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名为山茶的提取物对miRNA表达及其药代动力学特性的调节作用。

Regulatory Effects of Extract, Known as Mountain Tea, on miRNA Expression and Its Pharmacokinetic Properties.

作者信息

Sarı Muhammed Emin, Torunoğlu Emine Incilay, Sarı Zeynep Betül, Aytar Erdi Can, Gümrükçüoğlu Abidin, Durmaz Alper, Demirel Gamze

机构信息

Department of Medical Biology, Faculty of Medicine Necmettin Erbakan University Konya Türkiye.

Department of Medical Biochemistry, Faculty of Medicine Necmettin Erbakan University Konya Türkiye.

出版信息

Food Sci Nutr. 2025 May 25;13(6):e70341. doi: 10.1002/fsn3.70341. eCollection 2025 Jun.

DOI:10.1002/fsn3.70341
PMID:40444130
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12121518/
Abstract

The aim of this study is to investigate the anticancer potential of extract on MDA-MB-231 breast cancer cells, its regulatory effects on miRNA expression, the content analysis of its phytochemical components, and the roles of these compounds in the regulation of miRNA expression through pathways, as well as to examine its pharmacokinetic profiles. The plant was extracted with methanol. The obtained extracts were analyzed for phytochemical components using gas chromatography-mass spectrometry (GC-MS) and high-performance liquid chromatography (HPLC-DAD) techniques. Biological activity was assessed using the MTT assay on the MDA-MB-231 breast cancer cell line, while miRNA expression was measured by RT-PCR. Pharmacokinetic properties were calculated using ADMETSAR3 software, and molecular interactions were investigated through AutoDock Vina simulations. GC-MS analysis of extract identified 42 volatile compounds, with 1S-α-pinene, humulene, and caryophyllene being the most abundant. HPLC-DAD analysis detected 18 bioactive compounds, including catechin, oleuropein, and rutin. The extract inhibited the viability of MDA-MB-231 breast cancer cells in a dose-dependent manner, with an IC value of 0.8 mg/mL. Furthermore, upregulation of miR-19, miR-20a, miR-126, and miR-200c miRNAs was observed in MDA-MB-231 cells, while these miRNAs were downregulated in healthy cells. ADMET analysis revealed that α-pinene, caryophyllene, and catechin exhibited high bioavailability, absorption, and distribution properties, while oleuropein and rutin showed limited absorption and bioavailability. Molecular docking studies demonstrated the potential binding interactions of these compounds with key target proteins involved in cancer progression. Consequently, presents significant potential as a valuable natural source for cancer therapy through its anticancer activity, modulation of miRNA expression, and interaction with cancer-associated proteins.

摘要

本研究的目的是探究提取物对MDA-MB-231乳腺癌细胞的抗癌潜力、其对miRNA表达的调控作用、其植物化学成分的含量分析,以及这些化合物通过通路在miRNA表达调控中的作用,并检测其药代动力学特征。该植物用甲醇提取。使用气相色谱-质谱联用(GC-MS)和高效液相色谱(HPLC-DAD)技术对所得提取物进行植物化学成分分析。使用MTT法在MDA-MB-231乳腺癌细胞系上评估生物活性,同时通过RT-PCR测量miRNA表达。使用ADMETSAR3软件计算药代动力学性质,并通过AutoDock Vina模拟研究分子相互作用。提取物的GC-MS分析鉴定出42种挥发性化合物,其中1S-α-蒎烯、蛇麻烯和石竹烯含量最高。HPLC-DAD分析检测到18种生物活性化合物,包括儿茶素、橄榄苦苷和芦丁。提取物以剂量依赖性方式抑制MDA-MB-231乳腺癌细胞的活力,IC值为0.8mg/mL。此外,在MDA-MB-231细胞中观察到miR-19、miR-20a、miR-126和miR-200c miRNA上调,而在健康细胞中这些miRNA下调。ADMET分析表明,α-蒎烯、石竹烯和儿茶素具有高生物利用度、吸收和分布特性,而橄榄苦苷和芦丁的吸收和生物利用度有限。分子对接研究证明了这些化合物与参与癌症进展的关键靶蛋白之间的潜在结合相互作用。因此,提取物通过其抗癌活性、miRNA表达调节以及与癌症相关蛋白的相互作用,作为癌症治疗的宝贵天然来源具有巨大潜力。

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