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与金纳米颗粒共轭的吖啶衍生物的抗菌功效。

Antibacterial efficacy of acridine derivatives conjugated with gold nanoparticles.

作者信息

Mitra Piyali, Chakraborty Prabal Kumar, Saha Partha, Ray Pulak, Basu Samita

机构信息

Chemical Sciences Division, Saha Institute of Nuclear Physics, 1/AF, Bidhannagar, Kolkata 700064, India.

Crystallography and Molecular Biology Division, Saha Institute of Nuclear Physics, 1/AF, Bidhannagar, Kolkata 700064, India.

出版信息

Int J Pharm. 2014 Oct 1;473(1-2):636-43. doi: 10.1016/j.ijpharm.2014.07.051. Epub 2014 Aug 1.

Abstract

Adsorption of acridine derivatives viz. 9-aminoacridine hydrochloride hydrate (9AA-HCl), acridine yellow (AY), acridine orange (AO), and proflavine (Pro) on citrate stabilized gold nanoparticle surface were studied using different analytical techniques like UV-vis absorption spectroscopy, Fourier transform infrared spectroscopy (FT-IR), and transmission electron microscopy (TEM). The amine moiety of acridine derivative binds strongly to the gold nanoparticles as confirmed by spectroscopic studies. The plasmon band observed for the wine red colloidal gold at 525 nm in the UV-vis spectrum is characteristic of gold nanoparticles. However, with the addition of acridine derivatives the intensity of the absorption band at 525 nm decreases and a new peak emerges at red-end region - a signature of formation of gold-drug complex. The TEM images show the average size of citrate stabilized gold nanoparticles as 15-20 nm, which becomes larger in the presence of various drugs due to aggregation. From the thermogravimetric analyses (TGA) we have measured the number of drug molecules attached per gold nanoparticle (AuNP). These gold nanoparticles are very important as drug delivery vehicles and for clinical applications it is necessary to understand their activity in vivo. The antibacterial efficacy of drugs coated gold nanoparticles were studied against various strains of Gram positive and Gram negative bacteria. Among the four drugs, 9AA-HCl and AO showed antibacterial activity and for both of them the AuNP conjugated drug showed better antibacterial efficacy than the bare drug. Because of the high penetrating power and large surface area of Au(0), a single gold nanoparticle can adsorb multiple drug molecules, hence this total entity acts as a single group against the bacteria.

摘要

研究了吖啶衍生物,即9-氨基吖啶盐酸盐水合物(9AA-HCl)、吖啶黄(AY)、吖啶橙(AO)和普罗黄素(Pro)在柠檬酸盐稳定的金纳米颗粒表面的吸附情况,采用了紫外可见吸收光谱、傅里叶变换红外光谱(FT-IR)和透射电子显微镜(TEM)等不同分析技术。光谱研究证实,吖啶衍生物的胺部分与金纳米颗粒强烈结合。在紫外可见光谱中,525nm处观察到的酒红色胶体金的等离子体带是金纳米颗粒的特征。然而,随着吖啶衍生物的加入,525nm处吸收带的强度降低,并且在红色末端区域出现一个新峰——这是金-药物复合物形成的标志。TEM图像显示柠檬酸盐稳定的金纳米颗粒的平均尺寸为15-20nm,在存在各种药物的情况下,由于聚集,尺寸会变大。通过热重分析(TGA),我们测量了每个金纳米颗粒(AuNP)附着的药物分子数量。这些金纳米颗粒作为药物递送载体非常重要,对于临床应用来说,了解它们在体内的活性很有必要。研究了药物包覆的金纳米颗粒对各种革兰氏阳性和革兰氏阴性细菌菌株的抗菌效果。在这四种药物中,9AA-HCl和AO表现出抗菌活性,并且对于它们两者,AuNP偶联药物的抗菌效果都比裸药更好。由于Au(0)的高穿透力和大表面积,单个金纳米颗粒可以吸附多个药物分子,因此这个整体实体作为一个单一的基团对抗细菌。

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