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Increasing evidence supports the anti-estrogenic and/or anti-proliferative properties of luteolin, which is a natural flavonoid existing in herbs, vegetables and fruits. However, the molecular mechanisms responsible for these effects are only partially explored. In the present study, estrogen receptor-alpha (ER-α) was identified as a potential molecular target for luteolin. Our data indicated that treatment with luteolin engendered suppression of ER-α protein and mRNA expression in ER-α-positive breast cancer cells. Y-box binding protein-1 (YB-1) is a known transcriptional regulator of ER-α expression. In this studies it was demonstrated that luteolin decreased YB-1 protein and mRNA expression. Integrin-linked kinase (ILK) is able to phosphorylate many downstream effectors that have the potential to regulate YB-1 transcription. We provided evidence for a mechanism by which luteolin suppressed YB-1 expression through the downregulation of ILK/Akt/STAT3-regulated Twist expression in ER-α-positive breast cancer cells. Our data also showed that luteolin inhibited cancer migration and invasion through the inhibition of epithelial-mesenchymal transition (EMT). Taken together, these data indicate that the antitumorigenic effects of luteolin in ER-α-positive breast cancer cells may arise from its ability to reduce ER-α expression.

Non-small-cell lung cancer (NSCLC) accounts for approximately 85% of all lung cancers, and has highly metastatic capacity and poor prognosis. The anti-tumour activity and the corresponding signal pathways of spring Curcuma aromatica Salisb essential oil (CSEO) and autumn C. aromatica essential oil (CAEO) were evaluated. The results demonstrated that CAEO possessed more potent cytotoxicity than CSEO in NSLCL cells. CAEO induced apoptosis through the cleavage and activation of caspases 3, 8, 9, and poly (ADPribose) polymerase (PARP) in NCI-H1299 cells. After treatment with CAEO, pro-apoptosis protein Bax expression increased, and anti-apoptosis proteins Bcl-2 and Bcl-xL expression decreased. In addition, CAEO could promote tumour suppressor protein p53 expression, inhibit the phosphorylation of ERK1/2 and increase the phosphorylation of JNK1/2 and p38. CAEO treatment also inhibited Akt/NF-κB signal pathways in NCI-H1299 cells. In vivo experiments showed that CAEO significantly inhibited the growth of NSCLC in nude mice. Zingiberene (4.80 mg/g), β-sesquiphellandrene (1.88 mg/g) and turmerone (0.98 mg/g) were found in CAEO as potential active compounds. Thus, these results emphasize that the CAEO induced apoptosis and had a potential to become a new functional food ingredient for the prevention and treatment of NSCLC.

Zerumbone, a sesquiterpene compound of edible ginger (Zingiber zerumbet), has been tested for its anti-EMT and anti-metastatic properties in TGF-β1-stimulated human lung cancer (A549) cells. Zerumbone (10/20 µM) treatment prior to TGF-β1-stimulation reversed the adverse morphological changes (fibroblastic-to-epithelial phenotype) and up-regulated the E-cadherin expression against TGF-β1-induced down-regulation. Immunofluorescence and luciferase activity data confirmed the up-regulated E-cadherin expression and transcriptional activity by zerumbone under TGF-β1-stimulation. Further evidence showed that zerumbone decreased TGF-β1-mediated phosphorylation and transcriptional activity of Smad2, but not Smad3. These results revealed that zerumbone inhibits the TGF-β-induced EMT via up-regulation of E-cadherin and down-regulation of Smad2 signalling pathways. Findings from wound-healing, invasion and colony formation experiments proved that zerumbone inhibits TGF-β1-mediated (metastatic) migration, invasion and anchorage-independent growth. Besides, zerumbone alone is capable of inducing autophagy and apoptosis in A549 cells. These results conclude that anti-EMT and anti-metastatic activities of zerumbone may contribute to the development of food-based chemopreventive drugs for non-small cell lung cancer treatment.

Curcuminoids, including curcumin (CUR), demethoxycurcumin (DMC), and bisdemethoxycurcumin (BDMC), show the maximum absorption wavelength near blue light. Photodynamic therapy (PDT) has been developed as a therapeutic modality, which could induce cell death via the formation of ROS under illumination. Recently, it has been suggested that curcuminoids may be developed as potential photosensitizers. Here we found that curcuminoids-PDT significantly inhibited cell viability in breast cancer cell lines; in particular DMC-PDT has the highest anti-proliferative effect. A comprehensive analysis of cell response to DMC-PDT showed that autophagy was an early event and apoptosis was a late event. The generation of ROS by exciting the photosensitizer in PDT can activate MAPK pathway. Pre-treatment with a singlet oxygen scavenger or JNK inhibitor in DMC-PDT resulted in the reversion of cell viability, a reduced LC3 conversion and PARP cleavage. These results indicate that DMC may be considered as a new photosensitizer in PDT for cancer treatment.

Fatigue is a noticeable and highly prevalent symptom in tense, industriously, and economically affluent modern society. Therefore, new antifatigue agents to smooth the fatigue feature are an energetic topic. The total ethanol extract (ESI) of Saussurea involucrata Kar et Kir., known as Tian-Shan snow lotus, was evaluated for antifatigue activity in ICR mice with mice forced swimming test and the determination of the contents of blood lactic acid and serum urea nitrogen. ESI (0.05, 0.15, 0.25 g/kg) was administered orally to mice for 4 weeks. The average swimming times to exhaustion of the ESI-treated ICR mice (0.15, 0.25 g/kg) were prolonged by 132% and 180% (p