Discipline of Pharmacy, Graduate School of Health, University of Technology Sydney, Sydney, NSW, Australia.
Centre for Inflammation, Centenary Institute, Sydney, NSW, Australia.
J Food Biochem. 2021 Jan;45(1):e13572. doi: 10.1111/jfbc.13572. Epub 2020 Nov 29.
In this study, we had developed Naringenin-loaded liquid crystalline nanoparticles (LCNs) and investigated the anti-inflammatory and anticancer activities of Naringenin-LCNs against human airway epithelium-derived basal cells (BCi-NS1.1) and human lung epithelial carcinoma (A549) cell lines, respectively. The anti-inflammatory potential of Naringenin-LCNs evaluated by qPCR revealed a decreased expression of IL-6, IL-8, IL-1β, and TNF-α in lipopolysaccharide-induced BCi-NS1.1 cells. The activity of LCNs was comparable to the positive control drug Fluticasone propionate (10 nM). The anticancer activity was studied by evaluating the antiproliferative (MTT and trypan blue assays), antimigratory (scratch wound healing assay, modified Boyden chamber assay, and immunoblot), and anticolony formation activity in A549 cells. Naringenin LCNs showed promising antiproliferative, antimigratory, and anticolony formation activities in A549 cells, in vitro. Therefore, based on our observations and results, we conclude that Naringenin-LCNs may be employed as a potential therapy-based intervention to ameliorate airway inflammation and to inhibit the progression of lung cancer. PRACTICAL APPLICATIONS: Naringenin was encapsulated into liquid crystalline nanoparticles, thus, attributing to their sustained-release nature. In addition, Naringenin-loaded LCNs efficiently reduced the levels of pro-inflammatory markers, namely, IL-1β, IL-6, TNF-α, and IL-8. In addition, the Naringenin-loaded LCNs also possess potent anticancer activity, when tested in the A549 cell line, as revealed by the inhibition of proliferation and migration of cells. They also attenuated colony formation and induced apoptosis in the A549 cells. The findings from our study could form the basis for future research that may be translated into an in vivo model to validate the possible therapeutic alternative for lung cancer using Naringenin-loaded LCNs. In addition, the applications of Naringenin-loaded LCNs as an intervention would be of great interest to biological, formulation and respiratory scientists and clinicians.
在这项研究中,我们开发了柚皮素负载的液晶纳米颗粒(LCNs),并分别研究了柚皮素-LCNs 对人呼吸道上皮衍生的基底细胞(BCi-NS1.1)和人肺上皮癌细胞(A549)细胞系的抗炎和抗癌活性。通过 qPCR 评估的柚皮素-LCNs 的抗炎潜力显示,在脂多糖诱导的 BCi-NS1.1 细胞中,IL-6、IL-8、IL-1β和 TNF-α的表达降低。LCNs 的活性可与阳性对照药物丙酸氟替卡松(10 nM)相媲美。通过评估 A549 细胞的增殖(MTT 和台盼蓝检测)、迁移(划痕愈合试验、改良 Boyden 室试验和免疫印迹)和集落形成活性来研究抗癌活性。柚皮素 LCNs 在 A549 细胞中显示出有前途的抗增殖、抗迁移和抗集落形成活性,体外。因此,基于我们的观察和结果,我们得出结论,柚皮素-LCNs 可作为一种潜在的基于治疗的干预措施,以改善气道炎症并抑制肺癌的进展。实际应用:柚皮素被包裹在液晶纳米颗粒中,从而赋予其缓释性质。此外,负载柚皮素的 LCNs 可有效降低促炎标志物(即 IL-1β、IL-6、TNF-α和 IL-8)的水平。此外,负载柚皮素的 LCNs 在 A549 细胞系中也具有有效的抗癌活性,这可通过抑制细胞增殖和迁移来证明。它们还可减弱 A549 细胞的集落形成并诱导细胞凋亡。我们研究中的发现可能为未来的研究奠定基础,这些研究可能会转化为体内模型,以验证使用负载柚皮素的 LCNs 作为治疗肺癌的可能替代方法。此外,负载柚皮素的 LCNs 作为一种干预措施,将引起生物、制剂和呼吸科学家和临床医生的极大兴趣。