Pectolinarigenin is a dimethoxyflavone extracted from the leaves of Linaria vulgaris Mill and it has been found to specifically bind to the nuclear receptor RARγ (IC50 = 3.42 μM) to activate theJNK signaling pathway and induce apoptosis.
Pectolinarigenin is a dual inhibitor of COX-2/5-LOX with anti-inflammatory activity[3]. Pectolinarigenin has potent inhibitory activities on melanogenesis. Pectolinarigenin treatment resulted in growth inhibition and apoptosis induction in melanoma cells, and the potential of pectolinarigenin to impair the migration and invasion of melanoma cells in accordance with the changes in the expression of the associated proteins[4]. Intraperitoneal administrations of pectolinarigenin significantly inhibited breast cancer metastasis to lungs without affecting the tumor growth of incubated 4T1 breast cancer cells. Pectolinarigenin could also recruit CD8+ T cells to mediate tumor immune response. Furthermore, pectolinarigenin markedly impaired cancer cell migration and invasion by down-regulating phosphorylated-Stat3, and expression of matrix metalloproteinase (MMP)-2, MMP-9, while up-regulating the expression of TIMP2[5]. Treatment of pectolinarigenin inhibited cell viability and cell migration of NPC C666-1 cells in concentration- and time-dependent manner. The in vivo experiment of subcutaneous xenograft mice model also indicated that the administration of pectolinarigenin could decrease the tumor growth of NPC (Nasopharyngeal cancer) and no severe toxicity was observed[6].
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