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Enhancement of the cancer inhibitory effect of the bioactive food component resveratrol by nanoparticle based delivery.
Food & Function ( IF 5.1 ) Pub Date : 2020-03-26 , DOI: 10.1039/c9fo02445j Sameena Bano 1 , Faheem Ahmed , Farha Khan , Sandeep Chand Chaudhary , M Samim
Food & Function ( IF 5.1 ) Pub Date : 2020-03-26 , DOI: 10.1039/c9fo02445j Sameena Bano 1 , Faheem Ahmed , Farha Khan , Sandeep Chand Chaudhary , M Samim
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Naturally occurring bioactive food components such as dietary polyphenols have shown many beneficial biological activities due to their good antioxidant properties. Among them significant attention has been given to resveratrol (RV) in recent years as it plays a promising role in cancer prevention. It has demonstrated anti-proliferative effects, as well as the ability to inhibit the initiation and progression of induced cancer in a wide variety of tumor models. However, the benefits of its therapeutic effects were found to be limited due to its poor pharmacokinetic properties such as poor aqueous solubility, instability and extensive first pass metabolism. To overcome these limitations, the present study aimed to synthesize thermosensitive copolymeric nanoparticle encapsulated formulations of resveratrol-nanoresveratrol (NRV) and evaluate their in vitro anticancer activity and inhibitory effect on 12-O-tetradecanoylphorbol-13-acetate (TPA)-promoted skin inflammation and tumorigenesis in Swiss albino mice. For this purpose PNIPAAM-PEG based thermosensitive copolymeric nanoparticles were synthesized followed by the encapsulation of RV in their hydrophobic core. This enhanced the therapeutic bioavailability of resveratrol. Nanoresveratrol demonstrated stronger antioxidant activity and comparable anticancer efficacy to free resveratrol. Nanoparticles were characterized by IR, NMR, DLS and TEM. The best results were obtained with NRV at significantly lower doses. NRV demonstrated better in vitro anticancer activity against melanoma cell line B16. It showed comparable reduction of TPA induced skin edema, hyperplasia and oxidative stress response. In the promotion phase, a significant reduction was found in tumor incidence and tumor burden in mice pre-treated with NRV. Moreover, at all doses NRV altered Bax and Bcl2 expressions which lead to the induction of apoptosis.
中文翻译：
通过基于纳米颗粒的递送增强生物活性食品成分白藜芦醇的癌症抑制作用。
天然存在的生物活性食品成分，例如膳食多酚，由于其良好的抗氧化性能，已显示出许多有益的生物活性。其中，近年来，白藜芦醇（RV）在预防癌症中起着有希望的作用，因此受到了极大的关注。它已显示出抗增殖作用，以及在多种肿瘤模型中抑制诱导的癌症发生和发展的能力。然而，由于其不良的药代动力学性质，例如不良的水溶性，不稳定性和广泛的首过代谢，发现其治疗效果的益处受到限制。为了克服这些限制，本研究旨在合成白藜芦醇-nanoresveratrol（NRV）的热敏共聚物纳米颗粒封装制剂，并评估其体外抗癌活性和对12-O-十四烷酰佛波醇-13-乙酸盐（TPA）促进的瑞士白化病皮肤炎症和肿瘤发生的抑制作用。老鼠。为此目的，合成了基于PNIPAAM-PEG的热敏共聚物纳米颗粒，然后将RV封装在其疏水核中。这增强了白藜芦醇的治疗生物利用度。纳米白藜芦醇显示出更强的抗氧化活性，并且与游离白藜芦醇具有可比的抗癌功效。纳米颗粒通过IR，NMR，DLS和TEM表征。用NRV以低得多的剂量可获得最佳结果。NRV对黑色素瘤细胞系B16表现出更好的体外抗癌活性。它显示出可比的TPA诱导的皮肤水肿，增生和氧化应激反应的减少。在促进阶段，用NRV预处理的小鼠的肿瘤发生率和肿瘤负荷显着降低。此外，在所有剂量下，NRV都会改变Bax和Bcl2表达，从而导致细胞凋亡。
更新日期：2020-02-26
中文翻译：
通过基于纳米颗粒的递送增强生物活性食品成分白藜芦醇的癌症抑制作用。
天然存在的生物活性食品成分，例如膳食多酚，由于其良好的抗氧化性能，已显示出许多有益的生物活性。其中，近年来，白藜芦醇（RV）在预防癌症中起着有希望的作用，因此受到了极大的关注。它已显示出抗增殖作用，以及在多种肿瘤模型中抑制诱导的癌症发生和发展的能力。然而，由于其不良的药代动力学性质，例如不良的水溶性，不稳定性和广泛的首过代谢，发现其治疗效果的益处受到限制。为了克服这些限制，本研究旨在合成白藜芦醇-nanoresveratrol（NRV）的热敏共聚物纳米颗粒封装制剂，并评估其体外抗癌活性和对12-O-十四烷酰佛波醇-13-乙酸盐（TPA）促进的瑞士白化病皮肤炎症和肿瘤发生的抑制作用。老鼠。为此目的，合成了基于PNIPAAM-PEG的热敏共聚物纳米颗粒，然后将RV封装在其疏水核中。这增强了白藜芦醇的治疗生物利用度。纳米白藜芦醇显示出更强的抗氧化活性，并且与游离白藜芦醇具有可比的抗癌功效。纳米颗粒通过IR，NMR，DLS和TEM表征。用NRV以低得多的剂量可获得最佳结果。NRV对黑色素瘤细胞系B16表现出更好的体外抗癌活性。它显示出可比的TPA诱导的皮肤水肿，增生和氧化应激反应的减少。在促进阶段，用NRV预处理的小鼠的肿瘤发生率和肿瘤负荷显着降低。此外，在所有剂量下，NRV都会改变Bax和Bcl2表达，从而导致细胞凋亡。
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