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通过转化为碳量子点来提高姜黄素的抗病毒活性。

High Amplification of the Antiviral Activity of Curcumin through Transformation into Carbon Quantum Dots.

机构信息

Department of Bioscience and Biotechnology, National Taiwan Ocean University, Keelung, 20224, Taiwan.

Institute of Microbiology and Immunology, National Yang-Ming University, Taipei, 11221, Taiwan.

出版信息

Small. 2019 Oct;15(41):e1902641. doi: 10.1002/smll.201902641. Epub 2019 Aug 29.

DOI:10.1002/smll.201902641
PMID:31468672
Abstract

It is demonstrated that carbon quantum dots derived from curcumin (Cur-CQDs) through one-step dry heating are effective antiviral agents against enterovirus 71 (EV71). The surface properties of Cur-CQDs, as well as their antiviral activity, are highly dependent on the heating temperature during synthesis. The one-step heating of curcumin at 180 °C preserves many of the moieties of polymeric curcumin on the surfaces of the as-synthesized Cur-CQDs, resulting in superior antiviral characteristics. It is proposed that curcumin undergoes a series of structural changes through dehydration, polymerization, and carbonization to form core-shell CQDs whose surfaces remain a pyrolytic curcumin-like polymer, boosting the antiviral activity. The results reveal that curcumin possesses insignificant inhibitory activity against EV71 infection in RD cells [half-maximal effective concentration (EC ) >200 µg mL ] but exhibits high cytotoxicity toward RD cells (half-maximal cytotoxic concentration (CC ) <13 µg mL ). The EC (0.2 µg mL ) and CC (452.2 µg mL ) of Cur-CQDs are >1000-fold lower and >34-fold higher, respectively, than those of curcumin, demonstrating their far superior antiviral capabilities and high biocompatibility. In vivo, intraperitoneal administration of Cur-CQDs significantly decreases mortality and provides protection against virus-induced hind-limb paralysis in new-born mice challenged with a lethal dose of EV71.

摘要

研究表明,通过一步干法加热从姜黄素中得到的碳量子点(Cur-CQDs)是一种有效的抗肠道病毒 71 型(EV71)的抗病毒药物。Cur-CQDs 的表面性质及其抗病毒活性高度依赖于合成过程中的加热温度。姜黄素在 180°C 的一步加热保留了合成的 Cur-CQDs 表面上聚合姜黄素的许多部分,从而具有优异的抗病毒特性。据推测,姜黄素通过脱水、聚合和碳化经历了一系列的结构变化,形成了核壳结构的 CQDs,其表面仍然是热解姜黄素样聚合物,从而提高了抗病毒活性。结果表明,姜黄素对 RD 细胞中的 EV71 感染几乎没有抑制活性(半数有效浓度(EC )>200μg mL ),但对 RD 细胞具有很高的细胞毒性(半数细胞毒性浓度(CC )<13μg mL )。Cur-CQDs 的 EC (0.2μg mL )和 CC (452.2μg mL )分别比姜黄素低 1000 多倍和高 34 倍,这表明它们具有优异的抗病毒能力和良好的生物相容性。在体内,腹腔注射 Cur-CQDs 可显著降低死亡率,并为新生小鼠提供保护,使其免受致死剂量 EV71 感染引起的后肢瘫痪。

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