A phytochemical study of the nut shell of Camellia oleifera Abel led to the isolation of a new gallotannin, three known hydrolyzable tannins (2, 4, and 5), and gallic acid (1). The structure of the isolated new gallotannin was unambiguously elucidated on the basis of comprehensive spectroscopic data.

Ethnopharmacological relevance: The meadowsweet family (genus Filipendula) includes about 30 species, which have been traditionally used in folk medicine to treat various inflammatory diseases. Particularily, F. palmata (Pall.) Maxim. (Siberian meadowsweet) were traditionally and widely used as an ethnic herb in the Oroqen application. Aim of the study: Limited studies have been documented on most species, except for two main species, F. ulmaria (L.) Maxim. and F. vulgaris Moench. Thus, this study aimed to investigate the anti-inflammatory and skin -moisturizing effects of 70% ethanolic extract (FPE) of F. palmata on human epidermal keratinocytes. Materials and methods: HaCaT keratinocytes were treated with FPE under different conditions. Quantitative real time-PCR, enzyme-linked immunosorbent assay, western blotting methods were used to evaluate the effect and molecular mechanism of the cells treated with FPE. The bioactive compounds in FPE, which are responsible for biological activities, was explored using mass spectrometric analysis. Results: FPE did not show a cytotoxic effect on the cells at concentrations below 200 mu g/mL. FPE significantly suppressed the intracellular reactive oxygen species and mitochondrial superoxide of inflamed HaCaT cells induced by tumor necrosis factor-alpha and interferon-gamma (T + I) and inflammatory chemokine genes and proteins, such as CC chemokine ligands (CCL5, CCL17, and CCL27) and CXC chemokine ligand (CXCL8). These anti-inflammatory activities of FPE were mediated by the downregulation of mitogen-activated protein kinase (MAPK) and nuclear factor kappa-light-chain-enhancer of activated B cells (NF-kappa B) signaling pathways. In normal HaCaT cells, FPE significantly promoted the production of hyaluronic acid (HA) via the downregulation of hyaluronidase (HYAL1 and HYAL2) and upregulation of hyaluronic acid synthase (HAS1, HAS2, and HAS3) genes, and these effects seemed to be associated with the PI3K/Akt/NF-kappa B signaling. Ultraperformance liquid chromatography-tandem mass spectrometry indicated that FPE contains four flavonoids, including (+)-catechin, miquelianin, scutellarin, and quercitrin, as its major phytochemicals. Finally, we demonstrated that miquelianin and quercitrin contribute partially to the anti-inflammatory and HA-producing activity of FPE without cytotoxic effects on HaCaT cells. Conclusions: Our findings suggest that topical applications of FPE can be utilized as an alternative therapy for treating skin inflammation. Additionally, our findings serve as a reference in applying FPE as a functional ingredient to treat inflammatory skin diseases and promote skin health.

BACKGROUND:In our previous study, Hibiscus syriacus leaf tissue was successfully cultivated in an optimized callus culture system, and subsequently extracted with 70% ethanol to prepare H. syriacus callus extract (HCE). The previous study suggested that the callus culture is useful method for obtaining the anti-inflammatory ingredients from H. syriacus. PURPOSE:In the present study, we aimed to investigate the effect of HCE on the colorectal cancer (CRC) and its underlying mechanism of action using HT-29 cells and thymus-deficient mice bearing HT-29 xenografts. METHODS:The cytotoxicity of HCE was investigated by MTT and colonies formation. The underling mechanism by which HCE regulates specific proteins in HT-29 cells was evaluated by the proteomic analysis. These putative proteins were validated using qRT-PCR and immunoblotting analyses. Subsequently, oral administration of HCE for 15 days further evaluating the anti-tumor activity by mRNA and protein expressions levels and tumor histopathology. RESULTS:Results of cell viability and colony formation assays revealed a significant cytotoxic effect of HCE at doses below 100 μg/ml against HT-29 cells, but not against normal cells. Through differential protein expression analysis, signaling pathways underlying anti-CRC activity were predicted in HCE-treated HT-29 cells: Notch signaling, cholesterol biosynthesis, and AMPK signaling pathways. qRT-PCR and immunoblotting analyses indicated that the cytotoxic effect of HCE against HT-29 cells might be associated with the suppression of Notch signaling, which positively contributes to cholesterol biosynthesis. To our knowledge, this can be presented as the first study to demonstrate the detailed relationship between Notch signaling and cholesterol-AMPK signaling. Our in vivo result further corroborated the in vitro finding that 100 and 200 mg/kg HCE for 15 days exerts its anti-cancer effect via Notch signaling-mediated suppression of cholesterol synthesis without systemic toxicity. CONCLUSION:Our findings can serve as a starting point for developing the novel anti-CRC agent using HCE, as a targeted medicine acting on regulating Notch signaling and cholesterol synthesis.

Ligularia fischeri, indigenous to eastern Asia, has been used as a traditional herbal medicine. Ligularia fischeri reportedly possesses a number of biological activities such as antimutagenic, antioxidant, antigenotoxic, and anti-inflammation. This study demonstrated the effects of ethanol extracts of Ligularia fischeri (ELF) on a high-carbohydrate diet (HCD)-induced hyperlipidemia in C57BL/6 mice. The mice were divided into six groups (n = 7/group) as follows: normal diet, HCD, or HCD+ELF (100, 200, 400, and 800 mg/kg/day), which were orally administered daily for 12 weeks. Various lipid parameters and histological changes in liver and fat tissue were compared among the treatment and control groups. ELF remarkably reduced body weight gain and attenuated hyperlipidemia by improving the plasma levels of total cholesterol, triglycerides, high-density lipoprotein cholesterol, low-density lipoprotein cholesterol, atherogenic index, and cardiac risk factor. Moreover, ELF decreased the HCD-induced hepatic accumulation of lipid droplets and adipocyte hypertrophy. These regulatory effects of ELF appeared to be mediated through the phosphorylation of AMP-activated protein kinase, acetyl-CoA carboxylase, sterol regulatory element-binding protein-1c, and expression of fatty acid synthase. Taken together, these findings indicate a functional role for ELF in the regulation of HCD-induced obesity and hyperlipidemia.

In the present study, we investigated the effects and molecular mechanism of marmesin, a natural coumarin compound isolated from Broussonetia kazinoki, on non-small cell lung cancer (NSCLC) cell responses and tumor angiogenesis. Marmesin abrogated mitogen-stimulated proliferation and invasion in both p53 wild-type A549 and p53-deficient H1299 NSCLC cells. These antitumor activities of marmesin were mediated by the inactivation of mitogenic signaling pathways and downregulation of cell signaling-related proteins including vascular endothelial growth factor receptor-2 (VEGFR-2), integrin β1, integrin-linked kinase and matrix metalloproteinases-2. Furthermore, marmesin suppressed the expression and secretion of VEGF in both NSCLC cells, leading to inhibition of capillary-like structure formation in human umbilical vein endothelial cells. Collectively, these findings demonstrate the pharmacological roles and molecular targets of marmesin in regulating NSCLC cell responses and tumor angiogenesis.

In the present study, we investigated the effects and molecular mechanism of 5-caffeoylquinic acid (5-CQA), a natural phenolic compound isolated from Ligularia fischeri, on cell invasion, proliferation and adhesion in p53 wild-type A549 and p53-deficient H1299 non-small cell lung cancer (NSCLC) cells. 5-CQA abrogated mitogen-stimulated invasion, but not proliferation, in both A549 and H1299 cells. In addition, 5-CQA inhibited mitogen-stimulated adhesion in A549 cells only. Anti-invasive activity of 5-CQA in A549 cells was mediated by the inactivation of p70(S6K)-dependent signaling pathway. In contrast, in H1299 cells the inactivation of Akt was found to be involved in 5-CQA-mediated inhibition of cell invasion. Collectively, these findings demonstrate the pharmacological roles and molecular targets of 5-CQA in regulating NSCLC cell fate, and suggest further evaluation and development of 5-CQA as a potential therapeutic agent for the treatment and prevention of lung cancer.

The inhibitory effects of lipid accumulation on ethanol extract from stem bark of Japanese horse chestnut (JHC) were evaluated. Exposure to JHC extract (10–100 μg/mL) for a 72 h incubation period did not alter cell viability compared to the untreated control. JHC extract, with concentrations of 25, 50, and 100 μg/mL, inhibited lipid accumulation in 3T3-L1 adipocytes in a dose dependent manner. The expression of PPARγ and C/EBPα, important adpogenic key markers was significantly reduced when JHC extract was added to cells for 8 days compared with the untreated control group. These results suggest that JHC extract might be a potential therapeutic agent as a natural anti-obesity material.