomerates possessed neutral character. In vitro biological assays indicated that obtained C fullerenol-gentamicin conjugate possessed the same antibacterial activity as standard gentamicin against , , , and , which proves that combination of fullerenol with gentamicin does not cause the loss of antibacterial activity of antibiotic. Moreover, cytotoxicity assessment demonstrated that obtained fullerenol-gentamicin derivative did not decrease viability of normal human fibroblasts (model eukaryotic cells) compared to control fibroblasts. Thus, taking into account all of the results, it can be stated that this research presents effective method to fabricate C fullerenol-gentamicin conjugate and proves that such derivative possesses desired antibacterial properties without unfavorable cytotoxic effects towards eukaryotic cells in vitro. These promising preliminary results indicate that obtained C fullerenol-gentamicin conjugate could have biomedical potential. It may be presumed that obtained fullerenol may be used as an effective carrier for antibiotic, and developed fullerenol-gentamicin conjugate may be apply locally (i.e., at the wound site). Moreover, in future we will evaluate possibility of its applications in tissue engineering, namely as a component of wound dressings and implantable biomaterials.
本研究旨在开发、表征和评估新型富勒烯衍生物的抗菌和细胞毒性特性，该衍生物由 C 富勒醇和标准氨基糖苷类抗生素-庆大霉素组成（C 富勒醇-庆大霉素缀合物）。X 射线光电子能谱证实了庆大霉素成功引入富勒醇，热重和光谱分析表明其组成为 C(OH)(GLYMO)(庆大霉素)。动态光散射（DLS）表明，该缀合物在水中具有形成聚集体的能力（大小约为 115nm），而 Zeta 电位测量表明，这些聚集体具有中性特征。体外生物测定表明，所获得的 C 富勒醇-庆大霉素缀合物对 、 、 、 和 具有与标准庆大霉素相同的抗菌活性，这证明富勒醇与庆大霉素的结合不会导致抗生素抗菌活性的丧失。此外，细胞毒性评估表明，与对照成纤维细胞相比，所获得的富勒醇-庆大霉素衍生物并未降低正常人类成纤维细胞（模型真核细胞）的活力。因此，考虑到所有结果，可以说本研究提出了一种有效的方法来制备 C 富勒醇-庆大霉素缀合物，并证明了该衍生物具有所需的抗菌特性，而对真核细胞无不利的细胞毒性作用。这些有希望的初步结果表明，所获得的 C 富勒醇-庆大霉素缀合物可能具有生物医学潜力。可以推测，所获得的富勒醇可用作抗生素的有效载体，所开发的富勒醇-庆大霉素缀合物可局部应用（即在伤口部位）。此外，在未来，我们将评估其在组织工程中的应用可能性，即作为伤口敷料和可植入生物材料的组成部分。
