Luteolin: Overview and its Anticancer Perspectives

General Description

Luteolin, a flavonoid compound found in plants, exhibits potent bioactive properties, including antioxidant, anti-inflammatory, and anticancer effects. In breast cancer, luteolin inhibits cancer-promoting proteins, suppresses tumor growth, and induces apoptosis through various pathways. It interferes with key signaling molecules and enhances the activities of caspases, showing promise in inhibiting cancer progression. Similarly, in prostate cancer, luteolin inhibits cell invasiveness, halts growth progression, and triggers apoptosis in cancer cells. It also reduces tumor volume and suppresses cancer cell proliferation through multiple mechanisms. Overall, luteolin's multifaceted actions make it a promising candidate for breast and prostate cancer treatment.

Figure 1. Luteolin

Overview

Luteolin, a flavonoid compound found in various plants, possesses remarkable bioactive properties. It exhibits antioxidant, anti-inflammatory, and anticancer activities, making it a potential therapeutic agent. Its ability to modulate signaling pathways and gene expression contributes to its diverse biological effects. Luteolin has been studied for its potential in treating various diseases, including cancer and chronic inflammatory conditions. Its natural occurrence and relatively low toxicity enhance its appeal as a potential therapeutic option. ¹

Anticancer Perspectives

Breast cancer

Luteolin, a natural flavonoid compound, exhibits promising anti-breast cancer activity through various mechanistic routes. It has been shown to suppress the expression of cancer-promoting proteins, reduce tumor size and growth viability, inhibit progestin-dependent VGF secretion, and increase the expression of pro-apoptotic protein Bax. In breast cancer cells, luteolin inhibits proliferation and suppresses the expression of key signaling molecules such as p-STAT3, p-EGFR, p-Akt, and p-Erk1/2 induced by EGF. Furthermore, luteolin interferes with EGFR signaling pathways, including STAT3, MAPK/Erk1/2, and PI3K/Akt pathways, which play crucial roles in cancer progression. Studies have demonstrated that luteolin can inhibit the development of large tumors, reduce VEGF levels, inhibit cell cycle progression, and regulate miRNAs in breast cancer cells. Moreover, luteolin has been found to enhance the activities of caspases, induce apoptosis through intrinsic and extrinsic pathways, disrupt cell cycle progression, and modulate the expression of various proteins involved in cell death. Combination therapies involving luteolin have shown synergistic effects in inhibiting cancer cell growth and promoting cell death. Additionally, the use of luteolin-loaded nanoparticles has improved the bioavailability of luteolin, enhanced its targeting in breast cancer cells, and resulted in increased cancer cell death. These nanoparticles have also been shown to downregulate Nrf2 downstream genes, inhibit multi-drug resistance, and increase cancer cell death in combination with other chemotherapeutic agents. Overall, luteolin demonstrates significant potential as an anti-breast cancer agent through its multifaceted mechanisms of action, making it a promising candidate for further therapeutic development in breast cancer treatment. ²

Prostate cancer

Luteolin has demonstrated significant anti-prostate cancer activities through multiple mechanisms. Firstly, luteolin inhibits the invasiveness of cancer cells, halts cell growth progression, and triggers apoptosis in prostate cancer cells. It also reduces extracellular matrix contraction, diminishes Rho signaling, and suppresses VEGF-induced phosphorylation, all of which contribute to its chemopreventive and chemotherapeutic effects against prostate cancer. Studies have shown that luteolin can lower the malignancy of highly invasive prostate cancer cells, inhibit cancer cell invasiveness, and suppress the growth of both androgen-sensitive and androgen-independent prostate cancer cell lines. Luteolin also synergistically inhibits TGF-β-induced myofibroblast phenotypes and downstream signaling pathways involved in prostate cancer progression. Moreover, luteolin has been found to reduce the expression of genes related to cell cycle pathways and epidermal growth factor receptor signaling in prostate cancer cells, leading to G2/M cell cycle arrest. It also suppresses VEGF-induced phosphorylation, decreases pro-inflammatory cytokine levels, reduces tumor weight and volume, and inhibits the expression of various proteins associated with cancer cell proliferation and invasion. In human studies, luteolin has been shown to induce apoptosis in prostate carcinoma cells, regulate gene expressions related to prostate cancer progression, and block prostate-specific antigen expression by down-regulating androgen receptor expression. Additionally, luteolin in combination with gefitinib affects gene expressions involved in the cell cycle pathway through EGFR-associated tyrosine kinase. Overall, the multifaceted anti-prostate cancer activities of luteolin make it a promising candidate for the prevention and treatment of prostate cancer. ²

Reference

1. Lin Y, Shi R, Wang X, Shen HM. Luteolin, a flavonoid with potential for cancer prevention and therapy. Curr Cancer Drug Targets. 2008; 8(7): 634-646.

2. Imran M, Rauf A, Abu-Izneid T, et al. Luteolin, a flavonoid, as an anticancer agent: A review. Biomed Pharmacother. 2019; 112: 108612.

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