活性部位及其生物活性成分对三阴性乳腺癌细胞的抗糖酵解活性

Antiglycolytic Activities of Active Fraction and its Bioactive Components on Triple-Negative Breast Cancer Cells .

机构信息

Department of Chemical Pathology, School of Medical Sciences, Health Campus, Universiti Sains Malaysia, 16150, Kota Bharu, Kelantan, Malaysia.

出版信息

Anticancer Agents Med Chem. 2022;22(7):1363-1369. doi: 10.2174/1871520621666210427104804.

DOI:10.2174/1871520621666210427104804

PMID:33906591

Abstract

BACKGROUND

Survival and progression of cancer cells are highly dependent on aerobic glycolysis. Strobilanthes crispus has been shown to have promising anticancer effects on breast cancer cells. The involvement of the glycolysis pathway in producing these effects is unconfirmed, thus further investigation is required to elucidate this phenomenon.

OBJECTIVE

This study aims to determine the effect of S. crispus active fraction (F3) and its bioactive components on glycolysis in triple-negative breast cancer cells (MDA-MB-231).

METHODS

This study utilizes F3, lutein, β-sitosterol, and stigmasterol to be administered in MDA-MB-231 cells for measurement of antiglycolytic activities through cell poliferation, glucose uptake, and lactate concentration assays. Cell proliferation was assessed by MTT assay of MDA-MB-231 cells after treatment with F3 and its bioactive components lutein, β-sitosterol, and stigmasterol. The IC50 value in each compound was determined by MTT assay to be used in subsequent assays. The determination of glucose uptake activity and lactate concentration were quantified using fluorescence spectrophotometry.

RESULTS

Antiproliferative activities were observed for F3 and its bioactive components, with IC50 values of 100 μg/mL (F3), 20 μM (lutein), 25 μM (β-sitosterol), and 90 μM (stigmasterol) in MDA-MB-231 cells at 48 h. The percentage of glucose uptake and lactate concentration in MDA-MB-231 cells treated with F3, lutein, or β sitosterol were significantly lower than those observed in the untreated cells in a time-dependent manner. However, treatment with stigmasterol decreased the concentration of lactate without affecting the glucose uptake in MDA-MB-231 cells.

CONCLUSION

The antiglycolytic activities of F3 on MDA-MB-231 cells are attributed to its bioactive components.

摘要

背景

癌细胞的存活和发展高度依赖有氧糖酵解。糙苏已被证明对乳腺癌细胞具有有前景的抗癌作用。然而，糖酵解途径在产生这些作用中的参与尚未得到证实，因此需要进一步研究来阐明这一现象。

目的

本研究旨在确定糙苏活性部分（F3）及其生物活性成分对三阴性乳腺癌细胞（MDA-MB-231）糖酵解的影响。

方法

本研究采用 F3、叶黄素、β-谷甾醇和豆甾醇对 MDA-MB-231 细胞进行给药，通过细胞增殖、葡萄糖摄取和乳酸浓度测定来测量抗糖酵解活性。用 MTT 法测定 F3 及其生物活性成分叶黄素、β-谷甾醇和豆甾醇处理 MDA-MB-231 细胞后的细胞增殖情况。用 MTT 法测定各化合物的 IC50 值，用于后续试验。葡萄糖摄取活性和乳酸浓度的测定采用荧光分光光度法进行定量。

结果

F3 及其生物活性成分均表现出抗增殖活性，在 MDA-MB-231 细胞中，48 h 时的 IC50 值分别为 100 μg/mL（F3）、20 μM（叶黄素）、25 μM（β-谷甾醇）和 90 μM（豆甾醇）。用 F3、叶黄素或β-谷甾醇处理 MDA-MB-231 细胞后，细胞内葡萄糖摄取和乳酸浓度的百分比呈时间依赖性显著低于未处理细胞。然而，用豆甾醇处理会降低 MDA-MB-231 细胞中的乳酸浓度，而不影响葡萄糖摄取。