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载有氟伐他汀的磷脂、α-硫辛酸和蜂毒素的混合纳米颗粒系统，用于结肠癌的治疗。

Hybrid nanoparticulate system of Fluvastatin loaded phospholipid, alpha lipoic acid and melittin for the management of colon cancer.

机构信息

Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi Arabia.

Vaccines and Immunotherapy Unit, King Fahd Medical Research Center, King Abdulaziz University, Jeddah, Saudi Arabia.

出版信息

Sci Rep. 2022 Nov 14;12(1):19446. doi: 10.1038/s41598-022-24151-3.

DOI:10.1038/s41598-022-24151-3
PMID:36376469
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9663543/
Abstract

As a hydroxymethylglutaryl coenzyme A (HMG-CoA) reductase inhibitor, Fluvastatin (FLV) is used for reducing low-density lipoprotein (LDL) cholesterol as well as to prevent cardiovascular problems. FLV showed cell line cytotoxicity and antitumor effect. Melittin (MEL) exhibits antineoplastic activity and is known to be promising as a therapeutic option for cancer patients. The aim of this work was to investigate the combination of FLV with MEL loaded hybrid formula of phospholipid (PL) with alpha lipoic acid (ALA) nanoparticles to maximize anticancer tendencies. This study examines the optimization of the prepared formulation in order to minimize nanoparticles size and maximize zeta potential to potentiate cytotoxic potentialities in colon cancer cells (Caco2), cell viability, cell cycle analysis and annexin V were tested. In addition to biological markers as P53, Bax, bcl2 and Caspase 3 evaluation The combination involving FLV PL ALA MEL showed enhanced cytotoxic potentiality (IC50 = 9.242 ± 0.35 µg/mL), about twofold lower, compared to the raw FLV (IC50 = 21.74 ± 0.82 µg/mL). According to studies analyzing cell cycle, optimized FLV PL ALA MEL was found to inhibit Caco2 colon cancer cells more significantly than other therapeutic treatments, wherein a higher number of cells were found to accumulate over G2/M and pre-G1 phases, whereas G0/G1/S phases witnessed the accumulation of a lower number of cells. The optimized formulation may pave the way for a novel and more efficacious treatment for colon cancer.

摘要

作为羟甲基戊二酰辅酶 A（HMG-CoA）还原酶抑制剂，氟伐他汀（FLV）用于降低低密度脂蛋白（LDL）胆固醇，以预防心血管问题。FLV 显示出细胞系细胞毒性和抗肿瘤作用。蜂毒素（MEL）具有抗肿瘤活性，被认为是癌症患者有前途的治疗选择。本工作旨在研究 FLV 与载有磷脂（PL）和α-硫辛酸（ALA）纳米粒的 MEL 混合配方的联合使用，以最大程度地提高抗癌倾向。本研究考察了制备配方的优化，以最小化纳米颗粒的尺寸并最大化 zeta 电位，从而增强在结肠癌细胞（Caco2）中的细胞毒性潜力、细胞活力、细胞周期分析和 Annexin V。除了评估生物标志物如 P53、Bax、bcl2 和 Caspase 3 外，涉及 FLV-PL-ALA-MEL 的联合用药显示出增强的细胞毒性潜力（IC50=9.242±0.35µg/mL），比原始 FLV（IC50=21.74±0.82µg/mL）低约两倍。根据分析细胞周期的研究，发现优化的 FLV-PL-ALA-MEL 比其他治疗方法更能显著抑制 Caco2 结肠癌细胞，其中更多的细胞被发现积累在 G2/M 和 pre-G1 期，而 G0/G1/S 期则积累了较少的细胞。该优化配方可能为结肠癌的新型更有效治疗方法铺平道路。

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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d1e8/9663543/b874e98e7c49/41598_2022_24151_Fig8_HTML.jpg
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