Bano Sameena, Ahmed Faheem, Khan Farha, Chaudhary Sandeep Chand, Samim M
Department of Chemistry, School of Chemical and Life Sciences, Jamia Hamdard (Deemed to be University) New Delhi India
Department of Community Medicine, Hamdard Institute of Medical Sciences and Research, Jamia Hamdard (Deemed to be University) New Delhi India.
RSC Adv. 2020 Apr 27;10(28):16637-16649. doi: 10.1039/c9ra10686c. eCollection 2020 Apr 23.
Naturally occurring lycopene has been reported for its chemopreventive and chemotherapeutic efficiency in various cancers, but its exceptional lipophilicity, poor aqueous solubility, instability, and consequently poor bioavailability limit its usage as a chemopreventive and chemotherapeutic agent. The present study aimed to synthesize co-polymeric nanoparticle-encapsulated formulations of commercial lycopene (NLY) and extracted lycopene (NLX) and evaluate their anticancer activity and inhibitory effect on 12--tetradecanoylphorbol-13-acetate (TPA)-promoted skin inflammation and tumorigenesis in Swiss albino mice. To prepare the nanoparticle-encapsulated formulations of lycopene, thermosensitive PNIPAAM-PEG-based co-polymeric nanoparticles were synthesized and characterized by FTIR spectroscopy, NMR spectroscopy, DLS, and TEM. Nanolycopene, unlike free lycopene, could be readily dispersed in aqueous media. Nanolycopene demonstrated stronger antioxidant activity and comparable anticancer efficacy to free lycopene against the melanoma cell line B16. Furthermore, nanolycopene showed comparable reduction of TPA-induced skin edema, expression of COX-2, and oxidative stress response. Additionally, it showed significant inhibition of tumor promotion. It also altered Bax and Bcl2 expressions, which led to the induction of apoptosis. The results also supported that the extracted lycopene-encapsulated nanoparticles may be a good alternative to the expensive commercial lycopene for cancer treatment.
天然存在的番茄红素已被报道在多种癌症中具有化学预防和化疗功效，但其极高的亲脂性、较差的水溶性、不稳定性以及随之而来的低生物利用度限制了它作为化学预防和化疗药物的应用。本研究旨在合成商业番茄红素（NLY）和提取的番茄红素（NLX）的共聚物纳米颗粒包封制剂，并评估它们对瑞士白化小鼠中12-十四酰佛波醇-13-乙酸酯（TPA）诱导的皮肤炎症和肿瘤发生的抗癌活性及抑制作用。为制备番茄红素的纳米颗粒包封制剂，合成了基于热敏性聚N-异丙基丙烯酰胺-聚乙二醇（PNIPAAM-PEG）的共聚物纳米颗粒，并通过傅里叶变换红外光谱（FTIR）、核磁共振光谱（NMR）、动态光散射（DLS）和透射电子显微镜（TEM）对其进行表征。与游离番茄红素不同，纳米番茄红素能够很容易地分散在水性介质中。纳米番茄红素表现出更强的抗氧化活性，并且在抗黑色素瘤细胞系B16方面与游离番茄红素具有相当的抗癌功效。此外，纳米番茄红素在减轻TPA诱导的皮肤水肿、环氧化酶-2（COX-2）表达和氧化应激反应方面表现相当。另外，它对肿瘤促进有显著抑制作用。它还改变了Bax和Bcl2的表达，从而导致细胞凋亡的诱导。结果还支持提取的番茄红素包封纳米颗粒可能是昂贵的商业番茄红素用于癌症治疗的良好替代品。
