经最优生物合成、聚乙二醇化的金纳米粒子经槲皮素和喜树碱功能化后，增强了潜在的抗炎、抗癌和抗血管生成活性。
Optimally biosynthesized, PEGylated gold nanoparticles functionalized with quercetin and camptothecin enhance potential anti-inflammatory, anti-cancer and anti-angiogenic activities.
机构信息
School of Nanoscience and Biotechnology, Shivaji University, Kolhapur, Maharashtra, India.
Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Coimbra, Coimbra, Portugal.
出版信息
J Nanobiotechnology. 2021 Mar 25;19(1):84. doi: 10.1186/s12951-021-00836-1.
BACKGROUND
The development of nano delivery systems is rapidly emerging area of nanotechnology applications where nanomaterials (NMs) are employed to deliver therapeutic agents to specific site in a controlled manner. To accomplish this, green synthesis of NMs is widely explored as an eco-friendly method for the development of smart drug delivery system. In the recent times, use of green synthesized NMs, especially metallic NMs have fascinated the scientific community as they are excellent carriers for drugs. This work demonstrates optimized green, biogenic synthesis of gold nanoparticles (AuNPs) for functionalization with quercetin (QT) and camptothecin (CPT) to enhance potential anti-inflammatory, anti-cancer and anti-angiogenic activities of these drugs.
RESULTS
Gold nanoparticles were optimally synthesized in 8 min of reaction at 90 °C, pH 6, using 4 mM of HAuCl and 4:1 ratio of extract: HAuCl. Among different capping agents tested, capping of AuNPs with polyethylene glycol 9000 (PG9) was found best suited prior to functionalization. PG9 capped AuNPs were optimally functionalized with QT in 1 h reaction at 70 °C, pH 7, using 1200 ppm of QT and 1:4 ratio of AuNPs-PG9:QT whereas, CPT was best functionalized at RT in 1 h, pH 12, AuNPs-PG9:CPT ratio of 1:1, and 0.5 mM of CPT. QT functionalized AuNPs showed good anti-cancer activity (IC 687.44 µg/mL) against MCF-7 cell line whereas test of anti-inflammatory activity also showed excellent activity (IC 287.177 mg/L). The CAM based assessment of anti-angiogenic activity of CPT functionalized AuNPs demonstrated the inhibition of blood vessel branching confirming the anti-angiogenic effect.
CONCLUSIONS
Thus, present study demonstrates that optimally synthesized biogenic AuNPs are best suited for the functionalization with drugs such as QT and CPT. The functionalization of these drugs with biogenic AuNPs enhances the potential anti-inflammatory, anti-cancer and anti-angiogenic activities of these drugs, therefore can be used in biomedical application.
背景
纳米递药系统的发展是纳米技术应用中一个迅速兴起的领域，其中纳米材料（NMs）被用于以受控的方式将治疗剂递送到特定部位。为了实现这一目标，广泛探索了绿色合成纳米材料作为开发智能药物递送系统的环保方法。在最近的时间里，使用绿色合成的纳米材料，特别是金属纳米材料，引起了科学界的关注，因为它们是药物的优秀载体。这项工作展示了优化的绿色、生物合成金纳米粒子（AuNPs），用于与槲皮素（QT）和喜树碱（CPT）进行功能化，以增强这些药物的潜在抗炎、抗癌和抗血管生成活性。
结果
在 90°C、pH 6 的条件下，使用 4mM 的 HAuCl 和提取物：HAuCl 的 4:1 比例，反应 8 分钟，最优地合成了金纳米粒子。在所测试的不同封端剂中，发现用聚乙二醇 9000（PG9）封端 AuNPs 最适合于功能化之前。PG9 封端的 AuNPs 在 70°C、pH 7 的条件下，以 1200ppm 的 QT 和 AuNPs-PG9:QT 的 1:4 比例，最优地在 1 小时内与 QT 进行功能化，而 CPT 则在 RT 下以 AuNPs-PG9:CPT 的 1:1 比例和 0.5mM 的 CPT 在 1 小时内最佳地进行功能化。QT 功能化的 AuNPs 对 MCF-7 细胞系表现出良好的抗癌活性（IC 687.44µg/mL），而抗炎活性测试也表现出极好的活性（IC 287.177mg/L）。基于 CAM 的 CPT 功能化 AuNPs 的抗血管生成活性评估表明，血管分支的抑制证实了其抗血管生成作用。
结论
因此，本研究表明，最优合成的生物合成 AuNPs 最适合与 QT 和 CPT 等药物进行功能化。这些药物与生物合成的 AuNPs 进行功能化增强了这些药物的潜在抗炎、抗癌和抗血管生成活性，因此可用于生物医学应用。
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