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具有抗菌活性和可持续药物释放的含组氨酸两亲性肽非细胞毒性水凝胶形成剂。

Histidine-Containing Amphiphilic Peptide-Based Non-Cytotoxic Hydrogelator with Antibacterial Activity and Sustainable Drug Release.

机构信息

School of Biological Sciences, Indian Association for the Cultivation of Science, Jadavpur, Kolkata 700032, India.

Department of Life Science and Biotechnology, Jadavpur University, Jadavpur, Kolkata 700032, West Bengal, India.

出版信息

Langmuir. 2023 May 30;39(21):7307-7316. doi: 10.1021/acs.langmuir.3c00235. Epub 2023 May 16.

Abstract

A histidine-based amphiphilic peptide () has been found to form an injectable transparent hydrogel in phosphate buffer solution over a pH range from 7.0 to 8.5 with an inherent antibacterial property. It also formed a hydrogel in water at pH = 6.7. The peptide self-assembles into a nanofibrillar network structure which is characterized by high-resolution transmission electron microscopy, field-emission scanning electron microscopy, atomic force microscopy, small-angle X-ray scattering, Fourier-transform infrared spectroscopy, and wide-angle powder X-ray diffraction. The hydrogel exhibits efficient antibacterial activity against both Gram-positive bacteria () and Gram-negative bacteria (). The minimum inhibitory concentration of the hydrogel ranges from 20 to 100 μg/mL. The hydrogel is capable of encapsulation of the drugs naproxen (a non-steroidal anti-inflammatory drug), amoxicillin (an antibiotic), and doxorubicin, (an anticancer drug), but, selectively and sustainably, the gel releases naproxen, 84% being released in 84 h and amoxicillin was released more or less in same manner with that of the naproxen. The hydrogel is biocompatible with HEK 293T cells as well as NIH (mouse fibroblast cell line) cells and thus has potential as a potent antibacterial and drug releasing agent. Another remarkable feature of this hydrogel is its magnification property like a convex lens.

摘要

一种组氨酸基两亲性肽()在 pH 值为 7.0 到 8.5 的磷酸盐缓冲溶液中形成可注射透明水凝胶,具有固有抗菌性能。它在 pH = 6.7 的水中也形成水凝胶。该肽自组装成纳米纤维网络结构,其特点是高分辨率透射电子显微镜、场发射扫描电子显微镜、原子力显微镜、小角 X 射线散射、傅里叶变换红外光谱和广角粉末 X 射线衍射。水凝胶对革兰氏阳性菌()和革兰氏阴性菌()均表现出有效的抗菌活性。水凝胶的最低抑菌浓度范围为 20 至 100 μg/ml。水凝胶能够封装药物萘普生(一种非甾体抗炎药)、阿莫西林(一种抗生素)和阿霉素(一种抗癌药),但能选择性和可持续地释放萘普生,84 小时内释放 84%,阿莫西林的释放方式与萘普生大致相同。水凝胶与 HEK 293T 细胞以及 NIH(小鼠成纤维细胞系)细胞具有生物相容性,因此具有作为一种有效的抗菌和药物释放剂的潜力。这种水凝胶的另一个显著特点是其具有凸透镜的放大特性。

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