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基于黄酮-膜相互作用的芹菜素脂质体对结直肠癌化疗疗效的增强作用

Enhanced chemotherapeutic efficacy of apigenin liposomes in colorectal cancer based on flavone-membrane interactions.

作者信息

Banerjee Kacoli, Banerjee Shubhadeep, Mandal Mahitosh

机构信息

School of Medical Science and Technology, Indian Institute of Technology Kharagpur, Kharagpur 721302, India.

School of Medical Science and Technology, Indian Institute of Technology Kharagpur, Kharagpur 721302, India.

出版信息

J Colloid Interface Sci. 2017 Apr 1;491:98-110. doi: 10.1016/j.jcis.2016.12.025. Epub 2016 Dec 18.

Abstract

Recent endeavors in exploiting vast array of natural phytochemicals to ameliorate colorectal cancer led us to investigate apigenin, a naturally occurring dietary flavone as a potential chemo-therapeutic agent. The present study focuses on establishing apigenin as a potential chemotherapeutic agent for alleviating colorectal cancer and reports the development of a stable liposomal nanocarrier with high encapsulation of the hydrophobic flavone apigenin for enhanced chemotherapeutic effects. The enhanced pharmacological activity of apigenin has been assigned to its ability to interact and subsequently influence membrane properties which also resulted in optimal yield of a stable, rigidified, non-leaky nano-carrier with ideal release kinetics. Extensive testing of drug and its liposomal counterpart for potential clinical chemotherapeutic applications yielded hemocompatibility and cytocompatibility with normal fibroblast cells while enhanced antineoplastic activity was observed in tumor xenograft model. The increased chemotherapeutic potential of liposomal apigenin highlights the clinical potential of apigenin-based vesicles.

摘要

近期,人们致力于利用大量天然植物化学物质来改善结直肠癌,这促使我们研究芹菜素,一种天然存在的膳食黄酮,作为一种潜在的化学治疗剂。本研究重点在于将芹菜素确立为一种缓解结直肠癌的潜在化学治疗剂,并报告了一种稳定的脂质体纳米载体的研发情况,该载体对疏水性黄酮芹菜素具有高包封率,以增强化学治疗效果。芹菜素增强的药理活性归因于其相互作用并随后影响膜性质的能力,这也导致了具有理想释放动力学的稳定、刚性化、无渗漏纳米载体的最佳产量。对药物及其脂质体对应物进行广泛的潜在临床化学治疗应用测试,结果显示与正常成纤维细胞具有血液相容性和细胞相容性,同时在肿瘤异种移植模型中观察到增强的抗肿瘤活性。脂质体芹菜素增加的化学治疗潜力突出了基于芹菜素的囊泡的临床潜力。

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