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Table 1 Inhibition of HOTAIR expression by bioactive compounds, anticancer drugs and HOTAIR inhibitor

From: HOTAIR: a potential metastatic, drug-resistant and prognostic regulator of breast cancer

Bioactive compounds/

anticancer drugs/HOTAIR inhibitor

Mechanism of action

Ref

Delphinidin (DEL)

• Inhibits 1-methyl-1-nitrosourea-induced BC in rats by upregulating miR-34a via the targeting of HOTAIR expression

• Reduces the occupancy of EZH2 and histone H3 Lys27 trimethylation at the promoter site of miR-34a

[103]

DEL-3-glucoside

• Inhibits nitrosamine and benzopyrene-induced carcinogenesis in normal breast epithelial cells by reducing the expression of HOTAIR.

• Reduces the expression of HOTAIR and Akt by increasing the expression and binding of IRF1 to the of HOTAIR promoter

[104]

Calycosin and genistein

• Reduces HOTAIR expression by reducing Akt phosphorylation in MCF-7 BC cells

[105]

Peptide nucleic acid (PNA3)

• Reduces the invasion of BC cells by increasing the sensitivity to chemotherapy via reduction in NF-kB dependent expression of MMP9 and IL-6

[107]

Imatinib and lapatinib

• Synergistically reduces the expression of HOTAIR by regulating β-catenin recruitment at the promoter via interference with the LEF1/TCF4-binding site

[108]

AC1Q3QWB (AQB)

• Enhances the expression of tumor suppressors by interfering with the recruitment of PRC2 via the disruption of the interaction between HOTAIR and EZH2

• Upregulates HOTAIR target genes especially APC2 via the suppression of Wnt/catenin signaling and the promotion of transcription via RNA pol II

[109]

AC1NOD4Q (ADQ

• Inhibits BC metastasis by blocking HOTAIR activity via interference with the EZH2 interaction

• Impairs the H3K27-dependent trimethylation of the target gene and subsequent inhibition of the Wnt/catenin pathway in an orthotopic BC model

• Prevents the interaction of HOTAIR with EZH2 by binding to a specific HOTAIR domain

[110]

Metformin (MET)

• Inhibits HOTAIR expression by affecting the methylation pattern of CpG islands in the promoter region and reverses EMT by lowering vimentin and β-catenin levels

• Reduces the invasiveness and migratory potential of TNBC cells

[111]

Aurora kinase inhibitor (CCT137690)

• Inhibits the expansion of TNBC cells by reducing HOTAIR levels via its influence on AURK and associated network proteins

[112]

[113]

Steroidal saponin (Dioscin)

• Inhibits stem-like properties and EMT in BC.

[114]

• Reduces HOTAIR expression in gastric cancer

[115]

Polyphylla I

• Disrupts the interaction of HOTAIR with its upstream regulators and downstream mediators.

[116]

• Inhibits the cell cycle and induces apoptosis in BC

[117]

Berberine

• Inhibits BC and gefitinib and inhibits HOTAIR expression by inducing miR-34a-5p expression in lung cancer cells

[118]

[119]