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载丹酚酸 B 磷脂复合物纳米粒在头颈癌细胞及癌前病变细胞中的细胞摄取及抗癌活性。

Cellular uptake and anticancer activity of salvianolic acid B phospholipid complex loaded nanoparticles in head and neck cancer and precancer cells.

机构信息

Department of Oral Mucosal Diseases, Ninth People's Hospital, Shanghai Key Laboratory of Stomatology, Shanghai Jiao Tong University School of Medicine, Shanghai 200011, China.

Department of Oral & Maxillofacial-Head & Neck Oncology, Ninth People's Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai 200011, China.

出版信息

Colloids Surf B Biointerfaces. 2016 Nov 1;147:65-72. doi: 10.1016/j.colsurfb.2016.07.053. Epub 2016 Jul 28.

Abstract

Salvianolic acid B (SalB) was demonstrated to be a promising chemopreventive agent for head and neck squamous cell carcinoma (HNSCC) in the previous studies by our and other research institution, but the properties like low efficacy, poor systemic delivery, and low bioavailability has hampered its clinical applications. To continue our research program focused on the use of natural compounds on cancer chemoprevention, we propose a first example of phospholipid complex loaded nanoparticles (PLC-NPs) encapsulating SalB as a potential carrier for intervention of HNSCC (HN13, HN30) cells and precancer Leuk1 cells in this study. Qualitative and quantitive studies of cellular uptake showed that intracellular accumulation of SalB was significantly higher when HN13, HN30 and Leuk1 cells were incubated with SalB-PLC-NPs complex (nano-SalB) as against free-SalB. Cell viability assay revealed that the cell growth of HN13 and HN30 cells was significantly inhibited of 56.1% and 29.3%, respectively, for nano-SalB compared to an equivalent amount of free-SalB (P<0.001). Moreover, cell cycle and apoptosis assay showed that a clear trend of cell cycle arrest and induction of apoptosis was also observed within the HNSCC cells treated with nano-SalB. Collectively, this study demonstrated that nano-SalB was significantly more potent had an anticancer effect against HNSCC cells, which serves as the first step toward establishing SalB nano-formulations as promising cancer chemopreventive agents. The current study could pave a new way for the development of drugs that target HNSCC in the future.

摘要

丹酚酸 B(SalB)先前的研究表明,它是一种很有前途的头颈部鳞状细胞癌(HNSCC)化学预防剂,但由于其疗效低、系统传递差和生物利用度低等特性,限制了其临床应用。为了继续我们专注于使用天然化合物进行癌症化学预防的研究计划,我们提出了第一个磷脂复合物负载纳米颗粒(PLC-NPs)包裹 SalB 的例子,作为干预 HNSCC(HN13、HN30)细胞和癌前 Leuk1 细胞的潜在载体。细胞摄取的定性和定量研究表明,当 HN13、HN30 和 Leuk1 细胞用 SalB-PLC-NPs 复合物(纳米 SalB)孵育时,SalB 的细胞内积累明显更高。细胞活力测定显示,与等量的游离 SalB 相比,HN13 和 HN30 细胞的细胞生长分别显著抑制了 56.1%和 29.3%(P<0.001)。此外,细胞周期和凋亡测定表明,在接受纳米 SalB 治疗的 HNSCC 细胞中也观察到细胞周期阻滞和凋亡诱导的明显趋势。总之,这项研究表明,纳米 SalB 对 HNSCC 细胞具有更强的抗癌作用,这是将 SalB 纳米制剂作为有前途的癌症化学预防剂建立的第一步。本研究为未来针对 HNSCC 的药物开发开辟了新的途径。

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