Khatri Samreen, Das Nandita G, Das Sudip K
Department of Pharmaceutical Sciences, Butler University, Indianapolis, IN 46208, USA.
J Pharm Bioallied Sci. 2014 Oct;6(4):297-302. doi: 10.4103/0975-7406.142963.
The aim of this work was to synthesize methotrexate (MTX)-polyamidoamine (PAMAM) dendritic nanoconjugates and to study their effect on cell viability in uterine sarcoma cells. The amide-bonded PAMAM dendrimer-MTX conjugates were prepared by conjugation between the amine-terminated G5 dendrimer and the carboxylic groups of the MTX using a dicyclohexylcarbodiimide coupling reaction. The formation of conjugates was evaluated by ultraviolet (UV) and (1)H nuclear magnetic resonance ((1)H NMR) spectroscopy studies. The cell survival of MES-SA cells, a uterine sarcoma cell line, was evaluated in the presence of the dendrimer-MTX nanoconjugate, using appropriate controls. The UV and (1)H NMR study confirmed the formation of covalent bonds between the drug and the dendrimer. The cell viability study indicated that the nanoconjugates had significantly improved cell killing compared to the free MTX.
这项工作的目的是合成甲氨蝶呤(MTX)-聚酰胺胺(PAMAM)树枝状纳米缀合物,并研究它们对子宫肉瘤细胞活力的影响。通过二环己基碳二亚胺偶联反应,使胺端基G5树枝状大分子与MTX的羧基之间进行共轭反应,制备出酰胺键合的PAMAM树枝状大分子-MTX缀合物。通过紫外(UV)和氢核磁共振(¹H NMR)光谱研究对缀合物的形成进行了评估。在存在树枝状大分子-MTX纳米缀合物的情况下,使用适当的对照评估了子宫肉瘤细胞系MES-SA细胞的存活率。UV和¹H NMR研究证实了药物与树枝状大分子之间形成了共价键。细胞活力研究表明,与游离MTX相比,纳米缀合物的细胞杀伤能力有显著提高。
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