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负载提取物的壳聚糖纳米颗粒作为癌症增殖和微生物生长抑制剂的植物化学表征及功效

Phytochemical Characterization and Efficacy of Extract Loaded Chitosan Nanoparticles as Inhibitors of Cancer Proliferation and Microbial Growth.

作者信息

Qanash Husam, Bazaid Abdulrahman S, Aldarhami Abdu, Alharbi Bandar, Almashjary Majed N, Hazzazi Mohannad S, Felemban Hashim R, Abdelghany Tarek M

机构信息

Department of Medical Laboratory Science, College of Applied Medical Sciences, University of Ha'il, Hail 55476, Saudi Arabia.

Department of Medical Microbiology, Qunfudah Faculty of Medicine, Umm Al-Qura University, Al-Qunfudah 21961, Saudi Arabia.

出版信息

Polymers (Basel). 2023 Jan 11;15(2):391. doi: 10.3390/polym15020391.

Abstract

Despite the advanced development in the field of drug discovery and design, fighting infectious and non-infectious diseases remains a major worldwide heath challenge due to the limited activity of currently used drugs. Nevertheless, in recent years, the approach of designing nanoparticles for therapeutic applications has gained more interest and promise for future use. Thus, the current study is focused on the evaluation of extract and chitosan nanoparticles loaded extract (CNPsLE) for potential antimicrobial and anticancer activities. The HPLC analysis of the extract has shown the presence of various phenolic and flavonoid compounds, including kaempferol (3916.34 µg/mL), apigenin (3794.32 µg/mL), chlorogenic acid (1089.58 µg/mL), quercetin (714.97 µg/mL), vanillin (691.55 µg/mL), naringenin (202.14 µg/mL), and rutin (55.64 µg/mL). The extract alone showed higher MIC values against , , , , and (62.5, 15.65, 15.62, 31.25, and 31.25 µg/mL, respectively), whereas lower MIC values were observed when the extract was combined with CNPsLE (0.97, 1.95, 3.9, 4.1, and 15.62 µg/mL, respectively). The extract exhibited low cytotoxicity against normal Vero cells with IC 173.74 µg/mL in comparison with the cytotoxicity of the CNPsLE (IC, 73.89 µg/mL). However, CNPsLE showed more selective toxicity against the human prostate cancer cell line (PC3) with IC of 20.8 µg/mL than the extract alone with 76.09 µg/mL. In the docking experiments, kaempferol and apigenin were revealed to be suitable inhibitors for prostate cancer (2Q7L). Overall, the obtained data highlighted the promising potential therapeutic use of CNPsLE as an anticancer and antimicrobial agent.

摘要

尽管药物发现与设计领域取得了先进的发展,但由于目前使用的药物活性有限,对抗传染性和非传染性疾病仍然是一项重大的全球健康挑战。然而,近年来,设计用于治疗应用的纳米颗粒的方法已引起更多关注,并有望在未来得到应用。因此,当前的研究集中于评估提取物以及负载提取物的壳聚糖纳米颗粒(CNPsLE)的潜在抗菌和抗癌活性。提取物的高效液相色谱分析表明存在各种酚类和黄酮类化合物,包括山奈酚(3916.34μg/mL)、芹菜素(3794.32μg/mL)、绿原酸(1089.58μg/mL)、槲皮素(714.97μg/mL)、香草醛(691.55μg/mL)、柚皮素(202.14μg/mL)和芦丁(55.64μg/mL)。单独的提取物对金黄色葡萄球菌、大肠杆菌、枯草芽孢杆菌、白色念珠菌和黑曲霉显示出较高的最低抑菌浓度值(分别为62.5、15.65、15.62、31.25和31.25μg/mL),而当提取物与CNPsLE联合使用时观察到较低的最低抑菌浓度值(分别为0.97、1.95、3.9、4.1和15.62μg/mL)。与CNPsLE的细胞毒性(IC50,73.89μg/mL)相比,提取物对正常Vero细胞表现出较低的细胞毒性,IC50为173.74μg/mL。然而,CNPsLE对人前列腺癌细胞系(PC3)表现出比单独提取物(IC50为76.09μg/mL)更高的选择性毒性,IC50为20.8μg/mL。在对接实验中,山奈酚和芹菜素被证明是前列腺癌(2Q7L)的合适抑制剂。总体而言,所获得的数据突出了CNPsLE作为抗癌和抗菌剂的潜在治疗用途。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c058/9865519/b59382a5d10b/polymers-15-00391-g001.jpg

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