Department of Chemical Sciences, University of Johannesburg, P. O. Box 17011, Doornfontein, 2028, Johannesburg, South Africa.
Centre for Nanomaterials Science Research, University of Johannesburg, Johannesburg, South Africa.
Sci Rep. 2020 Mar 18;10(1):4936. doi: 10.1038/s41598-020-61881-8.
The toxicity of heavy metals present in binary semiconductor nanoparticles also known as quantum dots (QDs) has hindered their wide applications hence the advent of non-toxic ternary quantum dots. These new group of quantum dots have been shown to possess some therapeutic action against cancer cell lines but not significant enough to be referred to as an ideal therapeutic agent. In this report, we address this problem by conjugating red emitting CuInS/ZnS QDs to a 5,10,15,20-tetrakis(3-hydroxyphenyl)porphyrin -photosensitizer for improved bioactivities. The glutathione capped CuInS/ZnS QDs were synthesized in an aqueous medium using a kitchen pressure cooker at different Cu: In ratios (1:4 and 1:8) and at varied temperatures (95 °C, 190 °C and 235 °C). Optical properties show that the as-synthesized CuInS/ZnS QDs become red-shifted compared to the core (CuInS) after passivation with emission in the red region while the cytotoxicity study revealed excellent cell viability against normal kidney fibroblasts (BHK21). The highly fluorescent, water-soluble QDs were conjugated to 5,10,15,20-tetrakis(3-hydroxyphenyl)porphyrin (mTHPP) via esterification reactions at room temperature. The resultant water-soluble conjugate was then used for the cytotoxicity, fluorescent imaging and gene expression study against human monocytic leukemia cells (THP-1). Our result showed that the conjugate possessed high cytotoxicity against THP-1 cells with enhanced localized cell uptake compared to the bare QDs. In addition, the gene expression study revealed that the conjugate induced inflammation compared to the QDs as NFKB gene was over-expressed upon cell inflammation while the singlet oxygen (O) study showed the conjugate possessed large amount of O, three times than the bare porphyrin. Thus, the as-synthesized conjugate looks promising as a therapeutic agent for cancer therapy.
二元半导体纳米粒子(也称为量子点,QDs)中存在的重金属的毒性阻碍了它们的广泛应用,因此无毒的三元量子点应运而生。这些新的量子点已被证明对癌细胞系具有一定的治疗作用,但还不够显著,不能称之为理想的治疗剂。在本报告中,我们通过将红色发射的 CuInS/ZnS QD 与 5,10,15,20-四(3-羟基苯基)卟啉 - 光敏剂缀合来解决这个问题,以提高生物活性。谷胱甘肽封端的 CuInS/ZnS QD 是在不同的 Cu:In 比(1:4 和 1:8)和不同温度(95°C、190°C 和 235°C)下,在水介质中使用厨房压力釜合成的。光学性质表明,与核心(CuInS)相比,合成的 CuInS/ZnS QD 在经过红色区域发射的钝化后发生红移,而细胞毒性研究表明对正常肾成纤维细胞(BHK21)具有优异的细胞活力。高荧光、水溶性 QD 通过酯化反应在室温下与 5,10,15,20-四(3-羟基苯基)卟啉(mTHPP)缀合。然后将所得水溶性缀合物用于细胞毒性、荧光成像和基因表达研究,以对抗人单核细胞白血病细胞(THP-1)。我们的结果表明,与裸 QD 相比,该缀合物对 THP-1 细胞具有高细胞毒性,并且具有增强的局部细胞摄取。此外,基因表达研究表明,与 QD 相比,该缀合物诱导了炎症,因为 NFKB 基因在细胞炎症时过度表达,而单线态氧(O)研究表明,该缀合物具有大量的 O,是裸卟啉的三倍。因此,所合成的缀合物有望成为癌症治疗的治疗剂。