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Anti-Cancer Agents in Medicinal Chemistry

Author(s): Siti N.H. Muhammad, Nik S. Yaacob, Nur A.M. Safuwan and Agustine N. Fauzi*

DOI: 10.2174/1871520621666210427104804

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Antiglycolytic Activities of Strobilanthes crispus Active Fraction and its Bioactive Components on Triple-Negative Breast Cancer Cells In Vitro

Page: [1363 - 1369] Pages: 7

  • * (Excluding Mailing and Handling)

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.

Keywords: Strobilanthes crispus, glucose uptake, lactate concentration, MDA-MB-231, glucose metabolism, breast cancer.

Graphical Abstract

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